Search Result
Results for "
breast
" in MedChemExpress (MCE) Product Catalog:
1627
Inhibitors & Agonists
21
Biochemical Assay Reagents
67
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P10790
-
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Microtubule/Tubulin
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Cancer
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Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
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- HY-P991319
-
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Mucin
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Cancer
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TAB-004 is a human monoclonal antibody (mAb) targeting MUC1. TAB-004 specifically recognizes tMUC1 in all major subtypes of breast cancer without affecting normal breast epithelial cells. TAB-004 can be used in triple-negative breast cancer (TNBC) research .
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-
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- HY-149469
-
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BCRP
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Cancer
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BCRP/ABCG2-IN-1 is the inhibitor of breast cancer resistance protein (BCRP/ABCG2), with IC50 of 5.98 μM, that can be used in multidrug resistance of breast cancer .
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-
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- HY-163309
-
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Bcl-2 Family
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Cancer
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Bcl-2-IN-19 (compound 27) is a potent Bcl-2 inhibitor for targeting breast cancer .
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-
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- HY-122878
-
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HSP
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Cancer
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HS-131, a near infrared dye tethered Hsp90 inhibitor, is able to detect oncogene-driven breast cancers, including multiple different molecular subtypes of human breast cancers .
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-
-
- HY-169063
-
-
-
- HY-148368
-
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Bcl-2 Family
Apoptosis
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Cancer
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CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .
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-
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- HY-137931
-
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Cytochrome P450
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Cancer
|
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Testololactone is an aromatase inhibitor. Testololactone can be used for research of breast carcinoma .
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-
-
- HY-162292
-
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PI3K
Kinesin
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Cancer
|
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Anticancer agent 190 (compound 3e) is an inhibitor targeting KSP (Kinesin) and PI3Kδ with activity against breast cancer .
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-
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- HY-N8293
-
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Others
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Cancer
|
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Eupalinolide I inhibits the viability of breast cancer cells. Eupalinolide I can be isolated from Eupatorium lindleyanum .
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-
-
- HY-115514A
-
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BRK
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Cancer
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BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models .
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-
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- HY-122703
-
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Epigenetic Reader Domain
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Cancer
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BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors .
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-
-
- HY-79315
-
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Estrogen Receptor/ERR
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Others
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6-Dehydronandrolone acetate is a starting material for synthesis of Fulvestrant. Fulvestrant is an estrogen receptor antagonist that can be used for the research of breast cancer .
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-
-
- HY-108638
-
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MDM-2/p53
Apoptosis
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Cancer
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NSC 146109 hydrochloride is a small-molecule p53 activator that target MDMX and can be used for breast cancer research. NSC 146109 hydrochloride is a pseudourea derivative, promotes breast cancer cells to undergo apoptosis through activating p53 and inducing expression of proapoptotic genes .
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-
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- HY-N3800
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Others
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Cancer
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Eichlerialactone is a sesquiterpene compound isolated from Chisocheton penduliflorus. Eichlerialactone is weakly cytotoxic to breast cancer cells .
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- HY-101120
-
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Epigenetic Reader Domain
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Cancer
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666-15 is a potent and selective CREB inhibitor with an IC50 of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model .
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-
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- HY-P990552A
-
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MNPR-101
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Integrin
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Cancer
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huATN-658 (MNPR-101) is a humanized monoclonal antibody inhibitor targeting urokinase-type plasminogen activator receptor (uPAR). huATN-658 blocks the interaction between uPAR and integrins, inhibiting the proliferation, invasion and migration of tumor cells. huATN-658 is promising for research of breast cancer (especially triple-negative breast cancer) .
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-
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- HY-159994
-
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Amino Acid Derivatives
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Cancer
|
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AUPF02, a 5-arylurea uracil derivative, is a potent anti-breast cancer agent, with an IC50 of 23.4 µM for MCF-7 cells .
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- HY-13738
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Keoxifene; LY156758 free base; LY139481
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Estrogen Receptor/ERR
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Cancer
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Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
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-
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- HY-19972
-
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Wnt
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Cancer
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ML243 is a selective small-molecule inhibitor of breast cancer stem cells. ML243 has 32-fold greater selective inhibition in the breast CSC-like cell line HMLE_shECad than the control cell line HMLE_shGFP. ML243 may target the Wnt pathway at the protein level without altering RNA expression levels .
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- HY-P991245
-
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EGFR
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Cancer
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Anti-ERBB3/HER3 (SGP1) is a human monoclonal antibody (mAb) targeting ERBB3/HER3. Anti-ERBB3/HER3 (SGP1) inhibits Neuregulin stimulated growth of cultured breast cancer cells. Anti-ERBB3/HER3 (SGP1) can be used in breast cancer research .
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-
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- HY-146688
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Cytochrome P450
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Cancer
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SYN20028567 is an aromatase (CYP19) inhibitor with an IC50 of 9.4 nM. SYN20028567 can be used for breast cancer research .
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- HY-105375
-
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Cytochrome P450
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Cancer
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FR 901537 is a potent and competitive aromatase inhibitor. FR 901537, a novel naphthol derivative, has the potential for breast cancer research .
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-
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- HY-16395
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CGC-11047
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Others
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Cancer
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PG-11047 (CGC-11047) is a polyamine analogue. PG-11047 can be used for the research of breast cancer .
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-
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- HY-P2166
-
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MMP
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Cancer
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MMP3 inhibitor 3 is an inhibitor of MMP3. MMP3 inhibitor 3 can used to study breast cancer .
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-
-
- HY-100910
-
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CaMK
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Cancer
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W-13 hydrochloride is a calmodulin antagonist. W-13 hydrochloride can inhibit Tamoxifen (HY-13757A)-resistant human breast cancer cell growth .
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-
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- HY-144138
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 2 is a selective estrogen receptor downregulator. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 2 has the potential for the research of breast cancer diseases (extracted from patent WO2021228210A1, compound 3) .
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- HY-144137
-
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Estrogen Receptor/ERR
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Cancer
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Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4) .
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-
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- HY-125575
-
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Carbonic Anhydrase
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Cancer
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FC11409B is an ureido-sulfamate carbonic anhydrase IX (CAIX) inhibitor. FC11409B inhibits proliferation and migration of breast cancer cell lines in both hypoxic (0.5% O2) and normoxic conditions (21% O2). FC11409B also inhibits 3D spheroid of breast cancer subtypes invasion. FC11409B is promising for research of breast and ovarian cancers .
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-
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- HY-126899
-
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Microtubule/Tubulin
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Cancer
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TPI-287, a blood-brain barrier-permeable microtubule stabilizer, can significantly reduce metastatic colonization of breast cancer in the brain .
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-
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- HY-159741
-
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FCE 24928
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Cytochrome P450
|
Cancer
|
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Minamestane (FCE 24928) is a selective and competitive aromatase inhibitor with an IC50 value of 45.7 nM. Minamestane is promising for research of postmenopausal breast cancer .
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-
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- HY-149970
-
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Estrogen Receptor/ERR
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Cancer
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ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer .
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-
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- HY-P2166A
-
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MMP
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Cancer
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MMP3 inhibitor 3 (TFA) is an inhibitor of MMP3. MMP3 inhibitor 3 (TFA) can used to study breast cancer .
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-
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- HY-13442
-
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B1939; E7389; ER-086526
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Microtubule/Tubulin
Apoptosis
ADC Cytotoxin
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Cancer
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Eribulin (E7389) is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
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-
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- HY-149324
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-
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- HY-13442A
-
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B1939 mesylate; E7389 mesylate; ER-086526 mesylate
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Microtubule/Tubulin
Apoptosis
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Cancer
|
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Eribulin (E7389) mesylate is a microtubule targeting agent that is used for the research of metastatic breast cancer. Eribulin mesylate inhibits the proliferation of cancer cells by binding microtubule proteins and microtubules.
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-
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- HY-151565
-
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Others
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Cancer
|
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Anticancer agent 86 (compound 6i) shows potential activity against breast adenocarcinoma .
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-
-
- HY-149266
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THK01
1 Publications Verification
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ROCK
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Cancer
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THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer .
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- HY-N2547
-
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Others
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Cancer
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Steviolbioside is a rare sweetener that exists in stevia rebaudiana leaves. Steviolbioside presents inhibition on several human cancer cells and acts as potential remedy for human breast cancer .
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- HY-107967
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Fluorescent Dye
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Cancer
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Isosulfan blue is a blue dye for the identification of lymph vessels during lymphangiography. Isosulfan blueis is used during sentinel lymph node biopsies in breast cancer. Isosulfan blue is possible to have an allergic reaction during breast cancer operations .
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- HY-P0237
-
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Kallikrein
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Cancer
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KKI-5 is a specific inhibitor of tissue kallikrein. KKI-5 can attenuate breast cancer cell invasion .
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-
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- HY-116904
-
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Apoptosis
Akt
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Cancer
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Anticancer agent 253 (Compound 26) has anti-cancer activity against breast cancer cells, with IC50s of 6 μM (MCF-7), 10 μM (MDA-MB-231) and 6.4 μM (4T1 cells). Anticancer agent 253 arrests cell cycle and induces mitochondria-mediated apoptosis in cancer cells. Anticancer agent 253 inhibits Akt phosphorylation in human breast and prostate cancer .
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- HY-172783
-
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Cytochrome P450
Apoptosis
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Cancer
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Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. Aromatase-IN-5 effectively blocks estrogen production. Aromatase-IN-5 inhibits the proliferation of breast cancer cell lines like MCF-7, arrests the cell cycle at the G1 phase, and induces apoptosis. Aromatase-IN-5 is promising for research of breast cancer .
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-
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- HY-143257
-
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CDK
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Cancer
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CDK4/6-IN-7 is a potent, selective and orally active CDK4/6 inhibitor, with IC50s of 1.58 and 4.09 nM, respectively. CDK4/6-IN-7 can be used for the research of breast cancer .
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-
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- HY-168951
-
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Annexin A
Apoptosis
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Cancer
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(R)-SL18 is a degrader of ANXA3 and can degrade ANXA3 protein through the ubiquitination pathway. (R)-SL18 inhibits the proliferation, migration, invasion, and colony formation of breast cancer cells and induces apoptosis. (R)-SL18 can be used in the research of triple-negative breast cancer .
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-
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- HY-108162A
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-
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- HY-164238
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Others
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Cancer
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LysoPC(18:3) is a lysophospholipid (LyP). LysoPC(18:3) can be used as a lipid biomarker in the diagnosis of breast cancer .
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-
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- HY-122411
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EGIS 5650; GYKI-13504
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Estrogen Receptor/ERR
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Cancer
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Panomifene (EGIS 5650) is a tamoxifen (HY-13757A) analog with an antiestrogenic activity. Panomifene can be used in the research of breast cancer .
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-
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- HY-W392925
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d-Aminoglutethimide
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Cytochrome P450
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Cancer
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(R)-(+)-Aminoglutethimide is a potent and orally active aromatase inhibitor. (R)-(+)-Aminoglutethimide has the potential for the research of breast cancer .
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-
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- HY-13738R
-
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Estrogen Receptor/ERR
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Cancer
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Raloxifene (Standard) is the analytical standard of Raloxifene. This product is intended for research and analytical applications. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
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- HY-164789
-
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SKB264; MK-2870
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Antibody-Drug Conjugates (ADCs)
TROP2
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Cancer
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Sacituzumab tirumotecan (SKB264/MK-2870) is a TROP2 ADC. Sacituzumab tirumotecan can be used for the research of triple-negative breast cancer (TNBC) .
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- HY-N1823
-
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Apoptosis
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Metabolic Disease
Inflammation/Immunology
Cancer
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Pygenic acid A is a natural compound that can be found in Prunella vulgaris. Pygenic acid A induces apoptosis in metastatic breast cancer cells. Pygenic acid A can be used for the research of diabetes, inflammatory diseases, and cancers .
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- HY-P0237A
-
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Kallikrein
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Cancer
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KKI-5 (TFA) is a specific inhibitor of tissue kallikrein. KKI-5 (TFA) can attenuate breast cancer cell invasion .
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- HY-124909A
-
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Phosphatase
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Cancer
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FR054 is an inhibitor of the HBP enzyme PGM3, with a remarkable anti-breast cancer effect .
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-
- HY-B0323A
-
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Sulfafurazole diethanolamine
|
Endothelin Receptor
Antibiotic
Bacterial
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Infection
Endocrinology
Cancer
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Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A .
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-
- HY-B0323
-
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Sulfafurazole
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Endothelin Receptor
Bacterial
Antibiotic
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Infection
Endocrinology
Cancer
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Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A .
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- HY-119899
-
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Drug Derivative
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Cancer
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BO-0742, a derivative of AHMA and N-mustard, is a potent anti-cancer agent. BO-0742 significantly suppresses the growth of xenografts of human breast and ovarian cancers in mice .
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- HY-171158
-
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Liposome
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Cancer
|
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Glycerophosphoglycerol is a precursor for phospholipid biosynthesis. Glycerophosphoglycerol supports tumor cell membrane reconstruction and proliferation by promoting phospholipid synthesis. Glycerophosphoglycerol is promising for research of breast cancers .
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-
- HY-164479
-
-
- HY-106204
-
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EGFR
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Cancer
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Nelipepimut-S is a peptide vaccine which targets HER2. Nelipepimut-S has immune activity against HER2 positive breast cancer .
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-
- HY-W010248
-
-
- HY-149631
-
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HDAC
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Cancer
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HFY-4A is a HDAC inhibitor. HFY-4A inhibits breast cancer cell proliferation, migration, and invasion, and induces cell apoptosis. HFY-4A induces immunogenic cell death (ICD). HFY-4A inhibits tumor growth in breast cancer xenograft mouse models .
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-
- HY-108162
-
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COX
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Inflammation/Immunology
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Ataquimast free base is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast free base can be used in the study of advanced receptor-positive breast cancer .
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-
- HY-151564
-
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Others
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Cancer
|
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Anticancer agent 85 (compound 6j) is an anticancer agent that shows good cytotoxicity against MCF7 cells. Anticancer agent 85 can be used in breast cancer and other cancer studies .
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- HY-164463
-
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Estrogen Receptor/ERR
Apoptosis
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Cancer
|
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BMI-135 is a selective estrogen mimic, that exhibits agonist activity for estrogen receptor. BMI-135 induces rapid endoplasmic reticulum stress response (UPR) and apoptosis in breast cancer cells .
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- HY-161855
-
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VEGFR
Apoptosis
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Cancer
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VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer, with an IC50 value of 0.33 μM. VEGFR-2-IN-50 (Compound 10f) has growth inhibitory activity on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, which is expected to be used in the study of breast cancer diseases .
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-
- HY-P99458
-
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CG 10639
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c-Fms
|
Cancer
|
|
Balugrastim (CG 10639) is a novel long-acting recombinant granulocyte colony-stimulating factor (G-CSF) obtained by means of a genetic fusion between recombinant human serum albumin and granulocyte colony-stimulating factor. Balugrastim can be used for the research of breast cancer .
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-
- HY-157212
-
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Apoptosis
PARP
Proteasome
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Cancer
|
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PARP-1/Proteasome-IN-1 (compound 42i) is a dual PARP-1 and proteasome inhibitor with significant inhibitory effects on breast cancer. PARP-1/Proteasome-IN-1 can downregulate the expression of BRCA1 and RAD51 to inhibit homologous recombination repair function and induce apoptosis .
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-
- HY-152536
-
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NO Synthase
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Cancer
|
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iNOS inhibitor-10 is an iNOS inhibitor (IC50: 65 nM). iNOS inhibitor-10 has antiproliferative effect against triple negative breast cancer cells .
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-
- HY-159112
-
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HDAC
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Cancer
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AW01178 is a Class I HDAC inhibitor. AW01178 induces the upregulation of E-cadherin at both mRNA and protein levels and inhibits the EMT of breast cancer cells .
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-
- HY-162886
-
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JNK
Reactive Oxygen Species (ROS)
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Cancer
|
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BSO-07 is a ROS/JNK activator with significant anticancer effects, having an IC50 value of 24.81 μM against human breast cancer (BC) cells. BSO-07 induces apoptosis (Apoptosis) and paraptosis by activating JNK and increasing ROS levels, including enhancing the expression of apoptosis-associated proteins such as PARP, Bax, phosphorylated p53, ATF4, and CHOP, while decreasing the levels of anti-apoptotic proteins like Bcl-2, Bcl-xL, and Survivin. BSO-07 holds promise for research in the field of breast cancer .
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- HY-143323
-
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EGFR
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Cancer
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|
HER2-IN-9 is an orally active HER2 inhibitor, with an IC50 value of 0.03 μM. HER2-IN-9 inhibits HER-2 positive breast cancer cells proliferation and migration. HER2-IN-9 can be used in the research of breast cancers .
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-
- HY-146378
-
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Microtubule/Tubulin
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Cancer
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|
Tubulin polymerization-IN-20 (compound 11) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-20 has the potential for the research of breast cancers and chemoresistant colon cancers .
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-
- HY-146377
-
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-19 (compound 4) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-20 has the potential for the research of breast cancers and chemoresistant colon cancers .
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-
- HY-146376
-
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-18 (compound 8) is a potent inhibitor of tubulin polymerization. Tubulin polymerization-IN-18 has the potential for the research of breast cancers and chemoresistant colon cancers .
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-
- HY-W874892
-
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CBDP
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Reactive Oxygen Species (ROS)
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Cancer
|
|
Cannabidiphorol (CBDP) is a phytocannabinoid that increases the production of reactive oxygen species (ROS) and activates cellular pathways related to ROS signaling. Cannabidiphorol inhibits cell viability of breast cancer cells .
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- HY-14248
-
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CGS 20267
|
Cytochrome P450
Autophagy
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Cancer
|
|
Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
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-
- HY-P10371
-
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Reactive Oxygen Species (ROS)
Thrombopoietin Receptor
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Inflammation/Immunology
Cancer
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|
PKHB1 is a thrombospondin-1 peptide mimic with antitumor effects. PKHB1 induces mitochondrial alterations, ROS production, intracellular Ca 2+ accumulation, as well calcium-dependent cell death in breast cancer cells. PKHB1 induces immune system activation through immunogenic cell death induction in breast cancer cells .
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- HY-107967R
-
|
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Fluorescent Dye
|
Cancer
|
|
Isosulfan blue (Standard) is the analytical standard of Isosulfan blue. This product is intended for research and analytical applications. Isosulfan blue is a blue dye for the identification of lymph vessels during lymphangiography. Isosulfan blueis is used during sentinel lymph node biopsies in breast cancer. Isosulfan blue is possible to have an allergic reaction during breast cancer operations .
|
-
- HY-W013523
-
2-NP
5 Publications Verification
|
STAT
JAK
HSV
|
Infection
Cancer
|
|
2-NP is a selective enhancer of STAT1 transcription. 2-NP can enhance the ability of IFN-γ to inhibit the proliferation of human breast cancer and fibrosarcoma cells .
|
-
- HY-171830
-
|
YX39-105
|
PROTACs
Tyrosinase
Apoptosis
|
Cancer
|
|
MS105 (YX39-105) is an orally active and selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. MS105 recruits VHL E3 ligase via the VHL ligand moiety to promote PTK6 ubiquitination and proteasomal degradation, inhibiting breast cancer cell proliferation, migration, and inducing apoptosis. MS105 is promising for research of breast cancer. (Pink: BRK inhibitor P21d hydrochloride (HY-115514); Black: linker (HY-W105727); Blue: (S,R,S)-AHPC (HY-125845)) .
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-
- HY-133118
-
6RK73
2 Publications Verification
|
Deubiquitinase
|
Cancer
|
|
6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer .
|
-
- HY-163676
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
MI-217 is a potent SIRT3 inhibitor. MI-217 induces MDA-MB-231 apoptosis. MI-217 can be used in the study of breast cancer .
|
-
- HY-146064
-
|
|
Osteopontin
|
Cancer
|
|
OPN expression inhibitor 1 is an osteopontin (OPN) expression inhibitor. OPN expression inhibitor 1 has potential anti-breast cancer cell metastasis activity and can be used in the study of cancer .
|
-
- HY-155745
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-115 (SS-12) is an effective anti-tumor compound with an IC50 value of 0.34 μM-24.14 μM for cell line 4T1. Antitumor agent-115 can block the cell cycle of mouse breast cancer cell line 4T1, reduce the mitochondrial membrane potential, and induce apoptosis, and the IC50 value is 8-25 μmol/L for cell viability. Antitumor agent-115 can be used for breast cancer research .
|
-
- HY-N2547R
-
|
|
Others
|
Cancer
|
|
Steviolbioside (Standard) is the analytical standard of Steviolbioside. This product is intended for research and analytical applications. Steviolbioside is a rare sweetener that exists in stevia rebaudiana leaves. Steviolbioside presents inhibition on several human cancer cells and acts as potential remedy for human breast cancer .
|
-
- HY-122411A
-
|
(E/Z)-EGIS 5650 hydrochloride; (E/Z)-GYKI-13504 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
(E/Z)-Panomifene (hydrochloride) is an orally active tamoxifen (TMX) (HY-13757A) analog. (E/Z)-Panomifene (hydrochloride) is a selective anti-estrogenic compound. (E/Z)-Panomifene (hydrochloride) has anti-tumor activity and can be used in breast cancer research .
|
-
- HY-B0323R
-
|
|
Endothelin Receptor
Bacterial
Antibiotic
|
Infection
Endocrinology
Cancer
|
|
Sulfisoxazole (Standard) is the analytical standard of Sulfisoxazole. This product is intended for research and analytical applications. Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A .
|
-
- HY-108692
-
|
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Enterolactone is a bioactive phenolic metabolite known as a mammalian lignan derived from dietary lignans. Enterolactone has estrogenic properties and anti-breast cancer activity . Enterolactone is a radiosensitizer for human breast cancer cell lines through impaired DNA repair and increased apoptosis .
|
-
- HY-161831
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Antitumor agent-175 (Compound Ru2) is an antitumor agent with photocytotoxicity, demonstrating selective antitumor effects against triple-negative breast cancer (TNBC) cells .
|
-
- HY-153943
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-10 is a DNA-PK inhibitor. DNA-PK-IN-10 can be used for the research of breast cancer and non-small cell lung cancer .
|
-
- HY-119808
-
-
- HY-132294
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-502 is an orally active and potent degrader for estrogen receptor (ER). GNE-502 can be used for the research of breast cancer .
|
-
- HY-120046
-
|
|
HDAC
|
Cancer
|
|
YF479 is a potent inhibitor of histone deacetylase. YF479 abates cell viability, suppresses colony formation and tumor cell motility. YF479 significantly inhibits breast tumor growth and metastasis. YF479 has the potential for the research of clinical trials for breast cancer .
|
-
- HY-170332
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-15 (Compound 40) is an orally active degrader of the estrogen receptor (ER) with anticancer activity，which can be used in breast cancer research (Pink: Target Protein Ligand (HY-170334); Black: Linker (HY-30756); Blue: E3 Ligase Ligand (HY-138793); E3 Ligase Ligand-Linker Conjugate (HY-169979)) .
|
-
- HY-153909
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
SMP-33693 is a Drug-Linker Conjugate for ADC with a low payload shedding rate and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
|
-
- HY-114631
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
EM-800, an orally active anti-estrogen, serves as an antagonist to the transcriptional functions of estrogen receptors α (ERα) and β (ERβ). EM-800 possesses anticancer activity, capable of inhibiting the growth of breast cancer induced by 7,12-Dimethylbenz[a]anthracene (DMBA) (HY-W011845). Furthermore, in ovariectomized animals, EM-800 effectively slows down bone loss. Additionally, EM-800 shows potential in the research of breast and endometrial cancers, while exerting beneficial effects on bone and lipid metabolism .
|
-
- HY-162762
-
|
|
Protease Activated Receptor (PAR)
|
Cancer
|
|
PAR-2 antagonist 1 (Compound 9a) is a protease-activated receptor 2 (PAR2) antagonist with an IC50 value of 0.9 μM. PAR-2 antagonist 1 can effectively inhibit the proliferation and migration of breast cancer cells .
|
-
- HY-125209
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TH5427 is a promising, targeted inhibitor that can be used to further study NUDT5 activity and ADP-ribose metabolism. TH5427, blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells. NUDT5 is recently identified as a rheostat of hormone-dependent gene regulation and proliferation in breast cancer cells .
|
-
- HY-113110
-
|
|
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Cysteinylglycine is a dipeptide produced by the decomposition of extracellular glutathione catalyzed by γ-glutamyl transpeptidase. Cysteinylglycine is a highly reactive metabolite. Cysteinylglycine is currently mainly used in neurodegenerative diseases and breast cancer research .
|
-
- HY-P991410
-
|
MEDI0641 antibody
|
Wnt
|
Cancer
|
|
5T4_0108 (MEDI0641 antibody) is a human monoclonal antibody (mAb) targeting TPBG. 5T4_0108 can be used in breast and prostate cancer research .
|
-
- HY-110182
-
SP-141
2 Publications Verification
|
MDM-2/p53
|
Cancer
|
|
SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells .
|
-
- HY-163566
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 18, a potent inducer of apoptosis, shows significant cytotoxicity to the breast cancer cell line MCF-7 (IC50=0.559 μM). Apoptosis inducer 18 inhibits cell cycle progression and promotes apoptosis by binding to DNA and causing damage, and by binding to the active site of CDK-2, interfering with its kinase activity. Apoptosis inducer 18 can be used in anti-breast cancer research .
|
-
- HY-153908
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
SMP-93566 is a kind of antibody-drug conjugates (ADCs) with a low payload shedding rate and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
|
-
- HY-136447
-
ASP4132
1 Publications Verification
|
AMPK
|
Cancer
|
|
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models .
|
-
- HY-150757
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research .
|
-
- HY-Y0519
-
|
|
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Pyrimidine is a nitrogen-containing heterocyclic compound and endogenous metabolite. Pyrimidine derivatives can be used in pancreatic cancer, triple-negative breast cancer, colon carcinoma and neuron research .
|
-
- HY-112162
-
|
|
Mps1
|
Cancer
|
|
BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC50 of 11 nM and 63 nM for MPS1 (1 mM ATP) and P-MPS1, respectively. BOS-172722 also has potential for the study of various forms of breast cancer .
|
-
- HY-W354498
-
|
|
Endogenous Metabolite
|
Cancer
|
|
L-Octanoylcarnitine hydrochloride is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine hydrochloride can be used for the research of breast cancer .
|
-
- HY-113161
-
|
|
Endogenous Metabolite
|
Cancer
|
|
L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
|
-
- HY-172937
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 13 (compound MR3) is potent ERα degrader with an IC50 of 0.55 μM. ERα degrader 13 induces an obvious tumor regression in the breast cancer xenograft mouse model .
|
-
- HY-116896
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines .
|
-
- HY-105177
-
|
|
Progesterone Receptor
|
Endocrinology
Cancer
|
|
ORG 33628 is a potent and selective progesterone receptor modulator. ORG 33628 shows anti-progestational and anti-glucocorticoid activity. ORG 33628 shows ovulation-inhibitory activity. ORG 33628 has the potential for the research of breast and endometrium .
|
-
- HY-170580
-
|
|
Topoisomerase
|
Cancer
|
|
Topo I/II-IN-1 (compound 7t) is a potent Topo I and Topo II dual inhibitor. Topo I/II-IN-1 exhibits significant cytotoxicity against MCF-7 breast cancer cell line with an IC50 of 7.45 μM .
|
-
- HY-N10591
-
|
|
Others
|
Cancer
|
|
Bruceantarin is a potent antineoplastic agent. Bruceantarin can be used for leukemia and breast cancer research .
|
-
- HY-137144
-
|
ZB716
|
Estrogen Receptor/ERR
|
Cancer
|
|
Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells .
|
-
- HY-139376
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer .
|
-
- HY-108612A
-
|
CAY10593 hydrochloride
|
Phospholipase
|
Cancer
|
|
VU0155069 hydrochloride (CAY10593 hydrochloride) is a potent selective phospholipase D (PLD) inhibitor. The IC50 values for PLD1 and PLD2 are 46 and 933 nM, respectively. VU0155069 hydrochloride inhibits migration of human and mouse breast cancer cell lines .
|
-
- HY-118474
-
|
NSC 721648
|
Aryl Hydrocarbon Receptor
Cytochrome P450
|
Cancer
|
|
GW 610 (NSC 721648), an antitumor agent, is a potent AhR ligand with a Ki of 6.8 nM. GW 610 induces CYP1A1 expression in MCF-7 cells. GW 610 shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines .
|
-
- HY-108999A
-
|
BWA770U
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-108999
-
|
BWA770U mesylate
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (BWA770U) mesylate is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol mesylate shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-153907
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and human plasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
|
-
- HY-151890
-
|
|
Fluorescent Dye
|
Cancer
|
|
NIR-βgal-2 is a β-galactosidase-activated near-infrared fluorescent probe with superior sensitivity. NIR-βgal-2 can be used for visualizing β-galactosidase in breast cancer .
|
-
- HY-14248R
-
|
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Letrozole (Standard) is the analytical standard of Letrozole. This product is intended for research and analytical applications. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
|
-
- HY-B0448A
-
|
5,5-Diphenylhydantoin sodium salt
|
Sodium Channel
Virus Protease
|
Neurological Disease
Cancer
|
|
Phenytoin sodium (5,5-Diphenylhydantoin sodium salt) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
|
-
- HY-B0448
-
-
- HY-176418
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
BBOX-IN-1 (compound 58) is a potent BBOX inhibitor with an IC50 of 0.02 μM. BBOX-IN-1 can be used in the study of triple negative breast cancer (TNBC) .
|
-
- HY-149204
-
|
|
SDCBP
|
Cancer
|
|
SYNTi is a PDZ domain inhibitor targeting the syndecan/syntenin protein-protein Interaction. SYNTi exhibits an IC50 value of 400 nM and ligand efficiency (LE) value of 0.24. SYNTi can be used for breast cancer research .
|
-
- HY-162450
-
|
|
PROTACs
MDM-2/p53
Apoptosis
|
Cancer
|
Antitumor agent-150 (V10), an anti-breast cancer agent, is a PROTAC-based MDM2 protein degrader (Red: Ganoderic acid A; Black: 4O-PEG linker; Blue: VHL ligand) .
|
-
- HY-160049
-
|
|
Nucleoside Antimetabolite/Analog
Biochemical Assay Reagents
|
Cancer
|
|
BC15 aptamer sodium is an ssDNA aptamer targeting the intracellular protein hnRNP A1, which is highly expressed in cancerous liver tissue. BC15 aptamer sodium specifically recognizes breast cancer cells and can be used to detect cancer cells in other pathological types of breast cancer tissue .
|
-
- HY-W011338
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs) .
|
-
- HY-162477
-
|
|
Cathepsin
Apoptosis
|
Cancer
|
|
TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis .
|
-
- HY-119418
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Desketoraloxifene is an estrogen receptors alpha (ERα) activator at an AP-1 site. Desketoraloxifene can be used for the research of osteoporosis and breast cancer .
|
-
- HY-156419
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-16 (compound 36) is a potent, selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 can be used for the research of breast cancer and prostate cancer .
|
-
- HY-168101
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 11 (compound B16) is a selective ERα degrader that can be used as an estrogen receptor probe to investigate ER status in ER-positive breast cancer cells .
|
-
- HY-N12209
-
|
|
Others
|
Cancer
|
|
Neohelmanthicin A (compound 3A) is a phenylpropanoid compound with antitumor activity. The IC50s of Neohelmanthicin A for inhibiting leukemia cell line EL4, breast cancer cell line S180 and breast cancer cell line MCF7 are 0.13 μM, 7 μM and 23 μM respectively .
|
-
- HY-108692R
-
|
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Enterolactone (Standard) is the analytical standard of Enterolactone. This product is intended for research and analytical applications. Enterolactone is a bioactive phenolic metabolite known as a mammalian lignan derived from dietary lignans. Enterolactone has estrogenic properties and anti-breast cancer activity . Enterolactone is a radiosensitizer for human breast cancer cell lines through impaired DNA repair and increased apoptosis .
|
-
- HY-N7486
-
|
|
Others
|
Cancer
|
|
Chamaejasmenin B can be extracted from Stellera chamaejasme L. Chamaejasmenin B suppresses cancer cells migration and invasion. Chamaejasmenin B inhibits tumor metastasis. Chamaejasmenin B can be used in the research of cancers, such as breast cancers .
|
-
- HY-158649
-
|
|
Fatty Acid Synthase (FASN)
Apoptosis
|
Cancer
|
|
Fasnall benzenesulfonate is the benzenesulfonate salt form of Fasnall (HY-121250). Fasnall benzenesulfonate is the inhibitor for fatty acid synthase (FASN) with IC50 of 3.7 μM. Fasnall benzenesulfonate inhibits the proliferation and induces apoptosis in breast cancer cells. Fasnall benzenesulfonate exhibits antitumor efficacy in mice .
|
-
- HY-163812
-
|
|
Molecular Glues
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .
|
-
- HY-151162
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-12 is a HER2 inhibitor (IC50: 121 nM). HER2-IN-12 can be used in the research of cancers, such as breast cancer .
|
-
- HY-116896A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LY117018 TFA, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 TFA exerts antiproliferative effects on breast cancer cell lines .
|
-
- HY-12182
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
|
-
- HY-147402
-
|
D-0502
|
Estrogen Receptor/ERR
|
Cancer
|
|
Taragarestrant (D-0502) is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant shows potent activity in various ER+ breast cancer cell lines and xenograft models .
|
-
- HY-176444
-
|
|
CDK
|
Cancer
|
|
CDK2 degrader 6 (compound 6) is an orally active and potent CDK2 degrader with a DC50 of 46.5 nM. CDK2 degrader 6 can be used in the study of breast cancer .
|
-
- HY-149259
-
|
|
FAK
|
Cancer
|
|
FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis .
|
-
- HY-30236
-
|
|
Drug Intermediate
|
Cancer
|
|
5-Bromoindole is a chemical intermediate. 5-Bromoindole derivatives have anticancer activity against breast cancer. 5-Bromoindole can be used to synthesize GSK-3 inhibitors and anticancer active molecules .
|
-
- HY-107550
-
|
|
HDAC
|
Cancer
|
|
TCS HDAC6 20b is a HDAC6-selective inhibitor. TCS HDAC6 20b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells .
|
-
- HY-171777
-
|
ErPC3; Erucylphosphohomocholine
|
PI3K
Akt
Ras
Raf
p38 MAPK
|
Cancer
|
|
Erufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC50: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia .
|
-
- HY-102010
-
|
(+)-Pancratistatin
|
Apoptosis
|
Cancer
|
|
Pancratistatin is an isoquinoline alkaloid that can be isolated from Hymenocallis littoralis. Pancratistatin induces apoptosis of human melanoma cells. Pancratistatin can be used for the research of neuroblastoma, leukemia and breast cancer .
|
-
- HY-19634
-
|
|
Sirtuin
|
Cancer
|
|
YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells .
|
-
- HY-136255
-
|
AZD-9833
|
Estrogen Receptor/ERR
|
Cancer
|
|
Camizestrant (AZD-9833) is a potent and orally active estrogen receptor (ER) antagonist. Camizestrant is used for the study of ER + HER2-advanced breast cancer .
|
-
- HY-145143
-
|
|
Apoptosis
|
Cancer
|
|
anti-TNBC agent-1 is a potent anti-triple-negative breast cancer (TNBC) agent. anti-TNBC agent-1 exhibits potent activity against different breast cancer cells with IC50 values ranging from 0.20 μM to 0.27 μM. anti-TNBC agent-1 induces apoptosis of SUM-159 cells through mitochondria pathway and causes G1 phase arrest of SUM-159 cells .
|
-
- HY-22445
-
|
|
c-Myc
|
Cancer
|
MY05 selectively targets c-MYC in cells and disrupts MYC-MAX interaction. MY05 engages intracellular c-MYC, modulates c-MYC thermal stability, reduces c-MYC transcriptional targets, and possesses anticancer activity (TNBC, Triple-Negative Breast Cancer) .
|
-
- HY-15434A
-
|
|
MAP3K
MAP4K
|
Cancer
|
|
NG25 trihydrochloride is a dual TAK1 and MAP4K2 inhibitor (IC50: 149 nM and 21.7 nM respectively). NG25 sensitizes the breast cancer cells to Doxorubicin (HY-15142A), and enhances apoptosis. NG25 trihydrochloride can be used for research of various cancers .
|
-
- HY-N6007
-
|
|
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Chrysosplenol D is a methoxy flavonoid that induces ERK1/2-mediated apoptosis in triple negative human breast cancer cells. Chrysosplenol D also exhibits anti-inflammatory and moderate antitrypanosomal activities .
|
-
- HY-163112
-
|
|
Others
|
Cancer
|
|
Anticancer agent 179 (Compound 3) is a sambutoxin analogue. Anticancer agent 179 can impede migration of MDA-MB-231 breast cancer cells .
|
-
- HY-169293
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-63 (compound 4d), a ring-annulated analogue of Cannabidiol, is an anticancer agent. Antiproliferative agent-63 demonstrates a promising activity against breast and colorectal cancer. Antiproliferative agent-63 arrests the G1 phase of the cell cycle and induces apoptosis via the mitochondrial pathway in breast cancer cell lines .
|
-
- HY-12182A
-
|
|
Prostaglandin Receptor
|
Cancer
|
|
ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
|
-
- HY-113062
-
|
20-OH-P
|
Endogenous Metabolite
Cytochrome P450
|
Endocrinology
Cancer
|
|
20α-Dihydroprogesterone is the metabolite of Progesterone (HY-N0437). 20α-Dihydroprogesterone inhibits cell proliferation and migration in breast tissue. 20α-Dihydroprogesterone inhibits aromatase in cell MCF-7aro with IC50 about 5 μM .
|
-
- HY-P991239
-
|
|
EGFR
|
Cancer
|
|
NM-02 is an antibody targeting HER2 with an EC50 value of 1.2 nM. NM-02 binds to domains I and II of HER2-ECD, blocking HER2-related signaling pathways. NM-02 is promising for research of HER2-positive breast cancer .
|
-
- HY-128729
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive, and specific DNA2 nuclease inhibitor with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits the nuclease, DNA-dependent ATPase, helicase, and DNA-binding activities of DNA2. DNA2 inhibitor C5 can be used in breast cancer and colorectal cancer research .
|
-
- HY-149081
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
|
Cancer
|
|
ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
|
-
- HY-151120
-
|
|
Others
|
Cancer
|
|
Anticancer agent 79 (compound 3d) shows good anti-breast cancer activity. Anticancer agent 79 shows good cytotoxic activity in T47-D cells, with an IC50 of 13.64 ± 0.26 μM .
|
-
- HY-147402A
-
|
D-0502 meglumine
|
Estrogen Receptor/ERR
|
Cancer
|
|
Taragarestrant (D-0502) meglumine is a potent, orally active and selective estrogen receptor degrader (SERD). Taragarestrant meglumine shows potent activity in various ER+ breast cancer cell lines and xenograft models .
|
-
- HY-P99591
-
|
AS1402; huHMFG-1
|
Mucin
|
Cancer
|
|
Sontuzumab (AS1402) is a humanizedised IgG1κ MUC1 specific monoclonal antibody. Sontuzumab binds the extracellular MUC1 peptide sequence PDTR with a Kd of ~1 nM. Sontuzumab can be used for the research of breast cancer .
|
-
- HY-169671
-
|
|
Wnt
|
Cancer
|
|
21H7 is a selective inhibitor of the Wnt/b-catenin pathway. 21H7 markedly inhibits the growth of HFs. 21H7 potently decreases growth of breast and colon cancer cells .
|
-
- HY-174131
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC50=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC50=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer .
|
-
- HY-114979
-
|
|
Antibiotic
Fungal
Apoptosis
|
Infection
Cancer
|
|
Pyoluteorin is an antibiotic that inhibits Oomycete fungi, including the plant pathogen Pythium ultimum, and suppresses plant diseases caused by this fungus . Pyoluteorin induces human triple-negative breast cancer MDA-MB-231 cells apoptosis in vitro. Pyoluteorin can be used for the research of human triple-negative breast cancer .
|
-
- HY-B1785
-
|
Sulfosalicylic acid; Sulphosalicylic acid; Salicylsulfonic acid
|
Drug Derivative
|
Cancer
|
|
5-Sulfosalicylic acid is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid is effective against the breast cancer cell lines, with less toxicity . 5-Sulfosalicylic acid has antioxidant activities .
|
-
- HY-N8669
-
|
|
LIM Kinase (LIMK)
|
Cancer
|
|
Curcolonol is a furan type sesquiterpene. Curcolonol can be isolated from several medical herbs. Curcolonol has inhibitory activity for LIM kinase 1. Curcolonol can be used for the research of breast cancer .
|
-
- HY-144824
-
|
|
Cytochrome P450
Monoamine Oxidase
|
Neurological Disease
Cancer
|
|
Monoamine oxidase/Aromatase-IN-1 (compound 2q) is a highly potent monoamine oxidase (MAO) and aromatase dual inhibitor with IC50s of 39 nM and 31 nM for MAO-B and aromatase, respectively. Monoamine oxidase/Aromatase-IN-1 can be used for researching neurological disorder and breast cancer .
|
-
- HY-113110R
-
|
|
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Cysteinylglycine (Standard) is the analytical standard of Cysteinylglycine. This product is intended for research and analytical applications. Cysteinylglycine is a dipeptide produced by the decomposition of extracellular glutathione catalyzed by γ-glutamyl transpeptidase. Cysteinylglycine is a highly reactive metabolite. Cysteinylglycine is currently mainly used in neurodegenerative diseases and breast cancer research .
|
-
- HY-113293B
-
|
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Cancer
|
|
Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). Estrone sulfate can be used for the research of breast cancer .
|
-
- HY-148453
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-16 is an indolyl hydrazide-hydrazone compound with anticancer activity. Antiproliferative agent-16 exhibits specificity toward breast cancer cells (IC50 of 6.94 μM for MCF-7 cells) .
|
-
- HY-154790
-
|
Neu5Aca2-6GalNAc-a-Ser/Thr
|
Ser/Thr Protease
|
Cancer
|
|
STn/sialyl-Tn is a sialic acid associated with breast cancer and its expression is closely related to HER2-pos. STn/sialyl-Tn can be used as a marker to count cells in malignant nipple discharge (PND) .
|
-
- HY-P991358
-
|
LFA-102; X213
|
Estrogen Receptor/ERR
|
Cancer
|
|
XOMA-213 (LFA-102; X213) is a human monoclonal antibody (mAb) targeting PRLR/Prolactin Receptor. XOMA-213 inhibits hPRL-dependent growth of BaF3/hPRLR cells (EC50: 0.5 μg/mL). XOMA-213 inhibits PRLR signaling and tumor growth in the Nb2-11-luc xenograft mouse model and the DMBA-induced rat breast cancer model. XOMA-213 can be used in Breast cancer, Hyperprolactinaemia and Prostate cancer research .
|
-
- HY-164550
-
|
|
HDAC
|
Cancer
|
|
YF438 is an HDAC inhibitor with effective anticancer activity both in vitro and in vivo. YF438 inhibits the growth and metastasis of triple-negative breast cancer (TNBC) cells by blocking the interaction between HDAC and MDM2, inducing the dissociation of MDM2-MDMX, and promoting the degradation of MDM2 .
|
-
- HY-172964
-
|
|
PI3K
Akt
mTOR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
KIM-161 is a PIK3CA inhibitor. KIM-161 has significant antiproliferative activity with IC50 values of 1.428 and 1.562 µM against PI3KCA mutant breast cancer MCF7 and T47D cells, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway and inducing ROS production. KIM-161 can be used to study breast cancer and its PI3KCA mutant subtypes .
|
-
- HY-NP132
-
|
|
Biochemical Assay Reagents
Integrin
|
Cancer
|
|
Recombinant Humanized Type III Collagen 28.6kDa is a type III collagen 28.6kDa. Recombinant humanized type III collagen (rhCOLIII) has various biological functions, such as promoting skin extracellular matrix regeneration and improving the cell microenvironment. rhCOLIII inhibits the proliferation, migration, and invasion of breast cancer cells. Type III collagen functions in cell adhesion, migration, proliferation and differentiation through its interaction with integrins .
|
-
- HY-159560
-
|
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
PBA-AMF can be activated by H2O2 to release Amonafide (AMF) (HY-10982). PBA-AMF selectively inhibited the proliferation of breast cancer cells, while sparing non-cancerous cells. PBA-AMF inhibits tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing apoptosis, and arresting the cell cycle. PBA-AMF can be used for research of tumors and other diseases associated with increased H2O2 levels .
|
-
- HY-139682
-
-
- HY-N15577
-
|
|
Drug Derivative
|
Cancer
|
|
Antiproliferative agent-69 (Compound 1) is a prenylated kaempferol derivative found in the fresh bud’s fur of Platanus acerifolia. Antiproliferative agent-69 shows significant antiproliferative effects against human breast cancer cells (MCF-7) and human hepatocellular carcinoma cells (Hep-G2) with IC50 values of 38.2 μM and 39.5 μM, respectively. Antiproliferative agent-69 is promising for research of breast cancer and liver cancer .
|
-
- HY-147710
-
|
|
MicroRNA
|
Cancer
|
|
PIN1 inhibitor 2 (compound 12) is a potent PIN1 inhibitor. PIN1 inhibitor 2 shows antitumor activity with an IC50 of 9.55 µM for MCF7 cells. PIN1 inhibitor 2 has the potential for the research of breast cancer .
|
-
- HY-172091
-
|
|
EGFR
|
Cancer
|
|
CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib (HY-10158) .
|
-
- HY-164547
-
|
|
Porcupine
Wnt
β-catenin
|
Cancer
|
WHN-88 is a Porcupine (PORCN) inhibitor. WHN-88 can eliminate the palmitoylation of Wnt ligands, preventing their secretion and subsequent Wnt/β-catenin signaling. WHN-88 can inhibit cancer cell stemness and suppress the occurrence and development of breast tumors in MMTV-Wnt1 transgenic mice .
|
-
- HY-167114
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
(Rac)-Aurora A/PKC-IN-1 (Compund 2e) is an orally active Aurora A and PKC (α, β1, β2 and θ) kinase inhibitor. (Rac)-Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells in vitro and antimetastatic activity in vivo .
|
-
- HY-155233
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase-IN-5 (compound 10b) is a steroid sulfatase (STS) inhibitor (IC50: 0.32 nM). Steroid sulfatase-IN-5 inhibits T-47D cell proliferation with an IC50 of 35.7 μM. Steroid sulfatase-IN-5 can be used for research of breast cancer .
|
-
- HY-16230
-
|
|
ROS Kinase
Apoptosis
|
Cancer
|
|
GGTI-2417 is a potent and selective inhibitor of GGTase I. GGTI-2417 inhibits the Cdk2-mediated phosphorylation of p27 Kip1 at Thr187 and accumulates p27 Kip1 in the nucleus. GGTI-2417 also induces breast cancer cell apoptosis .
|
-
- HY-135276
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
|
-
- HY-N1300
-
|
|
Fungal
|
Infection
Cancer
|
|
Shizukanolide F is a dimeric sesquiterpene, which is derivated from Chloranthus japonicus Sieb. Shizukanolide F exhibits potent antifungal activities against various plant pathogenic fungi and anti-metastasis breast cancer .
|
-
- HY-113986B
-
|
(S)-Fadrozole; (S)-CGS 16949A free base; (S)-FAD286
|
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
Cancer
|
|
(S)-Dexfadrostat ((S)-Fadrozole) is an aromatase inhibitor with an IC50 of 4.6 nM in human placental microsomes in vitro. (S)-Dexfadrostat can be used in the study of estrogen-dependent breast cancer, gynecomastia, and systemic lupus erythematosus .
|
-
- HY-172869
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor modulator 13 (Compound 5D) is an estrogen receptor antagonist. Estrogen receptor modulator 13 shows significant cytotoxicity against MCF7 cells with an IC50 value of 8.50 μM. Estrogen receptor modulator 13 is promising for research of breast cancers .
|
-
- HY-W005288
-
|
4-Hydroxystyrene
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
|
-
- HY-N15340
-
|
|
PKC
|
Cancer
|
|
1-Oleoyl-2-linoleoyl-sn-glycerol is a diacylglycerol (DG). 1-Oleoyl-2-linoleoyl-sn-glycerol can activate protein kinase C (PKC), thus triggering downstream signaling cascades and promoting tumor growth. 1-Oleoyl-2-linoleoyl-sn-glycerol is promising for research of breast cancer .
|
-
- HY-155008
-
|
|
PROTACs
Hexokinase
|
Cancer
|
|
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .
|
-
- HY-172597
-
|
|
MDM-2/p53
CDK
|
Cancer
|
|
YL-1-9 is an inhibitor of the degradation of p53 by MDM2 through strong binding to the key hydrophobic pockets of MDM2. YL-1-9 induces cell cycle arrest and apoptosis in breast cancer cells .
|
-
- HY-N0595
-
|
Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway .
|
-
- HY-146889
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 μM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-14952
-
|
PLA-695
|
Phospholipase
|
Inflammation/Immunology
Cancer
|
|
Giripladib (PLA-695) is a indole-based inhibitor of cytosolic phospholipase A2 (cPLA2). Giripladib can be used for osteoarthritis and breast cancer research .
|
-
- HY-146890
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 μM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-171755
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-40 (Compound 15b) is a heat shock protein 90 (Hsp90) C-terminal inhibitor. Hsp90-IN-40 exhibits antiproliferative activity against SKBr3 and MCF-7 breast cancer cells (IC50 of 2.57 µM and 2.43 µM, respectively). Hsp90-IN-40 inhibits cancer cell growth by inhibiting the Hsp90 C-terminal function, leading to Hsp90-dependent protein degradation. Hsp90-IN-40 can be used in breast cancer research .
|
-
- HY-108999AR
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (Standard) is the analytical standard of Crisnatol. This product is intended for research and analytical applications. Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-120140
-
-
- HY-P10934
-
|
LXY2
|
Integrin
|
Cancer
|
|
LXY3 (LXY2) is a VLA-3-blocking peptide that inhibits the interaction between integrin α3β1 (VLA-3) on neutrophil surfaces and laminin in the basement membrane, thereby preventing neutrophil migration across the tumor vascular basement membrane barrier. LXY3 is used to block neutrophil-mediated nanoparticle release from perivascular pools into the tumor interstitium. LXY3 is commonly employed for targeted imaging of breast cancer .
|
-
- HY-145572
-
|
LY-3484356
|
Estrogen Receptor/ERR
|
Cancer
|
|
Imlunestrant (LY-3484356) is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
|
-
- HY-145572A
-
|
LY-3484356 tosylate
|
Estrogen Receptor/ERR
|
Cancer
|
|
Imlunestrant (LY-3484356) tosylate is an orally active, potent and selective estrogen receptor degrader (SERD) with pure antagonistic properties. Imlunestrant tosylate results in sustained inhibition of ER-dependent gene transcription and cell growth. Imlunestrant tosylate can be used for the research of ER-positive (ER+) advanced breast cancer (aBC) and endometrial endometrioid cancer (EEC) .
|
-
- HY-N10403
-
|
4-Hydroxy-17β-estradiol
|
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
4-Hydroxyestradiol (4-Hydroxy-17β-estradiol) is an endogenous metabolite of Estradiol (HY-B0141). 4-Hydroxyestradiol is carcinogenic and shows mutagenic activity in breast epithelial cells. 4-Hydroxyestradiol inhibits the binding of Estradiol to the estrogen receptor in a competitive manner, with a Ki of 0.48 nM .
|
-
- HY-146244
-
|
ODN 2006; PF-3512676; CpG 7909; ODN 7909
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
Cancer
|
|
Agatolimod (ODN 2006), a class B ODN (oligodeoxynucleotide), is a TLR9 agonist. Agatolimod is also an optimal CpG sequence for humans. Agatolimod stimulates very strong production of NO2 and IL-6 in HD11 cells. Agatolimod can be used for breast cancer research. Sequence: 5'-tcgtcgttttgtcgttttgtcgtt-3' .
|
-
- HY-18766
-
|
|
TGF-β Receptor
p38 MAPK
|
Cancer
|
|
EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung .
|
-
- HY-161601
-
|
|
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Ferroptosis inducer-2 (Compound 24) is an inducer for heme oxygenase-1 (HO-1). Ferroptosis inducer-2 exhibits anticancer activity against triple-negative breast cancer (TNBC) cells through induction of ferroptosis .
|
-
- HY-18719
-
|
|
Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
|
Endoxifen Z-isomer is an oral active Tamoxifen (HY-13757A) metabolite, inducing an anti-estrogenic effect in breast cancer cells expressing ERα. Endoxifen Z-isomer inhibits hERG. This effect is concentration-dependent, with an IC50 value of 1.6 μM .
|
-
- HY-P1651
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity .
|
-
- HY-163381
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-48 (compound PC-A1) shows selective antiproliferative activity against triple-negative breast cancer (TNBC) cells .
|
-
- HY-135276A
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
|
-
- HY-170786
-
|
IRX4647F
|
RAR/RXR
|
Cancer
|
|
IRX5010 (IRX4647F), an analogue of IRX4647, is a highly selective RARγ nuclear receptor agonist. IRX5010 demonstrates inhibition of in vivo growth of EMT-6 triple negative breast cancer .
|
-
- HY-14281
-
|
Win 24540
|
Others
|
Endocrinology
Cancer
|
|
Trilostane (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane is a synthetic nonhormonal steroid. Trilostane can be used for the research of breast cancer and prostate cancer .
|
-
- HY-101923B
-
|
|
ULK
Autophagy
Apoptosis
|
Cancer
|
|
LYN-1604 dihydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC) .
|
-
- HY-N0519
-
|
Cyclosin
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Calycosin is a compound that can be isolated from Radix Astragali. Calycosin has strong antioxidant, anti-inflammatory and apoptosis-modulating effects. Calycosin can be used for the research of ovarian cancer and breast cancer .
|
-
- HY-101923A
-
|
|
ULK
Autophagy
Apoptosis
|
Cancer
|
|
LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC) .
|
-
- HY-101923
-
|
|
ULK
Autophagy
Apoptosis
|
Cancer
|
|
LYN-1604 is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC) .
|
-
- HY-78216
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
2-Thiooxamic acid ethyl ester is an organic compound containing thiocarbonyl and ethyl ester groups. 2-Thiooxamic acid ethyl ester can be used in the study of cancer (such as chronic myeloid leukemia, breast cancer, etc.) .
|
-
- HY-137552
-
|
MASTL Kinase Inhibitor-1
|
MASTL
|
Cancer
|
|
MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer .
|
-
- HY-150158
-
|
|
Toll-like Receptor (TLR)
|
Cancer
|
|
TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research .
|
-
- HY-138642
-
|
ARV-471
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
|
-
- HY-P991317
-
|
|
Mucin
|
Cancer
|
|
BTH1704 is a human monoclonal antibody (mAb) targeting MUC1. BTH1704 enables PGG-primed leukocytes to kill iC3b-opsonized tumor cells. BTH1704 can be used in pancreatic and breast cancer research .
|
-
- HY-W011338R
-
|
|
Reference Standards
Aryl Hydrocarbon Receptor
|
Cancer
|
|
Benzyl butyl phthalate (Standard) is the analytical standard of Benzyl butyl phthalate. This product is intended for research and analytical applications. Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs) .
|
-
- HY-124403
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 -7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .
|
-
- HY-P99029
-
|
Hu5F9-G4
|
CD47
|
Cancer
|
|
Magrolimab (Hu5F9-G4) is a humanized anti-CD47 antibody. Magrolimab can block the "don't eat me" signal of CD47, thereby promoting macrophage mediated phagocytosis. Magrolimab has antitumor activity in malignant bone tumors and breast cancer .
|
-
- HY-113161R
-
|
|
Endogenous Metabolite
|
Cancer
|
|
L-Octanoylcarnitine (Standard) is the analytical standard of L-Octanoylcarnitine. This product is intended for research and analytical applications. L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
|
-
- HY-B1460B
-
|
(±)-Sulconazole
|
Fungal
|
Cancer
|
|
Sulconazole is a potent antifungal agent in the imidazole class. Sulconazole blocks the NF-κB/IL-8 signaling pathway and CSC (Cancer stem cells) formation. Sulconazole inhibits tumor growth, and can be used for breast cancer research .
|
-
- HY-B0448R
-
|
|
Sodium Channel
Virus Protease
|
Neurological Disease
Cancer
|
|
Phenytoin (Standard) is the analytical standard of Phenytoin. This product is intended for research and analytical applications. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na + channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
|
-
- HY-N2059
-
|
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Santalol is a mixture of α and β-isomer santalol. α-Santalol is found in sandalwood oil. α-Santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer. Santalol has sedative activity .
|
-
- HY-B0448AR
-
|
|
Sodium Channel
Virus Protease
|
Neurological Disease
Cancer
|
|
Phenytoin (sodium) (Standard) is the analytical standard of Phenytoin (sodium). This product is intended for research and analytical applications. Phenytoin sodium (5,5-Diphenylhydantoin sodium salt) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
|
-
- HY-136521
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
AZ13824374 is a potent and selective ATAD2 bromodomain inhibitor (pIC50 of 6.9 in HCT116 cells). AZ13824374 disrupts chromatin interactions and gene transcription by binding to the acetyl-lysine binding site of the ATAD2 bromodomain. AZ13824374 has anticancer activity against breast cancer .
|
-
- HY-P1651A
-
|
|
TRP Channel
|
Cancer
|
|
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity .
|
-
- HY-117102
-
|
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
|
-
- HY-172175
-
|
|
mTOR
Akt
PI3K
Apoptosis
Autophagy
|
Cancer
|
|
HYS-072 is an orally active derivative of chrysin (HY-14589) with antitumor activity. HYS-072 induces apoptosis and autophagy by inhibiting the PI3K/AKT/mTOR signaling pathway and suppresses tumor growth in vivo in xenograft models by modulating autophagy-related pathways. HYS-072 can be used in the research of triple-negative breast cancer .
|
-
- HY-116896R
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LY117018 (Standard) is the analytical standard of LY117018. This product is intended for research and analytical applications. LY117018, a Raloxifene analog, is a selective estrogen receptor modulator. LY117018 exerts antiproliferative effects on breast cancer cell lines .
|
-
- HY-W177546
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
CD00509 is a Tdp1 inhibitor, with an IC50 value of 0.71 μM. CD00509 can sensitize breast cancer cells to Camptothecin (HY-16560). CD00509 has anti-tumor activity .
|
-
- HY-138642A
-
|
(Rac)-ARV-471
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
|
(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
|
-
- HY-145102
-
|
|
HSP
Apoptosis
|
Cancer
|
|
NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
|
-
- HY-150543
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase-IN-3 (compound 1q) is a potent STS (Steroid sulfatase) inhibitor, with an IC50 of 25.8 nM. Steroid sulfatase-IN-3 shows antiproliferative activity against T-47D estrogen-dependent breast cancer cells, with an IC50 of 1.04 µM .
|
-
- HY-12352A
-
|
|
STAT
Apoptosis
|
Cancer
|
|
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study .
|
-
- HY-159130
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
AO-022 is a potent TALDO1 allosteric inhibitor. AO-022 decreases the expression of vimentin and snail. AO-022 shows antiproliferative activity and antitumor activity. AO-022 has the potential for the research of breast cancer .
|
-
- HY-151119
-
|
|
Cytochrome P450
|
Cancer
|
|
Anticancer agent 78 is a potent anticancer agent. Anticancer agent 78 shows cytotoxicity. Anticancer agent 78 exhibits anti-aromatase activity with an IC50 value of 0.9 µM. Anticancer agent 78 has the potential for the research of breast cancer .
|
-
- HY-123901
-
|
|
Apoptosis
|
Cancer
|
|
Garcinone E is a natural xanthone found in the rind of the mangosteen fruit. Garcinone E induces apoptosis and inhibits cancer cell migration. Garcinone E has anticancer effects on different human cancer cell lines, including colorectal, breast, and hepatocellular carcinomas .
|
-
- HY-117426
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
|
Cancer
|
|
MO-I-500 is a pharmacological of FTO inhibitor with an IC50 of 8.7 μM for the inhibition of purified FTO demethylase catalyzing demethylation of an artificial small methylated substrate. MO-I-500 can be used for the research of rare panresistant triple-negative inflammatory breast cancer .
|
-
- HY-158378
-
|
R-AST-OH
|
Glutaminase
|
Cancer
|
|
Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy .
|
-
- HY-161774
-
|
|
CD73
|
Cancer
|
|
ST80 is an inhibitor for interaction of OTUD4 and CD73. ST80 decreases CD73 protein level, increases CD73 protein turnover, reduces immune evasion of tumor cells, and thus exhibits antitumor efficacy against immunosuppressive triple-negative breast cancer (TNBC) .
|
-
- HY-144070A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(Rac)-ErSO-DFP is a derivative of ErSO-DFP and a selective small molecule Erα biomodulator. (Rac)-ErSO-DFP againsts ERα+ breast cancer (including resistant tumors) by hyperactiving the Erα-dependent a-UPR (extracted from patent WO2022087234A1) .
|
-
- HY-N3995
-
|
|
Apoptosis
Drug Metabolite
|
Cancer
|
|
5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis .
|
-
- HY-173593
-
|
|
Small Interfering RNA (siRNA)
|
Cancer
|
|
Adenosine-3',5'-bisphosphate is a XRN1 inhibitor (IC50: 36 nM). Adenosine-3',5'-bisphosphate can be used in the study of colorectal cancer, breast cancer and lung cancer .
|
-
- HY-100608
-
BMS453
1 Publications Verification
BMS-189453
|
RAR/RXR
|
Cancer
|
|
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ .
|
-
- HY-16247
-
|
HE3235
|
Biochemical Assay Reagents
|
Cancer
|
|
Apoptone, synthetic analogue of 3β-androstanediol, is an orally bioavailable anticancer agent. Apoptone is active in rodent models of prostate and breast cancer . Apoptone is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-Q45780
-
|
|
Akt
|
Cancer
|
|
ZINC00640089 is a specific Lipocalin-2 (LCN2) inhibitor. ZINC00640089 inhibits cell proliferation, cell viability and reduces AKT phosphorylation levels in SUM149 cells. ZINC00640089 has good potential for research in inflammatory breast cancer (IBC) .
|
-
- HY-169579
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
PLK1-IN-11 (Cluster 4, 16953209) is a PLK1 inhibitor, with IC50 of 1 μM. PLK1-IN-11 can be used in research on a variety of cancers, including pancreatic, ovarian, breast, and non-small cell lung carcinoma .
|
-
- HY-148364
-
|
|
Lipocalin Family
Akt
|
Cancer
|
|
ZINC00784494 is a specific Lipocalin-2 (LCN2) inhibitor. ZINC00784494 inhibits cell proliferation, cell viability and reduces AKT phosphorylation levels in SUM149 cells. ZINC00784494 has good potential for research in inflammatory breast cancer (IBC) .
|
-
- HY-143253
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 7 (compound 13) is a potent estrogen receptors (ER) antagonist. Estrogen receptor antagonist 7 has antiproliferative activity against breast and ovarian cancer cells. Anticancer and anti-uterotrophic activities .
|
-
- HY-157297
-
|
|
CDK
|
Cancer
|
|
CDK-IN-13 (compound 32E) is a potent and selective inhibitor of CDK12/cyclinK with an IC50 of 3 nM. CDK-IN-13 inhibits the growth of the HER2-positive breast cancer cell lines .
|
-
- HY-123604A
-
|
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity .
|
-
- HY-P99030
-
|
|
EGFR
|
Cancer
|
|
Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer .
|
-
- HY-144656
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase-IN-1 is a potent and orally active Steroid sulfatase inhibitor with an IC50 of 1.71 nM. Steroid sulfatase-IN-1 shows antitumor activity in vivo. Steroid sulfatase-IN-1 has the potential for the research of breast cancer .
|
-
- HY-P5297
-
|
|
Radionuclide-Drug Conjugates (RDCs)
CXCR
|
Cancer
|
|
DOTA-CXCR4-L is a CXCR4 targeting peptide. DOTA-CXCR4-L can be used in the study of cancers, including glioblastoma and triple-negative breast cancer. NODAGA-LM3 can be labeled with [68Ga]/[177Lu] for the synthesis/research of Radionuclide-Drug Conjugates (RDCs) .
|
-
- HY-155098
-
|
|
SHP2
|
Cancer
|
|
CNBCA is a potent, selective, competitive SHP2 enzyme inhibitor, with the IC50 of 0.87 μM. CNBCA binds to full-length SHP2 and inhibits enzyme activity. CNBCA inhibits pAkt and pERK1/2, and the cell growth of BT474 and MDA-MB468 cells. CNBCA can be used for breast cancer study .
|
-
- HY-153789
-
|
|
PI5P4K
|
Cancer
|
|
PI5P4Kγ-IN-1 (compound 2) is a selective PI5P4Kγ inhibitor. PI5P4Kγ-IN-1 can be used to signal mTORC1 in MCF-7 breast cancer cells and further characterize PI5P4Kγ in the cells .
|
-
- HY-123604
-
TH1834
2 Publications Verification
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity .
|
-
- HY-N3261
-
|
|
AP-1
ERK
STAT
|
Inflammation/Immunology
Cancer
|
|
Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis .
|
-
- HY-N0595R
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Genistin (Standard) is the analytical standard of Genistin. This product is intended for research and analytical applications. Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway .
|
-
- HY-113293BR
-
|
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Cancer
|
|
Estrone sulfate (sodium) (Standard) is the analytical standard of Estrone sulfate (sodium). This product is intended for research and analytical applications. Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). Estrone sulfate can be used for the research of breast cancer .
|
-
- HY-126932
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites .
|
-
- HY-111538
-
|
|
MAGL
|
Cancer
|
|
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .
|
-
- HY-118672
-
|
|
HDAC
MMP
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HNHA is a potent HDAC inhibitor with an IC50 of 100 nM. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer .
|
-
- HY-113161S
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
L-Octanoylcarnitine-d3 is the deuterium-labeled L-Octanoylcarnitine (HY-113161). L-Octanoylcarnitine-d3 is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine-d3 can be used for the research of breast cancer .
|
-
- HY-N8122
-
|
|
Akt
|
Cancer
|
|
24-Methylenecycloartanyl ferulate is a γ-oryzanol compound. 24-Methylenecycloartanyl ferulate promotes parvin-beta expression in human breast cancer cells. 24-Methylenecycloartanyl ferulate is a potential ATP-competitive Akt1 inhibitor (EC50= 33.3μM) .
|
-
- HY-162798
-
|
|
ROCK
|
Cancer
|
|
ROCK2-IN-9 (compound 7u) is a selective ROCK2 inhibitor (IC50=36.8 nM) with anticancer activity. ROCK2-IN-9 inhibits cancer cell migration and invasion by regulating multiple cellular activities of the actin cytoskeleton. ROCK2-IN-9 can be used in breast cancer research .
|
-
- HY-144318
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth .
|
-
- HY-114169
-
|
|
Discoidin Domain Receptor
|
Inflammation/Immunology
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice .
|
-
- HY-112746
-
|
DPC974; GW5638
|
Estrogen Receptor/ERR
|
Cancer
|
|
Etacstil (GW5638) is a estrogen receptor antagonist that displays minimal uterotropic activity in ovariectomized rats and inhibits the agonist activity of Estradiol (HY-B0141), Tamoxifen (HY-13757A) and Raloxifene (HY-13738) in the environment. Etacstil is promising for research of breast cancer and bone protection .
|
-
- HY-139109
-
|
ADS 780WS
|
Fluorescent Dye
Apoptosis
|
Others
|
|
IR-783 (ADS 780WS) is a near-infrared (NIR) heptamethine cyanine fluorescent probe. IR-783 significantly inhibits tumour growth and induces apoptosis in MDA-MB-231 xenograft model. IR-783 can be used to study breast cancer .
|
-
- HY-111522
-
|
|
Sirtuin
c-Myc
|
Cancer
|
|
RK-9123016 is a potent inhibitor of SIRT2. RK-9123016 inhibits the enzymatic activity of SIRT2 with an IC50 value of 0.18 µM but not other human sirtuin members including SIRT1 and SIRT3 at 100 µM. RK-9123016 increases the acetylation level of eukaryotic translation initiation factor 5A (eIF5A), a physiological substrate of SIRT2, and reduces cell viability of human breast cancer cells accompanied with a decrease in c-Myc expression .
|
-
- HY-145341
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer .
|
-
- HY-139662
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers .
|
-
- HY-16189
-
|
NSC 264137; Celiptium
|
DNA Stain
|
Cancer
|
|
Elliptinium acetate (NSC 264137) is a DNA intercalating agent that is highly cytotoxic to L1 210 cells and covalently binds to nucleic acids from L1210 cells. Elliptinium acetate can be used in cancer research, particularly in metastatic breast cancer .
|
-
- HY-172892
-
|
|
PI3K
Reactive Oxygen Species (ROS)
|
Cancer
|
|
PI3K-IN-59 (Compound 3d) is a PI3K inhibitor (IC50: 17.44 μM). PI3K-IN-59 has significant antiproliferative activity and exhibits potent inhibitory effects on breast cancer 4T1 cells (IC50: 3.70 μM) and colon cancer CT26 cells (IC50: 1.98 μM) as well as human breast cancer cells (IC50: 19.72 μM). PI3K-IN-59 exerts a dual anti-tumor mechanism by inhibiting PI3Kα enzymatic activity and triggering the Fenton reaction to generate hydroxyl radicals (•OH). PI3K-IN-59 shows promising anti-4T1 tumor effects and is suitable for synergistic targeting studies in breast and colon cancers .
|
-
- HY-18959
-
|
|
β-catenin
Wnt
|
Cancer
|
|
CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs) .
|
-
- HY-107096
-
|
TP3076
|
Topoisomerase
|
Cancer
|
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-P99205
-
|
|
ADC Antibody
|
Cancer
|
|
Glembatumumab is a fully human IgG2 monoclonal antibody directed against the extracellular structural domain of GPNMB expressed in human breast cancer and melanoma. Glembatumumab can be coupled to the microtubule inhibitor monomethyl auristatin E to form glembatumumab vedotin. Glembatumumab vedotin is an antibody-agent coupling (ADC) with antitumor activity .
|
-
- HY-162105
-
|
|
Cytochrome P450
|
Endocrinology
Cancer
|
|
Aromatase-IN-3 (compound 7d) is an aromatase inhibitor with an IC50 of 54 nM. Through suppressing the conversion of androstenedione to oestrogen caused by aromatase, Aromatase-IN-3 exerts an appreciable tumor growth inhibitory activities against breast cancer cell lines, suggesting its usage for ER+ cancer research .
|
-
- HY-158049
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
Anticancer agent 199 (Compound G-4) induces apoptosis in triple negative breast cancer (TNBC) cells via the mitochondrial pathway through inhibiting EGFR, AKT and MAPK pathways. Anticancer agent 199 also induces Ferroptosis by down-regulating LCN2. Anticancer agent 199 inhibits TNBC cell viability and migration, and induces S phase cell cycle arrest. Anticancer agent 199 is a derivate of cyclin-dependent kinase inhibitor Rocovitine .
|
-
- HY-155664
-
|
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
GPX4-IN-6 (Compound C25) is a GPX4 covalent inhibitor with an IC50 value of 0.13 μM. GPX4-IN-6 (Compound C25) can induce ferroptosis for the research of triple-negative breast cancer (TNBC) .
|
-
- HY-14281R
-
|
|
Others
|
Endocrinology
Cancer
|
|
Trilostane (Standard) is the analytical standard of Trilostane. This product is intended for research and analytical applications. Trilostane (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane is a synthetic nonhormonal steroid. Trilostane can be used for the research of breast cancer and prostate cancer .
|
-
- HY-150505
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer .
|
-
- HY-N7695
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro .
|
-
- HY-158377
-
|
|
CDK
STAT
|
Cancer
|
|
CDK8/19-IN-2 (compound 12) is an orally active and potent cyclin-dependent kinase 8/19 (CDK8 and CDK19) inhibitor, with IC50 values of 2.08 and 2.49 nM, respectively. CDK8/19-IN-2 can be used for acute myeloid leukemia (AML), breast cancer, and lymphoma research .
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-144724
-
|
|
HSP
Apoptosis
|
Cancer
|
|
HSP90-IN-10 (Compound 16s) is a potent inhibitor of HSP90. HSP90-IN-10 exhibits high antiproliferative potency against HCC1954 breast cancer cells with the IC50 value of 6 µM. HSP90-IN-10 does not inhibit the growth of normal epithelial cells. HSP90-IN-10 also induces apoptosis .
|
-
- HY-169019
-
|
|
PI3K
Apoptosis
|
Cancer
|
XJTU-L453 is a PI3Kα inhibitor with an IC50 value of 0.4 nM. XJTU-L453 can inhibit the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. XJTU-L453 can inhibit the PI3K pathway, induce cell cycle arrest, and trigger cell apoptosis (apoptosis). XJTU-L453 also has antitumor activity in MCF7 xenograft mice .
|
-
- HY-N0519R
-
|
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Calycosin (Standard) is the analytical standard of Calycosin. This product is intended for research and analytical applications. Calycosin is a compound that can be isolated from Radix Astragali. Calycosin has strong antioxidant, anti-inflammatory and apoptosis-modulating effects. Calycosin can be used for the research of ovarian cancer and breast cancer .
|
-
- HY-116473
-
|
|
APC
|
Cancer
|
|
CFM-1 is a small molecule antagonist of CARP-1/APC-2 binding with an EC50 value of 4.1 μM. CFM-1 induces G2M cell cycle arrest and suppresses viabilities of human breast cancer cells .
|
-
- HY-18643
-
TZ9
2 Publications Verification
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells .
|
-
- HY-146684
-
|
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research .
|
-
- HY-107096B
-
|
TP3076 TFA
|
Topoisomerase
|
Cancer
|
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein) .
|
-
- HY-155492
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 7 (compound B1) is a potent ERα degrader with an IC50 of 14.6 nM and a DC50 of 9.7 nM, respectively. ERα degrader 7 shows excellent antitumor activity, indicating its potential to evolve as a promising selective estrogen-receptor degrader (SERD) for breast cancer research .
|
-
- HY-13673
-
|
ICI 118630
|
GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
|
-
- HY-111934
-
|
|
Parasite
Potassium Channel
|
Others
Cancer
|
Cymarin, a cardiac glycoside, potently inhibits the Palytoxin (PTX)-induced K + release (IC50=0.42 μM). Cymarin reveals an antitumor activity against breast cancer and pancreatic cancer. Cymarin exhibits antifeedant and growth inhibitory effects as crop protectant .
|
-
- HY-110144
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
|
-
- HY-168894
-
|
|
Ferroptosis
|
Cancer
|
|
CT-1 is a derivative of Cryptotanshinone (HY-N0174). CT-1 is a ferroptosis inducer. CT-1 promotes the interaction between NCOA4 and ferritin by targeting FTH1, triggering ferritinophagy-mediated ferroptosis. CT-1 has anticancer activity against triple-negative breast cancer (TNBC). CT-1 induces ferroptosis in both N2-type tumor-associated neutrophils (TANs) and TNBC cancer cells .
|
-
- HY-164551
-
|
|
VEGFR
STAT
ERK
Apoptosis
|
Cancer
|
YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth .
|
-
- HY-144749
-
|
|
Aldose Reductase
|
Cancer
|
|
AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
|
-
- HY-132194
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent agentgability, can be used for HER + breast cancer research .
|
-
- HY-157210
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-26 (compound 36) is an orally active CDK7 inhibitor (IC50: 7.4 nM). CDK7-IN-26 potently inhibits the growth of triple-negative breast cancer (TNBC) cell line-derived xenograft (CDX) tumors in vivo and inhibits MDA-MB-453 cells in vitro with an IC50 of 0.15 μM .
|
-
- HY-144699
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
|
-
- HY-153728
-
|
|
WDR5
|
Cancer
|
|
WM-586 is a covalent WDR5 inhibitor. WM-586 specifically decreases WDR5 and MYC interaction with an IC50 of 101 nM. WM-586 is used in research on a variety of cancers including neuroblastoma, breast cancer, bladder cancer and colorectal cancer .
|
-
- HY-N3442
-
|
|
JNK
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Juglanin, a occurring flavonoid that can be isolated from crude Polygonum aviculare, is a JNK acticator, with anti-inflammatory, anti-oxidant and anti-tumor activities. Juglanin can induce apoptosis and autophagy on human breast cancer cells .
|
-
- HY-148761
-
|
PSMA I&T; PNT-2002
|
PSMA
|
Cancer
|
|
PSMA I&T is an effective inhibitor of prostate-specific membrane antigen (PSMA). PSMA I&T can be used for SPECT/CT imaging and radionuclide studies in triple-negative breast cancer and prostate cancer (PCa) .
|
-
- HY-13673A
-
|
ICI-118630 acetate
|
GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
|
-
- HY-120275
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
|
-
- HY-146307
-
|
|
TrxR
|
Cancer
|
|
TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins .
|
-
- HY-A0037
-
|
CP-336156
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
|
Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and postmenopausal osteoporosis .
|
-
- HY-N12200
-
|
|
Others
|
Cancer
|
|
Mollicellin I (compound 1) is a depsidone. The growth inhibitory activity of Mollicellin I on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines is not significant, with GI50s >10 μg/mL .
|
-
- HY-160694
-
|
|
PROTACs
|
Cancer
|
|
cBu-Cit-PROTAC BRD4 Degrader-5 is a PROTAC that degrades BRD4 by association with cBu-Cit. cBu-Cit-PROTAC BRD4 Degrader-5 can effectively inhibit BRD4 in HER2 positive and negative breast cancer cell lines. cBu-Cit-PROTAC BRD4 Degrader-5 has a single bond and can be conjugated to an ADC antibody to form a PAC .
|
-
- HY-145953
-
|
|
Acetyl-CoA Carboxylase
|
Cancer
|
|
VY-3-135 is a potent, orally active, and stable ACSS2 inhibitor with an IC50 value of 44 nM. VY-3-135 is specific to ACSS2 among the AcCoA synthetase family of enzymes. VY-3-135 does not inhibit ACSS1 or ACSS3 enzymatic activity. VY-3-135 can be used for the research of breast cancer .
|
-
- HY-169730
-
|
|
Wnt
|
Cancer
|
|
Wnt pathway inhibitor 5 (Compound 28) is wnt pathway inhibitor, with an IC50 value of < 0.003 μΜ. Wnt pathway inhibitor 5 inhibits many cancers, including ovarian teratocarcinoma cancer, breast cancer, osteosarcoma, head and neck squamous carcinoma .
|
-
- HY-126803
-
|
|
Antibiotic
|
Infection
Cancer
|
|
Saquayamycin B (compound 3) is a new angucycline antibiotic. Saquayamycin B has antitumor activities against a human lung (H-460) and a human breast cancer cell line (MCF-7) with GI50 values of 12.2 and 15.2 µM respectively .
|
-
- HY-136699
-
|
|
MMP
FAK
Src
Integrin
|
Cancer
|
|
Excisanin A is a potent anticancer agent. Excisanin A inhibits cell proliferation, migration, adhesion and invasion. Excisanin A decreases the expression of MMP-2, MMP-9, p-FAK, p-Src, integrin β1 protein. Excisanin A has the potential for the research of breast cancer .
|
-
- HY-143247
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-2 is a potent anticancer agent targeting to β-tubulin with an IC50 value of 0.92 μM. Tubulin polymerization-IN-2 shows promising activity against various leukemia, non-small lung, renal, prostate, and breast cancer cell lines .
|
-
- HY-123244
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
YC137 is a potent Bcl-2 antagonist with Kis of 1.3 μM and >100 μM for Bcl-2 and Bcl-xL when assayed in Bis-Tris buffer, respectively. YC137 inhibits the binding of the Bid BH3 peptide to Bcl-2, thus disrupting an interaction essential for the antiapoptotic activity of Bcl-2. YC137 selectively induces apoptosis of Bcl-2-dependent cells. YC137 has the potential for breast cancer research .
|
-
- HY-19671
-
|
SR-45023A; SR 9223i; SK&F-99085
|
Apoptosis
|
Cancer
|
|
Apomine (SR-45023A) is an antineoplastic agent that inhibits the mevalonate/isoprenoid pathway in cholesterol synthesis.
Apomine can accelerate the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR). Apomine can also inhibit the growth of various types of cancer cells, including lung cancer, colon cancer, breast cancer, and skin cancer. In addition, Apomine is able to induce apoptosis in tumor cell lines derived from leukemia, colon cancer, liver cancer, ovarian cancer, and breast cancer .
|
-
- HY-19731
-
|
MiR-544 Inhibitor 1
|
MicroRNA
Apoptosis
|
Cancer
|
|
SID 3712249 (MiR-544 Inhibitor 1) is a miR-544 biogenesis inhibitor. SID 3712249 binds directly to the precursor miRNA. SID 3712249 blocks production of the mature microRNA and decreases miR-544, HIF-1α, and ATM transcripts. SID 3712249 can be used in the research of cancers, such as breast cancer .
|
-
- HY-P991342
-
|
PCA062 antibody
|
Cadherin
|
Cancer
|
|
CQY684 (PCA062 antibody) is a human monoclonal antibody (mAb) targeting CDH3/P-cadherin. CQY684 stabilizes the X-dimer of P-cadherin, promoting its endocytosis and directing it to lysosomal degradation. CQY684 can be used in Breast, esophageal, and head and neck cancers research .
|
-
- HY-123024
-
|
BL-S-640; SK&F 60771
|
Apoptosis
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Cefatrizine (BL-S-640) is an orally active and broad-spectrum cephalosporin antibiotic. Cefatrizine is also a eEF2K inhibitor, with anti-proliferative activity in human breast cancer cells, which could induce ER stress, leading to cell death. Cefatrizine can be used in studies of cancer and bacterial infection .
|
-
- HY-B0412
-
Estriol
4 Publications Verification
Oestriol
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Cancer
|
|
Estriol (Oestriol), an orally active estrogen, is a ERα and ERβ agonist. Estriol is a potent GPR30 antagonist in estrogen receptor-negative breast cancer cells. Estriol can ameliorate disease severity through immunomodulatory mechanisms that decrease tissue inflammation. Estriol has powerful proconvulsant effects .
|
-
- HY-172801
-
|
|
CD73
|
Cancer
|
|
PSB-24000 (Compound 27) is a selective ecto-5'-nucleotidase (CD73) inhibitor with a Ki value of 563 nM against human CD73 (Ki= 481 nM at membrane-bound CD73 in triple-negative breast cancer cells). PSB-24000 interferes with CD73's recognition and action on the substrate AMP, and prevents the generation of immunosuppressive and cancer-promoting adenosine from AMP. PSB-24000 is promising for research of cancers .
|
-
- HY-173165
-
|
3-O-(6-Bromo-D-mannosyl)-28-acylamino-n-caproate methyl oleanolic acid
|
Phosphatase
Apoptosis
|
Cancer
|
|
OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo .
|
-
- HY-19822
-
|
RAD1901
|
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
- HY-19822A
-
|
RAD1901 dihydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant dihydrochloride also can inhibit growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
- HY-168704
-
|
|
YAP
TAM Receptor
Survivin
|
Cancer
|
|
YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that inhibits the interaction between YAP/TAZ and TEAD. YAP/TAZ-TEAD-IN-2 suppresses the transcriptional activity of TEAD, with an IC50 of 1.2 nM. YAP/TAZ-TEAD-IN-2 inhibits YAP/TAZ-TEAD target genes expression (Cyr61, CTGF, AXL and Survivin) and breast cancer cell proliferation .
|
-
- HY-108232
-
MK-2206
Maximum Cited Publications
368 Publications Verification
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. MK-2206 has anticancer activities .
|
-
- HY-163889
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
Ferroptosis/apoptosis inducer-1 (compound 4d) is a dual inducer of apoptosis and ferroptosis. Ferroptosis/apoptosis inducer-1 induces apoptosis and ferroptosis by reducing mitochondrial membrane potential and downregulating GPX4. Ferroptosis/apoptosis inducer-1 can significantly inhibit the proliferation and metastasis of triple-negative breast cancer (TNBC) both in vitro and in vivo, playing an important role in cancer research .
|
-
- HY-113787
-
|
|
Ack1
JAK
|
Cancer
|
|
(R)-9b is a potent inhibitor of ACK1 tyrosine kinase (IC50=56 nM) with anticancer activity. (R)-9b exhibits selectivity for ACK1 but has inhibitory effects on JAK family kinases JAK2 and Tyk2. (R)-9b can be used in the study of hormone-regulated cancers such as prostate and breast cancer .
|
-
- HY-128979
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Deruxtecan analog 2 (example 9 P3) is a Deruxtecan (HY-13631E) analog. Deruxtecan analog 2 is a agent-linker conjugate composed of Camptothecin (HY-16560) and a linker. Camptothecin (CPT) is a Topo I inhibitor with antineoplastic activity against colorectal, breast, lung and ovarian cancers. Deruxtecan analog 2 can be used for the preparation anti-FGFR2 ADC .
|
-
- HY-170648
-
|
|
Thymidylate Synthase
Apoptosis
PI3K
STAT
Bcl-2 Family
|
Cancer
|
|
TS-IN-5 (Compound 15) is a thymidylate synthase (TS) inhibitor. TS-IN-5 induces Apoptosis by modulating Bax, BCL-2, PI3K, and STAT1 proteins. TS-IN-5 shows antitumor effects against liver, breast and colon cancers .
|
-
- HY-N2098
-
|
|
NF-κB
|
Cancer
|
|
Obtusifolin, isolated from the seeds of Cassia obtusifolia, regulates the gene expression and production of MUC5AC mucin in airway epithelial cells via inhibiting NF-kB pathway . Obtusifolin suppresses phthalate esters-induced breast cancer bone metastasis by targeting parathyroid hormone-related protein .
|
-
- HY-P991378
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
MORAb-066 is a human monoclonal antibody (mAb) targeting CD142/F3/TF. MORAb-066 can be used in Breast cancer, Colorectal cancer, Non-small cell lung cancer and Pancreatic cancer research .
|
-
- HY-148595
-
|
|
Cytochrome P450
|
Cancer
|
|
Antitumor agent-88 exhibits potent antimitotic activity and arrests cell in the G2/M phase. Antitumor agent-88 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells. Antitumor agent-88 is also a competitive inhibitor of CYP1A1 (Ki: 1.4 μM) .
|
-
- HY-112096
-
eCF506
3 Publications Verification
NXP900
|
Src
|
Cancer
|
|
eCF506 (NXP900) is a highly potent and orally active YES1/SRC kinase inhibitor with an IC50 of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer .
|
-
- HY-P99682
-
|
hLIV22
|
ADC Antibody
|
Cancer
|
|
Ladiratuzumab (hLIV22) is a humanized monoclonal antibody against zinc transporter LIV-1/ZIP6. Ladiratuzumab is conjugated to MMAE (HY-15162) via a cleavable dipeptide linker to synthesize an antibody-drug conjugate (ADC) Ladiratuzumab vedotin (HY-P99683). Ladiratuzumab vedotin selectively targets LIV-1 protein overexpressed on the surface of tumor cells, enters cells through antibody-mediated receptor endocytosis, releases MMAE to inhibit microtubule polymerization, and kills adjacent tumor cells with a bystander effect. Ladiratuzumab can be used in the study of solid tumors such as metastatic triple-negative breast cancer (mTNBC) .
|
-
- HY-151110
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK12/13 Degrader-1 (7f) is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-161509
-
|
|
mTOR
|
Cancer
|
|
PT-88 is a highly selective inhibitor of mTOR (Mammalian target of rapamycin) (IC50=1.2 nM). PT-88 inhibits both mTORC1 and mTORC2 complexes, both of which are active forms of mTOR protein kinases and are closely associated with cell growth, proliferation, and survival. PT-88 can be used to study the role of mTOR in tumorigenesis and development, especially in the treatment of breast cancer .
|
-
- HY-103457
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
|
-
- HY-P991316
-
|
DX-2400; DX-2410
|
MMP
TGF-β Receptor
TGF-beta/Smad
NO Synthase
|
Cancer
|
|
KD014 (DX-2400) is a human monoclonal antibody (mAb) targeting MMP14 (Ki: 0.9 nM). KD014 inhibits TGFβ and SMAD2/3 activity, increases macrophage numbers and iNOS expression, and shifts macrophage phenotype toward anti-tumor M1-like. KD014 has anti-tumor activity in three different tumor models (MDA-MB-231, MDA-MB-435, and PC3). KD014 can be used in breast cancer research .
|
-
- HY-157169
-
|
AMU302
|
Pim
mTOR
Akt
PI3K
|
Cancer
|
|
IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629) .
|
-
- HY-156152A
-
|
|
Histone Methyltransferase
PROTACs
|
Cancer
|
|
CARM1 degrader-1 hydrochloride is the hydrochloride salt form of CARM1 degrader-1 (HY-156152). CARM1 degrader-1 hydrochloride is a PROTAC degrader for co-activator associated argininemethyltransferase 1 (CARM1), which degrades CARM1 in a VHL- and proteasome-dependent manner with a DC50 of 8.1 nM. CARM1 degrader-1 hydrochloride inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155, and thus inhibits breast cancer cell migration .
|
-
- HY-133017
-
|
SAR439859
|
Estrogen Receptor/ERR
|
Cancer
|
|
SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER + breast cancer.
|
-
- HY-147098
-
|
|
PROTACs
FKBP
|
Cancer
|
|
dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12 F36V). FKBP12 F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC) .
|
-
- HY-18953
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .
|
-
- HY-155070
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
SRE-II, an amide derivative, is an activatable photosensitizer for photodynamic cancer research with decreased fluorescence and photosensitizing capabilities. SRE-II can be further converted into the active photosensitizer SDU Red via carboxylesterase-catalyzed amide bond cleavage. SRE-II induces DNA damage and cell apoptosis in the presence of light. SRE-II can act as a promising theranostic agent for triple-negative breast cancer .
|
-
- HY-144307
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .
|
-
- HY-147556
-
|
|
Potassium Channel
|
Cancer
|
|
SK3 Channel-IN-1 (compound 7a) is a potent and specific SK3 channel modulator. SK3 Channel-IN-1 has efficient effect on breast cancer MDA-MB-435 cell migration while exhibiting low cytotoxicity in other cell lines. SK3 Channel-IN-1 can modulate ion channels’activity in cancer .
|
-
- HY-14281S
-
|
Win 24540-d3
|
Isotope-Labeled Compounds
|
Others
|
|
Trilostane-d3 is the deuterium-labeled Trilostane (HY-14281). Trilostane-d3 (Win 24540) is a competitive and orally active 3-β-hydroxysteroiddehydrogenase (3β-HSD) inhibitor. Trilostane-d3 is a synthetic nonhormonal steroid. Trilostane-d3 can be used for the research of breast cancer and prostate cancer .
|
-
- HY-101119
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GLL398 is a potent, orally bioavailable selective estrogen receptor degrader (SERD) with an IC50 value of 1.14 nM. GLL398 shows a strong dose-dependent binding to ER with a mutation at Y537S (IC50=29.5 nM). GLL398 blocks tumor growth in xenograft models of breast cancer.
|
-
- HY-151110A
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK12/13 Degrader-1 (7f) TFA is a highly selective cell cycle protein-dependent kinase CDK12/CDK13 dual degrader with the DC50 values of 2.2 nM and 2.1 nM, respectively. PROTAC CDK12/13 Degrader-1 TFA has anti-proliferative activity and can be used in breast cancer research .
|
-
- HY-155179
-
|
|
PAK
HDAC
|
Cancer
|
|
ZMF-23 is a PAK1/HDAC6 dual inhibitor. ZMF-23 inhibits PAK1 and HDAC6 regulated aerobic glycolysis and migration. ZMF-23 induces TNF-α-regulated necroptosis, and further enhances apoptosis. ZMF-23 inhibits the Warburg effect and cell migration. ZMF-23 can be used for research of triple-negative breast cancer (TNBC) .
|
-
- HY-163535
-
|
|
HDAC
DNA Methyltransferase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs) .
|
-
- HY-162006
-
|
|
PKC
Pim
|
Cancer
|
|
Pim-1 kinase inhibitor 8 (compound 12) is a potent inhibitor of Pim-1 kinase with an IC50 of 14.3 nM. Pim-1 kinase inhibitor 8 has potent cytotoxicity against MCF-7 and HepG2 cells with IC50s of 0.5 and 5.27 μM, respectively. Pim-1 kinase inhibitor 8 can used in study breast cancer .
|
-
- HY-164763
-
|
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
SHR-A1201 is a HER2-targeting antibody-drug conjugate (ADC). SHR-A1201 is composed of a humanized anti-HER2 antibody (HY-P9907), a linker SMCC (HY-42360), and a microtubulin inhibitor payload Mertansine (HY-19792). SHR-A1201 can be used for research in HER2-positive breast cancer .
|
-
- HY-130851
-
|
|
HSP
|
Cancer
|
|
HS-27, a fluorescently-tethered Hsp90 inhibitor, assays surface Hsp90 expression on intact tissue specimens. HS-27 is made up of the core elements of SNX-5422, an Hsp90 inhibitor, tethered via a PEG linker to a fluorescein derivative (fluorescein isothiocyanate or FITC), that binds to ectopically expressed Hsp90. HS-27 has potential use in a see-and-treat paradigm in breast cancer .
|
-
- HY-P991292
-
|
|
ADC Antibody
|
Cancer
|
|
AB-3A4 is a human IgG1 monoclonal antibody (mAb) targeting KAAG1. AB-3A4 can be used in the study of ovarian cancer, triple-negative breast cancer, and prostate cancer. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-P10686
-
|
|
EGFR
|
Cancer
|
|
CH401 peptide is a HER2-derived antigen peptide. After being bound to the artificial viral capsid by a self-assembled β-cyclic peptide, CH401 peptide is encapsulated in a lipid bilayer containing the lipid adjuvant α-GalCer, and can be studied as a self-adjuvant anti-breast cancer vaccine candidate .
|
-
- HY-161117
-
|
|
RSV
|
Cancer
|
|
AD-8007 is an acetyl CoA synthase 2 (ACSS2) inhibitor that can cross the blood-brain barrier. AD-8007 can significantly reduce lipid storage and cell colony formation in vitro models, and increase tumor cell death. AD-8007 has anti-cancer activity and can be used in the research of breast cancer .
|
-
- HY-126222
-
|
|
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
MitoTam bromide, hydrobromide, a Tamoxifen derivative , is an electron transport chain (ETC) inhibitor. MitoTam bromide, hydrobromide reduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology . MitoTam bromide, hydrobromide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells .
|
-
- HY-P99974
-
|
Nanoparticle albumin-bound Paclitaxel; Nanoparticle albumin-bound ABI-007
|
Microtubule/Tubulin
Apoptosis
Autophagy
|
Cancer
|
|
Nab-Paclitaxel (Nanoparticle albumin-bound Paclitaxel) is an albumin-bound nanoparticle formulation of Paclitaxel (HY-B0015). Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel, in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel is a solvent-free taxane with higher response rates and improved tolerability. Nab-Paclitaxel displays less toxicity and greater antitumor activity. Nab-Paclitaxel is more readily available for tumor cell uptake in three rhabdomyosarcoma, seven neuroblastoma cell lines, and one ostersarcoma cell line Nab-Paclitaxel can be studied in cancer research for example breast cancer and pediatric solid tumors .
|
-
- HY-18619
-
YL-109
2 Publications Verification
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
YL-109 is an antitumor agent that can induce carboxyl terminus of Hsp70-interacting protein (CHIP) expression through aryl hydrocarbon receptor (AhR) signaling. YL-109 has ability to inhibit breast cancer cell growth and invasiveness .
|
-
- HY-156403
-
|
|
Topoisomerase
|
Cancer
|
|
AuM1Phe, an N-Heterocyclic carbene (NHC) metal complexe, blocks the human topoisomerase I activity and actin polymerization reaction. AuM1Phe affects the growth of MDA-MB-231 breast cancer cells, with an IC50 value of 1.2 μM .
|
-
- HY-119437
-
FLTX1
2 Publications Verification
|
Estrogen Receptor/ERR
|
Cancer
|
|
FLTX1 is a fluorescent Tamoxifen derivative that can specifically label intracellular Tamoxifen-binding sites (estrogen receptors) under permeabilized and non-permeabilized conditions. FLTX1 exhibits the potent antiestrogenic properties of Tamoxifen in breast cancer cells. FLTX1 is devoid of the estrogenic agonistic effect on the uterus .
|
-
- HY-162312
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
|
-
- HY-149085A
-
|
|
RAR/RXR
|
Cancer
|
|
(E)-XS-060 is an isomer of XS-060. XS-060 is a RXRα antagonist. XS-060 inhibits pRXRα-PLK1 interaction. XS-060 induces RXRα-dependent mitotic arrest. XS-060 exhibits good antitumor activity against breast cancer, lung adenocarcinoma, and liver cancer .
|
-
- HY-13686
-
PQ401
2 Publications Verification
|
IGF-1R
Apoptosis
|
Cancer
|
|
PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis .
|
-
- HY-164762
-
|
SHR-A1811
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Trastuzumab rezetecan (SHR-A1811) is a HER2-targeting antibody-drug conjugate (ADC). Trastuzumab rezetecan is composed of a humanized anti-HER2 antibody (HY-P9907), a cleavable linker MC-Gly-Gly-Phe-Gly (HY-44246), and a topoisomerase I inhibitor payload Rezetecán (HY-147408). Trastuzumab rezetecan can be used for research in HER2-positive breast cancer .
|
-
- HY-108447
-
|
|
Ser/Thr Protease
SARS-CoV
PAI-1
|
Infection
Cancer
|
|
BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer .
|
-
- HY-149540
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
CTL-06 is an inhibitor of Fatty Acid Synthase (FASN) (IC50: 3 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
|
-
- HY-131339
-
SP-96
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC) .
|
-
- HY-156419A
-
|
|
PARP
|
Cancer
|
|
PARP7-IN-16 free base is the free base form of PARP7-IN-16 (HY-156419). PARP7-IN-16 free base is a selective and orally active inhibitor of PARP-1/2/7, with IC50s of 0.94, 0.87 and 0.21 nM, respectively. PARP7-IN-16 can be used for the research of breast cancer and prostate cancer .
|
-
- HY-151630
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
|
-
- HY-10357
-
|
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 free base is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206 free base. MK-2206 free base has anticancer activities .
|
-
- HY-125535
-
|
|
AMPK
mTOR
Autophagy
Atg8/LC3
|
Cancer
|
|
OSU-53 is an orally active AMPK activator (EC50: 0.3 μM) and a direct mTOR inhibitor. OSU-53 induces autophagy and increases conversion of LC3 I to LC3 II. OSU-53 also modulates energy homeostasis by suppressing fatty acid biosynthesis and shifting the metabolism to oxidation by up-regulating the expression of PGC1α and NRF-1. OSU-53 has antitumor activity in various tumor models, such as breast cancer and thyroid cancer .
|
-
- HY-N6796
-
|
|
Antibiotic
Farnesyl Transferase
Ras
Apoptosis
Phospholipase
TNF Receptor
Atg8/LC3
|
Infection
Inflammation/Immunology
Cancer
|
|
Manumycin A is a polyketide antibiotic and an inhibitor of thioredoxin reductase 1 (TrxR-1). Manumycin A can inhibit the growth of breast cancer cells and exert its anti-tumor activity through LC3. Manumycin A can downregulate the release of pro-inflammatory cytokines in human monocytes stimulated by TNF α, and has potential anti-inflammatory activity. Manumycin A can inhibit the Ras/Raf/ERK1/2 signaling and hnRNP H1 in castration resistant prostate cancer cells to suppress exosome biogenesis and secretion .
|
-
- HY-149633
-
|
|
EGFR
Dihydrofolate reductase (DHFR)
Apoptosis
|
Cancer
|
|
EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells .
|
-
- HY-A0038
-
|
CP-336156 tartrate
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
Lasofoxifene (CP-336156) tartrate is an orally active and selective estrogen receptor modulator (SERM) . Lasofoxifene tartrate exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene tartrate can be used for the research of breast cancer and postmenopausal osteoporosis .
|
-
- HY-132305
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth .
|
-
- HY-168099
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 10 is a selective and orally active estrogen receptor α (ERα) degrader. ERα degrader 10 exhibits potent ERα binding affinity (IC50 of 24.0 nM) and degradation ability (EC50 of 5.3 nM). ERα degrader 10 degrades ERα through the proteasome-mediated pathway. ERα degrader 10 can be used for the study of breast cancer .
|
-
- HY-158439
-
|
|
JAK
STAT
|
Cancer
|
|
anti-TNBC agent-7 (Compound 13c) possesses anticancer activity, serving as a molecular probe to recognize and regulate the signal transduction of the USP21/JAK2/STAT3 axis, exhibiting nanomolar-level cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC) .
|
-
- HY-N6885
-
|
|
Others
|
Cancer
|
|
Puerarin-4'-O-β-D-glucopyranoside (compound 8) is a isoflavone from Pueraria lobata root (PLR). Puerarin-4'-O-β-D-glucopyranoside has estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
|
-
- HY-163757
-
|
|
PROTACs
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
PROTAC PD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with a notable PD-L1 protein degradation capability. PROTAC PD-L1 degrader-1 shows potent PD-L1 degradation in 4T1 cells with a DC50 of 0.609 μM. PROTAC PD-L1 degrader-1 can be used for the study of breast cancer. (Blue: CRBN ligand (HY-150839), Black: linker; Pink: PD-L inhibitor (HY-19745)) .
|
-
- HY-19822S2
-
|
RAD1901-d10
|
Estrogen Receptor/ERR
Isotope-Labeled Compounds
|
Cancer
|
|
Elacestrant-d10 is the deuterium labeled of Elacestrant (HY-19822). Elacestrant is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant also inhibits growth of ER + breast cancer cell lines in vitro and in vivo .
|
-
- HY-151624
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP-2-IN-2 (compound 27) is a PARP 2 inhibitor with an IC50 value of 0.057 μM. PARP-2-IN-2 induces cell cycle arrest and apoptosis of MCF-7 breast cancer cells. PARP-2-IN-2 can be used for the research of cancer .
|
-
- HY-14833
-
|
TP300
|
Topoisomerase
|
Cancer
|
|
Atiratecan (TP300) is a proagent of camptothecin analog CH0793076 (HY-107096). Atiratecan does not inhibit acetylcholinesterase (AChE) activities. Atiratecan shows antitumor activity against both breast cancer resistance protein (BCRP)-positive and -negative xenografts in mouse xenograft models .
|
-
- HY-126222A
-
|
|
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
MitoTam iodide, hydriodide is a Tamoxifen derivative , an electron transport chain (ETC) inhibitor, spreduces mitochondrial membrane potential in senescent cells and affects mitochondrial morphology .
MitoTam iodide, hydriodide is an effective anticancer agent, suppresses respiratory complexes (CI-respiration) and disrupts respiratory supercomplexes (SCs) formation in breast cancer cells . MitoTam iodide, hydriodide causes apoptosis .
|
-
- HY-115947
-
|
|
Drug Derivative
|
Cancer
|
|
Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM .
|
-
- HY-135046
-
|
|
DNA/RNA Synthesis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
MTOB sodium is a potent C-terminal binding protein (CtBP) inhibitor. MTOB sodium attenuates repetitive head injury-elicited neurologic dysfunction and neuroinflammation via inhibition of the transactivation activity of CtBP1 and CtBP2. MTOB sodium antagonizes the transcriptional regulatory activity of CtBP1 and CtBP2 by eviction from their target promoters in breast cancer cell lines .
|
-
- HY-163002
-
|
|
Ferroptosis
|
Cancer
|
|
viFSP1 is a species-independent FSP1 inhibitor. viFSP1 directly inhibits FSP1 by targeting the highly conserved NAD(P)H binding pocket of FSP1. viFSP1 can induce Ferroptosis in FSP1-dependent cells. viFSP1 can be used in renal and breast cancer research .
|
-
- HY-122112
-
|
|
Sigma Receptor
|
Cancer
|
|
CM572 is a selective irreversible partial sigma-2 receptor agonist. CM572 has antitumor activity. CM572 induces dose-dependent cell death, with an EC50 of 7.6 μM in SK-N-SH neuroblastoma cells. CM572 can be used for the research of kinds of diseases such as neuroblastoma, breast cancer .
|
-
- HY-103100
-
-
- HY-117523
-
|
(Z)-Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
(Z)-RG-13022 is a tyrosine kinase (TK) inhibitor, which inhibits preferentially the TK activity of the EGF receptor and inhibits EGF-stimulated growth of cultured cells. (Z)-RG-13022 exerts an IC50 of 11 μM for DNA synthesis in the HN5 cells, which is 3 times more potent than (E)-RG-13022 (IC50=38 μM). (Z)-RG-13022 can be used for research of breast cancer cells .
|
-
- HY-119948
-
|
|
Cyclin G-associated Kinase (GAK)
MDM-2/p53
|
Cancer
|
AKCI is a type of AURKC-IκBα interaction inhibitor, with an IC50 value of 24.9 μM. In MDA-MB-231 cells, AKCI can induce G2/M cell cycle arrest by regulating the p53/p21/CDC2/cyclin B1 pathway, inhibit cell migration and invasion, and reduce colony formation and tumor growth. AKCI can be used for research on breast cancer .
|
-
- HY-149541
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
CTL-12 is an inhibitor of fatty acid synthase (FASN) (IC50: 2.5 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
|
-
- HY-112591
-
|
|
Apoptosis
HIV
Wnt
Bcl-2 Family
|
Cancer
|
|
NSC260594 induces Apoptosis. NSC260594 binds the shallow groove of the Mcl-1 protein, and inhibits Mcl-1 expression through down-regulation of Wnt signaling proteins. NSC260594 can also recognize G9-G10-A11-G12 RNA tetraloop of HIV and prevent the binding of the Gag protein within the 5’-UTR. NSC260594 inhibits tumor growth, and can be used for research of Triple-negative breast cancers (TNBCs) .
|
-
- HY-143616
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-7 is a potent inhibitor of EZH2. EZH2 overexpression or mutations in the SET region (Y641F, Y641N, A687V, A677G point mutations) all lead to abnormal elevation of H3K27me3 and promote the growth and development of many types of tumors, such as breast cancer, prostate cancer, leukemia, etc. EZH2-IN-7 has the potential for the research of cancer diseases (extracted from patent WO2021129629A1, compound 259) .
|
-
- HY-120234
-
|
Z-Leu-Leu-Nle-CHO; GSII
|
γ-secretase
Proteasome
Apoptosis
|
Cancer
|
|
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia .
|
-
- HY-146433
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 55 is a potent anticancer agent. Anticancer agent 55 shows anticancer activity via reducing the cell viability and cell migration in a dose-dependent manner. Anticancer agent 55 induces apoptosis. Anticancer agent 55 has the potential for the research of prostate cancer and breast cancer .
|
-
- HY-149354
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora kinase-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora kinase-IN-4 can be used for research of triple negative breast cancer (TNBC) .
|
-
- HY-164992
-
|
MRG002; Trastuzumab MMAE
|
Antibody-Drug Conjugates (ADCs)
EGFR
Microtubule/Tubulin
|
Cancer
|
|
Trastuzumab vedotin (MRG002) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab vedotin is composed of a humanized anti-HER2 antibody Trastuzumab (HY-P9907), an enzymatically cleavable peptide-linker Valine-citrulline, a tubulin inhibitor Monomethyl auristatin E (MMAE; HY-15162). Trastuzumab vedotin can be used for the research of HER2-positive breast cancer .
|
-
- HY-149497
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-19 (Compound 14g) is a HDAC6 inhibitor (IC50: 2.68 nM). HDAC6-IN-19 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 61.6 nM, 98.7 nM and 103 nM. HDAC6-IN-19 potently inhibits multiple cancer cell proliferation, including leukemia, colon cancer, melanoma, and breast cancer cell lines .
|
-
- HY-B0723
-
|
FC-1271a
|
Estrogen Receptor/ERR
Caspase
|
Neurological Disease
Endocrinology
Cancer
|
|
Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer .
|
-
- HY-N2666
-
|
|
VEGFR
|
Cancer
|
|
5α-Hydroxycostic acid, a eudesmane-type sesquiterpene, is isolated from the herb Laggera alata. 5α-Hydroxycostic acid inhibits angiogenesis and suppresses breast cancer cell migration through regulating VEGF/VEGFR2 and Ang2/Tie2 pathways .
|
-
- HY-122665
-
|
|
MELK
DYRK
Pim
mTOR
CDK
GSK-3
RIP kinase
|
Cancer
|
|
HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research .
|
-
- HY-134601
-
|
|
HuR
|
Cancer
|
|
KH-3 is a potent RNA-binding protein Hu antigen R (HuR) inhibitor with an IC50 value of 0.35 μM. KH-3 has anti-proliferative activity. KH-3 suppresses breast cancer cell invasion as well as delays the initiation of lung colonies by disrupting HuR-FOXQ1 mRNA interaction .
|
-
- HY-N0292
-
|
|
Cytochrome P450
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
|
-
- HY-13299
-
MK-8033
2 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-13299A
-
|
|
c-Met/HGFR
|
Cancer
|
|
MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC50s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs) .
|
-
- HY-144691
-
|
|
PROTACs
CDK
|
Cancer
|
|
PP-C8 is a potent and selective PROTAC CDK12-Cyclin K degrader. PP-C8 induces CDK12-Cyclin K degradation with DC50s of 416 and 412 nM for CDK12 and Cyclin K, respectively. PP-C8 demonstrates profound synergistic antiproliferative effects with PARP inhibitor in triple-negative breast cancer (TNBC) .
|
-
- HY-P10593
-
|
|
Transmembrane Glycoprotein
Influenza Virus
|
Cancer
|
|
Influenza A NP (383-391) (HLA-B27) is a peptide sequence derived from tetanus toxin. Influenza A NP (383-391) (HLA-B27) is a broadly immunogenic CD4+ T helper cell epitope that enhances CD8+ cytotoxic T lymphocyte (CTL) responses. Influenza A NP (383-391) (HLA-B27) can be used in breast cancer research .
|
-
- HY-145749
-
|
|
PARP
|
Cancer
|
|
PARPYnD is a PARP enzyme photoaffinity probe (AfBP) based on the triple PARP1/2/6 inhibitor AZ9482 (HY-119653), which induces breast cancer Formation of multipolar spindles (MPS) in cells. PARPYnD inhibits PAPR wih IC50 of 38 nM (PARP1), 6 nM (PARP2), 230 nM (PARP6), respectively. PARPYnD enriches recombinant PARP6 incorporated into cell lysates and inhibits PARP6 in cell-free assays, but it does not label PARP6 in intact cells .
|
-
- HY-155113
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively .
|
-
- HY-113205
-
|
15-keto-PGE2
|
Endogenous Metabolite
Prostaglandin Receptor
STAT
PPAR
|
Cancer
|
|
15-keto-Prostaglandin E2 is an endogenous metabolite. 15-keto-Prostaglandin E2 inhibits STAT3 activation by binding to its Cys259 residue. 15-keto-Prostaglandin E2 can bind and stabilize EP2 and EP4 receptor. 15-keto-Prostaglandin E2 inhibits breast cancer cell growth and progression. 15-keto-Prostaglandin E2 activates PPAR-γ and promotes fungal growth .
|
-
- HY-119694
-
|
|
Others
|
Cancer
|
|
Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively .
|
-
- HY-149480
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- HY-N2098R
-
|
|
NF-κB
|
Cancer
|
|
Obtusifolin (Standard) is the analytical standard of Obtusifolin. This product is intended for research and analytical applications. Obtusifolin, isolated from the seeds of Cassia obtusifolia, regulates the gene expression and production of MUC5AC mucin in airway epithelial cells via inhibiting NF-kB pathway . Obtusifolin suppresses phthalate esters-induced breast cancer bone metastasis by targeting parathyroid hormone-related protein .
|
-
- HY-136244
-
|
|
TGF-β Receptor
|
Cancer
|
|
PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer .
|
-
- HY-148334
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC) .
|
-
- HY-124822
-
COH-SR4
1 Publications Verification
|
AMPK
|
Metabolic Disease
Cancer
|
|
COH-SR4 is an AMPK activator. COH-SR4 shows potent anti-proliferative activities against leukemia, melanoma, breast and lung cancers. COH-SR4 inhibits adipocyte differentiation via AMPK activation. COH-SR4 can be used for the research of obesity and related metabolic disorders .
|
-
- HY-158251
-
|
|
Others
|
Cancer
|
|
BIBD-300 is a PARP-1 imaging agent with high affinity for PARP-1. BIBD-300 can accurately localize C6 and U87MG tumors, which can be used for research in the diagnosis of breast cancer, prostate cancer, glioma, and liver cancer .
|
-
- HY-147165
-
|
|
YAP
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P99683
-
|
SGN-LIV1A
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Ladiratuzumab vedotin (SGN-LIV1A) is a LIV-1 targeting antibody drug conjugate (ADC) (IC50: 5.6 nM for LIV-1). Ladiratuzumab vedotin consists of humanized IgG1 monoclonal antibody, MMAE and a protease-cleavable linker. Ladiratuzumab vedotin can drive immunogenic cell death (ICD) to elicit an immune response. Ladiratuzumab vedotin can be used for research of breast cancer .
|
-
- HY-172172
-
|
|
Thymidylate Synthase
Apoptosis
|
Cancer
|
|
TS-IN-6 (Compound 10) is a thymidylate synthase (TS) inhibitor with an IC50 value of 0.54 μM, demonstrating significant antiproliferative activity. TS-IN-6 induces G1 phase cell cycle arrest and apoptosis (marked by substantial increases in both early and late apoptotic rates) and shows potential for research on cancers such as colon, breast, and liver cancers .
|
-
- HY-50767C
-
|
PD-0332991 hydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-50767B
-
|
PD-0332991 dihydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-50767
-
|
PD 0332991
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-122665A
-
|
|
MELK
DYRK
Pim
mTOR
CDK
GSK-3
RIP kinase
|
Cancer
|
|
HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research .
|
-
- HY-168072
-
|
|
Interleukin Related
Apoptosis
Autophagy
|
Cancer
|
|
GP130-IN-1 (compound 49) is a potent GP130 inhibitor with significant in vitro antitumor activity and higher selectivity than Bazedoxifene (HY-A0031). GP130-IN-1 induces ultrastructural changes in cells, causing cell cycle arrest in the G0/G1 phase in a time-dependent manner and triggering apoptosis and autophagy. GP130-IN-1 can be used in the study of triple-negative breast cancer .
|
-
- HY-168850
-
|
|
Apoptosis
|
Cancer
|
|
MTDH-SND1 blocker 2 (compound C19) is a potent MTDH-SND1 blocker with an IC50 value of 487 nM. MTDH-SND1 blocker 2 binds to the SND1 protein with a Kd value of 279 nM. MTDH-SND1 blocker 2 degrades SND1 protein. MTDH-SND1 blocker 2 shows antiproliferative activity and induces apoptosis. MTDH-SND1 blocker 2 has the potential for the research of breast cancer .
|
-
- HY-W267205
-
|
|
17β-HSD
|
Endocrinology
Cancer
|
|
3-Acetyl-7-Hydroxycoumarin (Compound 2) is a high selective 17-beta-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitor. 3-Acetyl-7-Hydroxycoumarin shows a significant improvement of the inhibitory potency, with 57% inhibition of 17β-HSD1 at 6 μM. 3-Acetyl-7-Hydroxycoumarin is promising for research of hormone-dependent diseases, such as breast cancer and endometriosis .
|
-
- HY-172621
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-159 (compound 12), a dihydropyrimidine, is a potent EGFR inhibitor with an IC50 value of 29.00 nM. EGFR-IN-159 exhibits dose-dependent inhibition against EGFR and HER2. EGFR-IN-159 shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 has no BBB permeation. EGFR-IN-159 shows appreciable anti-cancer activity .
|
-
- HY-176066A
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
c-Myc inhibitor 16 iodide (Compound W11) is a selective c-Myc G-quadruplex (c-Myc G4) inhibitor. c-Myc inhibitor 16 iodide inhibits the transcription and translation of the c-Myc gene, disrupts the tumor cell cycle, arrests cell growth in the G0/G1 phase and activates the mitochondrial apoptosis pathway to induce early apoptosis of cancer cells. c-Myc inhibitor 16 iodide is promising for research of breast cancer .
|
-
- HY-152159
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo .
|
-
- HY-152208
-
|
|
SHP1
SHP2
|
Cancer
|
|
BPDA2 is a highly selective and competitive active site SHP2 inhibitor with IC50s of 92.0 nM, 33.39 μM, 40.71 μM for SHP2, SHP1, SHP1B, respectively. DBDA2 downregulates mitogenic and cell survival signaling and RTK expression. BPDA2 suppresses SHP2 mediated signaling and breast cancer cell phenotypes .
|
-
- HY-B2099
-
|
1-Butylbiguanide
|
AMPK
|
Metabolic Disease
Cancer
|
|
Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al) .
|
-
- HY-B2099A
-
|
1-Butylbiguanide hydrochloride
|
AMPK
|
Cancer
|
|
Buformin hydrochloride (1-Butylbiguanide hydrochloride), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin hydrochloride decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin hydrochloride also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al) .
|
-
- HY-15150G
-
|
R428 (GMP); BGB324 (GMP)
|
TAM Receptor
|
Cancer
|
|
Bemcentinib (R428) GMP is Bemcentinib (HY-15150) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy.Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer .
|
-
- HY-170948
-
|
|
Adenosine Receptor
|
Cancer
|
|
A2AR modulator-1 (Compound 45) is a selective negative allosteric adenosine A2a receptor (A2aR) modulator with an IC50 value of 9 nM. A2AR modulator-1 reduces the affinity of endogenous adenosine for the receptor and inhibits cAMP signaling pathway activation. A2AR modulator-1 potently restores pCREB phosphorylation in CD4 + T cells, reversing immunosuppression in the tumor microenvironment, and shows potential to suppress tumor growth and metastasis in triple-negative breast cancer models .
|
-
- HY-125209A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TH5427 hydrochloride is a potent, selective NUDT5 inhibitor (IC50=29 nM). TH5427 hydrochloride shows an apparent 690-fold selectivity for NUDT5 over MTH1. TH5427 hydrochloride blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells .
|
-
- HY-145857
-
|
|
HSP
Apoptosis
|
Cancer
|
|
GRP78-IN-1 exhibits several interactions with GRP78 residues with binding energy of -8.07 kcal/mol. GRP78-IN-1 shows the potent cytotoxic, anti-proliferative in cancer cells. GRP78-IN-1 exhibits promising apoptosis in breast cancer cells and wound healing properties .
|
-
- HY-147522
-
|
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
ADG-2e is a potent antibacterial agent with MICs of 16, 4, 2, and 2 μg/mL for E. coli [KCTC 1682], P. aeruginosa [KCTC 1637], B.subtilis [KCTC 3068], and S. aureus [KCTC 1621], respectively. ADG-2e shows anti-metastatic activity against breast cancer cells .
|
-
- HY-144306
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
|
-
- HY-112903A
-
|
|
Protein Arginine Deiminase
MDM-2/p53
PERK
mTOR
Autophagy
|
Cancer
|
|
YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer .
|
-
- HY-147574
-
|
|
TAM Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease .
|
-
- HY-50767D
-
|
PD 0332991 orotate
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-50767A
-
|
PD 0332991 monohydrochloride
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-A0065
-
|
PD 0332991 isethionate
|
CDK
|
Cancer
|
|
Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-14372
-
|
|
CDK
|
Cancer
|
|
BS-194 is an orally active, selective and potent CDK inhibitor. BS-194 inhibits CDK2, CDK1, CDK5, CDK7, CDK9 (IC50s: 3, 30, 30, 250, and 90 nM respectively). BS-194 potently inhibits cancer cells proliferation. BS-194 can be used in the research of cancers like breast cancer, colon cancer .
|
-
- HY-107408
-
|
|
Hedgehog
Gli
|
Metabolic Disease
Cancer
|
|
SANT 2 is a potent Hh-signaling pathway antagonist. SANT 2 interferes with the expression of Gli1. SANT 2 causes developmental delay in medaka embryos. SANT 2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers .
|
-
- HY-N9174
-
|
|
Others
|
Cancer
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
- HY-163629
-
|
|
Others
|
Cancer
|
|
Anticancer agent 224 (Compound 16) is an anticancer agent that can effectively inhibit the growth of central nervous system (CNS), kidney and breast cancer cell, with a GI50 value ranging from 0.6 to 12.8 μM .
|
-
- HY-13657
-
|
KOS-1584
|
Microtubule/Tubulin
|
Cancer
|
|
cis-9,10-Dehydroepothilone D (KOS-1584) is an epothilone derivative with antiproliferative activity and tubulin polymerization activity. cis-9,10-Dehydroepothilone D can be used for the study of lung cancer, colon cancer, prostate cancer and breast cancer .
|
-
- HY-P99843
-
|
|
TROP2
ADC Antibody
|
Cancer
|
|
Datopotamab (CDP7657) is a humanized anti trophoblast cell surface antigen 2 (TROP2) antibody. Datopotamab can generate antibody drug conjugates (ADC) (HY-141598) with DNA topoisomerase I inhibitor Deruxtecan (HY-13631E). Datopotamab can be used in the study of triple negative breast cancer and non-small cell lung cancer .
|
-
- HY-119358
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Traumatic Acid is a wound healing agent and a cytokinin (phytohormone). Traumatic Acid enhances the biosynthesis of collagen in cultured human skin fibroblasts. Traumatic Acid inhibits MCF-7 breast cancer cells viability and enhances apoptosis and oxidative stress. Traumatic Acid can be used in studies of cancer, circulatory disorders (including arterial hypertension), and skin diseases associated with oxidative stress and impaired collagen biosynthesis .
|
-
- HY-125961
-
|
|
Others
|
Cancer
|
|
T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 μM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream) .
|
-
- HY-153857
-
|
PHI-101
|
FLT3
Checkpoint Kinase (Chk)
|
Cancer
|
|
Lasmotinib (PHI-101) is a FLT3 and CHK2 inhibitor. Lasmotinib potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. Lasmotinib synergizes with Venetoclax (HY-15531) or Azacytidine to inhibit leukemia. Lasmotinib exhibits anticancer activity against ovarian and breast cancer .
|
-
- HY-155965
-
|
|
VEGFR
PARP
Apoptosis
|
Cancer
|
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
|
-
- HY-144060
-
|
|
Akt
|
Cancer
|
|
AKT-IN-10 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4) .
|
-
- HY-138295
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1 .
|
-
- HY-165245
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
|
-
- HY-144059
-
|
|
Akt
|
Cancer
|
|
AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1) .
|
-
- HY-164489
-
|
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
KU004 is a potent dual EGFR/HER2 inhibitor with anticancer effects. KU004 inhibits the proliferation of human breast cancer SKBR3 cells by inducing G1 phase arrest. KU004 blocks the activation of HER2, EGFR and downstream Akt and Erk pathways and induces cell Apoptosis mainly via the extrinsic pathway. KU004 is a quinazoline derivative .
|
-
- HY-150597
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-157913
-
|
|
Pyruvate Kinase
Apoptosis
|
Cancer
|
|
PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer .
|
-
- HY-Y1103
-
|
Ferrous sulfate heptahydrate, 99%
|
Biochemical Assay Reagents
|
Cardiovascular Disease
Cancer
|
|
Iron(II) sulfate heptahydrate, 99% (Ferrous sulfate heptahydrate, 99%) is an orally active iron salt. Iron(II) sulfate heptahydrate, 99% replaces iron found in hemoglobin and myoglobin, allowing for the transportation of oxygen via hemoglobin. Iron(II) sulfate heptahydrate, 99% is mainly used for the prevention of iron-deficiency anemia. Iron(II) sulfate heptahydrate, 99% also has anti-tumor effects on chronic myeloid leukemia and breast cancer .
|
-
- HY-101982
-
|
Lys-Nε-MCC-DM1
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is a agent-linker conjugates for ADC that can inhibit tubulin polymerization. Lys-SMCC-DM1 is the active metabolite of T-DM1. T-DM1 is a HER2-targeting ADC with a tubulin polymerization inhibitor DM1. Lys-SMCC-DM1 can be used in the research of breast cancer .
|
-
- HY-B1019
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Sulpiride is an orally active dopamine D2/D3 receptor antagonist. Sulpiride is an atypical antipsychotic agent of the benzamide family. Sulpiride can be used in research into anxiety, depression and breast cancer .
|
-
- HY-158108
-
|
|
Autophagy
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
anti-TNBC agent-6 (compound pt-3) is a potent anti-TNBC agent. anti-TNBC agent-6 shows cytotoxic activity. anti-TNBC agent-6 induces autophagy and ferroptosis. anti-TNBC agent-6 enhances intracellular ROS accumulatio. anti-TNBC agent-6 shows anti tumor activity and has the potential for the research of breast cancer .
|
-
- HY-126005
-
|
|
Sodium Channel
|
Cancer
|
|
VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability .
|
-
- HY-143232
-
|
|
Fungal
Bacterial
|
Infection
Cancer
|
|
Antibacterial agent 73 (compound 7a) is a potent antimicrobial agent. Antibacterial agent 73 exhibits very good antitubercular activity (MIC=0.65 µg/mL) against Mtb H37Rv. Antibacterial agent 73 shows good activity against fungal and bacterial. Antibacterial agent 73 also shows cytotoxicity in MCF-7 breast cancer cell lines, with IC50 of 8.20 μM .
|
-
- HY-172562
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines. Pink: (+)-JQ1-OH (HY-161125); Blue: BTR2000 (HY-172563); Black: Linker (HY-W015236) .
|
-
- HY-P10445
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4 that disrupts the BRD4/JMJD6 interaction. BRD4/JMJD6 is a protein complex that is critical for oncogene expression and breast cancer, and TAT-PiET inhibits BRD4/JMJD6 target gene expression and breast cancer cell growth. TAT-PiET also resists endocrine resistance in ERα-positive breast cancer cells and is a potential inhibitor of breast cancer .
|
-
- HY-110329
-
|
|
Others
|
Cancer
|
|
ML179 (SR-1309) is a inverse LRH1/NR5A2 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
|
-
- HY-N0841
-
|
Dihydrobrusatol; NSC310616
|
Parasite
NF-κB
p38 MAPK
Phosphatase
Apoptosis
|
Infection
Cancer
|
|
Bruceine A (Dihydrobrusatol) is a natural quassinoid. Bruceine A is an inhibitor of parasites, NF-κB, and PFKFB4 (Kd: 44 nM). Bruceine A is an activator of P38α MAPK. Bruceine A has antiparasitic activity. Bruceine A has antitumor activity and inhibits cancer cell migration. Bruceine A blocks the cell cycle and induces apoptosis. Bruceine A can be used in parasites, pancreatic cancer, and breast cancer research .
|
-
- HY-N0292R
-
|
|
Cytochrome P450
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Oleuropein (Standard) is the analytical standard of Oleuropein. This product is intended for research and analytical applications. Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
|
-
- HY-155246
-
|
|
Apoptosis
PARP
|
Cancer
|
|
PARP1-IN-15 (Compound 6) is a PARP1 inhibitor. PARP1-IN-15 inhibits tankyrase (TNKS) and facilitates DNA double-strand breaks damage. PARP1-IN-15 induces tumor cell apoptosis. PARP1-IN-15 has anti-cancer activity in triple-negative breast cancer (TNBC) cells and TNBC patient-derived organoids. PARP1-IN-15 can be used for research of TNBC with or without BRCA1 mutations .
|
-
- HY-163726
-
|
|
GLUT
EGFR
Apoptosis
|
Cancer
|
|
GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research .
|
-
- HY-50895B
-
|
ZD 1839 dihydrochloride
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
|
-
- HY-50895
-
|
ZD1839
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
|
-
- HY-168851
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-35 (compound T26) is a selective, orally active, cross -the blood-brain barrierPARP1 inhibitor with IC50 values of 0.2, 122 nM for PARP1, PARP2, respectively. PARP1-IN-35 shows antiproliferative activity and anticancer activity. PARP1-IN-35 has the potential for the research of breast cancer .
|
-
- HY-13270
-
|
E7010
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
|
-
- HY-120069
-
|
|
Apoptosis
|
Cancer
|
|
APX2009 is a specific APE1/REF-1 redox inhibitor with anticancer activities which decreases the proliferative, migratory, and invasive properties of breast cancer cell and induces apoptosis in breast cancer cell .
|
-
- HY-162494
-
|
|
Protein Arginine Deiminase
|
Cancer
|
|
PAD4-IN-4 (compound 28) is a potent PAD4 inhibitor (IC50=0.79±0.09 μM). PAD4-IN-4 improves the tumor immune microenvironment by reshaping neutrophil phenotype, upregulating the proportions of dendritic cells and M1 macrophages, and reducing the amount of myeloid-derived suppressor cells. PAD4-IN-4 can be used for Triple-negative breast cancer research .
|
-
- HY-50767R
-
|
|
CDK
|
Cancer
|
|
Palbociclib (Standard) is the analytical standard of Palbociclib. This product is intended for research and analytical applications. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-P9907A
-
|
Anti-Human HER2, Humanized Antibody (PBS)
|
ADC Antibody
EGFR
|
Cancer
|
|
Trastuzumab (PBS) is a humanized IgG1 monoclonal antibody for patients with invasive breast cancers that overexpress HER2. Trastuzumab (PBS) has the potential for HER2 Positive Metastatic Breast Cancer and HER2 Positive Gastric Cancer research.
|
-
- HY-138657
-
|
|
Phosphatase
|
Cancer
|
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model .
|
-
- HY-164525
-
|
SC-81490; PF-02881307
|
MMP
|
Cancer
|
|
SD-7300 (SC-81490) is an orally active inhibitor of MMP-2, MMP-9, and MMP-13 with Ki values ??of 0.03, 0.01, and 0.03 nM, respectively. SD-7300 can reduce the degradation of extracellular matrix by tumor cells, thereby inhibiting the invasion and metastasis of tumor cells. In addition, SD-7300 is also a dose-dependent inhibitor of mouse corneal angiogenesis and an inhibitor of interleukin-1-induced bovine cartilage degradation. SD-7300 can be used in breast cancer research .
|
-
- HY-150609
-
|
|
SHP2
Phosphatase
CDK
|
Cancer
|
|
SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-N10361
-
|
|
RAR/RXR
PPAR
Aldose Reductase
|
Cancer
|
|
Drupanin is an orally active and selective AKR1C3 enzyme inhibitor and an RXRα agonist with an EC50 value of 4.8 μM, which is found in green propolis. Drupanin also activates PPARγ moderately. Drupanin induces adipogenesis and elevates aP2 mRNA levels in 3T3-L1 fibroblasts Drupanin has the potential for the research of breast and prostate cancers .
|
-
- HY-119906
-
|
FW-04-806
|
HSP
Apoptosis
|
Cancer
|
|
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo .
|
-
- HY-173117
-
|
|
CaMK
|
Cardiovascular Disease
Cancer
|
|
RA306 is an orally active CAMK2 inhibitor. RA306 can block the PEAK1/CAMK2 signaling pathway. RA306 inhibits the proliferation, migration, and invasion of breast cancer cells and has anti-tumor activity. In addition, RA306 can improve dilated cardiomyopathy in mice and can be used in the research of heart diseases .
|
-
- HY-10812
-
|
|
PI3K
mTOR
|
Cancer
|
|
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
|
-
- HY-107216A
-
|
|
Adhesion G Protein-coupled Receptors (AGPCRs)
PI3K
|
Neurological Disease
Cancer
|
|
(3aS,4R,9bR)-G-1 is a highly selective G protein-coupled receptor GPR30 (GPER) agonist with a Ki value of approximately 7 nM. (3aS,4R,9bR)-G-1 activates rapid signaling pathways such as intracellular calcium mobilization and PI3K signaling through GPR30, promoting uterine epithelial cell proliferation and exerting antidepressant effects. (3aS,4R,9bR)-G-1 is promising for research of breast cancer and depression .
|
-
- HY-P10446
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Epigenetic Reader Domain
|
Cancer
|
|
TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445). TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can disrupt the interaction between the breast cancer oncogene BRD4/JMJD6 and inhibit the growth of breast cancer cells. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells and is a potential inhibitor of breast cancer . TAT-PiET-PROTAC can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P10759
-
|
|
Peptide-Drug Conjugates (PDCs)
Aminopeptidase
|
Cancer
|
|
DTS-201 sodium (CPI-0004Na) is a peptidic prodrug of Doxorubicin (HY-15142A). DTS-201, comprising the tetrapeptide portion, is cleaved by endopeptidases in the tumor environment to produce metabolites that subsequently enter the cell and are converted to active Doxorubicin. DTS-201 shows antitumoral efficacy in tumor xenograft models of prostate, breast, and lung cancer .
|
-
- HY-140739
-
|
|
Liposome
|
Neurological Disease
Cancer
|
|
DSPE-PEG2000-Maleimide is a phospholipid-PEG conjugate. DSPE-PEG2000-Maleimide utilizes the amphiphilicity of DSPE to insert into the lipid bilayer of liposomes or nanoparticles. DSPE-PEG2000-Maleimide covalently couples to the sulfhydryl (-SH) of ligands (such as antibodies, peptides, or proteins) via thiol-maleimide click chemistry, giving the particles targeting capabilities. DSPE-PEG2000-Maleimide can be used in the researches of breast cancer, lymphoma, and inherited retinal degeneration .
|
-
- HY-172888
-
|
|
Endogenous Metabolite
FAK
|
Cancer
|
|
SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50: 3.59 μM). SPP-037 exhibits anti-MDA-MB-231 cell migration activity by inhibiting integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used in breast cancer research .
|
-
- HY-Y1103A
-
|
Ferrous sulfate heptahydrate, for cell culture, 99%
|
Biochemical Assay Reagents
|
Cardiovascular Disease
Cancer
|
|
Iron(II) sulfate heptahydrate, for cell culture, 99% (Ferrous sulfate heptahydrate, for cell culture, 99%) is an orally active iron salt. Iron(II) sulfate heptahydrate, for cell culture, 99% replaces iron found in hemoglobin and myoglobin, allowing for the transportation of oxygen via hemoglobin. Iron(II) sulfate heptahydrate, for cell culture, 99% is mainly used for the prevention of iron-deficiency anemia. Iron(II) sulfate heptahydrate, for cell culture, 99% also has anti-tumor effects on chronic myeloid leukemia and breast cancer .
|
-
- HY-163747
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma .
|
-
- HY-P10789
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
The P160 peptide is a breast cancer-targeting peptide that binds to the keratin 1 (KRT1) receptor on breast cancer cells, with a Kd of approximately 1.1 μM, demonstrating significant potential for targeted drug delivery to breast cancer cells. The P160 peptide enhances the cellular uptake and anticancer activity of the pro-apoptotic antimicrobial peptide MccJ25 (microcin J25). The P160 peptide can be used in cancer research .
|
-
- HY-171048
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
GTx-027 is an orally active and non-steroidal selective androgen receptor modulator (SARM). GTx-027 shows androgen receptor (AR) transactivation effects with the EC50 of 1.8 nM. GTx-027 acts selectively increase muscle weight (anabolic) without affecting secondary sexual organs (androgenic). GTx-027 has the protential for the study of breast cancer and stress urinary incontinence (SUI) .
|
-
- HY-153588
-
|
|
HSP
|
Cancer
|
|
HSP90-IN-22 (Compound 35) is an Hsp90 inhibitor with antiproliferative properties on cells with IC50 values of 3.65 μM for MCF7 breast cancer cells and 2.71 μM for SKBr3 breast cancer cells, respectively.
|
-
- HY-173640
-
|
|
Androgen Receptor
Phosphodiesterase (PDE)
|
Cancer
|
|
ID11916 is an orally active androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. ID11916 blocks androgen binding to AR, nuclear translocation, and androgen-dependent transcriptional activity of AR, while increasing intracellular cGMP levels and activating PKG via inhibition. ID11916 shows potent anti-cancer effect in prostate cancer cell lines VCaP and 22Rv1 and in AR-positive breast cancer cell lines SK-BR-3 .
|
-
- HY-146452
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC) .
|
-
- HY-119358R
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Traumatic Acid (Standard) is the analytical standard of Traumatic Acid. This product is intended for research and analytical applications. Traumatic Acid is a wound healing agent and a cytokinin (phytohormone). Traumatic Acid enhances the biosynthesis of collagen in cultured human skin fibroblasts. Traumatic Acid inhibits MCF-7 breast cancer cells viability and enhances apoptosis and oxidative stress. Traumatic Acid can be used in studies of cancer, circulatory disorders (including arterial hypertension), and skin diseases associated with oxidative stress and impaired collagen biosynthesis[1][2].
|
-
- HY-173368
-
|
|
PI3K
|
Cancer
|
|
Antiproliferative agent-67 (Compound 5g) is a PI3K inhibitor with a selectivity index SI of 7.72 for breast cancer cells (MCF-7). Antiproliferative agent-67 inhibits the activity of PI3K protein by forming hydrogen bonds and intermolecular hydrophobic forces with it, exerting anti - proliferative activity against breast cancer cells (MCF-7), and can be used in the research of breast cancer .
|
-
- HY-13270A
-
|
E7010 hydrochloride
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
|
-
- HY-110354
-
|
G28UCM
|
Fatty Acid Synthase (FASN)
Bacterial
Antibiotic
|
Infection
Cancer
|
|
UCM05 (G28UCM) is a potent inhibitor of fatty acid synthase (FASN) shows activity against HER2+ breast cancer xenografts and is active in anti-HER2 drug-resistant cell lines. UCM05 is a Filamentous temperature-sensitive protein Z (FtsZ) inhibitor and inhibits the growth of the Gram-positive bacterium B. subtilis with MIC values of 100 μM but lack activity on the Gram-negative bacterium E. coli.
|
-
- HY-W004307
-
-
- HY-U00073
-
|
Butocin; Butocine
|
Others
|
Cancer
|
|
Benin is a potent cytostatic agent that can be used for the treatment of generalized carcinoma of the breast.
|
-
- HY-140739A
-
|
|
Liposome
|
Neurological Disease
Cancer
|
|
DSPE-PEG2000-Maleimide free acid is a phospholipid-PEG conjugate. DSPE-PEG2000-Maleimide free acid utilizes the amphiphilicity of DSPE to insert into the lipid bilayer of liposomes or nanoparticles. DSPE-PEG2000-Maleimide free acid covalently couples to the sulfhydryl (-SH) of ligands (such as antibodies, peptides, or proteins) via thiol-maleimide click chemistry, giving the particles targeting capabilities. DSPE-PEG2000-Maleimide free acid can be used in the researches of breast cancer, lymphoma, and inherited retinal degeneration .
|
-
- HY-144637
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
|
-
- HY-135312
-
|
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
|
AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer .
|
-
- HY-P991425
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
AT-1413 is a human monoclonal antibody (mAb) targeting CD43. AT-1413 induces antibody-dependent cell-mediated cytotoxicity (ADCC) in melanoma cell lines and acute myeloid leukemia (AML) cells. AT-1413 has antitumor activity in AML mouse models. AT-1413 can be used in Acute myeloid leukaemia, Breast cancer, Malignant melanoma and Myelodysplastic syndromes research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-158106
-
|
|
CDK
|
Cancer
|
|
AZD8421 is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer .
|
-
- HY-145804
-
|
AZD-9574
|
PPAR
|
Neurological Disease
Cancer
|
|
AZD-9574 is a potent and brain penetrant PARP1 inhibitor and shows >8000-fold selectivity for PARP1 compared to PARP2/3/5a/6. AZD-9574 acts by selectively inhibiting and trapping PARP1 at the sites of SSBs. AZD-9574 is an anti-cancer agent and can be used for HRD +?breast cancer and advanced solid malignancies research .
|
-
- HY-115625
-
|
|
Progesterone Receptor
Apoptosis
|
Cancer
|
|
AG-205 is a progesterone receptor membrane component-1 (PGRMC1) inhibitor with anti-mitotic, anti-migratory and anti-invasive activities. AG-205 increases expression of genes coding enzymes of the cholesterol biosynthetic pathway or of steroidogenesis. AG-205 promotes Apoptosis modified regulation of the cell cycle and reduces cell migration and invasion capacities in ovary and breast cancer cells .
|
-
- HY-117395
-
|
|
HSP
|
Cancer
|
|
PU-H54, a Grp94-selective inhibitor, can be used for the research of breast cancer. Hsp90 chaperone family, comprised in humans of four paralogs, Hsp90α, Hsp90β, Grp94 and Trap-1, has important roles in malignancy . PU-H54 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-172177
-
|
|
Apoptosis
HDAC
ROCK
|
Cancer
|
|
ROCK/HDAC-IN-2 (Compound C-9) is a ROCK/HDAC inhibitor, with IC50 values of 0.185 µM, 0.8 µM, and 0.7 µM for HDAC6, ROCK1, and ROCK2, respectively. ROCK/HDAC-IN-2 can induce apoptosis and changes in mitochondrial membrane potential in cancer cells, demonstrating significant antitumor activity. ROCK/HDAC-IN-2 can be used in the research of pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC) .
|
-
- HY-14590
-
-
- HY-13738S
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene-d4 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
|
-
- HY-13738S2
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene-d4 (hydrochloride) is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
|
-
- HY-13738S3
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene-d10 is the deuterium labeled Raloxifene. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
|
-
- HY-145716
-
|
Nafoxidene
|
Estrogen Receptor/ERR
|
Cancer
|
|
Nafoxidine, a nonsteroidal estrogen antagonist, is shown to possess antitumor activity against breast cancer.
|
-
- HY-135606
-
|
|
HDAC
|
Cancer
|
|
LW479, a novel HDAC inhibitor, could be a candidate agent for breast cancer prevention.
|
-
- HY-164530
-
|
|
Src
VEGFR
Raf
p38 MAPK
|
Cancer
|
|
SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines .
|
-
- HY-157151
-
|
|
Histone Methyltransferase
|
Cancer
|
|
iPRMT1 is a potent and selective PRMT1 inhibitor for breast cancer research. iPRMT1 inhibits breast cancer cell growth in vitro and in vivo with EC50 values of 90, 70, and 9 nM in MCF7, T47D, and MDA-MB-231 cells, respectively .
|
-
- HY-155197
-
|
|
Microtubule/Tubulin
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 7 (Compound 35t) is an ERα and ERβ degrader. ER degrader 7 inhibits tubulin polymerization. ER degrader 7 inhibits cell viability with IC50s of 0.06, 2.56, 15.84, 1.59, 1.67, 1.37 μM for MCF-7, T47D, MCF-10A, LCC2, T47D D538G, and T47D Y537S cells respectively. ER degrader 7 also inhibits breast cancer tumor growth .
|
-
- HY-13757A
-
|
ICI 47699; (Z)-Tamoxifen; trans-Tamoxifen
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Endocrinology
Cancer
|
|
Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER transgenic mouse .
|
-
- HY-170947
-
|
|
STAT
Quinone Reductase
|
Cancer
|
|
Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
|
-
- HY-13270R
-
|
|
Microtubule/Tubulin
Autophagy
Apoptosis
|
Cancer
|
|
ABT-751 (Standard) is the analytical standard of ABT-751. This product is intended for research and analytical applications. ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
|
-
- HY-13738S4
-
|
Keoxifene-d10; LY156758(free base)-d10; LY139481-d10
|
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene-d10-1 is the deuterium labeled Raloxifene . Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
|
-
- HY-163938
-
|
|
PROTACs
|
Cancer
|
|
PROTAC erf3a Degrader-1 (Compound C63) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-1 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-1 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: CRBN ligand (HY-41547)) .
|
-
- HY-14586
-
|
STX64; BN83495; 667-Coumate
|
Steroid Sulfatase
|
Cancer
|
|
Irosustat is a potent steroid sulfatase inhibitor, with an IC50 of 8 nM, and exhibits anti-breast cancer activity.
|
-
- HY-13724B
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Pipendoxifene hydrochloride is a selective estrogen receptor modulator (SERM) that can be used for the research of breast cancer .
|
-
- HY-142870
-
-
- HY-P99045
-
|
|
ADC Antibody
TROP2
|
Cancer
|
|
Sacituzumab is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab can be used for the synthesis of antibody-drug conjugates (ADC) drug Sacituzumab govitecan (HY-132254). Sacituzumab govitecan can be used in the field of triple-negative breast cancer .
|
-
- HY-162721
-
|
|
Others
|
Cancer
|
|
Anticancer agent 242 (7) possesses anticancer activity in A2780 (IC50 = 0.24 μM, ovarian adenocarcinoma), A2780cis (IC50 = 0.45 μM, resistant derivative of A2780), CCD18Co (IC50 = 0.59 μM, non-malignant human fibroblasts), A549 (IC50 = 0.32 μM, lung carcinoma), HT29 (IC50 = 0.26 μM, colorectal adenocarcinoma), and MCF7 (IC50 = 0.55 μM, breast adenocarcinoma) .
|
-
- HY-146440
-
|
|
Histone Demethylase
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM .
|
-
- HY-173020
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
W23-1006 is a selective and covalent ALKBH5 inhibitor. W23-1006 binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. W23-1006 shows ~30- and 8-fold stronger inhibitory activity than that against FTO and ALKBH3, respectively. W23-1006 can be used for the study of triple-negative breast cancer (TNBC) .
|
-
- HY-16916
-
NS1643
1 Publications Verification
|
Potassium Channel
Autophagy
|
Cancer
|
|
NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K + channels with an EC50 of 10.5 μM. NS1643 inhibits the growth of breast cancer tumors in TNBC mouse models. NS1643 inhibits cell migration and invasion of breast cancer cells .
|
-
- HY-103255
-
|
|
Apoptosis
|
Cancer
|
|
CFM-4 is a potent small molecular antagonist of CARP-1/APC-2 binding. CFM-4 prevents CARP-1 binding with APC-2, causes G2M cell cycle arrest, and induces apoptosis with an IC50 range of 10-15 μM. CFM-4 also suppresses growth of drug-resistant human breast cancer cells .
|
-
- HY-147373
-
|
|
PROTACs
Ligands for E3 Ligase
|
Cancer
|
|
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research .
|
-
- HY-N12198
-
|
|
Others
|
Cancer
|
|
Mollicellin H is a secondary metabolite of the fungus C. brasiliense and has a wide range of biological activities, including immunomodulation, cytotoxicity and anti-tumor effects. The growth inhibitory effects (GI50s) of Mollicellin H on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines are 5.1 μg/mL, 6.5 μg/mL and 2.5 μg/mL respectively .
|
-
- HY-P10944
-
|
NNS309
|
FAP
|
Cancer
|
|
Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with 68Ga and 177Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC) .
|
-
- HY-148923
-
|
|
STAT
|
Cancer
|
|
MC0704 is a STAT3 inhibitor with an IC50 value of 2.13 μM. MC0704 induces cell apoptosis and cell cycle arrest. MC0704 shows antitumor activity in mouse breast cancer models. MC0704 can be used for the research of metastatic triple-negative breast cancer (mTNBC) .
|
-
- HY-N6820
-
|
|
Others
|
Cancer
|
|
Iristectorin A, a natural product from Iris tectorum, has anti-cancer activities in breast cancer .
|
-
- HY-N6819
-
|
|
Others
|
Cancer
|
|
Iristectorin B is an isoflavone from Iris tectorum, has anti-cancer activities in breast cancer .
|
-
- HY-W040046
-
|
Nafoxidene hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Nafoxidine hydrochloride is a non-steroidal estrogen receptor antagonist with antitumor activity for breast cancer .
|
-
- HY-143654
-
|
|
HDAC
|
Cancer
|
|
WW437 is a histone deacetylase (HDAC) inhibitor with potent anti-breast cancer ability in vitro and in vivo.
|
-
- HY-19971
-
|
|
Others
|
Cancer
|
|
ML239 is a potent and selective inhibitor of breast cancer stem cells, with an IC50 of 1.16 μM.
|
-
- HY-162826
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer (IC50: 12.8 μM) and can induce early apoptosis in breast cancer cells. Apoptosis inducer 27 can bind to DNA molecules, Bax and Bcl-2 proteins, and induce DNA damage .
|
-
- HY-108692S
-
|
|
Isotope-Labeled Compounds
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Enterolactone-d6 is the deuterium labeled Enterolactone. Enterolactone is a bioactive phenolic metabolite known as a mammalian lignan derived from dietary lignans. Enterolactone has estrogenic properties and anti-breast cancer activity . Enterolactone is a radiosensitizer for human breast cancer cell lines through impaired DNA repair and increased apoptosis .
|
-
- HY-170946
-
|
|
STAT
Bcl-2 Family
|
Cancer
|
|
WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3 Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis .
|
-
- HY-141600
-
|
BAY 1187982
|
Antibody-Drug Conjugates (ADCs)
FGFR
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Aprutumab ixadotin (BAY 1187982) is the first antibody-drug conjugate (ADC) to target FGFR2 and the first to use Auristatin-based payload. Aprutumab ixadotin contains a fully human anti-FGFR2 monoclonal antibody (Aprutumab) (HY-P99007) conjugated by lysine side chains to a non-cleavable linker and via this an innovative Auristatin W derivative. Aprutumab ixadotin can be used for the study of advanced solid tumors, such as FGFR2-positive gastric cancer and triple-negative breast cancer .
|
-
- HY-N0563
-
|
|
AMPK
VEGFR
PI3K
Akt
NF-κB
Cytochrome P450
|
Cardiovascular Disease
Cancer
|
|
Alizarin is a natural dye. Alizarin can be extracted from the roots of madder plant. Alizarin activates AMPK and VEGFR2/eNOS pathway. Alizarin regulates PI3K/Akt and inhibits NF-κB pathway. Alizarin enhances CYP1A1 enzyme activity. Alizarin has protective effects on hypertension and vascular endothelial dysfunction. Alizarin has anti-tumor activity against multiple cancers including pancreatic cancer, breast cancer, osteosarcoma and liver cancer. Alizarin has been widely used as a pigment in textile fabrics and paintings .
|
-
- HY-13757
-
|
ICI 46474; (Z)-Tamoxifen Citrate; trans-Tamoxifen Citrate
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis . Tamoxifen Citrate also can induce gene knockout of CreER transgenic mouse .
|
-
- HY-139668
-
|
|
Neurotensin Receptor
|
Cancer
|
|
VGD071, a sortilin-targeting compound, is a promising candidate for future studies using mouse breast cancer models.
|
-
- HY-12015
-
|
BSI-201; NSC-746045; IND-71677
|
PARP
Influenza Virus
|
Cancer
|
|
Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer.
|
-
- HY-155180
-
|
|
PI3K
|
Cancer
|
|
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth .
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-169903
-
|
|
Apoptosis
|
Cancer
|
|
SMIP34 is a PELP1 inhibitor. SMIP34 binds to PELP1 with a Kd of 37.4 μM. SMIP34 inhibits cancer cell proliferation and tumor progression. SMIP34 can be used for breast cancer research, and is active against wild-type (WT), mutant (MT) ER + and therapy-resistant (TR)-ER + breast cancer .
|
-
- HY-169477
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
PAMAM Dendrimer G0.5 Carboxylate sodium is a polyamidoamine (PAMAM) dendrimer with carboxylate termini. PAMAM Dendrimer G0.5 Carboxylate sodium conjugated with DACHPt is cytotoxic to A2780 ovarian cancer cells, MCF-7 breast cancer cells, Caco-2 colon cancer cells and BJ fibroblasts with IC50 values of 0.03, 1.6, 0.18 and 3 µM, respectively .
|
-
- HY-P99437
-
|
KN-026
|
EGFR
|
Cancer
|
|
Anbenitamab (KN-026) is a bispecific antibody simultaneously targeting extracellular domains II and IV of human HER2. Anbenitamab blocks both ligand-dependent and ligand-independent HER2 signaling pathways. Anbenitamab mediates antibody-dependent cellular cytotoxicity (ADCC) via FcγIIIa binding. Ambrinitumab can be used in research for lung cancer, HER2-positive metastatic breast cancer (MBC), gastric cancer, and gastroesophageal junction cancer .
|
-
- HY-149295
-
|
|
PROTACs
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-4 (Compound ZD12) is a highly potent and selectivePROTAC ERα degrader (Ki: 5.08 μM). PROTAC ERα Degrader-4 contains OBHSAs, linker and E3 ligase ligands. PROTAC ERα Degrader-4 shows excellent cell inhibitory and ERα degradation activity against Tamoxifen-sensitive and -resistant ER + breast cancer (BC) cells and ERα-mutated BC cells. PROTAC ERα Degrader-4 can induce apoptosis and can be used for cancer research.
|
-
- HY-155493
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP19A1/CYP11B2-IN-1 (Compound X21) is a potent and selective aromatase and
aldosterone synthase dual inhibitor with IC50s of 2.3 nM and 29 nM for aromatase (CYP19A1) and aldosterone synthase (CYP11B2), respectively. CYP19A1/CYP11B2-IN-1 has excellent antiproliferative and pro-apoptotic activity against the cancer cell. CYP19A1/CYP11B2-IN-1 can be used for research of breast cancer .
|
-
- HY-153661
-
-
- HY-168681
-
|
|
Sirtuin
|
Cancer
|
|
Sirtuin-IN-2 (compound 20) is an inhibitor of Sirtuin5, which is a key target for leukemia and breast cancer .
|
-
- HY-107008
-
|
|
Drug Derivative
|
Cancer
|
|
SW 71425 inhibits cell growth against breast, colon, non-small cell lung, and ovarian tumors. .
|
-
- HY-14590R
-
|
Kempferol(Standard); Robigenin (Standard)
|
Estrogen Receptor/ERR
Autophagy
Mitophagy
Apoptosis
HIV
Parasite
Endogenous Metabolite
|
Cancer
|
|
Kaempferol (Standard) is the analytical standard of Kaempferol. This product is intended for research and analytical applications. Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer .
|
-
- HY-173042
-
|
|
CDK
|
Cancer
|
|
CDK12/13-IN-2 (Compound 24) is a covalent inhibitor of CDK12/13, with IC50 values of 15.5 nM and 12.2 nM for CDK12 and CDK13, respectively. CDK12/13-IN-2 can inhibit the proliferation of breast cancer cells and can be used in the research of triple-negative breast cancer .
|
-
- HY-170972
-
|
|
Apoptosis
PARP
NAMPT
|
Cancer
|
|
PARP/NAMPT-IN-1 (Compound 13j) is a dual PARP/NAMPT inhibitor with IC50 values of 0.8 nM and 18 nM for PARP1 and NAMPT, respectively. PARP/NAMPT-IN-1 can inhibit the proliferation, migration and induce apoptosis of breast cancer cells. PARP/NAMPT-IN-1 can be used for the research of triple-negative breast cancer .
|
-
- HY-149632
-
|
|
EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .
|
-
- HY-161577
-
|
|
Bcl-2 Family
|
Cancer
|
|
BFC1103 is a small-molecule compound whose primary mechanism of action involves interaction with a specific domain of Bcl-2, particularly its loop domain. This interaction induces a conformational change in Bcl-2, exposing its BH3 (Bcl-2 homology 3) domain, thereby switching Bcl-2's function from anti-apoptotic to pro-apoptotic. The cell death induced by BFC1103 is dependent on the presence of Bax or Bak, both of which are key proteins involved in the intrinsic apoptotic pathway mediated by mitochondria. BFC1103 has successfully inhibited lung metastasis of triple-negative breast cancer in mouse models. It can be utilized in studying the roles of Bcl-2 family proteins in cancer development and how they impact the survival and proliferation of cancer cells .
|
-
- HY-162633
-
|
|
Deubiquitinase
|
Cancer
|
|
USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
|
-
- HY-111329
-
|
ILS-JGB-1741
|
Sirtuin
Apoptosis
|
Cancer
|
|
JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research .
|
-
- HY-159519
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR/HER2-IN-16 (compound 12K) is an effective dual-target inhibitor of EGFR (IC50=6.15 nM) and HER-2 (IC50=9.78 nM) with anti-tumor activity. EGFR/HER2-IN-16 can inhibit the migration of SK-BR-3 cells, arrest the cell cycle in the G0/G1 phase, and induce apoptosis. EGFR/HER2-IN-16 exhibits good anti-proliferative activity against tumor cell models and has little damage to healthy cells. EGFR/HER2-IN-16 can be used in breast cancer research .
|
-
- HY-106031
-
|
|
Topoisomerase
|
Cancer
|
|
F-14512 is a targeted cytotoxic compound that utilizes the polyamine transport system (PTS) to selectively deliver polyamine-containing drugs to cancer cells. F-14512 combines an epipodophyllotoxin core that targets topoisomerase II with a spermine group that acts as a cell delivery vehicle, with improved selectivity for tumor cells. F-14512 exhibits significant cytotoxicity against cells with high PTS activity and demonstrates high potency in multiple human cell lines (median IC50=0.18 μM). In the MX1 breast tumor xenograft model, F-14512 exhibits potent antitumor activity .
|
-
- HY-171039
-
|
Tri-BBPA; 2,2',6-Tribromobisphenol A
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Tribromobisphenol A (Tri-BBPA; 2,2',6-Tribromobisphenol A) is a phenolic compound isolated from human breast milk .
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- HY-142908
-
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Endogenous Metabolite
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Cancer
|
|
Maximiscin, a fungal metabolite, induces DNA damage and shows selective cytotoxic activity against a subtype of triple-negative breast cancer.
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-
- HY-172392
-
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MNK
Ribosomal S6 Kinase (RSK)
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Cancer
|
|
HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro .
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-
- HY-107513
-
|
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mGluR
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Neurological Disease
Cancer
|
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
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-
- HY-123656
-
|
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Apoptosis
|
Cancer
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Antiproliferative agent-61 is a synthetic β-carlinyl chalcone with significant antiproliferative activity. Antiproliferative agent-61 showed significant effects in a range of solid tumor cell lines, with the most prominent effects in breast cancer. Antiproliferative agent-61 showed IC50 values of 2.25 and 3.29 μM in the human breast cancer MCF-7 cell line. Antiproliferative agent-61 significantly induced DNA fragmentation and apoptosis in breast cancer cells. Antiproliferative agent-61 inhibited the interaction of MDM2 with p53 and promoted the degradation of MDM2 .
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-
- HY-149209
-
|
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PROTACs
CDK
STAT
Early 2 Factor (E2F)
|
Cancer
|
|
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
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-
- HY-146283
-
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Histone Demethylase
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Cancer
|
|
LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively .
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-
- HY-N3210
-
|
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Others
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Cancer
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|
Nb-Demethylechitamine is an alkaloid isolated from the methanol extract of Alstonia rostrata twigs. Nb-Demethylechitamine has in vitro cytotoxic activity against several human cancer cell lines, including human myeloid leukemia HL-60, liver cancer SMMC-7721, lung cancer A-549, breast cancer MCF-7, and colon cancer SW480 cells .
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-
- HY-100390
-
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BCRP
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Cancer
|
|
(S)-ML753286 is a breast cancer resistance protein (BCRP) inhibitor with an IC50 of 0.6 μM on BCRP efflux transporter.
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-
- HY-130434
-
|
|
Endogenous Metabolite
|
Cancer
|
|
12-SAHSA is a fatty acid ester of hydroxy fatty acids (FAHFAs). 12-SAHSA decreases in the human serum of breast cancer .
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-
- HY-120766
-
|
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Histone Demethylase
|
Cancer
|
|
NCDM-32B is a potent and selective KDM4 inhibitor that impaires viability and transforming phenotypes of breast cancer .
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-
- HY-151570
-
|
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Others
|
Cancer
|
|
Anticancer agent 87 is a potent anticancer agent. Anticancer agent 87 can be used in the research of breast adenocarcinoma and liver cancer .
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-
- HY-N1305
-
|
Sideritiflavone
|
Others
|
Cancer
|
|
Sideritoflavone is a flavonoid. Sideritoflavone can be isolated from Baccharis densiflora. Sideritoflavone is toxic to JIMT-1 breast cancer cells .
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-
- HY-151572
-
|
|
Others
|
Cancer
|
|
Anticancer agent 88 is a potent anticancer agent. Anticancer agent 88 can be used in the research of breast adenocarcinoma and liver cancer .
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-
- HY-173361
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 270 (Compound 8e) is an inhibitor that acts on tubulin. Its IC50 value against MCF-7 breast cancer cells is 1.02 μM. Through a dual mechanism of action, namely inducing Apoptosis and destabilizing microtubules, it exerts significant anti-proliferative activity against breast cancer cells. Anticancer agent 270 can be applied to research in the field of cancer .
|
-
- HY-N8572
-
|
|
PARP
Reactive Oxygen Species (ROS)
Aryl Hydrocarbon Receptor
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
3',4'-Dimethoxyflavone is a lipophilic flavone, can be isolated from the leaves of Primula veris. 3',4'-Dimethoxyflavone can reduce the synthesis and accumulation of PARP and protect cortical neurones against cell death induced by Parthanatos. 3',4'-Dimethoxyflavone is also an aryl hydrocarbon receptor antagonist in human breast cancer cells. 3',4'-Dimethoxyflavone can promote the proliferation of human hematopoietic stem cells. 3',4'-Dimethoxyflavone has various biological activities, including antioxidant, anti-cancer, anti-inflammatory, anti-atherogenic, hypolipidaemic, and neuroprotective or neurotrophic effects .
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-
- HY-146284
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively .
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-
- HY-163938A
-
|
|
PROTACs
|
Cancer
|
|
PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-2 inhibits protein expression of SRD5A3 and GSPT1(eRF3a). PROTAC erf3a Degrader-2 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-2 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer. (Red: erf3a ligand (HY-13778); Black: linker (HY-163960); Blue: E3 ligase ligand (HY-W763812)) .
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-
- HY-13757S
-
|
ICI 46474-d3 hydrochloride; (Z)-Tamoxifen-d3 hydrochloride; trans-Tamoxifen-d3 hydrochloride
|
Apoptosis
Estrogen Receptor/ERR
Autophagy
HSP
Isotope-Labeled Compounds
|
Cancer
|
|
Tamoxifen-d3 hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
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-
- HY-112056
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
DAPK
Isocitrate Dehydrogenase (IDH)
PERK
|
Cancer
|
|
DIM-C-pPhCO2Me is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhCO2Me induces Apoptosis. DIM-C-pPhCO2Me decreases PAX3-FOXO1A, N-Myc, Rassf4, MyoD1, Grem1, and DAPK1 proteins. DIM-C-pPhCO2Me decreases expression of TXNDC5 and IDH1, induces markers of ER stress (CHOP, ATF4 and p-PERK). DIM-C-pPhCO2Me inhibits renal cell carcinoma, breast cancer. DIM-C-pPhCO2Me can also be used in rhabdomyosarcoma research .
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-
- HY-13757R
-
|
|
Estrogen Receptor/ERR
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Tamoxifen (Citrate) (Standard) is the analytical standard of Tamoxifen (Citrate). This product is intended for research and analytical applications. Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells .Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen Citrate activates autophagy and induces apoptosis .Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse .
|
-
- HY-146285
-
|
|
Histone Demethylase
Histone Methyltransferase
|
Cancer
|
|
LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
|
-
- HY-B0412S1
-
-
- HY-139742
-
|
|
Sirtuin
|
Cancer
|
|
ADTL-SA1215 is a first-in-class specific small-molecule activator of SIRT3 that modulates autophagy in triple negative breast cancer.
|
-
- HY-125848
-
-
- HY-144791
-
|
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-144792
-
|
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-172934
-
|
|
Toll-like Receptor (TLR)
NO Synthase
PROTACs
|
Inflammation/Immunology
Cancer
|
|
FGT-4 is a folate receptor β (FR-β) targeting chimeric molecule. FGT-4 is a TLR7 agonist. FGT-4 facilitates the secretion of iNOS and proinflammatory cytokine IL-6 associated with M1 macrophages and enhances the proliferation of cytotoxic CD8 + T cells. FGT-4 has anti-tumor activity in the 4T1 breast cancer mouse model. FGT-4 can be used for the study of cancer immunity. (Pink: target protein TLR7/8 agonist 1 ligand (HY-103698); black: linker (HY-172936); blue: FR-β ligand (HY-172935)) .
|
-
- HY-150613
-
|
|
Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-107309
-
|
|
Others
|
Cancer
|
|
Scabioside C is a main triterpenoid saponin for total secondary saponin (TSS). TSS, from A. raddeana, exhibits the potential anti-breast cancer effect .
|
-
- HY-P9912
-
|
|
EGFR
|
Cancer
|
|
Pertuzumab, a humanized IgG1 monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.
|
-
- HY-12619
-
|
|
HSP
|
Cancer
|
|
DMT003096 is a HSP70 inhibitor. HSP70 has been reported to be upregulated in various cancers including breast, lung, colon, and cervix .
|
-
- HY-123758
-
-
- HY-125465
-
|
|
Autophagy
|
Cancer
|
|
SLLN-15 is an oral active, selective and potent enhancer of autophagy that activates cytostatic macroautophagy/autophagy in triple-negative breast cancer (TNBC) .
|
-
- HY-121372
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
Lactandrate is a D-high nitrogen steroid alkylating agent. It can interact with the ligand-binding domain (LBD) of estrogen receptor-alpha (ERα). Lactandrate has a growth inhibitory effect on breast cancer cells, with a GI50 value ranging from 5 to 65 μM. It shows anti-tumor activity in mouse breast tumors (MXT and CD8F1) as well as in human xenograft MX-1 .
|
-
- HY-168608
-
|
|
TRP Channel
Apoptosis
PI3K
Akt
|
Cancer
|
|
TRPM7-IN-1 (compound SUD), a benzoylurea derivative, is an effective TRPM7 inhibitor. TRPM7-IN-1 induces cell cycle arrest and apoptosis, decreases the migration of MCF-7 and BGC-823 cells. TRPM7-IN-1 decreases vimentin expression and increases E-cadherin expression. TRPM7-IN-1 potentially reduces the TRPM7-like current and decreases TRPM7 expression through the PI3K/Akt signaling pathway. TRPM7-IN-1 is a potential agent to suppress the metastasis of breast and gastric cancer by inhibiting TRPM7 expression and function .
|
-
- HY-P991356
-
|
LAE-005
|
PD-1/PD-L1
|
Cancer
|
|
FAZ-053 is a human monoclonal antibody (mAb) targeting B7-H1/PD-L1/CD274. FAZ-053 inhibits the interaction of PD-L1 with PD-1 and B7-1 on monocytes, dendritic cells, and B cells. FAZ-053 enhances interleukin 2 production. FAZ-053 can be used in advanced alveolar soft tissue sarcoma (ASPS), chordoma, and triple-negative breast cancer research .
|
-
- HY-132883
-
|
|
EGFR
|
Cancer
|
|
EGFR/CSC-IN-1 is a potential EGFR (IC50 10.52 nM) and cancer stem cell (CSC) dual inhibitor for triple-negative breast cancer research.
|
-
- HY-W004066
-
-
- HY-B0412S
-
-
- HY-N8187
-
|
|
Apoptosis
|
Cancer
|
|
Eupalinolide O is a sesquiterpene lactone with anticancer activities. Eupalinolide O induces cell apoptosis in human MDA-MB-468 breast cancer cells .
|
-
- HY-128553A
-
|
|
Ras
Apoptosis
|
Cancer
|
|
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer .
|
-
- HY-N3755
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Dihydroresveratrol, a potent phytoestrogen, is a hormone receptor modulator. Dihydroresveratrol exhibits proliferative effects in androgen-independent prostate and breast cancer cells at picomolar and nanomolar concentrations .
|
-
- HY-B0412S2
-
-
- HY-P10788
-
|
|
Complement System
|
Cancer
|
|
CK3 peptide is an NRP-1 targeting peptide with the amino acid sequence CLKADKAKC. The CK3 peptide specifically binds to NRP-1 to target breast cancer cells. Single-photon emission computed tomography (SPECT) and near-infrared fluorescence (NIRF) imaging show significant accumulation of CK3 peptide in xenograft tumors in nude mice. CK3 peptide can be used for molecular imaging studies of breast cancer.
|
-
- HY-162868
-
|
|
c-Met/HGFR
HDAC
Apoptosis
|
Cancer
|
c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC50 value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G0/G1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines .
|
-
- HY-122182
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
|
-
- HY-138089
-
|
|
Androgen Receptor
Estrogen Receptor/ERR
LDLR
|
Metabolic Disease
Cancer
|
|
17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats .
|
-
- HY-167737
-
|
|
Cytochrome P450
|
Cancer
|
|
(-)-Vorozole is an orally active non-steroidal aromatase inhibitor with potent and selective properties. (-)-Vorozole demonstrates antitumor activity in in vivo experiments. (-)-Vorozole is utilized in the study of breast cancer.
|
-
- HY-P9912A
-
|
|
EGFR
|
Cancer
|
|
Pertuzumab (anti-HER2), a humanized monoclonal antibody, is a HER2 dimerization inhibitor for the treatment of metastatic HER2-positive breast cancer.
|
-
- HY-N4010
-
|
|
Others
|
Cancer
|
|
Iriflophenone, isolated from Aquilaria sinensis, stimulates MCF-7 and T-47D human breast cancer cells proliferation .
|
-
- HY-111645
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
3-Methylcytidine, a urinary nucleoside, can be used as a biomarker of four different types of cancer: lung cancer, gastric cancer, colon cancer, and breast cancer .
|
-
- HY-112749
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
ME-344 is a mitochondrial inhibitor. ME-344 has significant biological antitumor activity in HER2-negative breast cancer .
|
-
- HY-173296
-
|
|
Lipase
|
Cancer
|
|
MAGL-IN-222 (Compound ZQ-7) is a covalent inhibitor targeting monoacylglycerol lipase (MAGL) with an IC50 of 42.31 μM. MAGL-IN-222 can reduce the breakdown of 2-arachidonoylglycerol (2-AG) and increase the intracellular 2-AG level, thereby inhibiting the proliferation and migration of MDA-MB-231 breast cancer cells. MAGL-IN-222 can be used in the research of breast cancer and other related diseases .
|
-
- HY-N2013
-
|
Aristololactam; Aristolactam
|
Drug Metabolite
Aquaporin
Cadherin
TGF-beta/Smad
|
Endocrinology
Cancer
|
|
Aristolactam I is an AQP1 inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis .
|
-
- HY-138098
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
|
-
- HY-18719A
-
|
|
Estrogen Receptor/ERR
Potassium Channel
|
Cancer
|
|
Endoxifen Z-isomer hydrochloride is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα).
|
-
- HY-129246
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Cytembena is inhibitor for replicative DNA synthesis, purine synthesis and tetrahydrofolate formylase activity. Cytembena ameliorates ovarian or breast cancer, relieves the pain from skeletal metastases .
|
-
- HY-12825
-
-
- HY-B0412S3
-
-
- HY-169213
-
|
|
KLF
RAD51
|
Cancer
|
|
LN-439A (compound LN-439A) is a BAP1 inhibitor that inhibits the growth of basal-like breast cancer by degrading KLF5. .
|
-
- HY-136552
-
|
|
Others
|
Cancer
|
|
β-Bisabolene is a sesquiterpene isolated from opoponax (Commiphora guidotti). β-Bisabolene, an anti-cancer agent, can be used for the study of breast cancer .
|
-
- HY-N0399
-
|
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Wogonoside, a flavonoid glycoside isolated from Huangqin, possesses anti-inflammatory effects. Wogonoside induces autophagy in breast cancer cells by regulating MAPK-mTOR pathway .
|
-
- HY-135699
-
TD52
1 Publications Verification
|
Apoptosis
Phosphatase
Akt
|
Cancer
|
|
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-135699A
-
|
|
Akt
Phosphatase
Apoptosis
|
Cancer
|
|
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-128553
-
-
- HY-N10304
-
|
|
Apoptosis
|
Cancer
|
|
Isodispar B is an anticancer agent that inhibits the proliferation of nasopharyngeal carcinoma and breast cancer cells and induces cell apoptosis. Isodispar B is cytotoxic to a wide range of cancer cell lines .
|
-
- HY-139828
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 14 is a lead compound (IC50: 0.20 to 0.65 μM) that induces apoptosis, cell cycle arrest, and loss of mitochondrial membrane potential in breast cancer cells.
|
-
- HY-N10305
-
|
|
Autophagy
|
Cancer
|
|
Clionamine B is an autophagy stimulating aminosteroid isolated from the sponge Cliona celata. Clionamine B strongly stimulates autophagy in human breast cancer MCF-7 cells .
|
-
- HY-18719B
-
-
- HY-17557
-
|
NSC173328; 5-Methyl THF calcium
|
Antifolate
|
Cardiovascular Disease
Cancer
|
|
Calcium N5-methyltetrahydrofolate(NSC173328) is the calcium salt of levomefolic acid, which has been proposed for treatment of cardiovascular disease and advanced cancers such as breast and colorectal cancers.
|
-
- HY-126363
-
|
Diethyldithiocarbamic acid
|
HIV
|
Infection
Cancer
|
|
Ditiocarb (Diethyldithiocarbamic acid) is an accelerator of the rate of copper cementation. Ditiocarb (Diethyldithiocarbamic acid) reduces the incidence of HIV infection, and also enhances adjuvant immunoresearch of high risk breast cancer .
|
-
- HY-18719E
-
-
- HY-161954
-
|
|
HDAC
|
Cancer
|
|
HDAC8-IN-12 (compound 5k) is a non-hydroxamic acid, selective inhibitor of HDAC8 (IC50: 0.12 nM) and a potent inhibitor of breast cancer. HDAC8-IN-12 triggers anti-tumor immunity by activating T cells, increasing the proportion of M1 macrophages and decreasing the proportion of M2 macrophages. HDAC8-IN-12 (50 mg/kg) exerts tumor suppressive effects in an orthotopic mouse model of breast cancer .
|
-
- HY-12015R
-
|
|
PARP
Influenza Virus
|
Cancer
|
|
Iniparib (Standard) is the analytical standard of Iniparib. This product is intended for research and analytical applications. Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer.
|
-
- HY-144014
-
|
|
Liposome
|
Cancer
|
|
MVL5 is a non-degradable multivalent cationic lipid. MVL5 is a highly efficient vector for both DNA and siRNA. MVL5 can be used in breast cancer research .
|
-
- HY-19753
-
KS176
2 Publications Verification
|
BCRP
|
Cancer
|
|
KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter (IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively).
|
-
- HY-172961
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-162 (compound 20) is a potent EGFR inhibitor. EGFR-IN-162 increases early and late apoptosis and necrosis. EGFR-IN-162 is promising for research of breast cancer .
|
-
- HY-100395
-
|
|
Apoptosis
|
Cancer
|
|
F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
|
-
- HY-147802
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-59 (Compound 8c) is a EGFR inhibitor (IC50=190 nM) and apoptosis inducer. EGFR-IN-59 exhibits cytotoxicity against non-small lung cancer cell lines (A549) and normal lung fibroblasts (WI38) with IC50s of 8.62 and 52.6 µM, respectively. EGFR-IN-59 can be used for the research of various cancers such as non-small cell lung cancer (NSCLC), head and neck cancer, breast cancer and colorectal cancer .
|
-
- HY-153670
-
|
|
CCR
|
Cancer
|
|
IPG7236 is a selective CCR8 antagonist. IPG7236 exhibits significant tumor suppression in a mouse xenograft model of human breast cancer. IPG7236 can be used in cancer research .
|
-
- HY-N2483
-
|
|
Others
|
Cancer
|
|
Hydroprotopine is a alkaloid from Hypecoum leptocarpumand. Leptopidine can suppress growth and induce cytotoxicity in breast cancer cells and that the cytotoxicity of leptopidine may be related to its inhibitory effect on fatty acid synthase expression .
|
-
- HY-N7215
-
|
|
β-catenin
Wnt
|
Cancer
|
|
Jatrophone is a diterpenoid with anticancer activity isolated from Jatropha isabelli. Jatrophone interferes with the Wnt/β-catenin pathway to inhibit the proliferation and epithelial-mesenchymal transition (EMT) of triple-negative breast cancer cells.
|
-
- HY-171477
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
|
-
- HY-117885
-
|
|
PDK-1
|
Cancer
|
|
PF-5177624 is a specific and potent inhibitor of PDK1, a key enzyme in the PI3K/AKT signaling pathway that is frequently dysregulated in breast cancer. PDK1 phosphorylates AKT at T308 and other substrates, activating downstream signaling pathways that are important for tumor progression. PF-5177624 blocks IGF-1-stimulated PDK1 activity and downstream AKT and p70S6K phosphorylation, reducing cell proliferation and transformation in breast cancer cells .
|
-
- HY-156077
-
|
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
anti-TNBC agent-2 (3j) an anti-Triple negative breast cancer (TNBC) purine derivative. anti-TNBC agent-2 induces MDA-MB-231 cells apoptosis, and inhibits its migration and angiogenesis. anti-TNBC agent-2 inhibits tumor growth and metastasis and reduces the expression of Ki67 and CD31 protein in TNBC xenograft models. anti-TNBC agent-2 can be used for Triple negative breast cancer (TNBC) research .
|
-
- HY-123918
-
|
|
CX3CR1
|
Endocrinology
Cancer
|
|
JMS-17-2 is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. JMS-17-2 impairs metastatic seeding and colonization of breast cancer cells .
|
-
- HY-124454
-
|
|
Drug Derivative
|
Cancer
|
|
JCC76 is the derivative of Nimesulide (HY-B0363). JCC76 inhibits the proliferation of Her2 positive breast cancer cell SKBR-3 with IC50 of 3.43 μM .
|
-
- HY-121250
-
|
|
Fatty Acid Synthase (FASN)
Apoptosis
|
Cancer
|
|
Fasnall is a selective fatty acid synthase (FASN) inhibitor with an IC50 of 3.71 μM. Fasnall induces apoptosis in HER2 + breast cancer cell lines. Fasnall shows potent anti-tumor activities .
|
-
- HY-N6990
-
|
|
Others
|
Cancer
|
|
Anhydrosecoisolariciresinol is from the flower of Wedelia biflora, has anti-tumor activities .
Anhydrosecoisolariciresinol decreases the growth of human breast cancer MCF-7 and MDA-MB-231 cell lines .
|
-
- HY-132885
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.
|
-
- HY-113627A
-
|
|
Antibiotic
Bacterial
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Undecylprodigiosin hydrochloride, a member of the family of prodiginines, is a potent antibiotic. Undecylprodigiosin hydrochloride can selectively induce apoptosis in human breast carcinoma cells independent of p53. Undecylprodigiosin hydrochloride shows immunosuppressive, anticancer properties and antimicrobial activities .
|
-
- HY-123918A
-
|
|
CX3CR1
|
Endocrinology
Cancer
|
|
JMS-17-2 hydrochloride is a potent and selective CX3CR1 antagonist with an IC50 of 0.32 nM. JMS-17-2 hydrochloride impairs metastatic seeding and colonization of breast cancer cells .
|
-
- HY-119995
-
|
|
Apoptosis
Histamine Receptor
|
Cardiovascular Disease
Cancer
|
|
Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma .
|
-
- HY-13738A
-
|
Keoxifene hydrochloride; LY156758; LY139481 hydrochloride
|
Estrogen Receptor/ERR
Autophagy
|
Endocrinology
Cancer
|
|
Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue .
|
-
- HY-50879
-
|
GF120918; GW0918; GG918; GW120918
|
P-glycoprotein
BCRP
|
Cancer
|
|
Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer .
|
-
- HY-113627
-
|
|
Antibiotic
Bacterial
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Undecylprodigiosin, a member of the family of prodiginines, is a potent antibiotic. Undecylprodigiosin can selectively induce apoptosis in human breast carcinoma cells independent of p53. Undecylprodigiosin shows immunosuppressive, anticancer properties and antimicrobial activities .
|
-
- HY-N2585
-
|
|
Reactive Oxygen Species (ROS)
NF-κB
Autophagy
|
Cancer
|
|
Isodeoxyelephantopin is a sesquiterpene lactone isolated from Elephantopus scaber. Isodeoxyelephantopin induces ROS generation, suppresses NF-κB activation. Isodeoxyelephantopin also modulates LncRNA expression and exhibit activities against breast cancer .
|
-
- HY-112596A
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-6545 hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .
|
-
- HY-N0770
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Isoliensinine is a bisbenzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera, with anti-oxidant and anti-inflammatory and anti-cancer activities. Isoliensinine induces apoptosis in triple-negative human breast cancer cells .
|
-
- HY-112596
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer .
|
-
- HY-B2123
-
-
- HY-156402
-
|
|
Topoisomerase
|
Cancer
|
|
AuM1Gly is a topoisomerase I inhibitor. AuM1Gly affects the growth of MDA-MB-231 breast cancer cells, with IC50?values in the low nanomolar range .
|
-
- HY-N2028
-
|
|
Ser/Thr Protease
|
Cancer
|
|
Demethylwedelolactone is a naturally occurring coumestan isolated from Eclipta alba. Demethylwedelolactone is a potent trypsin inhibitor with an IC50 of 3.0 μM. Demethylwedelolactone suppresses cell motility and cell invasion of breast cancer cell .
|
-
- HY-B0515B
-
|
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Ibandronate Sodium is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium inhibits tumor cell proliferation (such as ER+ breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
|
-
- HY-W011338S
-
|
|
Aryl Hydrocarbon Receptor
|
Cancer
|
|
Benzyl butyl phthalate-d4 is the deuterium labeled Benzyl butyl phthalate . Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs) .
|
-
- HY-N0858
-
|
|
HIV
|
Infection
|
|
Gomisin G is a lignin from S. chinesis with anti-HIV (EC50 = 0.006 μg/mL), anti-liver cancer and anti-inflammatory activities. Gomisin G has an AKT-cyclin D1 dependent mechanism against triple-negative breast cancer (TNBC) cells through suppressing phosphorylation rather than inducing apoptosis. Gomisin G can inhibit AKT phosphorylation. Gomisin G can cause cell cycle arrest in the G1 phase. Gomisin G can be studied in research for diseases such as HIV, breast and liver cancers .
|
-
- HY-N2013R
-
|
Aristololactam (Standard); Aristolactam (Standard)
|
Caspase
Apoptosis
|
Inflammation/Immunology
|
|
Aristolactam I (Standard) is the analytical standard of Aristolactam I. This product is intended for research and analytical applications. Aristolactam I is an AQP1 inhibitor and Aristolochic acid I metabolite. Aristolactam I can be isolated from Aristolochia plants. Aristolactam I downregulates Twist1 expression, increases E-cadherin expression, and activates the TGF-β/Smad signaling pathway. Aristolactam I has anticancer activity against breast cancer. Aristolactam I is nephrotoxic. Aristolactam I is mainly used in the study of breast cancer and kidney diseases such as renal interstitial fibrosis .
|
-
- HY-163467
-
-
- HY-129578
-
-
- HY-110109
-
|
|
PI3K
DNA-PK
mTOR
|
Cancer
|
|
ETP-45658 is a potent PI3K inhibitor, with IC50s of 22.0 nM, 39.8 nM, 129.0 nM and 717.3 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. ETP-45658 also can inhibit DNA-PK (IC50=70.6 nM) and mTOR (IC50=152.0 nM). ETP-45658 can be used for the research of cancer .
|
-
- HY-P2246
-
|
|
JNK
|
Cancer
|
|
JTP10-△-TATi TFA is a selective JNK2 peptide inhibitor, with an IC50 of 92 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3 .
|
-
- HY-P2247
-
|
|
JNK
|
Cancer
|
|
JTP10-△-R9 TFA is a selective JNK2 peptide inhibitor, with an IC50 of 89 nM, exhibiting 10-fold selectivity for JNK2 over JNK1 and JNK3 .
|
-
- HY-158389
-
|
|
Topoisomerase
|
Cancer
|
|
Anticancer agent 216 (34A) is a Camptothecin compound, with IC50 values of 9.6 nM and 11.6 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
|
-
- HY-158390
-
|
|
Topoisomerase
|
Cancer
|
|
Anticancer agent 217 (35B) is a Camptothecin compound, with IC50 values of 6.2 nM and 7.1 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
|
-
- HY-129578R
-
|
|
Reference Standards
Autophagy
Cathepsin
|
Infection
Inflammation/Immunology
Cancer
|
|
Asperphenamate (Standard) is the analytical standard of Asperphenamate. This product is intended for research and analytical applications. Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively[1][2].
|
-
- HY-151118
-
|
|
Apoptosis
|
Cancer
|
|
HER2-IN-11 is a psoralen derivative. HER2-IN-11 has anti-breast cancer activity and light-activated cytotoxicity. HER2-IN-11 induces apoptosis .
|
-
- HY-127079
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Epothilone F is a Microtubule/Tubulin-stabilizing agent with anti-tumor activity. Epothilone F inhibits the proliferation of breast cancer cells, non-small cell lung cancer cells, drug-resistant ovarian cancer cells .
|
-
- HY-W010248S
-
-
- HY-156228
-
|
|
Ras
|
Cancer
|
|
RGB-1 is a polycyclic aromatic hydrocarbon molecule and a stabilizer of RNA G-quadruplexes. RGB-1 can promote the inhibition of RNA translation and reduce the expression of NRAS proto-oncogene in breast cancer cells .
|
-
- HY-152010S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
L-Octanoylcarnitine-d3 (hydrochloride) is deuterium labeled L-Octanoylcarnitine. L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer .
|
-
- HY-149847
-
|
|
Ras
|
Cancer
|
|
JH530 is an effective methuosis inducer that inhibits the triple-negative breast cancer (TNBC) cells proliferation by causing intracellular complete vacuolization. JH530 has anti-tumor activity and can be used for cancer research .
|
-
- HY-139682A
-
-
- HY-151116
-
|
|
Apoptosis
|
Cancer
|
|
HER2-IN-10 is a psoralen derivative. HER2-IN-10 has anti-breast cancer activity and light-activated cytotoxicity. HER2-IN-10 induces apoptosis .
|
-
- HY-108315
-
|
6-Chrysenamine
|
Others
|
Inflammation/Immunology
Cancer
|
|
6-Aminochrysene (6-Aminochrysene) is an aromatic amine used as a chemotherapeutic agent in the treatment of splenomegaly, myeloid leukemia, and breast cancer. 6-Aminochrysene is activated by CYP450 in rat liver .
|
-
- HY-131463
-
|
|
Neurokinin Receptor
|
Cancer
|
|
ASN-1377642 is a NK1 receptor antagonist with a Ki value of 251 nM. ASN-1377642 shows antitumor action in breast cancer cells with NK1R-Tr high expression .
|
-
- HY-129037
-
|
|
BCRP
|
Cancer
|
|
BCRP-IN-1 (compound 48) is a potent inhibitor of breast cancer resistance protein (BCRP), with IC50s of 2.92 μM and 2.46 μM in Hoechst 33342 assay and Pheophorbide A assay, respectively .
|
-
- HY-N10528
-
-
- HY-15587
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells .
|
-
- HY-173040
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 266 (Compound 3B) is an anticancer agent that can inhibit the proliferation of tumor cells. Anticancer agent 266 has an IC50 of 0.13 μM for MCF-7 breast cancer cell line .
|
-
- HY-163275
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MDM2-IN-24 (compound A3f) exhibits MDM2-inhibiting and MDMX-activating properties in triple-negative breast cancer (TNBC) cells, with apoptotic and anti-proliferative activities .
|
-
- HY-N1513
-
|
|
AP-1
NF-κB
|
Cancer
|
|
Ganoderic acid H is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderic acid H suppresses growth and invasive behavior of breast cancer cells through the inhibition of transcription factors AP-1 and NF-kappaB signaling .
|
-
- HY-119377
-
|
|
Glutaminase
|
Cancer
|
|
UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines .
|
-
- HY-N7640
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Desoxylimonin is an orally active triterpenoid compound found from grapefruit seed. Desoxylimonin shows anti-proliferative activities to breast cancer cells. Desoxylimonin derivatives shows better anticancer, analgesic and anti-inflammatory activity than the lead compound .
|
-
- HY-170806
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 12 (Compound RA3) is an estrogen receptor α (ERα) degrader with antitumor properties. ERα degrader 12 induces pronounced tumor growth inhibition in a breast cancer xenograft mouse model .
|
-
- HY-150542
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase -IN-2 is an active steroid sulfatase (STS) inhibitor with an IC50 value of 109.5 nM. Steroid sulfatase-IN-2 can be used for the research of hormone-dependent cancers, such as estrogen-dependent breast and endometrial cancer .
|
-
- HY-N13118
-
|
|
Others
|
Cancer
|
|
Sinopodophylline B (compound 2) is a flavonoid glycoside compound that is cytotoxic to breast cancer cells. For example, the IC50 of Sinopodophylline B is 1.5 μM (T47D) and 44.2 μM (MDA-MB-231), respectively .
|
-
- HY-147526
-
|
|
Apoptosis
|
Cancer
|
|
RM-581, an aminosteroid derivative, is an endoplasmic reticulum stress (ERS) inducer. RM-581 induces cancer cells apoptosis. RM-581 can be used for the study of pancreatic, prostate and breast cancers .
|
-
- HY-18719ES
-
|
|
Cytochrome P450
Estrogen Receptor/ERR
Drug Metabolite
Parasite
|
Cancer
|
|
Endoxifen-d5 is the deuterium labeled Endoxifen. Endoxifen is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen has the potential for breast cancer study .
|
-
- HY-164980
-
|
|
Kinesin
|
Cancer
|
|
KIF18A-IN-16 (Compound 15) is a fused ring KIF18A inhibitor. KIF18A-IN-16 can be used in oncology (e.g., colon, breast, lung cancer) studies .
|
-
- HY-163308
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bcl-2-IN-18 (Compound 23) is a breast cancer Bcl-2 inhibitor with a IC50 value of 4.7 μM for MCF-7. Bcl-2-IN-18 has antitumor activity .
|
-
- HY-121582
-
|
(E)-EPH 116
|
Drug Isomer
|
Cancer
|
|
(E)-SI-2 is an isomer of SI-2, an inhibitor of the steroid receptor coactivator SRC-3. SI-2 has anticancer activity and increases the number of cytotoxic immune cells in mice with breast cancer .
|
-
- HY-118618
-
|
Hiyodorilactone A; Schkuhrin I
|
STAT
|
Cancer
|
|
Eucannabinolide is a STAT3 inhibitor. Eucannabinolide suppresses STAT3 activation at tyrosine 705, inhibiteds its translocation to nucleus, and decreases its DNA binding capacity. Eucannabinolide can be used for triple negative breast cancer (TNBC) diseases research .
|
-
- HY-112721
-
FDI-6
3 Publications Verification
|
DNA/RNA Synthesis
|
Cancer
|
|
FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.
|
-
- HY-B0812
-
|
SSA dihydrate
|
Biochemical Assay Reagents
|
Cancer
|
|
5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
|
-
- HY-168143
-
|
|
Histone Methyltransferase
|
Cancer
|
|
YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors. .
|
-
- HY-50880
-
|
GF120918A
|
P-glycoprotein
BCRP
|
Cancer
|
|
Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer .
|
-
- HY-P10853
-
|
|
Autophagy
|
Cancer
|
|
Bacilotetrin C analogue is cytotoxic to triple-negative breast cancer cell line MDA-MB-231 with an IC50 of 0.48 μM. Bacilotetrin C analogue can induce tumor cell autophagy and has anti-tumor activity .
|
-
- HY-122943
-
|
|
Fungal
Apoptosis
|
Infection
Cancer
|
|
Moracin D is a flavonoid that can be isolated from Morus alba. Moracin D induces cell apoptosis and shows hypoglycemic, antiadipogenic, antifungal and antitumor effects. Moracin D can be used for fungal infection and breast cancer research .
|
-
- HY-B0448S
-
-
- HY-13593
-
|
CB-1348; WR-139013
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease .
|
-
- HY-13632
-
|
FCE 24304; EXE
|
Cytochrome P450
|
Endocrinology
Cancer
|
|
Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
|
-
- HY-N0431
-
|
|
MMP
ERK
JNK
|
Cancer
|
|
Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
|
-
- HY-N11438
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
3'-Hydroxymirificin (compound 3) is a naural compound that can be isolated from Pueraria lobata roots. 3'-Hydroxymirificin (compound 3) possesses estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
|
-
- HY-113161S1
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cancer
|
|
L-Octanoylcarnitine-d9 is deuterium labeled L-Octanoylcarnitine. L-Octanoylcarnitine is a plasma metabolite and a physiologically active form of octanoylcarnitine. L-Octanoylcarnitine can be used for the research of breast cancer . .
|
-
- HY-162805
-
|
|
NO Synthase
Topoisomerase
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
|
iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM) .
|
-
- HY-B0515
-
|
BM-210955; RPR-102289A
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium Monohydrate can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium Monohydrate inhibits tumor cell proliferation (such as ER + breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium Monohydrate is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
|
-
- HY-N0308
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Octyl acetate is an orally active aliphatic ester. Octyl acetate has certain antioxidant properties. Octyl acetate contributes to the formation of fruit aroma and affects the flavor of fruits such as strawberries. Octyl acetate can be used in the research of malignant melanoma, colon cancer and breast cancer .
|
-
- HY-155309
-
|
|
YAP
|
Cancer
|
|
LM-41 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2. LM-41 inhibits migration of human MDA-MB-231 breast cancer cells .
|
-
- HY-N7083
-
Citral
1 Publications Verification
|
Parasite
|
Inflammation/Immunology
Cancer
|
|
Citral is an orally active monoterpene compound in lemon grass essential oil and a natural ALDH1A inhibitor, which can induce apoptosis and cycle arrest in breast cancer cell lines, and has analgesic, anti-injurious and anti-inflammatory effects [2][3].
|
-
- HY-14907
-
|
MPC 6827
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin (MPC-6827) is a highly potent and broad-spectrum microtubule blocker. Verubulin has antitumor activity against breast cancer, melanoma, and ovarian cancer. Verubulin can be used in non-small cell lung cancer research .
|
-
- HY-N0036
-
|
(+)-Costunolide; Costus lactone
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest and apoptosis on breast cancer cells .
|
-
- HY-W040270
-
|
|
PROTAC Linkers
|
Cancer
|
|
Amino-PEG10-amine, a PEG-based PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer .
|
-
- HY-W702106
-
|
|
Endogenous Metabolite
|
Cancer
|
2-Methyl estradiol, an endogenous metabolite of Estradiol (HY-B0141), inhibits cell proliferation and angiogenesis, with IC50 values of 3 and 2.39 μM for HUVEC and MCF-7 human breast cancer cell proliferation, respectively .
|
-
- HY-169130
-
|
|
Fluorescent Dye
|
Cancer
|
|
Lyso BD-1, preferentially colocalized in lysosomes and lipid droplets, displays excellent photocytotoxicity (5.57 μM) on triple negative breast cancer cells under white light. Lyso BD-1 displays emission band at 560nm .
|
-
- HY-N6635
-
|
|
Fungal
|
Infection
Cancer
|
|
trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (DOX) (HY-15142A) against intestinal cancer and breast cancer cells in vitro. trans-Nerolidol increases accumulation of DOX inside cells in vitro. trans-Nerolidol activates apoptosis in vivo .
|
-
- HY-N0399R
-
|
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Wogonoside (Standard) is the analytical standard of Wogonoside. This product is intended for research and analytical applications. Wogonoside, a flavonoid glycoside isolated from Huangqin, possesses anti-inflammatory effects. Wogonoside induces autophagy in breast cancer cells by regulating MAPK-mTOR pathway .
|
-
- HY-N2330R
-
|
|
Lipase
|
Metabolic Disease
|
|
Ginsenoside F2 (Standard) is the analytical standard of Ginsenoside F2. This product is intended for research and analytical applications. Ginsenoside F2, a metabolite from Ginsenoside Rb1, induces apoptosis accompanied by protective autophagy in breast cancer stem cells .
|
-
- HY-155251
-
|
|
Apoptosis
Bcl-2 Family
|
Cancer
|
|
anti-TNBC agent-3 (compound 3g) is an apoptosis inducer with anti-cancer cell proliferation activity. anti-TNBC agent-3 inhibits tumor growth and metastasis in triple-negative breast cancer (TNBC) xenograft models .
|
-
- HY-156919
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 8 (compound 5) is a p53 activator. p53 Activator 8 has potent anti-proliferative activity against MCF7 breast cancer cell lines with an IC 50 value of 0.5 μM .
|
-
- HY-125848R
-
|
|
Apoptosis
Autophagy
Endogenous Metabolite
|
Cancer
|
|
Ginsenoside F2 (Standard) is the analytical standard of Ginsenoside F2. This product is intended for research and analytical applications. Ginsenoside F2, a metabolite from Ginsenoside Rb1, induces apoptosis accompanied by protective autophagy in breast cancer stem cells .
|
-
- HY-N4227
-
|
|
Others
|
Cancer
|
|
Conicasterol is a 4-mercaptosteroid with significant cytotoxic activity. Conicasterol showed an IC50 value of 6.23 μg/mL in a test on a human breast adenocarcinoma cell line (MCF-7). Conicasterol's antitumor activity makes it a potential bioactive lead molecule .
|
-
- HY-P991332
-
|
|
CD73
|
Cancer
|
|
JAB-BX102 is a human monoclonal antibody (mAb) targeting NT5E/CD73. JAB-BX102 can be used in the study of cancers such as breast cancer, pancreatic cancer, and prostate cancer .
|
-
- HY-A0267
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Bitolterol is a β2-adrenergic agonist with bronchodilator activity. Bitolterol is classified as a prodrug and is primarily used for the suppression of respiratory diseases. Bitolterol is considered safe for use during breastfeeding, as the amount that can enter breast milk is very limited .
|
-
- HY-P99768
-
|
TTAC-0001
|
VEGFR
|
Cancer
|
|
Olinvacimab (TTAC-0001) is a fully human anti-VEGFR2 monoclonal antibody. Olinvacimab inhibits VEGF binds to KDR with a Kd value of 0.23 nM. Olinvacimab has antiangiogenic activity. Olinvacimab can be used for the research of recurrent glioblastoma and breast cancer .
|
-
- HY-162012
-
|
|
YAP
|
Cancer
|
|
HC-258 (compound 26) binds with the cysteine in TEAD’s PA pocket. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells .
|
-
- HY-156422
-
|
|
HDAC
|
Neurological Disease
Cancer
|
|
KPZ560 is a potent inhibitor of HDAC1 and HDAC2, with IC50s of 12 nM and 68 nM, respectively. KPZ560 can increase in the spine density of granule neuron dendrites of mice and inhibitor cell growth of breast cancer cell line MCF .
|
-
- HY-P99010
-
|
|
FGFR
|
Cancer
|
|
Bemarituzumab is a humanized IgG1 monoclonal antibody against FGFR2b (a FGF receptor). Bemarituzumab blocks fibroblast growth factors from binding and activating FGFR2b. Bemarituzumab has antitumor activity against gastric and breast cancer .
|
-
- HY-114206
-
|
|
Histone Methyltransferase
|
Cancer
|
|
SKI-73 is a chemical probe for CARM1 with prodrug properties. SKI-73 can rapidly penetrate cell membranes and be processed into active inhibitors. SKI-73 inhibits the invasion of breast cancer cells and can be used in the study of cancer .
|
-
- HY-N13213
-
|
|
Others
|
Cancer
|
|
Fenugreek Seed Extract is a fenugreek extract. Fenugreek Seed Extract has potential antibacterial and anticancer activities, can inhibit Staphylococcus aureus and Pseudomonas aeruginosa, and inhibit the proliferation of MCF-7 breast cancer cells (no significant effect on liver cancer cells). .
|
-
- HY-173146
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR-IN-153 (Compound 5l) is an EGFR inhibitor. EGFR-IN-153 can inhibit the proliferation (IC50: 0.73 μM) and induce apoptosis of MDA-MB-231 cell. EGFR-IN-153 can be used for the research of breast cancer .
|
-
- HY-163947
-
|
|
VD/VDR
|
Cancer
|
|
UG-480 is a gemini analog that effectively stabilizes the active VDR conformation. UG-480 has antiproliferative effects in estrogen receptor-positive MCF-7 breast adenocarcinoma cells. UG-480 can be used in cancer research .
|
-
- HY-147081
-
|
AGRO-100
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
|
-
- HY-119272
-
EF24
1 Publications Verification
|
ERK
Caspase
NF-κB
Apoptosis
p38 MAPK
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
|
-
- HY-N0858R
-
|
|
Reference Standards
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
Gomisin G (Standard) is the analytical standard of Gomisin G. This product is intended for research and analytical applications. Gomisin G is a lignin from S. chinesis with anti-HIV (EC50 = 0.006 μg/mL), anti-liver cancer and anti-inflammatory activities. Gomisin G has an AKT-cyclin D1 dependent mechanism against triple-negative breast cancer (TNBC) cells through suppressing phosphorylation rather than inducing apoptosis. Gomisin G can inhibit AKT phosphorylation. Gomisin G can cause cell cycle arrest in the G1 phase. Gomisin G can be studied in research for diseases such as HIV, breast and liver cancers .
|
-
- HY-W012349
-
|
|
NF-κB
Fungal
Apoptosis
Autophagy
|
Infection
Cancer
|
|
2′-Hydroxychalcone is a hydroxyl derivative of chalcones with anticancer activities. 2'-Hydroxychalcone inhibits NF-κB pathway and induces autophagy and apoptosis in breast cancer cells . 2′-Hydroxychalcone shows a better antifungal activity against the complex Paracoccidioides spp .
|
-
- HY-172139
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-25 (Compound Djh1) is a selective PI3Kα inhibitor. PI3Kα-IN-25 can be used in triple-negative breast cancer research .
|
-
- HY-155109
-
|
|
STING
|
Inflammation/Immunology
Cancer
|
|
Antitumor agent-114 is a potent stimulator of interferon genes (STING) agonist. Antitumor agent-114 activates immunity and reduces tumor volume in a mouse model of breast cancer. Antitumor agent-114 can be used for immunity and cancer diseases research .
|
-
- HY-18719BR
-
|
|
Cytochrome P450
Estrogen Receptor/ERR
Drug Metabolite
Parasite
|
Cancer
|
|
Endoxifen (hydrochloride) (Standard) is the analytical standard of Endoxifen (hydrochloride). This product is intended for research and analytical applications. Endoxifen hydrochloride is a key active metabolite of Tamoxifen (TAM) with higher affinity and specificity to estrogen receptor that also inhibits aromatase activity. Endoxifen hydrochloride has the potential for breast cancer study[1][2].
|
-
- HY-N0153A
-
|
Naringoside hydrate
|
Cytochrome P450
Apoptosis
Mitophagy
|
Cancer
|
|
Niacinamide ascorbate is a vitamin complex that combines niacinamide (vitamin B3) and ascorbic acid (vitamin C). Niacinamide ascorbate reduces the risk of radiation-induced acute leukemia, breast cancer, thyroid cancer, and other somatic and genetic mutations following exposure to ionizing radiation doses .
|
-
- HY-116494
-
|
|
BCRP
|
Cancer
|
|
ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
|
-
- HY-165473
-
|
|
Calcium Channel
|
Cancer
|
|
Hexadecylphosphoserine is a phospholipid molecule that contains a long-chain alkyl (hexadecyl) and a phosphoserine group, giving it a high affinity for the cell membrane. Hexadecylphosphoserine can exert antitumor activity by modulating [Ca ++]i and its related signaling pathways, making it useful for research in the field of breast cancer .
|
-
- HY-Y0519R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Pyrimidine (Standard) is the analytical standard of Pyrimidine. This product is intended for research and analytical applications. Pyrimidine is a nitrogen-containing heterocyclic compound and endogenous metabolite. Pyrimidine derivatives can be used in pancreatic cancer, triple-negative breast cancer, colon carcinoma and neuron research .
|
-
- HY-130411
-
|
|
PROTAC Linkers
|
Cancer
|
|
Amino-PEG11-amine, a PEG-based (12 units) PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer .
|
-
- HY-155490
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
|
Cancer
|
|
Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KD SPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells .
|
-
- HY-141520
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .
|
-
- HY-13556
-
|
LY353381; SERM III
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile .
|
-
- HY-N15584
-
|
Isoheraclenin
|
Others
|
Cancer
|
|
Pabularinone is a compound found in the plant Clausena lansium. Pabularinone has potent cytotoxic activity, and its activity showed inhibitory effects in human breast cancer (MCF-7) cells (IC50: 33.74 μg/mL). Pabularinone can be used in anti-tumor research .
|
-
- HY-173210
-
|
|
Apoptosis
TNF Receptor
|
Cancer
|
|
TNF-α-IN-22 (Compound 30) is a TNFα inhibitor. It can induce Apoptosis by inhibiting the downregulation of IkBα induced by TNFα and blocking the cell cycle. TNF-α-IN-22 can be used in the research of triple-negative breast cancer .
|
-
- HY-W004066R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Ac-Ala-OH (Standard) is an analytical standard for Ac-Ala-OH. This product is intended for use in research and analytical applications. Ac-Ala-OH is an endogenous metabolite. Ac-ALA-OH inhibits APEH. Ac-Ala-OH is useful in breast cancer research .
|
-
- HY-101567
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively .
|
-
- HY-13673S2
-
|
|
Isotope-Labeled Compounds
Apoptosis
GnRH Receptor
|
Endocrinology
Cancer
|
|
Goserelin-d7 (TFA) is deuterium labeled Goserelin. Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
|
-
- HY-N10959
-
|
|
Others
|
Cancer
|
|
4,15-Isoatriplicolide methylacrylate is a germacrane-type sesquiterpene lactone. 4,15-Isoatriplicolide methylacrylate also is a cytotoxic agent. 4,15-Isoatriplicolide methylacrylate has cytotoxic activity for MCF-7 human breast cancer cell line .
|
-
- HY-133737
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-5 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-5 can potent degrade BRD4 in HER2 positive and negative breast cancer cell lines .
|
-
- HY-114988
-
|
tetranor-PGEM
|
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
PGE-M is a metabolite of prostaglandin E2 (PEG2) as a biomarker of inflammation and cancer including advanced colorectal neoplasia, ovarian cancer, prostate cancer and so on. Urinary PGE-M is positively associated with obesity, smoking and lung metastases with breast cancer .
|
-
- HY-164064
-
|
|
ClpP
|
Cancer
|
|
Anticancer agent 230 (example 65) is a caseinolytic protease P (ClpP) activator with anticancer activity. Anticancer agent 230 is able to induce the degradation of mitochondrial proteins in SUM159 and MDA-MB-231 triple-negative breast cancer cells in a time-dependent manner .
|
-
- HY-B2123R
-
|
|
Endogenous Metabolite
Interleukin Related
ERK
NF-κB
|
Inflammation/Immunology
|
|
Lactose (Standard) is the analytical standard of Lactose. This product is intended for research and analytical applications. Lactose is a β-galactoside consisting of galactose and glucose residues, the main carbohydrate in mammalian breast milk. Lactose, a macronutrient and an inducer of host innate immune responses, possesses immune modulatory functions .
|
-
- HY-N1252
-
|
|
Others
|
Cancer
|
|
Scillascillin (compound 10) is a homoisoflavanone. Scillascillin can be isolated from S. scilloides. Scillascillin shows anticancer activity towards MCF-7 (breast cancer) and DU-145 (prostate cancer) cells with the IC50 of 9.59 and 11.32 ug/ml, respectively .
|
-
- HY-163113
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Anticancer agent 180 (compound 4) is a secondary metabolite present in fungal strains and extracted through physical interaction with Streptomyces sp. Anticancer agent 180 has potential anti-tumor activity and can inhibit the migration of MDA-MB-231 breast cancer cells .
|
-
- HY-N3354
-
|
8-prenylgenistein
|
Apoptosis
|
Cancer
|
|
Lupiwighteone is an isoflavone present widely in wild-growing plants, with antioxidant, antimicrobial and anticancer effects. Lupiwighteone induces caspase-dependent and -independent apoptosis on human breast cancer cells via inhibiting PI3K/Akt/mTOR pathway .
|
-
- HY-111645R
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
3-Methylcytidine (Standard) is the analytical standard of 3-Methylcytidine. This product is intended for research and analytical applications. 3-Methylcytidine, a urinary nucleoside, can be used as a biomarker of four different types of cancer: lung cancer, gastric cancer, colon cancer, and breast cancer .
|
-
- HY-100544
-
FLLL32
5 Publications Verification
|
STAT
JAK
Apoptosis
|
Cancer
|
|
FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells .
|
-
- HY-173220
-
|
|
Dihydrofolate reductase (DHFR)
Apoptosis
|
Cancer
|
DHFR-IN-23 (compound 5) is a dual DNA binders/DHFR inhibitor, with an IC50 of 0.08 μM for hDHFR. DHFR-IN-23 (compound 5) is also an apoptosis inducer. DHFR-IN-23 (compound 5) can be used for the research of ER+ breast cancer .
|
-
- HY-N3945
-
|
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
MMP
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid extracted from Glaucium flavum that possesses various activities, including cough relief, bronchodilation, anti-inflammatory effects, analgesia, antipyretic properties, and anticancer effects. Glaucine acts as a selective and orally active inhibitor of phosphodiesterase 4 (PDE4), with a Ki of 3.4 µM in human bronchial tissues and polymorphonuclear leukocytes. Glaucine induces relaxation of human isolated bronchi by antagonizing calcium channels. Additionally, Glaucine inhibits the activation of NF-κB, leading to a reduction in the expression of the MMP-9 gene, thereby suppressing the migration and invasion of breast cancer cells. Therefore, Glaucine holds potential for research in asthma and breast cancer .
|
-
- HY-150803
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
VHL Ligand 14 (Compound 11) is a VHL ligand for design of PROTAC estrogen receptor α (ERα) degraders, with a binding affinity IC50 of 196 nM .
|
-
- HY-160613
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-11 (compound 20) is an orally active dual inhibitor for human epidermal growth factor receptor 2 (HER2) and epidermal growth factor receptor (EGFR), with IC50s of 7.7 and 22 nM, respectively. EGFR/HER2-IN-11 exhibits antitumor efficacy and inhibits proliferation against cancer cells BT-474 with GI50 of 601 nM .
|
-
- HY-116939
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(E)-Broparestrol is a biologically active tetrasubstituted olefin, which is used as an estrogen in dermatology .
|
-
- HY-119653
-
|
|
PARP
|
Cancer
|
|
AZ9482 is a triple PARP1/2/6 inhibitor, with IC50 values of 1 nM, 1 nM and 640 nM for PARP1, PARP2 and PARP6, respectively .
|
-
- HY-170552
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
KC12 is an inhibitor for FOXM1 transcription factor. KC12 exhibits cytotoxicity in cancer cell MDA-MB-231 with an IC50 of 6.13 µM .
|
-
- HY-163490
-
|
|
Wee1
|
Cancer
|
|
PKMYT1-IN-1 (Compound 1) is an inhibitor for membrane-associated tyrosine and threonine kinase (PKMYT1), with an IC50 of 8.8 nM. PKMYT1-IN-1 inhibits proliferation of tumor cell HCC1569 with IC50 of 42 nM .
|
-
- HY-159897
-
|
|
PAK
LIM Kinase (LIMK)
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.) .
|
-
- HY-158208
-
|
|
Apoptosis
|
Cancer
|
|
PMMB276 is a potent inhibitor of β-tubulin isotype III (Tubb3) polymerization and induced apoptosis. PMMB276 plays an important role in cancer research .
|
-
- HY-139362
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Enpp-1-IN-2 (Compound C) is a potent ENPP1 (ectonucleotide pyrophosphatase/phosphodiesterase 1) inhibitor with IC50 values of 0.26, 0.48 and 2.0 μM evaluated by means of TG-mAMP, pNP-TMP, and ATP assays, respectively. TG (Tokyo Green)-mAMP: a newly synthesized sensitive ENPP1 fluorescence probe .
|
-
- HY-50767S
-
|
PD 0332991-d8
|
Isotope-Labeled Compounds
CDK
|
Cancer
|
|
Palbociclib-d8 is a deuterium labeled Palbociclib. Palbociclib is a selective and orally active CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .
|
-
- HY-165473A
-
|
|
Calcium Channel
|
Cancer
|
|
Hexadecylphosphoserine TFA is a phospholipid molecule that contains a long-chain alkyl (hexadecyl) and a phosphoserine group, giving it a high affinity for the cell membrane. Hexadecylphosphoserine TFA can exert antitumor activity by modulating [Ca ++]i and its related signaling pathways, making it useful for research in the field of breast cancer .
|
-
- HY-78726A
-
|
Amprenavir phosphate sodium; GW 433908 sodium
|
HIV
Endogenous Metabolite
|
Infection
|
|
Fosamprenavir sodium (Amprenavir phosphate sodium) is an anti-HIV drug with antiviral activity. Fosamprenavir sodium is a water-soluble prodrug of amprenavir. Fosamprenavir sodium can help achieve and maintain viral suppression during antiretroviral suppression, thereby reducing the risk of HIV transmission through breast milk. Fosamprenavir sodium is not recommended for use during breastfeeding .
|
-
- HY-169804
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ENPP3 Inhibitor 1 is a selective inhibitor of ENPP3, with IC50s of 0.15 µM (ENPP3) and 41.4 µM (ENPP1) respectively. ENPP3 Inhibitor 1 shows anti-tumor activities against breast cancer and cervical cancer .
|
-
- HY-P4144
-
|
Phor18-LHRH (338613); EP-100
|
GnRH Receptor
|
Endocrinology
Cancer
|
|
Onvitrelin ucalontide ([Phor18-LHRH (338613)]) is an analogue of luteinizing hormone releasing hormone (LHRH) with antineoplastic activity. Onvitrelin ucalontide is a peptide with sequences of KFAKFAKKFAKFAKKFAKQHWSYGLRPG. Onvitrelin ucalontide effectively inhibits breast cancer, ovarian cancer and prostate cancer xenografts in mouse model .
|
-
- HY-168950
-
|
|
Annexin A
|
Cancer
|
|
ANXA3 degrader 1 (Compound 18a5) is a highly selective ANXA3 degrader with cancer cell inhibition activity. ANXA3 degrader 1 displays excellent inhibitory effect in a triple-negative breast cancer (TNBC) tumor xenograft model (TGI=96%) .
|
-
- HY-50767S1
-
|
PD 0332991-d4 hydrochloride
|
Isotope-Labeled Compounds
CDK
|
Cancer
|
|
Palbociclib-d4 (hydrochloride) is the deuterium labeled Palbociclib hydrochloride. Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research .
|
-
- HY-114338A
-
|
SHR-6390 hydrochloride
|
CDK
|
Cancer
|
|
Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively . Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma .
|
-
- HY-116865
-
|
|
Endogenous Metabolite
|
Endocrinology
Cancer
|
|
Equilenin is a B-ring unsaturated estrogen and one of the main ingredients in Premarin, a drug commonly used in estrogen replacement therapy. Equilenin can bind to estrogen receptors in the body and exert effects similar to endogenous estrogen. Equilenin can be used in estrogen replacement therapy and breast cancer research .
|
-
- HY-N6797
-
|
|
Bacterial
c-Met/HGFR
Antibiotic
|
Infection
Cancer
|
|
Meleagrin is a roquefortine C-derived alkaloid produced by fungi of the genus Penicillium and has antimicrobial and anti-proliferative activities. Meleagrin is a class of FabI inhibitor. Meleagrin is a lead c-Met inhibitory entity useful for the control of c-Met-dependent metastatic and invasive breast malignancies .
|
-
- HY-W009722
-
|
Ditiocarb sodium trihydrate
|
HIV
Biochemical Assay Reagents
|
Infection
|
|
Sodium diethylcarbamodithioate (Ditiocarb sodium) trihydrate is a copper reagent. The reaction with Cu 2+ solution resulted in the formation of a complex, which increased the copper displacement precipitation rate. Sodium diethylcarbamodithioate trihydrate can reduce HIV infection and can be used in adjuvant immune research of high-risk breast cancer .
|
-
- HY-114338
-
|
SHR-6390
|
CDK
|
Cancer
|
|
Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively . Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma .
|
-
- HY-13738AR
-
|
Keoxifene (hydrochloride)(Standard); LY156758(Standard); LY139481 (hydrochloride) (Standard)
|
Estrogen Receptor/ERR
Autophagy
|
Endocrinology
Cancer
|
|
Raloxifene (hydrochloride) (Standard) is the analytical standard of Raloxifene (hydrochloride). This product is intended for research and analytical applications. Raloxifene hydrochloride (Keoxifene hydrochloride) is a second generation selective and orally active estrogen receptor modulator. Raloxifene hydrochloride produces estrogen-agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue .
|
-
- HY-15731S
-
-
- HY-12762
-
QS11
1 Publications Verification
|
β-catenin
Wnt
Arf Family GTPase
|
Cancer
|
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 activates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells .
|
-
- HY-106056
-
|
D 16726
|
Estrogen Receptor/ERR
|
Cancer
|
|
Zindoxifene is a partial anti-estrogen. Zindoxifene works primarily by binding to estrogen receptors, thereby inhibiting the growth of estrogen-dependent tumor cells. Zindoxifene is able to exhibit the dual properties of estrogen agonists and antagonists and can be used in research and development to target estrogen-dependent tumors, such as prostate and breast cancer .
|
-
- HY-153468
-
|
|
Sodium Channel
TRP Channel
|
Cancer
|
|
ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy exhibits low nanomolar cytotoxicity in ERα+ breast cancer cell lines (IC50 = 5-25 nM) through induction of necrosis. ErSO-TFPy exhbits antitumor efficacy in mouse models .
|
-
- HY-P9921
-
|
Ado-Trastuzumab emtansine; PRO132365; T-DM 1
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer .
|
-
- HY-N15497
-
|
|
Reactive Oxygen Species (ROS)
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Terpestacin is found in Phoma exigua var. heteromorpha. Terpestacin binds to UQCRB to inhibit the production of mitochondrial ROS and HIF-1α. Terpestacin inhibits tumor angiogenesis in the FM3A breast cancer cell xenograft mouse model. Terpestacin has antitumor activity and phytotoxicity .
|
-
- HY-P9921A
-
|
Ado-Trastuzumab emtansine (solution) ; PRO132365 (solution) ; T-DM 1 (solution)
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody-drug conjugate (ADC) that incorporates the HER2-targeted antitumor properties of trastuzumab with the cytotoxic activity of the microtubule-inhibitory agent DM1 (derivative of maytansine). Trastuzumab emtansine can be used for the research of advanced breast cancer .
|
-
- HY-B0448S1
-
|
|
Sodium Channel
Virus Protease
|
Neurological Disease
|
|
Phenytoin- 15N2, 13C is the 13C and 15N labeled Phenytoin . Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice .
|
-
- HY-173211
-
|
|
Photosensitizer
|
Cancer
|
|
anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic agent targeting mitochondrial DNA G4 (mtG4). Under white light irradiation, its IC50 against 4T1 cells is 0.42 μM. anti-TNBC agent-8 binds tightly to mtG4 and generates a large amount of reactive oxygen species (ROS) under white light irradiation, leading to the loss of mitochondrial membrane potential (MMP), a decrease in ATP production, and an increase in the ROS level. This, in turn, induces significant apoptosis in triple-negative breast cancer (TNBC) cells, exerting the activity of inhibiting tumor cell growth. anti-TNBC agent-8 can be used in the research of triple-negative breast cancer.
|
-
- HY-173408
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Ferroptosis
Reactive Oxygen Species (ROS)
Glutathione Peroxidase
|
Cancer
|
|
Nur77 agonist-1 (Compound 8f) is an orally active Nur77 agonist. Nur77 agonist-1 induces ferroptosis by upregulating Nur77 protein expression, increasing reactive oxygen species (ROS) and lipid peroxidation levels, and decreasing GPX4 protein expression. Nur77 agonist-1 has binding affinity to the ligand binding domain (LBD) of Nur77 (KD: 13.80 μM). Nur77 agonist-1 exhibits significant antiproliferative activity against a variety of breast cancer cells (IC50: 2.15-3.26 μM) and has low toxicity to normal cells. Nur77 agonist-1 can be used in breast cancer research .
|
-
- HY-134418
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Cardiovascular Disease
Cancer
|
|
NOTA is a bifunctional chelate which acts as the framework to construct PET imaging tools. NOTA also can be used for probe design and signal amplification via the multivalent effect. NOTA can be used in multiple myeloma, breast cancer, lymphoma and myocardial infarction research .
|
-
- HY-13593S
-
|
CB-1348-d8; WR-139013-d8
|
Isotope-Labeled Compounds
DNA Alkylator/Crosslinker
|
Cancer
|
|
Chlorambucil-d8 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease .
|
-
- HY-113293BS
-
|
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Endogenous Metabolite
|
Cancer
|
|
Estrone sulfate-d5 (sodium) is the deuterium labeled Estrone sulfate sodium. Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer .
|
-
- HY-13632S
-
|
FCE 24304-d2; EXE-d2
|
Isotope-Labeled Compounds
Cytochrome P450
|
Endocrinology
Cancer
|
|
Exemestane-d2 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
|
-
- HY-B0448S2
-
-
- HY-13632S2
-
|
FCE 24304-d3; EXE-d3
|
Isotope-Labeled Compounds
Cytochrome P450
|
Endocrinology
Cancer
|
|
Exemestane-d3 is the deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
|
-
- HY-113293BS1
-
|
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Cancer
|
|
Estrone sulfate-d4 (sodium) is deuterium labeled Estrone sulfate (sodium). Estrone sulfate, a biologically inactive form of estrogen, is a major circulating plasma estrogen that is converted into the biologically active estrogen, estrone (E1) by steroid sulfatase (STS). strone sulfate can be used for the research of breast cancer .
|
-
- HY-13673S
-
|
ICI 118630-d10
|
Isotope-Labeled Compounds
|
Endocrinology
Cancer
|
|
Goserelin-d10 (ICI 118630-d10) is deuterium labeled Goserelin. Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
|
-
- HY-173151
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
BRCA2-IN-1 (Compound 3j) is a potential BRCA2 inhibitor that exhibits antiproliferative activity against the breast cancer MCF-7 cell lines. BRCA2-IN-1 also demonstrates DPPH radical scavenging ability, with an IC50 of 12.36 µM .
|
-
- HY-126363S
-
|
Diethyldithiocarbamic acid-d10
|
Isotope-Labeled Compounds
HIV
|
Infection
|
|
Ditiocarb-d10 (Diethyldithiocarbamic acid-d10) is the deuterium labeled Ditiocarb (HY-126363) . Ditiocarb (Diethyldithiocarbamic acid) is an accelerator of the rate of copper cementation. Ditiocarb (Diethyldithiocarbamic acid) reduces the incidence of HIV infection, and also enhances adjuvant immunoresearch of high risk breast cancer .
|
-
- HY-13673S1
-
|
ICI 118630-d7
|
Isotope-Labeled Compounds
GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Goserelin-d7 (ICI 118630-d7) is deuterium labeled Goserelin. Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer .
|
-
- HY-170453
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .
|
-
- HY-N10777
-
|
|
Others
|
Cancer
|
|
1-Ketoaethiopinone is an abietane-diterpenoid. 1-Ketoaethiopinone has an α, β-unsaturated carbonyl function. 1-Ketoaethiopinone shows cytotoxic activity against human cancer cell lines MOLT-4 (human lymphoblastic leukemia) and MCF-7 (human breast adenocarcinoma) .
|
-
- HY-119724
-
|
|
BCRP
|
Cancer
|
|
ABCG2-IN-3 (Compound 52) is a selective inhibitor for breast cancer resistance protein (ABCG2), with an IC50 of 0.238 µM. ABCG2-IN-3 reverses the ABCG2-mediated resistance toward SN-38 and inhibit the ATPase activity .
|
-
- HY-142974
-
|
1,2-Olein-3-Docosohexaenoin; 18:1/18:1/22:6-TG; C1OO
|
Endogenous Metabolite
|
Metabolic Disease
|
|
1,2-Dioleoyl-3-docosohexaenoyl-rac-glycerol is a triacylglycerol that contains oleic acid (HY-N1446) at the sn-1 and sn-2 positions and docosahexaenoic acid (HY-B2167) at the sn-3 position. It has been detected in human breast milk.
|
-
- HY-157487
-
|
|
Others
|
Cancer
|
|
Anticancer agent 185 (compound 9d) is a glycohybrid derivative of pyrazolopyrimidine [1,5-a]. Anticancer agent 185 has good anti-breast cancer activity. Anticancer agent 185 shows good cytotoxic activity against MCF-7 cells with IC50 value of 15.3 μM .
|
-
- HY-159605
-
|
|
Autophagy
JNK
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Autophagy inducer 5 (compound 21o) is a potent MCF-7 inhibitor (IC50: 2 μM), and a potential breast cancer inhibitor. Autophagy inducer 5 induces cellular autophagy by activating the ROS/JNK signaling pathway, which increases ROS generation and JNK phosphorylation, exerting cytotoxic effects .
|
-
- HY-13593S1
-
|
CB-1348-d8-1; WR-139013-d8-1
|
Isotope-Labeled Compounds
DNA Alkylator/Crosslinker
|
Cancer
|
|
Chlorambucil-d8-1 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease .
|
-
- HY-153910
-
|
|
Others
|
Cancer
|
|
AGPS-IN-1 (Compound 2i) is an effective AGPS binder. AGPS-IN-1 reduces ether lipids levels and cell migration rate. AGPS-IN-1 inhibits epithelial-mesenchymal transition (EMT) in prostate PC-3 and breast MDA-MB-231 cancer cells .
|
-
- HY-155663
-
|
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
GPX4-IN-5 is a covalent inhibitor of GPX4 (IC50: 0.12 μM). GPX4-IN-5 can induce ferroptosis and has anti-tumor effects. GPX4-IN-5 can be used in the study of triple-negative breast cancer (TNBC) .
|
-
- HY-106376A
-
|
L-Buthionine sulfoximine; L-BSO
|
Ferroptosis
|
Cancer
|
|
L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.
|
-
- HY-113319
-
|
|
Endogenous Metabolite
|
Cancer
|
|
β-D-Fructose is a β-fruit sugar that can be produced by the hydrolysis of sucrose. β-D-Fructose can be used as a sweetness potentiator. β-D-Fructose can be designed as a units of antiproliferative agents against breast (MCF-7) and colon (MDST8) cancer cell lines .
|
-
- HY-N5011
-
|
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .
|
-
- HY-111550
-
|
|
Ras
MDM-2/p53
|
Cancer
|
|
Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells .
|
-
- HY-N1833
-
|
|
Others
|
Cancer
|
|
3'-Geranyl-3-prenyl-2',4',5,7-tetrahydroxyflavone displays cytotoxicity of 1.32, 3.92 and 5.22 μm against the human cervical carcinoma HeLa, human breast carcinoma MCF-7, and human hepatocarcinoma Hep3B cells .
|
-
- HY-13632R
-
|
FCE 24304(Standard); EXE (Standard)
|
Cytochrome P450
|
Endocrinology
Cancer
|
|
Exemestane (Standard) is the analytical standard of Exemestane. This product is intended for research and analytical applications. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
|
-
- HY-155787
-
|
|
CDK
|
Cancer
|
|
SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM) .
|
-
- HY-103489
-
PI-273
5 Publications Verification
|
PI4K
Apoptosis
|
Cancer
|
|
PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis .
|
-
- HY-14248S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
Autophagy
|
Cancer
|
|
Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
|
-
- HY-19992
-
|
Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP
|
Hexokinase
Apoptosis
Autophagy
|
Cancer
|
|
3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities .
|
-
- HY-13632S1
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Endocrinology
Cancer
|
|
Exemestane- 13C3 is the 13C-labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
|
-
- HY-168993
-
-
- HY-162985
-
|
|
CDK
|
Cancer
|
|
JHD205 is a CDK4/6 inhibitor that induces apoptosis and DNA damage. JHD205 inhibits DNA repair by upregulating Caspase3 and p-H2AX. JHD205 has superior potency to Abemaciclib (HY-16297A) in a xenograft chick embryo breast cancer model. .
|
-
- HY-B0777
-
|
CL301423
|
Antibiotic
BCRP
P-glycoprotein
Parasite
|
Infection
|
|
Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
- HY-P10844
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
ANK peptide is a novel peptide designed based on the conserved residues of single ankyrin motif. ANK peptide is a synuclein-γ (SNCG) inhibitor that binds to SNCG and competes with SNCG-BubR1 interaction to enhance the sensitivity of breast cancer cells to antimicrotubule drugs such as nocodazole and paclitaxel. ANK peptide can be used in the study of cancer .
|
-
- HY-146230
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells .
|
-
- HY-151519
-
|
|
Sirtuin
|
Cancer
|
|
SIRT2-IN-9 (compound 12) is a selective inhibitor of SRIT2 with an IC50 value of 1.3 μM. SIRT2-IN-9 inhibits proliferative activity of MCF-7 breast cancer cells. SIRT2-IN-9 can be used for the research of cancer .
|
-
- HY-162444
-
|
|
Ras
|
Cancer
|
|
KRAS G12D inhibitor 22 (compound 6) is a inhibitor of KRAS mutation. KRAS G12D inhibitor 22 has high activity (IC50＜100 nM), good selectivity and low toxicity.KRAS G12D inhibitor 22 can be used in breast cancer research .
|
-
- HY-B1019R
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Sulpiride (Standard) is the analytical standard of Sulpiride. This product is intended for research and analytical applications. Sulpiride is an orally active dopamine D2/D3 receptor antagonist. Sulpiride is an atypical antipsychotic agent of the benzamide family. Sulpiride can be used in research into anxiety, depression and breast cancer .
|
-
- HY-13593R
-
|
CB-1348 (Standard); WR-139013 (Standard)
|
Reference Standards
DNA Alkylator/Crosslinker
|
Cancer
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Chlorambucil (Standard) is the analytical standard of Chlorambucil. This product is intended for research and analytical applications. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease .
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- HY-121684
-
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7-Methyljuglon
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PI3K
Apoptosis
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Cancer
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Ramentaceone (7-Methyljuglon), a naphthoquinone that can be isolated from Drosera sp., inhibits PI3K activity. Ramentaceone (7-Methyljuglon) reduces the expression of the PI3K protein and inhibits the phosphorylation of the Akt protein in breast cancer cells. Ramentaceone (7-Methyljuglon) induces apoptosis .
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- HY-B0515R
-
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BM-210955 (Standard); RPR-102289A (Standard)
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Apoptosis
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Cancer
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Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) (Standard) is the analytical standard of Ibandronate Sodium Monohydrate (HY-B0515). This product is intended for research and analytical applications. Ibandronate Sodium Monohydrate (BM-210955; RPR-102289A) is an orally active, selective inhibitor of farnesyl pyrophosphate synthase (FPP synthase). Ibandronate Sodium Monohydrate can block the mevalonate pathway to inhibit the isoprenylation modification of small GTPases (such as RAS, RHO family proteins), induce tumor cell apoptosis and inhibit bone resorption. Ibandronate Sodium Monohydrate inhibits tumor cell proliferation (such as ER + breast cancer cells), promotes the expression of the pro-apoptotic gene FAS, and can produce synergistic anti-tumor effects with anti-estrogen compounds. Ibandronate Sodium Monohydrate is used in the study of osteoporosis and bone metastatic tumors (such as breast cancer bone metastasis) .
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- HY-114527
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Apoptosis
Stearoyl-CoA Desaturase (SCD)
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Cancer
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TPMP-I-2 is an anticancer agent that induces cancer cell lines Apoptosis and decreases protein levels of stearoyl-CoA desaturase. TPMP-I-2 prolongs the survival time of nude rats in a simulated micrometastatic cervical cancer model and reduces tumor growth in a breast cancer model in nude mice combined with immunotoxins .
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- HY-111216
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Melatonin Receptor
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Cancer
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CGP52608 is a selective agonist for the RZR/ROR receptor, known for its anti-tumor activity, and has almost no affinity for the cell surface G-protein coupled melatonin receptor. CGP52608 can inhibit the growth of mouse 16/C breast cancer cells. CGP52608 can induce the formation of vesicles in diatoms .
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- HY-163760
-
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HuR
MMP
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Cancer
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ZM-32 is an inhibitor for human antigen R (HuR), that downregulates the expression of VEGF-A and MMP9, and thus inhibits breast cancer tumor angiogenesis. ZM-32 exhibits broad-spectrum anti-proliferative effects in a variety of cancer cell lines, and exhibits antitumor efficacy against MDA-MB-231 in mouse models .
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- HY-155055
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Others
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Cancer
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Antiproliferative agent-26 (compound 4g) is an antiproliferative agent with much broad range of activity targeting Leukemia, CNS, Melanoma, Renal and Breast (at the concentration of 10 μM). Antiproliferative agent-26 inhibits colony forming and arrests cell cycle at G1 phase/S phase at 5 μM and 25 μM, respectively .
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- HY-P99268
-
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SAR 256212; MM 121; Anti-Human ERBB3/ErbB 3 Recombinant Antibody
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EGFR
Apoptosis
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Cancer
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Seribantumab (MM 121) is a fully human IgG2 monoclonal antibody that targets HER3. Seribantumab blocks the activation of epidermal growth factor receptor (ErbB) family members and its downstream signal. Seribantumab inhibits neuregulin 1 (NRG1) fusion-dependent tumorigenesis in vitro and in vivo in breast, lung and ovarian patient-derived cancer models .
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- HY-151618
-
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Apoptosis
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Cancer
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Antitumor agent-79 shows good antiproliferative activities against hepatocellular carcinoma and breast cancer cells with IC50 values of 0.7-7.9 μM. Antitumor agent-79 induces cancer cells apoptosis and shows in vivo antitumor effects. Antitumor agent-79 can be used for the research of cancer .
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-
- HY-162250
-
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PROTACs
Histone Methyltransferase
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Cancer
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MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells .
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- HY-128588
-
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STAT
Apoptosis
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Cancer
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STAT3-IN-3 is a potent and selective inhibitor of signal transducer and activator of transcription 3 (STAT3), with anti-proliferative activity. STAT3-IN-3 induces apoptosis in breast cancer cells. STAT3-IN-3 acts as a promising mitochondria-targeting STAT3 inhibitor for cancer research .
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- HY-N0036R
-
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Apoptosis
Endogenous Metabolite
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Cancer
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Costunolide (Standard) is the analytical standard of Costunolide. This product is intended for research and analytical applications. Costunolide ((+)-Costunolide) is a naturally occurring sesquiterpene lactone, with antioxidative, anti-inflammatory, antiallergic, bone remodeling, neuroprotective, hair growth promoting, anticancer, and antidiabetic properties. Costunolide can induce cell cycle arrest and apoptosis on breast cancer cells .
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-
- HY-10293
-
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INCB007839; INCB7839
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MMP
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Cancer
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Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 + breast cancer, gliomas, et al .
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-
- HY-161257
-
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Autophagy
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Cancer
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CDC20-IN-1 (Compound E1) is a specific inhibitor of CDC20 and can be used in triple-negative breast cancer research. CDC20-IN-1 can induce autophagy in cancer cells and inhibit MDA-MB-231 cell proliferation, with an IC50 value of 1.43 μM .
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- HY-N7083R
-
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Apoptosis
Aldehyde Dehydrogenase (ALDH)
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Inflammation/Immunology
Cancer
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Citral (Standard) is the analytical standard of Citral. This product is intended for research and analytical applications. Citral is an orally active monoterpene compound in lemon grass essential oil and a natural ALDH1A inhibitor, which can induce apoptosis and cycle arrest in breast cancer cell lines, and has analgesic, anti-injurious and anti-inflammatory effects .
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- HY-168094
-
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PARP
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Cancer
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PARP1-IN-30 (Compound 3) is a specific and potent PARP1 inhibitor with cytotoxicity. PARP1-IN-30 allows precise inhibition of PARP1 in tumor cells with breast cancer 1 protein (BRCA1) or BRCA2 deficiencies. PARP1-IN-30 is promising for research of cancers .
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-
- HY-172595
-
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Apoptosis
E1/E2/E3 Enzyme
|
Cancer
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Apoptotic agent-5 (5d) is an apoptotic agent. Apoptotic agent-5 inhibits the growth of triple-negative breast cancer cells. Apoptotic agent-5 attenuates proteasomal degradation via the ubiquitin-proteasome pathway, leading to G2/M phase cell cycle arrest and the induction of apoptotic .
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- HY-N0431R
-
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MMP
ERK
JNK
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Cancer
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Astragaloside IV (Standard) is the analytical standard of Astragaloside IV. This product is intended for research and analytical applications. Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
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- HY-B0723S2
-
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FC-1271a-d5
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
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Ospemifene-d5 (FC-1271a-d5) is deuterium labeled Ospemifene. Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer .
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- HY-110350
-
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Haspin Kinase
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Cancer
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CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer .
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- HY-15841
-
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Anaplastic lymphoma kinase (ALK)
FAK
|
Cancer
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CEP-37440 is a potent, orally active dual FAK/ALK inhibitor with IC50 values of 2.3 nM and 3.5 nM for FAK and ALK, respectively. CEP-37440 decreases the cell proliferation by blocking the autophosphorylation kinase activity of FAK1 (Tyr 397) .
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- HY-151625
-
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PARP
Apoptosis
|
Cancer
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|
PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability .
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- HY-161446
-
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Deubiquitinase
|
Cancer
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USP1-IN-7 (Compound 3) is an inhibitor for ubiquitin specific peptidase 1 (USP1) and its cofactor UAF1, with IC50 ≤50 nM. USP1-IN-7 inhibits proliferation of MDA-MB-436 with IC50 ≤50 nM .
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- HY-169633
-
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CDK
|
Cancer
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CDK8-IN-17 (Compound WS-2) is a CDK8 inhibitor with an IC50 value of 9 nM, which can be used in cancer research .
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-
- HY-124909
-
-
- HY-N2331R
-
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Topoisomerase
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Cancer
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Proscillaridin A (Standard) is the analytical standard of Proscillaridin A. This product is intended for research and analytical applications. Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively .
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-
- HY-131404
-
TPBM
1 Publications Verification
|
Estrogen Receptor/ERR
|
Cancer
|
|
TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth .
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- HY-N9954
-
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Apoptosis
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Cancer
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Isoharringtonine is a natural alkaloid that can be purified from Cephalotaxus koreana Nakai. Isoharringtonine can inhibit cancer cell proliferation and migration, and induce cancer cell apoptosis. Isoharringtonine can be used for the research of cancers .
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- HY-118916
-
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Farnesyl Transferase
|
Cancer
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|
FTI-2148 is a RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 1.4 nM and 1.7 μM, respectively .
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- HY-160469
-
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Akt
PROTACs
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Cancer
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|
INY-05-040 is a AKT degrader that can selectively and quickly degrade all three AKT isoforms. INY-05-040 can inhibit downstream signaling and cell proliferation in 288 cancer cell lines, with anti-cancer activity .
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- HY-146810
-
-
- HY-114071
-
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RAR/RXR
|
Cancer
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|
BMS270394 is a nuclear retinoic acid receptor (RAR-γ) agonist with the EC50 values of 30 nM and 400 nM for humanRAR-γ and RAR-β, respectively .
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-
- HY-P99813
-
|
HER3-DXd; U3-1402
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) consisting of a fully human anti-HER3 IgG1 monoclonal antibody Patritumab (HY-P99275) attached to a topoisomerase I inhibitor payload via a tetrapeptide-based cleavable linker. Patritumab deruxtecan shows anticancer activity .
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-
- HY-156958
-
-
- HY-147997
-
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EGFR
|
Cancer
|
|
EGFR-IN-68 (Compound 8d) is a potent EGFR inhibitor with an IC50 of 0.33 μM. EGFR-IN-68 shows anticancer activity .
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-
- HY-14971
-
|
(E)-AKTIV
|
Akt
|
Cancer
|
|
(E)-Akt inhibitor-IV ((E)-AKTIV) is a PI3K-Akt inhibitor, with potent cytotoxic .
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-
- HY-N2331
-
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Topoisomerase
|
Cancer
|
|
Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively .
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-
- HY-161447
-
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|
Deubiquitinase
|
Cancer
|
|
USP1-IN-8 (Compound 16) is an inhibitor for ubiquitin specific peptidase 1 (USP1) and its cofactor UAF1, with IC50 ≤50 nM. USP1-IN-8 inhibits proliferation of MDA-MB-436 with IC50 ≤50 nM .
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-
- HY-170989
-
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AUTACs
Epigenetic Reader Domain
Autophagy
|
Cancer
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|
BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC50 = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC50 of 20.6 μM .
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-
- HY-135309
-
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PROTACs
Estrogen Receptor/ERR
|
Cancer
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|
PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM .
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- HY-P5425A
-
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Transmembrane Glycoprotein
|
Cancer
|
|
Tetanus Toxin (830–844) TFA is a biological active peptide. (tetanus toxin-derived peptide TT830–844 CD4 + T-cell epitope. This promiscuous CD4 + T-cell epitope can bind to a wide range of HLA–DRB molecules and is thus expected to activate CD4 + T-cell responses in a large part of the human population) .
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-
- HY-W106456
-
-
- HY-147996
-
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EGFR
|
Cancer
|
|
EGFR-IN-67 (Compound 7d) is a potent EGFR inhibitor with an IC50 of 0.34 μM. EGFR-IN-67 shows anticancer activity .
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-
- HY-147995
-
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EGFR
|
Cancer
|
|
EGFR-IN-64 (Compound 3c) is a potent EGFR inhibitor with an IC50 of 0.33 μM. EGFR-IN-64 shows anticancer activity .
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-
- HY-13646C
-
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HM30181 mesylate hydrochloride; HM30181A mesylate hydrochloride
|
P-glycoprotein
|
Cancer
|
|
Encequidar (HM30181) mesylate hydrochloride is a potent and selective inhibitor of P-glycoprotein (MDR1). Encequidar mesylate hydrochloride improves anti-tumor efficacy of Paclitaxel (HY-B0015) in mouse tumor models .
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-
- HY-124674A
-
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Monoamine Oxidase
EGFR
Akt
TGF-beta/Smad
|
Cancer
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|
CCT365623 hydrochloride is an orally active lysyl oxidase (LOX) inhibitor, with an IC50 of 0.89 μM. CCT365623 hydrochloride suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. CCT365623 hydrochloride is extremely well tolerated, and has good pharmacokinetic properties .
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-
- HY-N7266
-
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Cytochrome P450
Parasite
|
Infection
Cancer
|
|
Obtusifoliol is a specific CYP51 inhibitor, Obtusifoliol shows the affinity with Kd values of 1.2 μM and 1.4 μM for Trypanosoma brucei (TB) and human CYP51, respectively .
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-
- HY-153749
-
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NEKs
|
Cancer
|
|
Nek2/Hec1-IN-2 (Compound 14) is an inhibitor of Nek2/Hec1. Nek2/Hec1-IN-2 inhibits cancer cell proliferation with IC50 >25 μM .
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-
- HY-146424
-
-
- HY-134886
-
-
- HY-W179181
-
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GLUT
|
Metabolic Disease
Cancer
|
|
MSNBA is a potent and selective GLUT5 fructose transport inhibitor with an IC50 of 0.10 mM. MSNBA does not affect the transport activity of human GLUT1, GLUT2, GLUT3, GLUT4 or bacterial GlcPSe. MSNBA competitively inhibits GLUT5 fructose uptake with a Ki of 3.2 μM in MCF7 cells. MSNBA can be used for the study of cancer or diabetes .
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-
- HY-101447A
-
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EPH 116 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
SI-2 (EPH 116 hydrochloride) is a highly promising SRC-3 inhibitor (PPI). SI-2 (EPH 116 hydrochloride) has a much improved toxicity and pharmacokinetic profile, with acceptable oral availability .
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-
- HY-162487
-
|
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HDAC
|
Cancer
|
|
HDAC-IN-72 (compound 7j) is the most potent HDAC1 (IC50=0.65 μM), HDAC2 (IC50=0.78 μM), HDAC3 (IC50=1.70 μM) inhibitor and antiproliferative compound. HDAC-IN-72 can be used for breast cancer research .
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-
- HY-172204
-
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Sirtuin
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
SIRT-IN-7 (Compound 7ba) is a SIRT inhibitor. SIRT-IN-7 can inhibit the expression of SIRT1, SIRT2, and SIRT3, and increase the acetylation and activation of p53. SIRT-IN-7 can inhibit the proliferation, and induce apoptosis and autophagy of breast cancer cells. SIRT-IN-7 has anti-tumor activity .
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-
- HY-W021377
-
|
|
ADC Cytotoxin
Drug Intermediate
|
Cancer
|
|
Exatecan Intermediate 2 (Compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
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-
- HY-W142080
-
|
α-Methyltryptophan
|
mTOR
Autophagy
Apoptosis
Amino Acid Derivatives
|
Metabolic Disease
Cancer
|
|
α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .
|
-
- HY-135023
-
|
5-trans Prostaglandin E2
|
Cytochrome P450
Prostaglandin Receptor
|
Cancer
|
|
5-trans-PGE2 (5-trans Prostaglandin E2) is the active isomer of PGE2 and a potent activator of aromatase. Supplements the process of paracrine signaling between epithelial cells (expressing high levels of PGE2) and surrounding stromal cells (expressing high levels of aromatase). This process is involved in the growth and development of breast cancer .
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-
- HY-152774
-
|
|
Akt
PI3K
|
Cancer
|
|
Antitumor agent-86 (compound 5a) inhibits MCF-7 breast cancer cells with an IC50 value of 2.62 µM. Antitumor agent-86 induces cell apoptosis and cell cycle arrest, and shows antineoplastic activity by targeting RAS/PI3K/Akt/JNK signaling cascades .
|
-
- HY-103367
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
|
-
- HY-164518
-
|
|
Mps1
Apoptosis
|
Cancer
|
|
PF-3837 is an Mps1 kinase inhibitor with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. PF-3837 interferes with the cell cycle checkpoint by inhibiting Mps1 catalytic activity, reducing genomic stability, thereby inducing cancer cell apoptosis (Apoptosis). PF-3837 can be used in research on breast cancer .
|
-
- HY-123870
-
|
|
Survivin
IAP
NF-κB
|
Inflammation/Immunology
Cancer
|
|
MX107 is a selective and potent survivin inhibitor that suppresses triple-negative breast cancer (TNBC) cell proliferation. MX107 induces degradation of survivin and inhibitor-of-apoptosis proteins (IAPs), which inhibits nuclear factor κB (NF-κB) activation induced by DNA damage. MX107 enhances tumoricidal efficacy of genotoxic treatments synergized with chemotherapeutic drugs .
|
-
- HY-P991235
-
|
|
EGFR
Caspase
|
Cancer
|
|
FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a KD value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer .
|
-
- HY-W021377C
-
|
|
ADC Cytotoxin
Drug Intermediate
|
Cancer
|
|
Exatecan Intermediate 4 dihydrochloride (Compound 14f) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
|
-
- HY-B2099S
-
|
1-Butylbiguanide-d9 hydrochloride
|
Isotope-Labeled Compounds
AMPK
|
Metabolic Disease
Cancer
|
|
Buformin-d9 (hydrochloride) is the deuterium labeled Buformin. Buformin (1-Butylbiguanide), a potent AMPK activator, acts as an orally active biguanide antidiabetic agent. Buformin decreases hepatic gluconeogenesis and lowers blood glucose production in vivo. Buformin also has anti-cancer activities and is applied in cancer study (such as, cervical cancer and breast cancer, et al) .
|
-
- HY-W021377A
-
|
|
ADC Cytotoxin
Drug Intermediate
|
Cancer
|
|
Exatecan Intermediate 2 hydrochloride (Compound B) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
|
-
- HY-106376C
-
|
L-Buthionine sulfoximine hydrochloride; L-BSO hydrochloride
|
Ferroptosis
|
Metabolic Disease
Cancer
|
|
L-Buthionine-(S,R)-sulfoximine hydrochloride is a cell-permeable, potent, fast acting, orally active and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively .
|
-
- HY-121881
-
|
|
HSP
|
Cancer
|
|
PU3 is an Hsp90 inhibitor that competes with geldanamycin (GM) and others for the conserved ATP/ADP pocket of Hsp90. PU3 also induces degradation of proteins such as Her2 and inhibits breast cancer cell growth by causing retinoblastoma protein hypophosphorylation, G1 arrest, and cell differentiation. PU3 has the potential to be a cancer inhibitor. .
|
-
- HY-P9907
-
|
Anti-Human HER2, Humanized Antibody
|
Radionuclide-Drug Conjugates (RDCs)
EGFR
ADC Antibody
|
Cancer
|
|
Trastuzumab is a humanized IgG1 monoclonal antibody that selectively binds to HER2 with high affinity. Trastuzumab can be used for the research of HER2-positive metastatic breast cancer and gastric cancer . (Note: The product specifications below only indicate the effective content of Trastuzumab. The component ratio of this product is Trastuzumab : excipients = 44 : 78.)
|
-
- HY-N0331
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics . Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC) .
|
-
- HY-13632S6
-
|
FCE 24304-d4; EXE-d4
|
Isotope-Labeled Compounds
Cytochrome P450
|
Endocrinology
Cancer
|
|
Exemestane-d4 (FCE 24304-d4) is deuterium labeled Exemestane. Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
|
-
- HY-108694
-
|
|
Endogenous Metabolite
NF-κB
|
Metabolic Disease
Inflammation/Immunology
|
|
γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
|
-
- HY-132173
-
|
|
Bcl-2 Family
|
Cancer
|
|
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo .
|
-
- HY-W194810
-
|
|
Mitochondrial Metabolism
Calcium Channel
|
Neurological Disease
Cancer
|
|
MCU-i11 is a negative regulator of the mitochondrial calcium uniporter (MCU) complex. MCU-i11 can reduce mitochondrial Ca 2+ uptake. MCU-i11 impairs muscle cell growth. MCU-i11 can be used to study breast cancer, cervical cancer and neurological diseases .
|
-
- HY-13617
-
|
CGP 30694
|
Antifolate
|
Cancer
|
|
Edatrexate (CGP 30694), as known as 10-Ethyl-10-deazaaminopterin, is Methotrexate (HY-14519) analog, exhibits antitumor activity against MTX-resistant tumors. Edatrexate is an antifolate antimetabolite, can be used for reasearch of non-small-cell lung cancer, breast cancer, non-Hodgkin's lymphoma, and cancer of the head and neck .
|
-
- HY-W021377B
-
|
|
ADC Cytotoxin
Drug Intermediate
|
Cancer
|
|
Exatecan Intermediate 4 (Compound 14f) is an intermediate of Exatecan (DX-8951, HY-13631). Exatecan is an anticancer agent belonging to the class of camptothecin analogs. Exatecan interferes with the proliferation and division of tumor cells by interacting with DNA, thereby inhibiting tumor growth. Exatecan is primarily used for research of a variety of cancers including ovarian, lung and breast cancers .
|
-
- HY-N6635R
-
|
|
Reference Standards
Fungal
|
Infection
Cancer
|
|
trans-Nerolidol (Standard) is the analytical standard of trans-Nerolidol. This product is intended for research and analytical applications. trans-Nerolidol improves the anti-proliferative effect of Doxorubicin (DOX) (HY-15142A) against intestinal cancer and breast cancer cells in vitro. trans-Nerolidol increases accumulation of DOX inside cells in vitro. trans-Nerolidol activates apoptosis in vivo .
|
-
- HY-D2620
-
|
|
Photosensitizer
Reactive Oxygen Species (ROS)
Ferroptosis
|
Cancer
|
|
CAR-2 is a BODIPY-based photosensitizer that induces ferroptosis in photodynamic therapy (PDT) by targeting the endoplasmic reticulum (ER) and lipid droplets (LDs). CAR-2 exhibits phototoxicity in breast cancer cells with IC50 of 0.01-0.02 μM. CAR-2 exhibits antitumor efficacy in 4T1 xenograft mouse models .
|
-
- HY-W010713
-
|
Fimaporfin free base
|
Photosensitizer
|
Cancer
|
|
Meso-tetraphenylchlorin (TPCS2a) is a photosensitizer with poor water solubility, which limits its use in the blood circulation. However, TPCS2a@NPs nanoparticles can be prepared based on polylactic-co-polyethylene glycol acid (PLGA) polymer core loaded with TPCS2. Such nanoparticles can be coated with mesenchymal stem cell-derived plasma membranes (mMSCs) to form mMSC-TPCS2a@NPs, which prolongs blood circulation time and improves tumor targeting ability. Compared with uncoated TPCS2a@NPs, mMSC-TPCS2a@NPs can reduce macrophage uptake by 54% to 70% under different conditions. Both nanoparticle forms are effectively accumulated in MCF7 and MDA-MB-231 breast cancer cells, while uptake in normal breast epithelial cells MCF10A is significantly lower .
|
-
- HY-168996
-
|
|
CDK
Apoptosis
|
Cancer
|
|
LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
|
-
- HY-172365
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
P7-2302 inhibits PDE7 and PDE4B with IC50 of 0.18 nM and 77.3 nM. P7-2302 inhibits the efflux of P-gp and BCRP (breast cancer resistance protein), exhibits low uptake in rats brain. P7-2302 can be used as a PET tracer when labeled with 18F .
|
-
- HY-P10843
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer .
|
-
- HY-100012
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis .
|
-
- HY-B0166D
-
|
|
Drug Derivative
|
Others
|
|
Niacinamide ascorbate is a micronutrient with radioprotective properties. Niacinamide ascorbate works as an antioxidant along with vitamin C, vitamin E and other compounds to mitigate the risks associated with exposure to ionizing radiation. Niacinamide ascorbate helps reduce the likelihood of radiation-induced diseases such as acute leukemia, breast cancer, thyroid cancer and mutations, thereby protecting the human body from the harmful effects of radiation .
|
-
- HY-13632S5
-
|
FCE 24304-13C,d2; EXE-13C,d2
|
Cytochrome P450
Isotope-Labeled Compounds
|
Endocrinology
Cancer
|
|
Exemestane- 13C,d2 is 13C and deuterated labeled Exemestane (HY-13632). Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research .
|
-
- HY-76574
-
|
|
Drug Intermediate
|
Cancer
|
|
3-(Trifluoromethyl)benzaldehyde is a key intermediate in organic synthesis. 3-(Trifluoromethyl)benzaldehyde can be used to synthesize 2,3-di- and 2,2,3-trisubstituted-3-methoxycarbonyl-γ-butyrolactones. 3-(Trifluoromethyl)benzaldehyde derivatives have antitumor effects against nasopharyngeal carcinoma, leukemia, and breast cancer .
|
-
- HY-N3995S
-
|
|
Isotope-Labeled Compounds
Apoptosis
Drug Metabolite
|
Cancer
|
|
5β-Dihydrocortisol-d6 is the deuterium labeled 5β-Dihydrocortisol. 5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis .
|
-
- HY-155807
-
|
|
STAT
JAK
Apoptosis
|
Cancer
|
|
DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety .
|
-
- HY-168043
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-35 is a STAT3 inhibitor that binds to SH2 domain. STAT3-IN-35 inhibits the phosphorylation of STAT3 and possesses antiproliferative activities against triple-negative breast cancer (TNBC) cell lines. STAT3-IN-35 also has a toxicity and potent antitumor activity in a TNBC xenograft model .
|
-
- HY-121983
-
|
|
Phospholipase
|
Cancer
|
|
CAY10594 is a potent phospholipase D2 (PLD2) inhibitor both in vitro (IC50=140 nM) and in cells (IC50=110 nM) . CAY10594 strongly inhibits the invasive migration of breast cancer cells in vitro and ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis .
|
-
- HY-137742
-
|
|
ULK
Autophagy
|
Cancer
|
|
SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-16231
-
|
|
Apoptosis
|
Cancer
|
|
GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors .
|
-
- HY-E70301
-
|
ST8SIA4
|
Endogenous Metabolite
|
Cancer
|
|
ST8 alpha-2,8-Sialyltransferase 4 (ST8SIA4) is a sialyltransferase that participates in the sialylation mechanism. ST8 alpha-2,8-Sialyltransferase 4 has also been implicated in breast cancer development and mediates cell proliferation and invasion of cancer cells in a sialyltransferase-dependent manner .
|
-
- HY-117769
-
|
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
|
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer .
|
-
- HY-12098
-
|
MPC-6827 hydrochloride
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
|
-
- HY-139342
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-4 (compound I) is a potent CDK7 (Cyclin-dependent kinase 7) inhibitor. CDK7-IN-4 shows anticancer activity. CDK7-IN-4 inhibits the in vitro growth of cancer cell lines from a variety of histologies including colon , breast , lung , ovary and stomach , in a dose dependent manner .
|
-
- HY-N7271
-
|
|
RAD51
MDM-2/p53
|
Cardiovascular Disease
Cancer
|
|
Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice .
|
-
- HY-P10740
-
|
|
Peptide-Drug Conjugates (PDCs)
Antifolate
|
Cancer
|
|
CBP-1018 is a PDC (peptide drug conjugate) consisting of a dual targeting FRα/prostate-specific membrane antigen (PSMA) ligand (blue part) coupled to Monomethyl auristatin E (HY-15162) (red part) via a linker (HY-78738) (black part). CBP-1018 is expected to be used in breast cancer research .
|
-
- HY-125374
-
|
XRP9881
|
Apoptosis
|
Cancer
|
|
Larotaxel (XRP9881) is a taxane analogue with preclinical activity against taxane-resistant breast cancer. Larotaxel (XRP9881) exerts its cytotoxic effect by promoting tubulin assembly and stabilizing microtubules, ultimately leading to cell death by apoptosis. It presents the ability to cross the blood brain barrier and has a much lower affinity for P-glycoprotein 1 than Docetaxel .
|
-
- HY-W009722A
-
|
Ditiocarb sodium trihydrate, ACS, 99.0%
|
HIV
Biochemical Assay Reagents
|
Infection
|
|
Sodium diethylcarbamodithioate trihydrate, ACS, 99.0% (Ditiocarb sodium trihydrate, ACS, 99.0%) is a copper reagent. The reaction with Cu 2+ solution resulted in the formation of a complex, which increased the copper displacement precipitation rate. Sodium diethylcarbamodithioate trihydrate, ACS, 99.0% can reduce HIV infection and can be used in adjuvant immune research of high-risk breast cancer .
|
-
- HY-111244
-
|
|
CDK
HSP
|
Others
|
|
DCB-3503 is an allosteric modulator of heat shock cognate protein HSC70 and an inhibitor of Cyclin D1. DCB-3503 inhibits Cyclin D1 translation by allosterically modulating the ATPase and chaperone activities of HSC70. DCB-3503 may inhibit malignancies such as hepatocellular carcinoma or breast cancer with elevated expression of cyclin D1 .
|
-
- HY-N1440
-
|
|
Bcl-2 Family
|
Inflammation/Immunology
Cancer
|
|
Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells . Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities , protects against the development of arthritis in Rheumatoid arthritis (RA) animal models .
|
-
- HY-169367
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-1233 is a potent and orally active estrogen receptor PROTAC degrader, with the DC50 of 0.9 nM. ERD-1233 plays an important role in ER + breast cancer research (Pink: ligand for target protein (HY-201580); Black: linker (HY-W889109); Blue: E3 ligase ligand (HY-W1009348)) .
|
-
- HY-N0308R
-
|
|
Reference Standards
Biochemical Assay Reagents
|
Cancer
|
|
Octyl acetate (Standard) is the analytical standard of Octyl acetate (HY-N0308). This product is intended for research and analytical applications. Octyl acetate is an orally active aliphatic ester. Octyl acetate has certain antioxidant properties. Octyl acetate contributes to the formation of fruit aroma and affects the flavor of fruits such as strawberries. Octyl acetate can be used in the research of malignant melanoma, colon cancer and breast cancer .
|
-
- HY-152479
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-7 is an DNA topoisomerase IIα inhibitor with an IC50 value of 7.7 µM. Topoisomerase IIα-IN-7 has broad-spectrum cytotoxicity to leukemia, lung, colon, melanoma, ovarian, kidney, prostate and breast cancer cells. Topoisomerase IIα-IN-7 has metabolic stability .
|
-
- HY-116494A
-
|
|
BCRP
|
Cancer
|
|
(6R)-ML753286 is an isomer of ML753286 (HY-116494). ML753286 is an orally active and selective BCRP (Breast cancer resistance protein) inhibitor with an IC50 of 0.6 μM. ML753286 has high permeability and low to medium clearance in rodent and human liver S9 fractions, and is stable in plasma cross species .
|
-
- HY-152188
-
-
- HY-B1844
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Flucythrinate is a synthetic pyrethroid with endocrine suppressive properties. Flucythrinate showed good binding affinity to the vitamin D nuclear receptor (VDR) with a score of -11.0 kcal/mol. Flucythrinate has been proposed as a multi-target ligand that may interact with several proteins associated with breast cancer. The screening method for Flucythrinate showed good accuracy in binding site prediction and affinity estimation .
|
-
- HY-N9228
-
|
|
Others
|
Cancer
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8-geranylflavone is a prenylflavone with anti-proliferation effect on breast cancer cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8-geranylflavone can be isolated from an ethyl acetate-soluble extract of the barks of Broussonetia papyrifera .
|
-
- HY-114906
-
|
|
Sirtuin
|
Cancer
|
|
SIRT1/2/3-IN-2 (compound 9) is a potent SIRT inhibitor, with inhibition rates of 27%, 72%, and 71% targeting SIRT1, SIRT2, and SIRT3, respectively, at 200 μM. SIRT3 is a potential tumor suppressor or promoter, and its increased transcription may be associated with lymph node-positive breast cancer and oral squamous cell carcinoma .
|
-
- HY-132913
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Cyclopropenone probe 1 can specifically and efficiently modify a triple-negative breast cancer driver, glutathione S-transferase pi-1 (GSTP1), by covalently binding at the catalytic active site. Cyclopropenone probe 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146516
-
|
|
MDM-2/p53
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer .
|
-
- HY-P10511
-
|
|
Apoptosis
|
Infection
Cancer
|
|
Pantinin-3 is an antimicrobial peptide with antitumor activity found in the venom of the emperor scorpion (Pandinus imperator). Pantinin-3 shows selective toxicity against breast cancer cells (MDA-MB-231) and prostate cancer cells (DU-145). Pantinin-3 can induce apoptosis in tumor cells. Pantinin-3 can be used in cancer research .
|
-
- HY-P99101
-
|
AEX-4089
|
ADC Antibody
|
Cancer
|
|
Vobramitamab is a humanized B7-H3 monoclonal antibody (mAb). Vobramitamab conjugated with prodrug seco-DUBA (HY-132180A) via a cleavable linker, to form antibody-drug conjugate (ADC), the MGC018. MGC018 displays potent antitumor activity in preclinical tumor models of breast, ovarian, and lung cancer, as well as melanoma .
|
-
- HY-P991236
-
|
|
EGFR
DNA Alkylator/Crosslinker
|
Cancer
|
|
MHES0488A is a selective humanized antibody that targets HER2 with a KD value of 0.8 nM. MHES0488A is an antibody part of DHES0815A. MHES0488A is internalized by cells and transported to lysosomes, and then releases PBD-monoamide that enters the nucleus, alkylates DNA and induces DNA damage and apoptosis. MHES0488A is promising for research of cancers, such as HER2-positive breast cancer and gastric cancer .
|
-
- HY-134418R
-
|
|
Radionuclide-Drug Conjugates (RDCs)
|
Cardiovascular Disease
Cancer
|
|
NOTA (Standard) is the analytical standard of NOTA. This product is intended for research and analytical applications. NOTA is a bifunctional chelate which acts as the framework to construct PET imaging tools. NOTA also can be used for probe design and signal amplification via the multivalent effect. NOTA can be used in multiple myeloma, breast cancer, lymphoma and myocardial infarction research .
|
-
- HY-42487B
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
(R)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer .
|
-
- HY-156285
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
ZZM-1220 is a histone lysine methyltransferase G9a/GLP covalent inhibitor with IC50s of of 458 nM and 924 nM, respectively. ZZM-1220 inhibits H3K9me2 in cells and significantly induces apoptosis of triple-negative breast cancer (TNBC) cells and blocks the cell cycle in the G2/M phase .
|
-
- HY-125221
-
|
|
ROCK
Cdc42-binding kinase
|
Cancer
|
|
DJ4 is a ATP-competitive inhibitor of ROCK1/2 (IC50 values:5 and 50 nM) and MRCKα/β (IC50 values:10 and 100 nM). DJ4 blocks stress fiber formation and inhibits migration and invasion of cancer cells. DJ4 can be used for study of lung cancer, breast cancer, and pancreatic (PANC-1) cancer .
|
-
- HY-W338764
-
|
|
Apoptosis
Aryl Hydrocarbon Receptor
|
Cancer
|
|
AHR agonist 3 is an aryl hydrocarbon receptor (AhR) agonist, that can induces cell cycle arrest or apoptosis via activation of tumor-suppressive transcriptional programs. AHR agonist 3 inhibits triple-negative breast cancer (TNBC) stem cell growth via AhR while exhibits minimal cytotoxicity against normal human primary cells and can be used for cancer research .
|
-
- HY-16560
-
|
Campathecin; (S)-(+)-Camptothecin; CPT
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
|
-
- HY-42487A
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
(rac)-Exatecan Intermediate 1 is an isomer of Exatecan Intermediate 1 (HY-42487). Exatecan Intermediate 1 (compound 6) is an intermediate of Exatecan (HY-13631), a camptothecin-based anticancer agent. Exatecan inhibits tumor growth by interfering with the proliferation and division of tumor cells by interacting with DNA. Exatecan is primarily used in research into a variety of cancers including ovarian, lung and breast cancer .
|
-
- HY-157876
-
|
|
P-glycoprotein
BCRP
|
Cancer
|
|
Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research .
|
-
- HY-162575
-
|
|
ERK
|
Cancer
|
|
Anticancer agent 231 (Compound P5) is a tyrosine protein kinase inhibitor with a IC50 value of 3.95 μM. Anticancer agent 231 inhibits the cell viability, cell proliferation, cell migration and cancer dryness of triple negative breast cancer (TNBC) cells by targeting EGFR-ERK 1/2 signaling pathway, and is expected to play an important role in the field of TNBC disease therapy .
|
-
- HY-162616
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
|
-
- HY-159957
-
|
|
Histone Acetyltransferase
Estrogen Receptor/ERR
|
|
|
BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC50 of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth .
|
-
- HY-121410
-
|
|
Bacterial
Apoptosis
Parasite
NF-κB
Antibiotic
|
Infection
Cancer
|
|
Narasin is a cationic ionophore antibiotic and coccidiostat agent. Narasin inhibits NF-κB signaling and induces tumor cells apoptosis. Narasin has antimicrobial, antiviral anticancer activity. Narasin inhibits tumor metastasis and growth of ERα‑positive breast cancer cells by inactivation of the TGF-β/SMAD3 and IL‑6/STAT3 signaling pathways .
|
-
- HY-125010
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Dicycloplatin is a DNA damage inducer. Dicycloplatin induces DNA damage by activating biphosphorylated checkpoint kinase 2 (CHK2), breast cancer 1 (BRCA1) and triphosphorylated p53. Dicycloplatin can induce cell cycle arrest, inhibit proliferation and lead to apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. Dicycloplatin can be used in cancer researchr .
|
-
- HY-172900
-
|
|
Akt
Apoptosis
|
Cancer
|
|
AKT-IN-27 (4a) is a potential anticancer agent through selective therapeutic targeting of Akt-driven pathways. AKT-IN-27 (4a) induces apoptosis via caspase-3 activation, G2/M cell cycle arrest, and mitochondrial membrane potential disruption. AKT-IN-27 (4a) can be used in the research for TNBC (triple-negative breast cancer) .
|
-
- HY-W005288S
-
|
4-Hydroxystyrene-d4
|
Apoptosis
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
|
4-Vinylphenol-d4 is deuterated labeled 4-Vinylphenol (HY-W005288). 4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
|
-
- HY-173279
-
|
|
Cytochrome P450
|
Endocrinology
|
|
CYP19A1-IN-1 (Compound 9) is a CYP19A1 inhibitor with an IC50 of 271 nM. CYP19A1-IN-1 inhibits the activity of converting androgens to estrogens by binding to CYP19A1. CYP19A1-IN-1 can be used in the research of sex hormone-related diseases such as estrogen-dependent breast cancer .
|
-
- HY-N3626
-
|
|
Others
|
Cancer
|
|
Coronalolide is a natural triterpene with anticancer effects. Coronalolide exhibits a broad cytotoxic activity for human breast (BT474), gastric (KATO-3), lung (CHAGO), colon (SW-620), and liver (Hep-G2) cancer cell lines, with IC50 values of 6.59 µg/mL, 5.85 µg/mL, 5.42 µg/mL, 4.98 µg/mL, and 6.41 µg/mL, respectively .
|
-
- HY-P991149
-
|
|
TNF Receptor
|
Cancer
|
|
Nesfrotamig is a humanized immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody targeting human epidermal growth factor receptor 2 (ERBB2) and human tumor necrosis factor receptor superfamily member 9 (TNFRSF9). Nesfrotamig is promising for research of cancers, especially in ERBB2-positive related tumor diseases, such as breast cancer and gastric cancer .
|
-
- HY-130250
-
|
|
CDK
Apoptosis
|
Cancer
|
|
SR-4835 is a potent, highly selective and ATP competitive dual inhibitor of CDK12/CDK13 (CDK12: IC50=99 nM, Kd=98 nM; CDK13: Kd=4.9 nM). SR-4835 acts in synergy with DNA-damaging chemotherapy and PARP inhibitors and provokes triple-negative breast cancer (TNBC) cell death .
|
-
- HY-155841
-
|
|
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
Tubulin polymerization-IN-46 (compound 9q) is a microtubule/Tubulin inhibitor that inhibits tubulin polymerization and induces apoptosis. Tubulin polymerization-IN-46 inhibits mitosis and arrests MCF-7 cells in the G2/M phase. Tubulin polymerization-IN-46 has anti-proliferative activity against MCF-7 breast cancer cells with an IC50 of 10 nM .
|
-
- HY-163126
-
|
|
Cholinesterase (ChE)
|
Cancer
|
|
AChE-IN-52 (compound A6) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-52 shows antitumor efficacy, especially against breast cancer MCF-7 cells. AChE-IN-52 significantly disrupts the amino acid metabolism and inhibits migration of MCF-7. AChE-IN-52 plays anticancer role by regulating Best1 and HIST1H2BJ .
|
-
- HY-19822S3
-
|
RAD1901-d6
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant-d6 (RAD1901-d6) is a deuterated labeled Elacestrant (HY-19822). Elacestrant is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
|
-
- HY-B0777R
-
|
CL301423 (Standard)
|
Antibiotic
BCRP
P-glycoprotein
Parasite
|
Infection
|
|
Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
- HY-144449
-
|
|
mTOR
HDAC
Apoptosis
Autophagy
|
Cancer
|
|
mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC) .
|
-
- HY-164537
-
|
|
Phosphatase
MDM-2/p53
Apoptosis
|
Cancer
|
|
SPI-001 is a PPM1D-specific inhibitor (IC50=0.48 μM) with anticancer activity. SPI-001 inhibits PPM1D phosphatase activity and increases p53 phosphorylation in PPM1D-overexpressing human breast cancer cells. In addition, SPI-001 inhibits cell proliferation by inducing apoptosis .
|
-
- HY-16773
-
|
GS-9451
|
HCV Protease
BCRP
P-glycoprotein
|
Infection
|
|
Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC50 of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC50 of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs .
|
-
- HY-15150
-
|
R428; BGB324
|
TAM Receptor
|
Cancer
|
|
Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer .
|
-
- HY-100574D
-
-
- HY-10127A
-
|
AZD1152 dihydrochloride
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Barasertib (AZD1152 dihydrochloride), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152 dihydrochloride) induces growth arrest and apoptosis in cancer cells .
|
-
- HY-158388
-
|
|
Topoisomerase
|
Cancer
|
|
Anticancer agent 215 (1) is a Camptothecin compound, with IC50 values of 5.2 nM and 8.2 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
|
-
- HY-N3974
-
|
(+)-Griffipavixanthone
|
Apoptosis
|
Cancer
|
|
Griffipavixanthone can be extracted from Garcinia schomburgkiana. Griffipavixanthone induces cell apoptosis through mitochondrial apoptotic pathway accompanying with ROS production. Griffipavixanthone is an anti-cancer agent. Griffipavixanthone is a weak sucrase inhibitor (IC50: 4.58 mM) .
|
-
- HY-123163
-
|
RWJ-66826; RTI-6617-003
|
Progesterone Receptor
Glucocorticoid Receptor
Androgen Receptor
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
JNJ-1250132 (RWJ-66826) is an orally active and potent steroidal progesterone receptor (PR) antagonist, with an IC50 of 1.3 nM. JNJ-1250132 inhibits binding of the receptor to DNA in vitro. JNJ-1250132 is a potent competitive inhibitor of binding to the human glucocorticoid receptor (GR) (IC50=0.50 nM) and the rat androgen receptor (AR) (IC50=5.6 nM), and was a weak inhibitor of binding to human Estrogen receptor (ER) (IC50 >3000 nM) .
|
-
- HY-128027
-
|
|
mTOR
|
Cancer
|
|
eCF309 is a potent and highly selective mTOR inhibitor with remarkably low off-target activities (IC50 = 10-15 nM, both in vitro and in cells) .
|
-
- HY-137449
-
|
G1T48
|
Estrogen Receptor/ERR
CDK
|
Cancer
|
|
Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor .
|
-
- HY-145685
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RECQL5-IN-1 (Compound 4a) acts as an orally effective RECQL5 inhibitor (targeting both enzymatic and nonenzymatic domain). RECQL5-IN-1 is a potent inhibitor of RECQL5 helicase activity (IC50=46.3 nM), stabilizes the interaction between RECQL5-RAD51 proteins, causes RAD51 aggregation and homologous recombination repair (HRR) inhibition, thereby exhibiting selective cytotoxicity in RECQL5-expressing cancer cells .
|
-
- HY-157290
-
|
|
Epigenetic Reader Domain
Src
|
Cancer
|
|
HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC50 values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity .
|
-
- HY-137099A
-
|
|
Fluorescent Dye
|
Endocrinology
|
|
Genistein 7-sulfate sodium is a metabolite of genistein that can reduce the activity of estrogen agonists in MCF-7 cells. Genistein 7-sulfate sodium can promote the growth of MCF-7 cells at concentrations of 10 μM and above .
|
-
- HY-163369
-
|
|
HDAC
|
Cancer
|
|
HDAC6-IN-35 (compound C4 (ZINC000077541942)) is a potent and BBB-penetrated HDAC6 inhibitor with the IC50 of 4.7 μM. HDAC6-IN-35 shows cell toxicity against MDA-MB-231 with EC50 of 40.6 μM .
|
-
- HY-144697
-
-
- HY-115672
-
KS15
2 Publications Verification
|
Cryptochrome
|
Cancer
|
|
KS15 is an inhibitor of the interactions between cryptochromes (CRYs: CRY1 and CRY2) and the CLOCK:BMAL1 heterodimer. KS15 impairs the feedback actions of CRYs on E-box-dependent transcription (EC50=4.9 μM) by CLOCK:BMAL1 heterodimer, an indispensable transcriptional regulator of the mammalian circadian clock. Anti-proliferative activity .
|
-
- HY-P3498
-
|
ZP1846
|
GCGR
|
Others
|
|
Elsiglutide (ZP1846) is a GLP-2 analogue, an orally active and selective GLP-2 receptor agonist, increases cell proliferation and reduces apoptosis in the intestine. Elsiglutide improves Lapatinib (HY-50898)-induced diarrhoea in rat model .
|
-
- HY-150401
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
Exatecan-amide-cyclopropanol (compound 1) is a anticancer agent. Exatecan-amide-cyclopropanol shows anti-proliferation activity against SK-BR-3 and U87 cells, with IC50 values of 0.12 and 0.23 nM, respectively .
|
-
- HY-D2363
-
|
|
FAP
Radionuclide-Drug Conjugates (RDCs)
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
DOTA.SA.FAPi TFA inhibits fibroblast activation protein (FAP) with an IC50 of 0.9 nM. DOTA.SA.FAPi TFA targets protease PREP with an IC50 of 5.4 μM. DOTA.SA.FAPi TFA can be used a PET tracer, when labeled with 68Ga, and used for research about cancer . DOTA.SA.FAPi (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-137450A
-
|
IMP4297 hydrochloride; JS109 hydrochloride
|
PARP
|
Cancer
|
|
Senaparib hydrochloride (IMP4297 hydrochloride) is an oral, selective PARP1/2 inhibitor with potent anti-tumor activity. Senaparib hydrochloride shows antitumor activity against advanced ovarian cancer .
|
-
- HY-20403
-
|
VS-6062(hydrochloride)
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
|
-
- HY-130798
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
(S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180) .
|
-
- HY-N10403R
-
|
|
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
ABZ-amine (Standard) is the analytical standard of ABZ-amine. This product is intended for research and analytical applications. ABZ-amine (Amino albendazole) is an impurity of Albendazole. Albendazole is a member of the benzimidazole compounds used as a agent indicated for the treatment of a variety of worm infestations .
|
-
- HY-P3207A
-
-
- HY-10459
-
|
VS-6062
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
|
-
- HY-10127
-
|
AZD1152
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells .
|
-
- HY-161252
-
|
|
ADC Cytotoxin
|
Cancer
|
|
PBD-monoamide, a modified PBD (pyrrolobenzodiazepine) dimer, is an ADC Cytotoxin. PBD-monoamide can be used for synthesis of DHES0815A (an HER2 ADC). PBD-monoamide has DNA-binding activity and reduces cell viability .
|
-
- HY-16394
-
|
CGC-11047 tetrahydrochloride
|
Drug Derivative
|
Cancer
|
|
PG-11047 (CGC-11047), a polyamine analogue, is a nonfunctional competitor of the natural polyamine spermine. PG-11047 has broad spectrum anticancer activities .
|
-
- HY-137099
-
|
|
Fluorescent Dye
|
Endocrinology
|
|
Genistein 7-sulfate is a metabolite of genistein that can reduce the activity of estrogen agonists in MCF-7 cells. Genistein 7-sulfate can promote the growth of MCF-7 cells at concentrations of 10 μM and above .
|
-
- HY-10127R
-
|
AZD1152 (Standard)
|
Reference Standards
Aurora Kinase
Apoptosis
|
Cancer
|
|
Barasertib (Standard) is the analytical standard of Barasertib. This product is intended for research and analytical applications. Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells .
|
-
- HY-176481
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
ML-20, Malabaricone C (HY-N8518) analogue, is a autophagy inhibitor and radiosensitizer. ML-20 inhibits cell growth, induces cell apoptosis . ML-20 induces DNA double-strand breaks, loss of mitochondrial membrane potential (MMP), and lysosomal membrane permeabilization (LMP). ML-20 induces endoplasmic reticulum stress and concurrent inhibition of autophagy flux due to LMP .
|
-
- HY-108398A
-
-
- HY-N8207
-
|
|
Apoptosis
MicroRNA
|
Cancer
|
|
Gypenoside LI, a gypenoside monomer, possesses anti-tumor activity. Gypenoside LI induces cell apoptosis, cell cycle and migration .
|
-
- HY-116447
-
|
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
Antitumor agent-159 (Compound 13b) targets the mitochondria and downregulates cardiolipin levels. Antitumor agent-159 inhibits the proliferation of cancer cell MDA-MB-231, arrests the cell cycle at sub-G1 phase, and induces apoptosis in MDA-MB-231. Antitumor agent-159 exhibits antitumor efficacy in MDA-MB-231 xenograft mouse models .
|
-
- HY-100574C
-
-
- HY-149858
-
|
|
Wnt
|
Cancer
|
|
β-catenin-IN-7 (Compound 9) is a β-catenin inhibitor. β-catenin-IN-7 inhibits the interaction between β-catenin and Tcf-4, and inhibits Wnt-dependent target gene expression. β-catenin-IN-7 has anti-cancer activity .
|
-
- HY-114668
-
|
Camptothecin-20-O-propionate
|
Topoisomerase
|
Cancer
|
|
Camptothecin-20(S)-O-propionate (CZ48), the C20-propionate ester of CPT, is a highly effective anticancer agent. Camptothecin-20(S)-O-propionate (CZ48) is a topoisomerase-Ι inhibitor .
|
-
- HY-16069A
-
|
Irbinitinib hemiethanolate; ARRY-380 hemiethanolate; ONT-380 hemiethanolate
|
EGFR
|
Cancer
|
|
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
|
-
- HY-10126
-
|
AZD2811; INH-34; AZD1152-HQPA
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells .
|
-
- HY-162416
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-27 (Compound 37) is a selective inhibitor for cyclin-dependent kinase 7 (CDK7), with Ki of 3 nM. CDK7-IN-27 arrests the cell cycle at G0/G1 phase .
|
-
- HY-158743
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Indium (III) thiosemicarbazone 5b (compound 5b) is an Indium (III) thiosemicarbazone agent. Indium (III) thiosemicarbazone 5b effectively inhibits MCF-7 and DDP tumor cells growth .
|
-
- HY-158045
-
|
|
PROTACs
PARP
|
Inflammation/Immunology
Cancer
|
|
PROTAC PARP1 degrader-1 (Compound CN0) is a PROTAC degrader of PARP1. PROTAC PARP1 degrader-1 activates the cGAS/STING immunity pathway and eventually enhances T cell killing of tumor cells. PROTAC PARP1 degrader-1 inhibits DNA damage repair, resulting in highly efficient accumulation of cytosolic DNA fragments (Blue: CRBN ligand, Black: linker; Pink: PARP1 inhibitor) .
|
-
- HY-161326
-
|
|
FGFR
|
Cancer
|
|
CXF-007 is a potent and specific FGFR4 inhibitor with a IC50 value of 7 nM. CXF-007 has antitumor activity .
|
-
- HY-151092
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 77 (Compound 6c) shows anticancer activity, and can be widely used in synthesis and medicinal chemistry research .
|
-
- HY-137450
-
|
IMP4297; JS109
|
PARP
|
Cancer
|
|
Senaparib (IMP4297) is a highly potent, selective and orally active PARP1/2 inhibitor. Senaparib (IMP4297) exhibits strong antitumor activity in animal models .
|
-
- HY-14171S
-
|
LGD1069 d4
|
RAR/RXR
Autophagy
|
Cancer
|
|
Bexarotene-d4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma .
|
-
- HY-117047
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
ALC67 is a cytotoxic thiazolidine compound with an IC50 of approximately 5 μM against liver, breast cancer, colon cancer, and endometrial cancer cell lines. ALC67 induces apoptosis in cancer cells by activating caspase-9 and causing cell cycle arrest at the SubG1/G1 phase, via a pathway that is independent of death receptors. ALC67 can be used in cancer research .
|
-
- HY-149552
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Ac4-5SGlcNAc is a pro-inhibitor of carbohydrate-based glycosyltransferases (OGTs). Ac4-5SGlcNAc inhibits o-GlcN acylation and interferes with the effects of o-GlcN on neural induction of human embryonic stem cells (hESCs), and reduces the invasive phenotype of breast cancer cells. Ac4-5SGlcNAc also targets other carbohydrate-processing enzymes .
|
-
- HY-168877
-
|
|
MDM-2/p53
Reactive Oxygen Species (ROS)
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
|
FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of γ-H2AX and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer .
|
-
- HY-P9933
-
|
APN-311
|
Apoptosis
PERK
mTOR
|
Cancer
|
|
Dinutuximab (APN-311) is a chimeric human-mouse anti-GD2 monoclonal antibody. Dinutuximab can bind to GD2 on the cell surface, triggering antibody-dependent cell-mediated cytotoxicity and complement-dependent cytotoxicity, and promoting tumor regression. Dinutuximab can inhibit the growth, invasion, and migration and induce apoptosis of tumor cells. Dinutuximab can be used in the research of tumors such as neuroblastoma and breast cancer .
|
-
- HY-15176
-
|
RR82
|
G-quadruplex
|
Cancer
|
|
Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells .
|
-
- HY-160700
-
|
|
Deubiquitinase
JNK
|
Cancer
|
|
TNG348 is an orally available allosteric inhibitor of the ubiquitin-specific protease USP1. TNG348 specifically and efficiently inhibits the activity of USP1, inhibiting its deubiquitination of proliferative PCNA and FANCD2, thereby disrupting the DNA repair process. TNG348 has inhibitory activity against breast and ovarian cancers carrying BRCA1/2 mutations and other homologous recombination defects (HRD) .
|
-
- HY-149894
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
MC-1-F2 is a FOXC2 inhibitor that reduces epithelial-mesenchymal transition (EMT) markers in breast cancer cells, suppresses cancer stem cell (CSC) properties and reduces invasiveness in castration-resistant prostate cancer (CRPC) cells. There is a synergistic effect between MC-1-F2 and Docetaxel, which has the potential to be used in combination to study CRPC .
|
-
- HY-156939
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
ZnDTPA is an orally effective chelating agent, which belongs to the class of amino carboxylic acid chelating agents and is mainly used to form stable complexes with metal ions. DTPA (diethylenetriaminepentaacetic acid) itself is a polydentate ligand that can form stable cyclic or chain-like complexes with a variety of metal ions. ZnDTPA can be used to reduce the long-term toxicity of 239Pu to rats and reduce the incidence of osteosarcoma, breast cancer, etc. in rats .
|
-
- HY-13072
-
|
AS-703569; R-763
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-15176A
-
|
RR82 hydrochloride
|
G-quadruplex
|
Cancer
|
|
Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells .
|
-
- HY-19822S
-
|
RAD1901-d4
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
|
Cancer
|
|
Elacestrant-d4 (RAD1901-d4) is a deuterated labeled Elacestrant (HY-19822). Elacestrant (RAD1901) is a selective estrogen receptor (estrogen receptor, ER) degrader (SERD) with oral activity, with IC50 values of 48 and 870 nM for ERα and ERβ, respectively. Elacestrant can also effectively inhibit the growth of ER + breast cancer cell lines both in vitro and in vivo.
|
-
- HY-109583
-
|
4-Oxo-4-HPR
|
Apoptosis
Reactive Oxygen Species (ROS)
Drug Metabolite
|
Cancer
|
|
4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
|
-
- HY-W082856A
-
|
|
BCRP
|
Cancer
|
|
Butein tetramethyl ether (Compound 20) is a potent and selective breast cancer resistance protein/ATP-binding cassette subfamily G member 2 (BCRP/ABCG2) inhibitor. Butein tetramethyl ether has inhibitory potencies against MCF-7 MX and MDCK BCRP cells with IC50 values of 2.2 and 1.03 μM, respectively. Butein tetramethyl ether is promising for research of cancers .
|
-
- HY-W654305
-
|
PD 0332991-d4
|
Isotope-Labeled Compounds
CDK
|
Cancer
|
|
Palbociclib-d4 is deuterium labeled Palbociclib. Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
|
-
- HY-E70188
-
|
EC:3.1.6.4; GALNS
|
Biochemical Assay Reagents
|
Cancer
|
|
N-Acetylgalactosamine-6-Sulfatase (GALNS) is a potential general biomarker for multiple malignancies (such as lung cancer, breast cancer, head and neck cancer, etc.). N-Acetylgalactosamine-6-Sulfatase deficiency causes mucopolysaccharidosis type IVA (MPS IVA), also known as Morquio A syndrome. N-Acetylgalactosamine-6-Sulfatase can be used in MPS IVA as well as cancer research .
|
-
- HY-15738
-
GNF-5
3 Publications Verification
|
Bcr-Abl
|
Cancer
|
|
GNF-5, the N-hydroxyethyl carboxamide analog of GNF-2, is an orally active Bcr-Abl inhibitor. GNF-5 has Bcr-Abl inhibition activity with an IC50 value of 0.22 µM. GNF-5 has good favorable pharmacokinetic properties. GNF-5 can be used for the research of kinds of cancer including chronic myelogenous leukemia (CML) and breast cancer .
|
-
- HY-15096
-
|
FJ-776
|
Fluorescent Dye
HSP
|
Cancer
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-N15378
-
|
|
IAP
Bcl-2 Family
COX
TNF Receptor
Caspase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
β-carotene-15,15ʹ-epoxide is a XIAP antagonist with apoptosis-inducing and antitumor activity, found in the leaves of Spondias mombin. In a DMBA (HY-W011845)-induced rat model of breast cancer, β-carotene-15,15ʹ-epoxide binds to the BIR3 domain of the anti-apoptotic protein XIAP, blocking its interaction with caspase-9 and thereby promoting tumor cell apoptosis. In addition, β-carotene-15,15ʹ-epoxide significantly downregulates the expression of BCL-2, COX-2, and TNF-α in tumor tissues, reduces MDA levels, increases catalase activity, and modulates serum levels of LDH, ALP, and ALT, demonstrating strong antioxidant, anti-inflammatory, and metabolic protective effects. β-carotene-15,15ʹ-epoxide may be used in research on inflammation-related conditions and cancers such as breast cancer .
|
-
- HY-B0281A
-
|
|
Histamine Receptor
|
Metabolic Disease
Cancer
|
|
Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .
|
-
- HY-76474A
-
|
|
Apoptosis
Syk
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
|
-
- HY-173232
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 value of 0.509 µM and an IC50 value of 7.48 μM for inhibiting the proliferation of MCF-7 cells. VEGFR-2-IN-66 exerts its anti-cancer activity by arresting the cell cycle, inducing apoptosis, and regulating gene expression, and can be used in the research of the breast cancer field .
|
-
- HY-P10793
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
Cyclic(YCDGFYACYMDV) is a HER2 signaling pathway inhibitor with anti-cancer activity. This compound self-assembles into nanoparticles in aqueous solution and transforms into nanofibers upon specific binding to HER2 on cancer cells. This transformation disrupts HER2 dimerization and subsequent downstream signaling events, leading to cancer cell apoptosis (Apoptosis). The inhibitory effects on HER2 positive breast cancer have been demonstrated to be effective in a murine xenograft model .
|
-
- HY-N0411
-
|
Provitamin A; beta-Carotene
|
Endogenous Metabolite
Apoptosis
Reactive Oxygen Species (ROS)
|
Metabolic Disease
Cancer
|
|
β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities .
|
-
- HY-155956
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
JNK
PARP
|
Cancer
|
|
GM-90257 is a microtubule acetylation inhibitor. GM-90257 binds directly to α-tubulin. GM-90257 prevents the recruitment of α-tubulin acetyltransferase 1 (αTAT1) to the K40 residue in α-tubulin. GM-90257 causes Apoptosis, downregulates BCl-2, and activates JNK and PARP. GM-90257 has anticancer activity against breast cancer .
|
-
- HY-171543
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-37 (Compound 8) is an orally active and selective poly(ADP-ribose) polymerase 1 and 2 (PARP1/2) inhibitor with an IC50 value of 24 nM for PARP1. PARP1-IN-37 inhibits PARP activity in cells with an EC50 value of 3.7 μM. PARP1-IN-37 is promising for research of BRCA-mutated tumors, such as breast and ovarian cancers .
|
-
- HY-138298A
-
|
DS-8201; DS-8201a
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
|
-
- HY-B0860
-
|
|
Herbicide
Reactive Oxygen Species (ROS)
MDM-2/p53
|
Cancer
|
|
Diuron is an orally active phenylurea herbicide. Diuron inhibits photosynthesis in plants by blocking the formation of ATP and NADH. Diuron increases the production of ROS. Diuron increases expression of p53 in certain cell lines. Diuron has herbicidal activity against annual and perennial broadleaf weeds and grass weeds. Diuron promotes DMBA/BBN-induced bladder cancer. Diuron can be used in breast cancer research .
|
-
- HY-100624
-
-
- HY-N15201
-
|
|
STAT
|
Cancer
|
|
Betavulgarin is an anticancer agent. Betavulgarin can be isolated from Sugar Beet (Beta vulgaris). Betavulgarin suppresses the proliferation, migration, colony formation, and mammosphere formation of breast cancer cells, and reduces the size of the CD44 +/CD24 − subpopulation and the expression of the self-renewal- related genes C-Myc, Nanog and Oct4. Betavulgarin promotes BCSCs death through the regulation of Stat3/Sox2 signaling .
|
-
- HY-174160
-
|
|
TAM Receptor
Apoptosis
|
Cancer
|
|
MerTK-IN-2 (compound 15f) is an orally active MerTK inhibitor with an IC50 of 37.5 nM. MerTK-IN-2 can induce apoptosis. MerTK-IN-2 has antitumor activity with IC50 values of 1.79, 18.32, and 2.18 μM for human ovarian cancer cells A2780, breast cancer cells MDA-MB-231, and colon cancer cells HCT116, respectively .
|
-
- HY-P2729
-
|
EC 3.4.21.14
|
Ser/Thr Protease
Apoptosis
Interleukin Related
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Subtilisin (EC 3.4.21.14) is a bacterial serine protease. Subtilisin induces Apoptosis. Subtilisin stimulates the expression of pro-allergic cytokines (IL-1α, IL-33). Subtilisin induces prototypic allergic lung inflammation. Subtilisin exhibits anticancer activity against breast and colon cancer. Subtilisin shows antifouling activity. Subtilisin can be used as a detergent additive .
|
-
- HY-161659
-
|
|
Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Apoptosis inducer 19 (Compound 7g) is an Apoptosis inducer. Apoptosis inducer 19 elevates expression of pro-apoptotic proteins (Bax and caspase-3) and downregulates anti-apoptotic protein (Bcl-2). Apoptosis inducer 19 upregulates cellular reactive oxygen species (ROS) levels and disrupts mitochondrial membrane potential (MMP). Apoptosis inducer 19 can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-159613
-
|
|
Apoptosis
|
Cancer
|
|
PELP1-IN-1 is a PELP1 inhibitor. SMIP34 reduces cell viability and colony formation. PELP1-IN-1 induces apoptosis and cell cycle arrest at S phase. PELP1-IN-1 decreases the expression of PELP1. PELP1-IN-1 shows antitumor activity. SMIP34 has the potential for the research of triple-negative breast cancer (TNBC) .
|
-
- HY-173310
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-44 (Compound 46) is an inhibitor of cyclin-dependent kinase 2 (CDK2). CDK2-IN-44 can effectively inhibit the proliferation of cancer cells and exert its activity in inhibiting cancer cell growth by arresting the cell cycle, promoting Apoptosis, and inducing cellular senescence. CDK2-IN-44 holds promise for use in the research of ovarian cancer and breast cancer .
|
-
- HY-122583
-
|
|
RAD51
|
Cancer
|
|
D-G23 is a selective RAD52 inhibitor. D-G23 disrupts RAD52-mediated DNA repair pathways and suppresses the growth of BRCA1- and BRCA2-deficient cancer cells. D-G23 is promising for research of homologous recombination-related cancers, such as hereditary breast cancer and ovarian cancer caused by BRCA1/2 mutations .
|
-
- HY-B0693
-
|
|
Histamine Receptor
|
Metabolic Disease
Cancer
|
|
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice .
|
-
- HY-147165A
-
|
|
YAP
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-114169S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
WRG-28-d5 is the deuterium labeled WRG-28(HY-114169).WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic
|
-
- HY-N2025
-
|
|
PPAR
Glycosidase
|
Metabolic Disease
|
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
- HY-103712
-
|
CT7001; ICEC0942
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects .
|
-
- HY-N1440R
-
|
|
Bcl-2 Family
|
Inflammation/Immunology
Cancer
|
|
Koumine (Standard) is the analytical standard of Koumine. This product is intended for research and analytical applications. Koumine is an alkaloid separated from Gelsemium elegans, shows potent anti-tumor activity. Koumine up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in human breast cancer cells . Koumine has anxiolytic, antistress, antipsoriatic, and analgesic activities , protects against the development of arthritis in Rheumatoid arthritis (RA) animal models .
|
-
- HY-12757
-
|
|
BCRP
|
Cancer
|
|
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
|
-
- HY-P9974
-
|
OMP-18R5
|
Wnt
|
Cancer
|
|
Vantictumab (OMP-18R5) is a fully human IgG2 monoclonal antibody. Vantictumab inhibits Wnt pathway signaling by binding to FZD1/2/5/7/8 receptors. Vantictumab can be studied against cancers through direct actions on tumor cells, including CSCs, and effects on the stroma, such as metastatic HER2-negative breast cancer and metastatic pancreatic adenocarcinoma .
|
-
- HY-150540
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research .
|
-
- HY-141520G
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
ART558 (GMP) is ART558 (HY-141520) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. ART558 is a potent, selective and allosteric DNA polymerase theta (Polθ) inhibitor (IC50=7.9 nM). ART558 elicits BRCA-gene synthetic lethality and DNA damage. ART558 can be used for the research of cancer, such as breast cancer .
|
-
- HY-N7271R
-
|
|
RAD51
MDM-2/p53
|
Cardiovascular Disease
Cancer
|
|
Solanidine (Standard) is the analytical standard of Solanidine. This product is intended for research and analytical applications. Solanidine is an orally active cholestane alkaloid. Solanidine can be isolated from potato. Solanidine decreases RAD51 and increases γH2AX and p53. Solanidine has anti-tumor effects on LLC tumors and lung cancer. Solanidine promotes breast cancer cell proliferation. Solanidine reduces neovascularization. Solanidine causes abortion in some pregnant mice .
|
-
- HY-76474
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-N12606
-
|
|
Fungal
|
Infection
|
|
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
|
-
- HY-155458
-
|
|
PARP
|
Inflammation/Immunology
Cancer
|
|
HYDAMTIQ is a PARP-1/2 inhibitor (IC50: 29-38 nM) with anticancer, anti-inflammatory, and ischemic protective effects. HYDAMTIQ inhibits pulmonary PARP activity, is effective against allergen-induced cough and dyspnea, and inhibits bronchial hyperresponsiveness to methacholine. HYDAMTIQ has broad-spectrum tumor suppressor effects, including ovarian and breast cancers, prostate and pancreatic tumors, and glioblastoma multiforme. HYDAMTIQ has demonstrated in vivo efficacy in animal models of cerebral ischemia, asthma, cancer, and more .
|
-
- HY-150775
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP19A1-IN-2 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC50=0.09 nM). CYP19A1-IN-2 has potential for breast cancer research . CYP19A1-IN-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-50895R
-
|
ZD1839 (Standard)
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer .
|
-
- HY-118054
-
|
|
Orphan Receptor
|
Cancer
|
|
LRH-1 Inhibitor-3 is a small molecule that inhibits LRH-1 transcriptional activity, thereby decreasing the expression of target genes associated with cell growth and proliferation. LRH-1 Inhibitor-3 has shown potential in reducing cancer cell proliferation in human pancreatic, colon, and breast adenocarcinoma cell lines. LRH-1 Inhibitor-3 serves as a molecular probe for investigating the role of LRH-1 in various malignancies.
|
-
- HY-N5011R
-
|
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
5,7-Dimethoxyflavone (Standard) is the analytical standard of 5,7-Dimethoxyflavone. This product is intended for research and analytical applications. 5,7-Dimethoxyflavone is one of the major components of Kaempferia parviflora, has anti-obesity, anti-inflammatory, and antineoplastic effects. 5,7-Dimethoxyflavone inhibits cytochrome P450 (CYP) 3As. 5,7-Dimethoxyflavone is also a potent Breast Cancer Resistance Protein (BCRP) inhibitor .
|
-
- HY-12098R
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Verubulin (hydrochloride) (Standard) is the analytical standard of Verubulin (hydrochloride). This product is intended for research and analytical applications. Verubulin hydrochloride (MPC-6827 hydrochloride) is a blood brain barrier permeable microtubule-disrupting agent, with potent and broad-spectrum in vitro and in vivo cytotoxic activities. Verubulin hydrochloride (MPC-6827 hydrochloride) exhibits potent anticancer activity in human MX-1 breast and other mouse xenograft cancer models. Verubulin hydrochloride (MPC 6827 hydrochloride) is a promising candidate for the treatment of multiple cancer types .
|
-
- HY-13072B
-
|
AS-703569 benzoate; R-763 benzoate
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-15176B
-
|
RR82 TFA
|
G-quadruplex
|
Cancer
|
|
Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells .
|
-
- HY-118129
-
|
Ganwuweizic acid
|
PARP
Apoptosis
|
Cancer
|
|
Schisandronic acid is a triterpenoid antioxidant and anticancer agent extracted from Schisandra chinensis, which has potent cytotoxicity against human breast cancer cells, especially MCF-7. Schisandronic acid induces apoptosis and reduces cell viability in a time-dependent manner (MCF-7, IC50=8.06 μM). Schisandronic acid can upregulate active caspase-3 expression and cleave PARP, reduce the generation of reactive oxygen species and exhibit antioxidant effects .
|
-
- HY-170999
-
|
|
Caspase
Apoptosis
Ferroptosis
|
Cancer
|
|
Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer activity, showing an IC50 of 90 nM against MCF-7 breast cancer cells.
Antitumor agent-196 promotes Apoptosis by regulating the Bax-caspase 3 signaling pathway, and induces Ferroptosis through the modulation of key signaling molecules, including GPX4.
Antitumor agent-196 holds promising potential for further research in the field of cancer therapy .
|
-
- HY-138298
-
|
DS-8201 (solution); DS-8201a (solution)
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Trastuzumab deruxtecan (T-DXd; DS-8201a) (solution) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, a topoisomerase I inhibitor (a toxin component of Dxd). Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer .
|
-
- HY-16560S
-
|
Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5
|
Isotope-Labeled Compounds
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells .
|
-
- HY-14985
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-15731
-
|
|
Estrogen Receptor/ERR
Endogenous Metabolite
NO Synthase
|
Cardiovascular Disease
Cancer
|
|
Estetrol, an orally active estrogen synthesized exclusively during pregnancy by the human fetal liver, is a selective nuclear estrogen receptor modulator. Estetrol binds ERα as well as ERβ (with a fourfold lower affinity). Estetrol increases eNOS expression/activity and NO synthesis in endothelial cells. Estetrol exerts estrogenic actions on the endometrium or the central nervous system but presents antagonistic effects on the breast. Estetrol can be used in contraception and menopausal hormone research .
|
-
- HY-120625
-
|
|
HSP
|
Cancer
|
|
PU3 is a small molecule inhibitor of Hsp90 that competes with geldanamycin for Hsp90. PU3 induces degradation of proteins, including Her2, similar to geldanamycin. PU3 inhibits the growth of breast cancer cells, causing retinoblastoma protein hypophosphorylation, G1 arrest, and differentiation. PU3 represents a novel class of synthetic compounds that bind to Hsp90 and inhibit the proliferation of cancer cells. PU3 could provide a new strategy for the treatment of cancers .
|
-
- HY-103712A
-
|
CT7001 hydrochloride; ICEC0942 hydrochloride
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
|
-
- HY-103712C
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-169122
-
|
|
Others
|
Cancer
|
|
LLC1 is an amiloride (HY-B0285) derivative with cytotoxicity against breast cancer cells, particularly those resistant to treatment. The IC50 values of LLC1 for MCF7, MCF7 MX-100, MCF7 TS, MCF7 TR-1, and MCF7 TR-5 are 13, 12, 25, 26, and 19 mM, respectively. LLC1 shows potential for research in the field of cancer therapy .
|
-
- HY-N0331R
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Ziyuglycoside I (Standard) is the analytical standard of Ziyuglycoside I. This product is intended for research and analytical applications. Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics . Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC) .
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-
- HY-NP132A
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Recombinant humanized type III collagen (MW 55900) is a type III collagen with a molecular weight of 55900 Da. Recombinant humanized type III collagen has various biological functions, such as promoting skin extracellular matrix regeneration and improving the cell microenvironment. Recombinant humanized type III collagen inhibits the proliferation, migration, and invasion of breast cancer cells. Type III collagen functions in cell adhesion, migration, proliferation and differentiation through its interaction with integrins .
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-
- HY-N2877
-
|
|
Potassium Channel
Sodium Channel
Na+/K+ ATPase
Calcium Channel
Apoptosis
|
Neurological Disease
Cancer
|
|
Annonacin is an acetylgenin that is toxic by inhibiting the pathway of the mitochondrial complex. Annonacin increases tau phosphorylation in R406W +/+ mice. Annonacin acts as an inhibitor of the sodium/potassium and sarcoplasmic reticulum (SERCA) ATPase pumps. Annonacin has significant killing effect on ovarian cancer cell, cervical cancer cell, breast cancer cell, bladder cancer cell and skin cancer cell. Annonacin induces apoptosis through Bax and Caspase-3-related pathways .
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- HY-N0401A
-
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Bacterial
Estrogen Receptor/ERR
FATP
|
Infection
Metabolic Disease
|
|
(Z)-Ligustilide is extracted from Ligusticum chuanxiong Hort, has antimicrobial and antifungal activity, exhibits an average antifungal score of 5.6 . (Z)-Ligustilide is orally active, it inhibits the expression of FATP5 and DGAT, inhibits fatty acid uptake and esterification in mice and has potential as therapeutics for nonalcoholic fatty liver disease (NAFLD) . (Z)-Ligustilide is also able to reactivate ERα, has epigenetic regulation, and is used in the study of tamoxifen-resistant breast cancer .
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-
- HY-101562
-
|
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
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-
- HY-148664
-
|
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Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4E-IN-4 (Compound 33) is a selective inhibitor of eukaryotic initiation factor 4E (eIF4E) with biochemical
activity value of 95 nM. eIF4E-IN-4 inhibits cap-dependent mRNA translation with an IC50 value of 2.5 μM. eIF4E-IN-4 can be used for breast cancer, colon cancer, and head and neck cancer study .
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-
- HY-B0777S
-
|
CL-301423-d3
|
Isotope-Labeled Compounds
BCRP
Parasite
Antibiotic
P-glycoprotein
|
Infection
|
|
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
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-
- HY-167952
-
|
|
PI3K
|
Cancer
|
|
mTOR inhibitor-25 is an enzyme inhibitor that is more selective than PI3K and has good anticancer activity. mTOR inhibitor-25 shows strong inhibitory effects on mTOR and may be used to study leukemia, skin cancer, breast cancer, lung cancer and colon cancer. mTOR inhibitor-25 showed excellent activity in cell proliferation experiments, but its inhibitory ability on PI3K was relatively weak .
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-
- HY-W703549
-
|
INCB007839-d3; INCB7839-d3
|
Isotope-Labeled Compounds
MMP
|
Cancer
|
|
Aderbasib-d3 (INCB007839-d3) is deuterium labeled Aderbasib. Aderbasib (INCB007839) is a potent, orally active and target specific low nanomolar hydroxamate-based inhibitor of ADAM10 and ADAM17. Aderbasib exhibits robust antineoplastic activity and can be used for cancer research, including diffuse large B-cell non-Hodgkin lymphoma, HER2 +?breast cancer, gliomas, et al .
|
-
- HY-108694R
-
|
|
Endogenous Metabolite
NF-κB
|
Metabolic Disease
Inflammation/Immunology
|
|
γ-Tocotrienol (Standard) is the analytical standard of γ-Tocotrienol. This product is intended for research and analytical applications. γ-Tocotrienol is an active form of vitamin E. γ-tocotrienol reverses the multidrug resistance (MDR) of breast cancer cells through the signaling pathway of NF-κB and P-gp. γ-Tocotrienol is also a novel radioprotector agent, can mitigate bone marrow radiation damage during targeted radionuclide treatment .
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-
- HY-103712B
-
|
CT7001 hydrochloride dihydrate; ICEC0942 hydrochloride dihydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-173132
-
|
|
Aldose Reductase
|
Cancer
|
|
AKR1Cs-IN-1 (Compound 29) is a potent and broad-spectrum inhibitor targeting members of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). By simultaneously occupying the SP2 and SP3 pockets, it effectively inhibits multiple isoforms and disrupts metabolic pathways associated with drug resistance. In enzymatic activity assays, AKR1Cs-IN-1 exhibited significant inhibitory potency, with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM against AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. In the doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, AKR1Cs-IN-1 showed remarkable resensitization effects and significantly enhanced the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on overcoming drug resistance in breast cancer .
|
-
- HY-141890
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BAZ1A-IN-1 is a potent inhibitor of BAZ1A (bromodomain-containing protein). BAZ1A-IN-1 shows a KD value of 0.52 μM against BAZ1A bromodomain. BAZ1A-IN-1 shows good anti-viability activity against cancer cell lines expressing a high level of BAZ1A, but weak or no activity against cancer cells with a low expression level of BAZ1A .
|
-
- HY-161276
-
|
|
Apoptosis
Bcl-2 Family
|
Cancer
|
|
BFC1108 is a small molecule Bcl-2 functional converter. BFC1108 induces a conformational change in Bcl-2, resulting in the exposure of its BH3 domain both in vitro and in vivo. BFC1108 effectively induces apoptosis in Bcl-2 expressing cancers. .
|
-
- HY-144733
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
|
-
- HY-P5831
-
|
|
Others
MDM-2/p53
|
Cancer
|
|
Biotin-H10 is a specific anterior gradient homolog 2 (AGR2) inhibitor with a KD of 6.4 nM. Biotin-H10 inhibits cancer cells viability .
|
-
- HY-152185
-
|
|
p38 MAPK
|
Cancer
|
|
BSJ-04-122 is a covalent MKK4/7 dual inhibitor. BSJ-04-122 inhibits MKK4 and MKK7 with IC50 values of 4 nM and 181 nM, respectively. BSJ-04-122 can be used for the research of cancer .
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-
- HY-151245
-
|
|
Others
|
Cancer
|
|
Neolinustatin is a cyanogenic glycoside that can be isolated from flaxseeds .
|
-
- HY-146007
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCA IX-IN-1 (Compound 6f) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 331.4, 28.4, 9.4 and 17.8 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-1 shows anticancer activity .
|
-
- HY-164296
-
|
|
ADC Linker
|
Cancer
|
|
SMP-96745 is a dual-drug targeting linker-drug conjugate and can be used for study of cancer .
|
-
- HY-172160
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-21 (compound 657994) is a human epidermal growth factor receptor 2 (HER2) inhibitor, with an IC50 of 3.85 μM .
|
-
- HY-157490
-
|
|
PARP
HDAC
|
Cancer
|
|
PARP/HDAC-IN-1 (compound B102) is a potent dual inhibitor of PARP and HDAC. PARP/HDAC-IN-1 inhibits PARP1, PARP2 and HDAC1 with IC50s of 19.01, 2.13, 1690 nM, respectively .
|
-
- HY-W127505S
-
|
|
Biochemical Assay Reagents
Isotope-Labeled Compounds
|
Others
|
|
trans-2-Undecenal-d5 is deuterated labeled trans-2-Undecenal (HY-W127505). Trans-2-UndecenalIt is an organic compound belonging to aldehydes. It has a strong, pungent smell and is commonly found in a variety of foods, including fruits and vegetables. Trans-2-UndecenalIt has a variety of applications in the flavor and fragrance industry, especially as a fragrance agent in products such as perfume, cologne and air fresheners. In addition, it can also be used as an intermediate in the synthesis of various chemicals and drugs.
|
-
- HY-W029411
-
|
|
Drug Derivative
|
Cancer
|
|
4-(Benzo[d]oxazol-2-yl)aniline is a potent antitumor agent. 4-(Benzo[d]oxazol-2-yl)aniline has inhibitory activity against mammary carcinoma cell lines .
|
-
![4-(Benzo[d]oxazol-2-yl)aniline](//file.medchemexpress.com/product_pic/hy-w029411.gif)
- HY-145663
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
HS-(CH2)3CO-L-Ala-D-Ala-L-Ala-NH-CH2-S-(CH2)5-CO-DM is a agent-linker (peptide-cleavable) conjugate for ADC. DM indicates the maytansinoid moiety .
|
-
- HY-147912
-
|
|
PI3K
COX
|
Inflammation/Immunology
Cancer
|
|
COX-2/PI3K-IN-2 (compound 5f) is a potent PI3K inhibitor with IC50 value of 2.78 nM. COX-2/PI3K-IN-2 is a selective COX-2 inhibitor with Ki value of 3.02 nM. COX-2/PI3K-IN-2 shows anti-inflammatory and anti-cancer properties .
|
-
- HY-10262
-
|
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
BMS-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50s of 100 nM and 73 nM, respectively. BMS-536924 has anti-cancer activity .
|
-
- HY-168627
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-135 (compound 3d) is a EGFR inhibitor with the IC50 of 0.086 μM. EGFR-IN-135 inhibitor cell growth and arrests the cell cycle at the S phase of reast cancer cell lines .
|
-
- HY-19514
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Fosfluridine Tidoxil is comprised of a specific carrier molecule, coupled through a phosphate group to 5-Fluorouridine (5-FUrd), a metabolite of 5- Fluorouracil (5-FU). Fosfluridine Tidoxil is a oral active anticancer agent .
|
-
- HY-159734
-
|
|
Apoptosis
|
Cancer
|
|
TPP-resveratrol is a conjugate of Resveratrol (HY-16561) and triphenylphosphine (TPP) with anticancer activity. TPP-resveratrol increases the potency of Resveratrol through mitochondrial-targeted delivery and induces mitochondria-mediated apoptosis .
|
-
- HY-N3710
-
|
Kumujian G; O-Methylpicrasidine I
|
JAK
Apoptosis
|
Neurological Disease
Cancer
|
Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain .
|
-
- HY-155391
-
|
|
Carbonic Anhydrase
P-glycoprotein
Wnt
β-catenin
|
Cancer
|
|
hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity. hCA/Wnt/β-catenin-IN-1 also inhibits Wnt/β-catenin signaling pathway. hCA/Wnt/β-catenin-IN-1 inhibits cancer cell viability, including the NCI/ADR-RES DOX-resistant cell line .
|
-
- HY-167021
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Cholesterol-doxorubicin is a cholesterol conjugate with good storage stability, low hematotoxicity, and controllable drug delivery properties. Cholesterol-doxorubicin can be used in drug delivery research .
|
-
- HY-114803
-
-
- HY-17381A
-
|
4-Demethoxydaunorubicin
|
Topoisomerase
Bacterial
Fungal
Autophagy
c-Myc
DNA/RNA Synthesis
Antibiotic
|
Infection
Cancer
|
|
Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts .
|
-
- HY-144998
-
|
|
IKZF Family
Molecular Glues
|
Inflammation/Immunology
Cancer
|
|
NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2 .
|
-
- HY-P3212
-
|
|
Neuropeptide Y Receptor
Others
|
Cancer
|
|
Allo-aca, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca blocks leptin signaling and action in numerous in vitro and in vivo models .
|
-
- HY-17381
-
-
- HY-147202
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A) .
|
-
- HY-120279A
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
CFI-400437 is an indolinone-derived, ATP-competitive kinase inhibitor with high selectivity for PLK4 (IC50 of 0.6 nM) .
|
-
- HY-124181
-
|
|
IAP
Apoptosis
|
Cancer
|
|
SM-1295 is an inhibitor of apoptosis protein (IAP) antagonist, with Kd values of 3077 nM, 3.2 nM and 9.5 nM for XIAP-BIR3, c-IAP1-BIR3 and c-IAP2-BIR3, respectively .
|
-
- HY-N5112B
-
|
Isoarnebin I
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
Notch
NO Synthase
Bcl-2 Family
|
Cancer
|
|
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative that can be isolated from Lithospermum erythrorhizon Sieb. et Zucc. β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin inhibits Notch-1 activation. β,β-Dimethylacrylshikonin inhibtis tumor cell proliferation, induces tumor cell apoptosis, and inhibits tumor growth .
|
-
- HY-161995
-
|
|
Apoptosis
Necroptosis
FGFR
VEGFR
PDGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells .
|
-
- HY-155127
-
|
|
Fungal
|
Cancer
|
|
Antiproliferative agent-33 (Compound 2g) is an anti-proliferative, antifungal, and antibacterial agent. Antiproliferative agent-33 inhibits MDA-MB-231 cell proliferation (IC50: 16.38 μM). Antiproliferative agent-33 inhibits gram-negative bacteria growth, and inhibits S. faecalis with an MIC value of 8 μg/mL .
|
-
- HY-146008
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAII-IN-3 (Compound 16) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 403.8, 5.1, 10.2 and 5.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-2 shows anticancer activity .
|
-
- HY-17381R
-
|
|
Topoisomerase
Bacterial
Fungal
Autophagy
Antibiotic
DNA/RNA Synthesis
c-Myc
|
Infection
Cancer
|
|
Idarubicin (hydrochloride) (Standard) is the analytical standard of Idarubicin (hydrochloride). This product is intended for research and analytical applications. Idarubicin hydrochloride is an anthracycline antileukemic agent. It inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin hydrochloride inhibits the growth of bacteria and yeasts.
|
-
- HY-NP131
-
|
|
Discoidin Domain Receptor
Apoptosis
Autophagy
|
Cancer
|
|
Recombinant Humanized Type III Collagen 10.4kDa is a novel biomaterial that have anticancer effects. Recombinant Humanized Type III Collagen 10.4kDa activates discoidin domain receptor 1 (DDR1), and thus inhibits autophagy, proliferation, and migration of cancer cells, and induces apoptosis .
|
-
- HY-P3212A
-
|
|
Neuropeptide Y Receptor
|
Cancer
|
|
Allo-aca TFA, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca TFA blocks leptin signaling and action in numerous in vitro and in vivo models .
|
-
- HY-156026
-
|
|
FAK
|
Cancer
|
|
FAK-IN-11 (Compound 4l) is a FAK inhibitor. FAK-IN-11 binds to the ATP binding pocket of FAK, and inhibits phosphorylation of FAK protein. FAK-IN-11 shows cytotoxic activity against the MDA-MB-231 cells with an IC50 of 13.73? μM. FAK-IN-11 induces non-apoptotic cell death in MDA-MB-231 cells .
|
-
- HY-147911
-
|
|
PI3K
COX
|
Inflammation/Immunology
Cancer
|
|
COX-2/PI3K-IN-1 (compound 5d) is a potent PI3K inhibitor with IC50 value of 1.14 nM. COX-2/PI3K-IN-1 is a selective COX-2 inhibitor with Ki value of 3.24 nM. COX-2/PI3K-IN-1 has anti-inflammatory and anti-cancer properties.
|
-
- HY-144869
-
|
|
FLT3
|
Cancer
|
|
OTS447 is a potent FLT3 inhibitor with an IC50 of 21 nM (WO2012016082A1, compound 335) .
|
-
- HY-170967
-
|
|
Apoptosis
Caspase
PARP
Reactive Oxygen Species (ROS)
|
Cancer
|
|
IPH10 is an anti-cancer agent that exhibits a strong anti-tumor effect in vivo without hepatic and renal toxicity. IPH10 can significantly increase the content of ROS, decrease the mitochondrial membrane potential, and induce apoptosis in tumor cells .
|
-
- HY-149398
-
|
|
Apoptosis
PARP
CDK
|
Cancer
|
|
PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .
|
-
- HY-W240322
-
|
|
Apoptosis
|
Cancer
|
|
PSF-IN-1 (Compound No.10-3) is a RNA-binding protein (PSF) inhibitor and can effectively inhibit the PSF-RNA interaction (IC50: 2.2 pM). PSF-IN-1 can increase histone acetylation, inhibit tumor cell proliferation and induce apoptosis. PSF-IN-1 has antitumor activity .
|
-
- HY-111065
-
|
|
mTOR
|
Cancer
|
|
OXA-01 is a potent mTORC1 and mTORC2 inhibitor, with IC50 values of 29 nM and 7 nM, respectively .
|
-
- HY-122416
-
|
Lonchocarpol A; Senegalensin
|
BCRP
|
Metabolic Disease
Cancer
|
|
6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin .
|
-
- HY-141551
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.
|
-
- HY-103455
-
|
|
Estrogen Receptor/ERR
|
Others
|
|
ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.
|
-
- HY-124757
-
|
|
Proteasome
Mitosis
|
Cancer
|
|
FiVe1 is a vimentin (VIM) inhibitor. FiVe1 binds to the rod domain of VIM, causing metaphase VIM disassembly and hyperphosphorylation at Ser56, ultimately leading to mitotic catastrophe, multinucleation, and loss of stemness. FiVe1 has anticancer activity against soft tissue sarcomas. FiVe1 increases the sensitivity of ovarian cancer to Cisplatin (HY-17394). FiVe1 can be used for researches of mesenchymal cancers (including breast cancer and soft tissue sarcoma) and ovarian cancers .
|
-
- HY-163616
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 221 (Compound 4h) is an orally active anticancer agent and an antioxidant agent. Anticancer agent 221 exhibits cytotoxicity to cancer cells A549 (IC50=22.09 µg/mL) and MCF-7 (IC50=6.40 µg/mL), and induces apoptosis. Anticancer agent 221 exhibits antioxidant efficacy with an IC50 of 42.46 μM in DPPH experiment. Anticancer agent 221 exhibits antitumor efficacy against breast cancer in mouse models .
|
-
- HY-168106
-
|
|
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
|
ZMF-24 is an anti-triple-negative breast cancer (TNBC) agent with IC50 values of 0.22 μM and 0.44 μM against TNBC proliferation in BT-549 cells and MDA-MB-231 cells, respectively. ZMF-24 inhibits Eukaryotic translation initiation factor 3 subunit D (EIF3D) that disrupts the energy supply of TNBC by inhibiting glycolysis and further induces profound TNBC apoptosis by stimulating persistent ER stress .
|
-
- HY-114770
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .
|
-
- HY-151158
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM) .
|
-
- HY-158328A
-
-
- HY-16560R
-
|
Campathecin (Standard); (S)-(+)-Camptothecin (Standard); CPT (Standard)
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
Camptothecin (Standard) (Campathecin (Standard)) is the analytical standard of Camptothecin (HY-16560). This product is intended for research and analytical applications. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells.
|
-
- HY-12964
-
|
|
TAM Receptor
|
Cancer
|
|
SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].
|
-
- HY-Y1168
-
|
4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride
|
Biochemical Assay Reagents
|
Neurological Disease
Cancer
|
|
DMTMM (4-(4,6-dimethoxy-1,3,5-triazine-2-yl)-4-methylmorpholinium chloride) is a coupling agent. DMTMM can activate carboxyl groups and promote the formation of amide bonds. DMTMM plays an important role in promoting the chemical modification of biomacromolecules such as polysaccharides and proteins. DMTMM can be used for research of tissue engineering, breast cancer, corneal regeneration, and biomaterials .
|
-
- HY-139002
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP4Z1-IN-2 (compound 7) is a reversible inhibitor of CYP4Z1 (Ki=2.2 μM), which inhibits the production of 14,15-EET in breast cancer cells. CYP4Z1-IN-2 inhibits the CYP4Z1-mediated Luc-BE O-debenzylation reaction with an IC50 of 5.9 μM .
|
-
- HY-172820
-
|
DP303c
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Trastuzumab envedotin (DP303c) is a anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab envedotin is composed of the tubulin polymerization inhibitor Monomethyl auristatin E (MMAE) (HY-15162) to the anti-HER2 antibody DP001 via a cleavable linker. Trastuzumab envedotin can be used for the research of HER2-positive solid tumors, such as breast cancer, colorectal cancer, and gastric cancer .
|
-
- HY-108016
-
|
Encordin
|
Src
PI3K
JNK
STAT
EGFR
Apoptosis
Autophagy
|
Cancer
|
|
Peruvoside is a potent inhibitor of Src, PI3K, JNK, STAT, and EGFR. Peruvoside induces apoptosis and autophagy and possesses a broad spectrum of anticancer activity in breast, lung, liver cancers and leukemia. Peruvoside is a broad-spectrum and potent antiviral activity against positive-sense RNA viruses. Peruvoside sensitizes Gefitinib (HY-50895)-resistant tumour cells (A549, PC9/gef and H1975) to Gefitinib .
|
-
- HY-164519
-
|
|
Apoptosis
Mps1
Mitosis
|
Cancer
|
|
PF-7006 is an Mps1 kinase inhibitor with a Ki value of 0.27 nM and an IC50 value of 2.5 nM. PF-7006 interferes with cell cycle checkpoints by inhibiting the catalytic activity of Mps1, reducing histone H3 levels, and shortening the duration of mitosis, leading to apoptosis in cancer cells. Combined use of PF-7006 with Palbociclib (HY-50767) increases cancer cell tolerance to PF-7006. PF-7006 can be used for breast cancer research .
|
-
- HY-13072R
-
|
|
Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
|
Cancer
|
|
Cenisertib (Standard) is the analytical standard of Cenisertib. This product is intended for research and analytical applications. Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
|
-
- HY-173150
-
|
|
YAP
|
Cancer
|
|
YAP-IN-1 (Compound (+)-1) is an autophagy (Autophagy) inhibitor targeting YAP1. YAP-IN-1 binds to the Hippo pathway transcription factor YAP1 with a Kd of 9.13 μM and induces its degradation via the chaperone-mediated autophagy (CMA) pathway. This process inhibits Rab7-mediated fusion of autophagosomes and lysosomes, thereby reducing overall autophagy levels without affecting lysosomal function. YAP-IN-1 holds promise for research in cancer (e.g., liver cancer, breast cancer, etc.) .
|
-
- HY-164480
-
|
|
IKK
NF-κB
|
Inflammation/Immunology
Cancer
|
|
GTCpFE inhibits IKKα/β in the NF-κB pathway with anti-inflammatory activities and blocks p65 nuclear entry, which consists of Dimethyl fumarate (DMF) (HY-17363) linked to Aspirin (ASA) (HY-14654). GTCpFE exhibits selective anti-cancer stem-like cell (CSC) activity by reducing mammosphere growth and the CD44 + CD24 - immunophenotype. GTCpFE inhibits breast cancer stem cells, an important NFκB- and PGE2-dependent phenotype in aggressive cancers .
|
-
- HY-128600
-
ERD-308
1 Publications Verification
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity. (Pink: Target Protein Ligand (HY-48027); Black: Linker (HY-172643); Blue: VHL Ligand (HY-112078); VHL Ligand+Linker：(HY-172645))
|
-
- HY-158618
-
|
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia .
|
-
- HY-18758
-
IN-1130
1 Publications Verification
|
TGF-β Receptor
|
Inflammation/Immunology
Cancer
|
|
IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
|
-
- HY-111940
-
|
|
Raf
p38 MAPK
ERK
|
Inflammation/Immunology
|
|
LUT014 is a topical inhibitor targeting BRAF that cannot pass through the blood-brain barrier. LUT014 inhibits BRAF kinase and abnormally activates the MAPK/ERK signaling pathway, promoting the proliferation of epidermal keratinocytes, repairing skin barrier damage caused by radiation damage, and alleviating inflammatory responses. LUT014 is independent of RAS signaling and accelerates the repair and regeneration of damaged skin cells. LUT014 can be used to study radiation dermatitis, especially skin damage caused by breast cancer radiotherapy .
|
-
- HY-150084
-
|
(±)14(15)-EET
|
Cytochrome P450
Mitosis
|
Cancer
|
|
(±)14,15-Epoxyeicosatrienoic acid ((±)14(15)-EET) is the Cytochrome P450 metabolite of arachidonic acid. While CYP3A4 may be involved in breast cancer cell growth, (±)14,15-Epoxyeicosatrienoic acid may promote mitosis and anchorage-dependent cloning through STAT3 affected by CYP3A4. (±)14,15-Epoxyeicosatrienoic acid exhibits STAT3-dependent cell growth promotion and may also participate in the autocrine/paracrine pathway that drives cell growth .
|
-
- HY-124843
-
|
CLT-005
|
STAT
Apoptosis
|
Cancer
|
|
LLL3 (CLT-005) is a STAT3 inhibitor. LLL3 inhibits dimerization and phosphorylation of STAT3, thereby preventing intraconuclear transfer of STAT3 and inhibits the expression of STAT3 dependent genes, which encode proteins such as Bcl-xL and cyclin D1. In addition, LLL3 can induce cell growth inhibition and apoptosis in human breast cancer and rhabdomyosarcoma cells via the caspase pathway. LLL3 can be used in the study of STAT3 persistent activation types of cancer .
|
-
- HY-156153
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PROTAC CARM1 degrader-2 (compound 3e) is a degrader (DC50=8.8 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-2 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-2 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
|
-
- HY-B0281AS
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
|
Metabolic Disease
Cancer
|
|
Ranitidine-d6 hydrochloride is the deuterium labeled Ranitidine hydrochloride (HY-B0281A) . Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice .
|
-
- HY-169216
-
|
|
EGFR
VEGFR
CDK
|
Cancer
|
|
Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM .
|
-
- HY-113319R
-
|
|
Endogenous Metabolite
|
Cancer
|
|
β-D-Fructose,98%(mixtures) (Standard) is the analytical standard of β-D-Fructose,98%(mixtures). This product is intended for research and analytical applications. β-D-Fructose is a β-fruit sugar that can be produced by the hydrolysis of sucrose. β-D-Fructose can be used as a sweetness potentiator. β-D-Fructose can be designed as a units of antiproliferative agents against breast (MCF-7) and colon (MDST8) cancer cell lines .
|
-
- HY-P10762
-
|
LDC 10B
|
Peptide-Drug Conjugates (PDCs)
Folate Receptor (FR)
TRP Channel
|
Cancer
|
|
CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) conjugated to MMAE (HY-15162), targeting Folate receptor α (FRα) and TRPV6. CBP-1008 binds to FRα with high affinity and TRPV6 with low affinity. CBP-1008 has antitumor activity, and can be used in advanced solid tumor research (eg: colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma and follicular dendritic cell sarcoma) .
|
-
- HY-157231A
-
|
|
PERK
|
Cancer
|
|
HC-5404-Fu is a PERK inhibitor with an antitumor activity. HC-5404-Fu inhibits endoplasmic reticulum stress response signalling. HC-5404-Fu sensitizes renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). HC-5404-Fu is promising for research of renal cell carcinoma, gastric cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors .
|
-
- HY-124053
-
|
|
HDAC
|
Cancer
|
|
BRD2492 (compound 6d) is a potent, selective HDAC1 and HDAC2 inhibitor with IC50s of 13.2 nM and 77.2 nM, respecrtively. BRD2492 exhibits >100-fold selectivity for HDAC1/2 over selectivity over HDAC3 and HDAC6. BRD2492 inhibits breast cancer cell lines growth with IC50s of 1.01 μM and 11.13 μM for T-47D and MCF-7 cells, respectively .
|
-
- HY-N3405
-
|
|
Glycosidase
Bcl-2 Family
Apoptosis
TGF-β Receptor
NF-κB
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Lariciresinol is an orally active ingredient. Lariciresinol can be isolated from Arabidopsis thaliana. Lariciresinol inhibits α-glucosidase activity (IC50 of 6.97 μM; Ki of 0.046 μM). Lariciresinol dereases Bcl-2, upregulates Bax and induces Apoptosis. Lariciresinol regulates TGF-β and NF-κB pathways. Lariciresinol has antitumor activity against liver cancer, gastric cancer, and breast cancer. Lariciresinol shows antifungal activity and anti-diabetic activity .
|
-
- HY-126077
-
MTI-31
1 Publications Verification
LXI-15029
|
mTOR
|
Inflammation/Immunology
Cancer
|
|
MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer .
|
-
- HY-156152
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PROTAC CARM1 degrader-1 (compound 3b) is a degrader (DC50=8.1 nM) of co-activator associated argininemethyltransferase (CARM1). PROTAC CARM1 degrader-1 degrades CARM1 in a VHL- and proteasome-dependent manner. Thus, PROTAC CARM1 degrader-1 inhibits methylation of CARM1 substrates such as poly(A)-binding protein PABP1 and BGR1-associated factor BAF155 and inhibits breast cancer cell migration .
|
-
- HY-172966
-
|
|
EGFR
|
Cancer
|
|
EG31 is an EGFR inhibitor. EG31 effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells (GI50 values of MDA-MB-231 and Hs578T cells are 498.90 nM and 740.73 nM, respectively) and induces apoptosis by inhibiting the EGFR signaling pathway. EG31 still maintains antiproliferative activity against 5-fluorouracil (5-FU)-resistant TNBC cells (GI50: 519.5 nM). EG31 can be used to study TNBC resistance .
|
-
- HY-110294
-
|
A37
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
CM037 is a highly selective and competitive ALDH1A1 inhibitor (IC50=4.6 μM). CM037 blocks the catalytic activity of ALDH1A1, thereby inhibiting the activation of the downstream HIF-1α/VEGF pathway. CM037 is mainly used to study the ALDH1A1-mediated regulation of cancer stem cells (CSCs) and angiogenesis, especially in breast cancer, showing the potential to inhibit tumor angiogenesis and stem cell characteristics .
|
-
- HY-B0860S
-
|
|
Isotope-Labeled Compounds
Herbicide
Reactive Oxygen Species (ROS)
MDM-2/p53
|
Cancer
|
|
Diuron-d6 is the deuterium labeled Diuron (HY-B0860). Diuron is an orally active phenylurea herbicide. Diuron inhibits photosynthesis in plants by blocking the formation of ATP and NADH. Diuron increases the production of ROS. Diuron increases expression of p53 in certain cell lines. Diuron has herbicidal activity against annual and perennial broadleaf weeds and grass weeds. Diuron promotes DMBA/BBN-induced bladder cancer. Diuron can be used in breast cancer research .
|
-
- HY-155808
-
|
|
STAT
JAK
Apoptosis
COX
|
Cancer
|
|
STAT3-IN-18 (compound SPP) is a platinum (IV) complex with an axial ligand derived from sandalwood. STAT3-IN-18 inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, with anti-proliferative activity. STAT3-IN-18 activates caspase-3 and increases cleaved polyADP-ribose polymerase to induce apoptosis. STAT3-IN-18 promotes maturation and antigen presentation of dendritic cells and demonstrates safety in vivo.
|
-
- HY-B0281AR
-
|
|
Histamine Receptor
|
Metabolic Disease
Cancer
|
|
Ranitidine hydrochloride (Standard) is the analytical standard of Ranitidine hydrochloride (HY-B0281A). This product is intended for research and analytical applications. Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice.
|
-
- HY-169021
-
|
|
JNK
|
Cancer
|
|
JNK-1-IN-3 (Compound 9e) is an inhibitor of JNK1 that downregulates JNK1 gene expression and inhibits the protein levels of its phosphorylated form, concurrently reducing the expression of its downstream targets, c-Jun and c-Fos, in tumors while restoring p53 activity. JNK-1-IN-3 exhibits broad-spectrum antiproliferative activity, particularly with high inhibitory activity against renal and breast cancer cell lines, demonstrating both in vivo and in vitro anticancer activity .
|
-
- HY-135023R
-
|
|
Cytochrome P450
Prostaglandin Receptor
|
Cancer
|
|
5-trans-PGE2 (Standard) is the analytical standard of 5-trans-PGE2. This product is intended for research and analytical applications. 5-trans-PGE2 (5-trans Prostaglandin E2) is the active isomer of PGE2 and a potent activator of aromatase. Supplements the process of paracrine signaling between epithelial cells (expressing high levels of PGE2) and surrounding stromal cells (expressing high levels of aromatase). This process is involved in the growth and development of breast cancer .
|
-
- HY-168589
-
|
|
Apoptosis
Cytochrome P450
Caspase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
|
-
- HY-P5910A
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Azurin p28 peptide TFA is a tumor-penetrated antitumor peptide. Azurin p28 peptide TFA redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide TFA induces apoptosis or cell cycle arrest. Azurin p28 peptide TFA inhibits p53-positive tumor growths. Azurin p28 peptide TFA shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
|
-
- HY-146267
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 5 (Compound 40) is a selective, orally bioavailable estrogen receptor (ER) degrader (SERD) with an EC50 of 1.1 nM against ERα. ERα degrader 5 shows antitumor effect in vivo .
|
-
- HY-163587
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-39-d3 is the deuterated form of PRMT5-IN-39. PRMT5-IN-39-d3 is an orally active PRMT5 inhibitor and can be used for study of cancer .
|
-
- HY-16106
-
|
BMN-673; LT-673
|
PARP
|
Cancer
|
|
Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity .
|
-
- HY-138951
-
-
- HY-W016604
-
|
4-Pentanoylphenol; 4-Valerylphenol
|
17β-HSD
|
Cancer
|
|
4'-Hydroxyvalerophenone (Compound 4) is an inhibitor of 17β-hydroxysteroid dehydrogenase (17β-HSD) with an IC50 of 60.52 μM .
|
-
- HY-163585
-
-
- HY-151904
-
|
|
TAM Receptor
FLT3
PDGFR
|
Cancer
|
|
AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion .
|
-
- HY-N6877
-
|
|
Others
|
Cancer
|
|
Purpurogallin carboxylic acid, isolated from Macleaya microcarpa (Maxim.) Fedde, is an oxidation product of gallic acid in fermented tea. Purpurogallin carboxylic acid has anti-cancer activity .
|
-
- HY-136578
-
-
- HY-N8405
-
|
|
Cytochrome P450
|
Cancer
|
|
Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC50=25.60 μM) properties .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-170922
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-110 (compound Bb1) is a SARS-CoV-2 inhibitor. SARS-CoV-2-IN-110 exhibits antiviral efficacy against SARS-CoV-2 with an EC50 of 1.10 μM and significantly lower toxicity compared to Lapatinib (HY-50898). SARS-CoV-2-IN-110 inhibits SARS-CoV-2 with a CC50 of > 100 μM, with a selectivity index (SI) of >91 .
|
-
- HY-15861
-
|
TGP-210
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM) . Targapremir-210 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-161083
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
|
-
- HY-N0183
-
|
Biochanin B; Flavosil; Formononetol
|
FGFR
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth .
|
-
- HY-163588
-
-
- HY-163561
-
|
|
Histone Methyltransferase
|
Cancer
|
|
CARM1-IN-6 (iCARM1) is an effective and selective inhibitor of CARM1 with an IC50 value of 12.3 μM. CARM1-IN-6 exhibits cell growth inhibitory activity and can be used in cancer research .
|
-
- HY-107999
-
CADD522
4 Publications Verification
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
CADD522 is a RUNX2-DNA binding inhibitor (downregulates RUNX2-mediated transcription of downstream target genes), with an IC50 of 10 nM. CADD522 inhibits primary tumor growth and experimental metastasis of tumor cells in the lungs of immune-compromised mice. CADD522 can be used in study of cancer .
|
-
- HY-15340
-
|
LG268
|
RAR/RXR
Autophagy
|
Metabolic Disease
|
|
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy .
|
-
- HY-161267
-
-
- HY-115673
-
LAS17
1 Publications Verification
|
Glutathione S-transferase
|
Cancer
|
|
LAS17 is a potent and selective tyrosine-directed irreversible inhibitor for glutathione S-Transferase Pi (GSTP1) . LAS17 inhibits GSTP1 activity with an IC50 of 0.5 μM . LAS17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-149132
-
|
DDA
|
LXR
|
Cancer
|
|
Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
|
-
- HY-139950
-
|
|
Ras
|
Cancer
|
Rasarfin is a dual Ras and ARF6 inhibitor .
|
-
- HY-143439
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity .
|
-
- HY-160662
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4-IN-5 (example 51) is a BRD4 inhibitor. The Ki values of the two BRD4 domains BDI_K57-E168 and BDII_E352-M457 are 9.7 nM and 16.1 nM, respectively. BRD4-IN-5 can be used in cancer research .
|
-
- HY-114243
-
|
|
Others
|
Cancer
|
|
DpC is an anti-tumor agent. DpC inhibits cancer cell proliferation (IC50: 0.007-0.096 μM). DpC synergizes with multiple anti-cancer therapeutics .
|
-
- HY-15338
-
TG003
5 Publications Verification
|
CDK
|
Cancer
|
|
TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P5910
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Azurin p28 peptide is a tumor-penetrated antitumor peptide. Azurin p28 peptide redues proteasomal degradation of p53 through formation of a p28: p53 complex. Azurin p28 peptide induces apoptosis or cell cycle arrest. Azurin p28 peptide inhibits p53-positive tumor growths. Azurin p28 peptide shows antiangiogenic effect by inhibiting phosphorylation of VEGFR-2, FAK and Akt .
|
-
- HY-15338A
-
|
|
CDK
|
Cancer
|
|
(E/Z)-TG003 is a racemic compound of (Z)-TG003 and (E)-TG003. (Z)-TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively .
|
-
- HY-135793
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Macropa-NH2 diester is a compound can be used for imaging during the investigation of cancer. Macropa-NH2 diester is compound 210 extracted from patent WO2018187631 .
|
-
- HY-N0183R
-
|
|
FGFR
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Formononetin (Standard) is the analytical standard of Formononetin. This product is intended for research and analytical applications. Formononetin is a potent FGFR2 inhibitor with an IC50 of ~4.31 μM. Formononetin potently inhibits angiogenesis and tumor growth .
|
-
- HY-P10841
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
CyPep-1 is a novel cationic lytic peptide with antitumor activity. CyPep-1 is highly cytotoxic by interacting with the negatively charged cell membrane of cancer cells. CyPep-1 has strong cytolytic activity on cancer cells both in vivo and in vitro, and can be used in the study of solid tumors .
|
-
- HY-163586
-
-
- HY-170668
-
-
- HY-163591
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-IN-36-d3 is the deuterated derivative of PRMT5-IN-36. PRMT5-IN-36-d3 (compound 4) is an orally active PRMT5 inhibitor for cancer research .
|
-
- HY-155038
-
|
|
PARP
CDK
|
Cancer
|
|
Antitumor agent-104 (Compound 9) is an antitumor agent by inhibiting DNA damage repair in tumors. Antitumor agent-104 inhibits PARP1 enzymatic activity and the PAR protein level. Antitumor agent-104 also inhibits the expression of CDK12 .
|
-
- HY-132991
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
ML 2-14 is a PROTAC targeting BRD4 with a C4 alkyl linker. ML 2-14 consists of the E3 ligase ligand EN219 (HY-115715) (bule part), the target protein ligand JQ-1 (HY-13030) (red part), and the PROTAC linker (balck part). ML 2-14 can effectively degrade BRD4 in 231MFP breast cancer cells, and this effect can be reversed by the proteasome inhibitor Bortezomib (HY-10227) and the E1 activase inhibitor TAK-243 (HY-100487) .
|
-
- HY-131089
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-VC-PABC-C6-α-Amanitin is an antibody agent conjugate consisting of an anticancer toxin alpha-Amanitin (HY-19610) and a monoclonal antibody MC-VC-PABC-C6. Among them, alpha-Amanitin is a potent inhibitor of RNA polymerase IIα. MC-VC-PABC-C6-α-Amanitin accurately targets HER2 receptors, specifically recognizes HER2-positive tumor cells. It is widely used in breast cancer and gastric cancer research .
|
-
- HY-16468
-
|
MSI-1256
|
Bacterial
HBV
FAK
Dengue Virus
|
Infection
Neurological Disease
Cancer
|
|
Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson ,s disease mouse models .
|
-
- HY-P991217
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
EU-103 is a humanized monoclonal antibody targeting V-Set And Immunoglobulin Domain Containing 4 (VSIG4) with a KD value ranging from 10 −7 and 10 −9. EU-103 blocks the interaction between VSIG4 and CD8+ T cells, promotes the conversion of M2 macrophages into M1 macrophages, induces the proliferation of CD8+ T cells and the secretion of pro-inflammatory cytokines, thereby inhibiting tumor growth. EU-103 is promising for research of cancers, such as bladder cancer, breast cancer, and colon cancer .
|
-
- HY-100575
-
|
Acriflavinium chloride 3,6-Acridinediamine mix
|
Fluorescent Dye
HIF/HIF Prolyl-Hydroxylase
Bacterial
SARS-CoV
Monocarboxylate Transporter
Fungal
|
Infection
Cancer
|
|
Acriflavine (Acriflavinium chloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine is an antiseptic agent. Acriflavine is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2 .
|
-
- HY-N13772
-
|
(+)-Dihydroisorhamnetin
|
Apoptosis
|
Cancer
|
|
3'-O-Methyltaxifolin ((+)-Dihydroisorhamnetin) is a dihydroflavanol found in Pulicaria jaubertii. A mixture of these alcohol compounds including 3'-O-Methyltaxifolin found in Pulicaria jaubertii exhibits antitumor activity with IC50 values of 19.1 μg, 20.0 μg, and 24.1 μg against prostate cancer (PC-3), breast cancer (MCF-7), and hepatocellular carcinoma (HepG-2) cell lines, respectively. Furthermore, 3'-O-Methyltaxifolin can induce cell apoptosis, making it a promising candidate for anticancer research. .
|
-
- HY-B0860R
-
|
|
Herbicide
Reference Standards
Reactive Oxygen Species (ROS)
MDM-2/p53
|
Cancer
|
|
Diuron (Standard) is the analytical standard of Diuron (HY-B0860). This product is intended for research and analytical applications. Diuron is an orally active phenylurea herbicide. Diuron inhibits photosynthesis in plants by blocking the formation of ATP and NADH. Diuron increases the production of ROS. Diuron increases expression of p53 in certain cell lines. Diuron has herbicidal activity against annual and perennial broadleaf weeds and grass weeds. Diuron promotes DMBA/BBN-induced bladder cancer. Diuron can be used in breast cancer research .
|
-
- HY-173119
-
|
|
ERK
Autophagy
|
Cancer
|
|
SKLB-D18 is a potent and selective inhibitor of ERK1/2 and ERK5, with IC50s of 38.69, 40.12 and 59.72 nM, respectively. SKLB-D18 is also an autophagy agonist, plays a role in mTOR/p70S6K and NCOA4-mediated ferroptosis, which may mitigate multidrug resistance. SKLB-D18 exhibits significantly superior efficacy in vitro and in vivo against triple-negative breast cancer (TNBC) .
|
-
- HY-N0411R
-
|
|
Endogenous Metabolite
Apoptosis
Reactive Oxygen Species (ROS)
|
Metabolic Disease
Cancer
|
|
β-Carotene (Standard) is the analytical standard of β-Carotene. This product is intended for research and analytical applications. β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities .
|
-
- HY-104048
-
|
|
Histone Demethylase
|
Cancer
|
|
QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
|
-
- HY-12302
-
|
9-Bromopaullone; NSC-664704
|
CDK
GSK-3
|
Cancer
|
|
Kenpaullone is a potent inhibitor of CDK1/cyclin B and GSK-3β, with IC50s of 0.4 μM and 23 nM, and also inhibits CDK2/cyclin A, CDK2/cyclin E, and CDK5/p25 with IC50s of 0.68 μM, 7.5 μM, 0.85 μM, respectively. Kenpaullone, a small molecule inhibitor of KLF4, reduces self-renewal of breast cancer stem cells and cell motility in vitro.
|
-
- HY-N2025R
-
|
|
PPAR
Glycosidase
|
Metabolic Disease
|
|
Oroxin A (Standard) is the analytical standard of Oroxin A. This product is intended for research and analytical applications. Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE). Oroxin A acts as a partial PPARγ agonist that can activate PPARγ transcriptional activation. Oroxin A activates PPARγ by docking into the PPARγ protein ligand-binding domain. Oroxin A also exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity . Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence .
|
-
- HY-112096S
-
|
NXP900-d5
|
Src
Isotope-Labeled Compounds
|
Cancer
|
|
eCF506-d5 (NXP900-d5) is deuterated labeled eCF506 (HY-112096). eCF506 is a highly potent and orally active YES1/SRC kinase inhibitor with an IC50 of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer .
|
-
- HY-B1513
-
|
|
Microtubule/Tubulin
SARS-CoV
|
Infection
Metabolic Disease
Cancer
|
|
α-Cyclodextrin (α-CD) is a soluble fiber derived from corn. α-Cyclodextrin can deplete sphingolipids and phospholipids from cell membranes. α-Cyclodextrin interacts with tubulin. α-Cyclodextrin improves defenses against SARS-CoV-2 infection. α-Cyclodextrin enhances the anticancer efficacy of Crcumin (HY-N0005) against breast, lung and cervical cancer. α-Cyclodextrin has beneficial effects on body weight and blood lipids .
|
-
- HY-153066
-
|
KIF18A-IN-7
|
Kinesin
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
VLS-1272 (Compound 22) is an orally active KIF18A inhibitor that binds to the KIF18A-microtubule complex in an ATP-noncompetitive manner (IC50 = 41 nM), blocking its ATPase activity and inhibiting microtubule translocation. This leads to abnormal accumulation of KIF18A at spindle poles, disrupting chromosome alignment and inducing mitotic arrest and apoptosis in CIN High tumor cells (e.g., ovarian cancer OVCAR-3, breast cancer JIMT-1). VLS-1272 is a promising candidate for anti-tumor research .
|
-
- HY-151154
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .
|
-
- HY-173522
-
|
|
Kinesin
|
Cancer
|
|
KIF2C-IN-1 (Compound 7S9) is a selective and potent small-molecule KIF2C inhibitor. KIF2C-IN-1 stabilizes the KIF2C-tubulin interaction, blocking the depolymerization of polyglutamylated microtubules. KIF2C-IN-1 enhances the cytotoxicity of Paclitaxel (HY-B0015) in paclitaxel-resistant triple-negative breast cancer (TNBC) cells and significantly reduces tumor growth combined with Paclitaxel in mouse models .
|
-
- HY-P10947
-
|
|
Epigenetic Reader Domain
YAP
|
Cancer
|
|
MACTIDE-V is an orally active and selective peptide-drug conjugate targeting CD206. MACTIDE-V delivers Verteporfin (HY-B0146) to CD206 + tumor-associated macrophages (TAM) to inhibit the YAP/TAZ signaling pathway, prompting YAP exclusion from the nucleus, inducing TAM polarization toward an anti-tumoral phenotype with enhanced phagocytosis and antigen presentation, and boosting T cell infiltration and NK cell activity. MACTIDE-V suppresses primary tumor growth and lung metastasis in triple-negative breast cancer (TNBC) mouse models .
|
-
- HY-171786
-
|
|
CDK
|
Cancer
|
|
CDK12-IN-8 (Compound Cpd143) is an orally active and highly selective inhibitor of cyclin-dependent kinase 12 (CDK12). CDK12-IN-8 inhibits CDK12-mediated phosphorylation of the C-terminal domain (CTD) serine 2 of RNA polymerase II, interfering with gene transcription elongation and DNA damage repair pathways. CDK12-IN-8 is promising for research of cancers with high CDK12 expression such as small cell lung cancer and triple-negative breast cancer .
|
-
- HY-159569
-
|
|
Transferrin Receptor
Ferroptosis
|
Cancer
|
|
TfR-1-IN-1 (compound C4) is an inhibitor of transferrin receptor 1 (TfR-1) with anticancer activity. TfR-1-IN-1 strongly increases intracellular iron (II) levels as a driving force for the induction of ferroptosis. TfR-1-IN-1 significantly reduces the metabolic activity of ovarian cancer (A2780cis), breast cancer (MDA-MB 231), and leukemia (HL-60) cell lines with IC50 values of 0.51, 0.46, and 0.48 μM, respectively .
|
-
- HY-161778
-
|
|
HDAC
VD/VDR
|
Inflammation/Immunology
Cancer
|
|
ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization .
|
-
- HY-W088075
-
|
Acriflavinium chloride hydrochloride
|
Fluorescent Dye
HIF/HIF Prolyl-Hydroxylase
Bacterial
SARS-CoV
Monocarboxylate Transporter
Fungal
|
Infection
Cancer
|
|
Acriflavine (Acriflavinium chloride) hydrochloride is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic agent. Acriflavine hydrochloride is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine hydrochloride inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine hydrochloride is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine hydrochloride is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2 .
|
-
- HY-145547
-
|
14:0 Lyso PE; 1-Myristoyl-2-hydroxy-sn-glycero-3-PE; 1-Tetradecanoyl-sn-glycero-3-phosphoethanolamine
|
Liposome
|
Metabolic Disease
|
|
1-Myristoyl-2-hydroxy-sn-glycero-3-phosphoethanolamine (14:0 Lyso PE) is a lysophospholipid with a phosphoethanolamine head and a myristoyl tail. The free amine group can conjugate with NHS active ester or coupled with carboxylic acid in the presence of a coupling agent. It also induces transient increases in intracellular calcium in PC12 cells . Serum levels of 1-Myristoyl-2-hydroxy-sn-glycero-3-phosphoethanolamine are elevated in patients with malignant breast cancer compared to healthy controls .
|
-
- HY-104040
-
|
Orin1001
|
IRE1
|
Cancer
|
|
MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM . MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth .
|
-
- HY-P991243
-
|
|
EGFR
PI3K
Akt
|
Cancer
|
|
MP-RM-1 is a selective murine monoclonal antibody inhibitor targeting human epidermal growth factor receptor 3 (ErbB-3). MP-RM-1 blocks the activation of ErbB-3 induced by neuregulin 1 (NRG-1β) and promotes the internalization and degradation of ErbB-3, inhibiting downstream signaling pathways such as PI3K-Akt. MP-RM-1 is promising for research of ErbB-3 highly expressed solid tumors such as breast cancer, melanoma, and prostate cancer .
|
-
- HY-155760
-
|
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
|
hCA/VEGFR-2-IN-3 (compound 8j) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-3 inhibits VEGFR-2 (IC50=358 nM), has high binding activity to hCAs with Ki of 4.2 nM (hCA IX), 22.9 nM (hCA II), 25.1 nM (hCA I), 28.0 nM (hCA XII), respectively. hCA/VEGFR-2-IN-3 has antiproliferative activity against VEGFR-2 overexpressing breast cancer cells .
|
-
- HY-P991234
-
|
|
EGFR
p38 MAPK
PI3K
Akt
|
Cancer
|
|
COVA208 is a bispecific FynomAb (a fusion protein of an antibody and a Fyn SH3-derived binding protein) that targets HER2. COVA208 induces the degradation of HER2, reduces the levels of HER2, HER3, and EGFR, thereby effectively blocking the downstream signaling pathways of HER2, including the HER3-PI3K-AKT and MAPK pathways, and simultaneously inducing apoptosis of tumor cells. COVA208 is promising for research of cancers, such as HER2-positive breast cancer, gastric cancer, and colorectal cancer .
|
-
- HY-N0411S4
-
|
Provitamin A-13C10; beta-Carotene-13C10
|
Isotope-Labeled Compounds
Endogenous Metabolite
Apoptosis
Reactive Oxygen Species (ROS)
|
Metabolic Disease
Cancer
|
|
β-Carotene- 13C10 (Provitamin A- 13C10) is the 13C-labeled β-Carotene (HY-N0411). β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities .
|
-
- HY-150510A
-
|
|
Histone Methyltransferase
|
Neurological Disease
Cancer
|
|
MS8511 (hydrochloride) is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 (hydrochloride) reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 (hydrochloride) can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
|
-
- HY-144638
-
|
|
Apoptosis
|
Cancer
|
|
JMX0293 is an O-alkylamino-tethered salicylamide derivative compound. JMX0293 maintains good potency against MDA-MB-231 cell line (IC50 = 3.38 μM) while exhibiting very low toxicity against human non-tumorigenic breast epithelial cell line MCF-10A (IC50> 60 μM). JMX0293 inhibits STAT3 phosphorylation and contribute to apoptosis in TNBC MDA-MB-231 cells. JMX0293 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo without significant toxicity .
|
-
- HY-117649
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
|
-
- HY-N6932
-
|
|
Cannabinoid Receptor
P-glycoprotein
PI3K
Akt
mTOR
Apoptosis
Autophagy
EGFR
|
Metabolic Disease
Cancer
|
|
Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer .
|
-
- HY-150510
-
|
|
Histone Methyltransferase
|
Neurological Disease
Cancer
|
|
MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
|
-
- HY-171558
-
|
|
PI3K
Akt
|
Cancer
|
|
PI3K-IN-56 (Compound 1) is an orally active, potent and selective irreversible inhibitor of phosphoinositide 3-kinase (PI3K). PI3K-IN-56 irreversibly blocks the phosphatidylinositol-3,4,5-triphosphate (PIP3) production and downstream AKT signaling pathway. PI3K-IN-56 is promising for research of PI3Kα-driven cancers, such as breast and ovarian cancers .
|
-
- HY-115997
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-164978
-
|
|
Kinesin
|
Cancer
|
|
KIF18A-IN-14 (Compound Example 81) is a KIF18A inhibitor. KIF18A-IN-14 is available in two forms, EX81-A and its enantiomer EX81-B. EX81-A and EX81-B inhibit OVCAR-3 cells viability with IC50s of 0-0.01 μM and 0.01-0.1 μM, respectively. KIF18A-IN-14 can be used in tumor (e.g. colon, breast, lung) studies .
|
-
- HY-137441
-
|
PU-HZ151
|
HSP
|
Neurological Disease
Cancer
|
|
Icapamespib (PU-HZ151; PU-AD) is a selective, orally active inhibitor of Epichaperomes assembled by HSP90 with slow dissociation kinetics. Icapamespib can cross the blood-brain barrier (BBB) ??and induce epichaperome disassembly by non-covalently binding to HSP90, restoring the normal protein-protein interaction network. Icapamespib can specifically disrupt disease-related abnormal protein interaction networks, reduce neurotoxic protein aggregation and tumor cell survival signals. Icapamespib can be used in the research of neurodegenerative diseases such as Alzheimer's disease, as well as cancers such as glioblastoma and metastatic breast cancer .
|
-
- HY-137441A
-
|
PU-HZ151 hydrochloride
|
HSP
|
Neurological Disease
Cancer
|
|
Icapamespib (PU-HZ151; PU-AD) hydrochloride is a selective, orally active inhibitor of Epichaperomes assembled by HSP90 with slow dissociation kinetics. Icapamespib hydrochloride can cross the blood-brain barrier (BBB) ??and induce epichaperome disassembly by non-covalently binding to HSP90, restoring the normal protein-protein interaction network. Icapamespib hydrochloride can specifically disrupt disease-related abnormal protein interaction networks, reduce neurotoxic protein aggregation and tumor cell survival signals. Icapamespib hydrochloride can be used in the research of neurodegenerative diseases such as Alzheimer's disease, as well as cancers such as glioblastoma and metastatic breast cancer .
|
-
- HY-170551
-
|
|
Carbonic Anhydrase
VEGFR
|
Cancer
|
|
CA IX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. CA IX/VEGFR-2-IN-3 exhibits anticancer activity, inhibiting the growth of MCF-7 breast cancer cells (with an IC50 of 22.33 μM) and mouse fibroblast cell line 3T3 (where cell viability is less than 40% at a concentration of 100 μM). CA IX/VEGFR-2-IN-3 can be used for research in the field of cancer treatment .
|
-
- HY-134997
-
|
4-oxo DHA
|
PPAR
|
Cancer
|
|
4-oxo Docosahexaenoic acid (4-oxo DHA) is a putative metabolite of Docosahexaenoic acid (HY-B2167) with antiproliferative and PPARγ agonist activity. It inhibits the growth of several triple negative breast cancer cell lines (MCF-10F, trMCF, bsMCF, MDA-MB-231, and BT549) at 50-100 μM, however it increased proliferation of MCF-7 cells. 4-oxo DHA binds covalently to PPARγ and activates gene transcription in luciferase reporter assays and in dendritic cells with EC50 values of approximately 8-16 μM.
|
-
- HY-109583S
-
|
4-Oxo-4-HPR-d4
|
Isotope-Labeled Compounds
Reactive Oxygen Species (ROS)
Drug Metabolite
Apoptosis
|
Cancer
|
|
4-Oxofenretinide-d4 (4-Oxo-4-HPR-d4) is deuterium labeled 4-Oxofenretinide. 4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
|
-
- HY-N0726
-
|
Dracohodin perochlorate
|
Apoptosis
Akt
PI3K
NF-κB
MDM-2/p53
Caspase
Reactive Oxygen Species (ROS)
Toll-like Receptor (TLR)
PARP
|
Metabolic Disease
Cancer
|
|
Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product. Dracorhodin perchlorate can be obtained from the natural active molecule Dragon's blood. Dracorhodin perchlorate inhibits PI3K/Akt and NF-κB activation, upregulates p53 expression, activates caspase, produces ROS, and promotes Apoptosis. Dracorhodin perchlorate regulates the TLR4. Dracorhodin perchlorate promotes wound healing, improves diabetes. Dracorhodin perchlorate has anti-tumor activity against prostate cancer, breast cancer, cervical cancer and other cancers .
|
-
- HY-F0002R
-
|
Sodium NADP (Standard)
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
NADP (sodium salt) (Standard) is the analytical standard of NADP (sodium salt). This product is intended for research and analytical applications. NADP sodium salt is the sodium salt form of NADP (HY-113325). NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes[1][4].
|
-
- HY-P2588
-
-
- HY-115979
-
-
- HY-115677
-
|
|
Integrin
DYRK
|
Cancer
|
|
ILK-IN-3 is an orally active integrin linked kinase (ILK) inhibitor. ILK-IN-3 improves the anticancer efficacy of Docetaxel (HY-B0011) in orthotopic LCC6 model .
|
-
- HY-153691
-
|
|
mGluR
|
Others
|
|
BTB01303 is a (glutamate release) inhibitor. Cancer cells release high levels of (glutamate), which disrupts normal bone turnover and may lead to cancer-induced bone pain. BTB01303 has the potential to improve cancer-induced bone pain .
|
-
- HY-N3149A
-
|
|
Wnt
β-catenin
STAT
Apoptosis
|
Inflammation/Immunology
|
|
2-Hydroxycinnamaldehyde is a phenylpropanoid that can be isolated from the bark of Cinnamomum cassia. 2-Hydroxycinnamaldehyde inhibits Wnt/β-catenin, STAT3 signaling. 2-Hydroxycinnamaldehyde induces cell apoptosis 2-Hydroxycinnamaldehyde has antitumor and anti-inflammation activities .
|
-
- HY-124632
-
WJ460
2 Publications Verification
|
Ferroptosis
Autophagy
|
Cancer
|
|
WJ460 is a potent inhibitor of myoferlin (MYOF) that interacts directly with MYOF. WJ460 inhibits the migration and growth, induces cell cycle arrest, mitochondrial autophagy, lipid peroxidation and ferroptosis in tumor cells. WJ460 has anti-tumor activity .
|
-
- HY-120852
-
JG26
1 Publications Verification
|
Angiotensin-converting Enzyme (ACE)
MMP
EGFR
ERK
SARS-CoV
|
Infection
Cardiovascular Disease
Cancer
|
|
JG26 is an ADAM inhibitor with IC50 values of 12 nM, 1.9 nM, and 150 nM for ADAM8, ADAM17, and ADAM10, respectively. JG26 inhibits MMP-12 with an IC50 value of 9.4 nM. JG26 inhibits AngII (HY-13948)-induced EGFR transactivation and ERK activation. JG26 increases the expression of ACE2, inhibits the cleavage of CD23, reduces the infection of SARS-CoV-2. JG26 inhibits colorectal cancer metastasis. JG26 can be used for research on Hodgkin lymphoma and vascular diseases .
|
-
- HY-160183
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-29 (compound 6) is a Lysine specific demethylase 1 (LSD1) inhibitor with the IC50 of 19 nM .
|
-
- HY-161366
-
|
|
PI3K
|
Cancer
|
|
OMS14 is exhibits inhibitory activity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells .
|
-
- HY-125916
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Pseurotin A, a secondary metabolite of Aspergillus and other fungi, is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50=3.6 μM). Antitumor activity .
|
-
- HY-41570
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
3-Formylsalicylic acid is a noncompetitive estrone sulfatase inhibitor with an IC50 value of 0.15 mM, a Ki value of 0.12 mM. 3-Formylsalicylic acid shows a low acute toxicity .
|
-
- HY-11038D
-
|
PU-H71 formic
|
HSP
|
Cancer
|
|
Zelavespib formic (PU-H71 formic) is a potent Hsp90 inhibitor with an IC50 value of 51 nM for Hsp90 in MDA-MB-468 cells .
|
-
- HY-P5133
-
|
SSTN92-119
|
Integrin
|
Cancer
|
|
Synstatin (92-119) is an anti-tumor agent that inhibits angiogenesis and cancer cell invasion. Synstatin (92-119) down-regulates integrin α?β3 and reduces the activation of angiogenic growth factors VEGF and FGF-2 .
|
-
- HY-157435
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumor effect .
|
-
- HY-144774
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
|
-
- HY-16023A
-
|
EM-652; SCH 57068
|
Estrogen Receptor/ERR
|
Cancer
|
|
Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties .
|
-
- HY-19313
-
|
|
Histone Methyltransferase
|
Cancer
|
|
LLY-507 is a potent and selective inhibitor of protein-lysine methyltransferase SMYD2. LLY-507 potently inhibits the ability of SMYD2 to methylate p53 peptide with an IC50 <15 nM. LLY-507 serves as a valuable chemical probe to aid in the dissection of SMYD2 function in cancer and other biological processes .
|
-
- HY-N3995R
-
|
|
Apoptosis
Drug Metabolite
|
Cancer
|
|
D-Psicose (Standard) is the analytical standard of D-Psicose. This product is intended for research and analytical applications. D-Psicose is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-158090
-
|
|
Others
|
Cancer
|
|
Triptolide palmitate is the derivative of Triptolide (HY-32735). Triptolide palmitate exhibits cytotoxicity against cancer cell MCF-7 and A549, with IC50 of 7.5 and 6.4 μM. Triptolide palmitate exhibits a half-time T1/2 of 50.4 min in Sprague Dawley rats. Triptolide palmitate can be utilizd as drug carrier .
|
-
- HY-121149
-
|
3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
|
-
- HY-P10439
-
|
|
PD-1/PD-L1
|
Inflammation/Immunology
Cancer
|
|
CVRARTR is a programmed cell death ligand-1 (PD-L1) antagonist with a KD of 281 nM. CVRARTR induces the internalization of PD-L1 and downregulates PD-L1 on the cell surface. CVRARTR restores cytokine secretion and T cell proliferation in cell CT26. CVRARTR exhibits antitumor efficacy against in CT26 homograft mouse model. CVRARTR can be used in melanoma research .
|
-
- HY-168460
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RNA recruiter 2 is a QSOX1 mRNA ligand. RNA recruiter 2 can serve as a ligand for target RNA (Ligands for Target RNA for RIBOTAC) for the development of RIBOTAC RNA degraders with antitumor activity. RNA recruiter 2 can be used for the synthesis of F1-RIBOTAC (HY-171148) .
|
-
- HY-133124
-
|
|
PARP
PI3K
Apoptosis
|
Cancer
|
|
PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases .
|
-
- HY-112626
-
|
|
CDK
|
Cancer
|
|
CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12 .
|
-
- HY-N9232
-
|
|
Others
|
Others
|
|
Rutaevin 7-acetate (compound 1) is a limonoid .
|
-
- HY-102087
-
JPM-OEt
3 Publications Verification
|
Cathepsin
|
Cancer
|
|
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .
|
-
- HY-176191
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora kinase-IN-7 (compound 4b) is an orally active and selective AURKB inhibitor. Aurora kinase-IN-7 can be used in the study of aggressive cancers .
|
-
- HY-160899A
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Thailanstatin A cyclohexane diamine formic is an analog of Spliceostatin (HY-16466). Thailanstatin A cyclohexane diamine formic inhibits proliferations of cells N87 (IC50 is 0.33 μM), BT474 (IC50 is 0.34 μM), MDA-MB-361-DYT2 (IC50 is 0.88 μM) and MDA-MB-468 (IC50 is 0.27 μM). Thailanstatin A cyclohexane diamine formic is used as a drug-linker conjugate for ADC molecule .
|
-
- HY-156816
-
|
|
Casein Kinase
DYRK
|
Cancer
|
|
ON 108600 is a inhibitor for CK2 (Casein Kinase2)/TNIK/DYRK1 , with the IC50s for DYRK1A/DYRKB, DYRK2, CK2α1/CK2α2, and TNIK of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM, respectively. ON 108600 has antitumor activity .
|
-
- HY-148838
-
|
|
c-Myc
|
Cancer
|
|
c-Myc inhibitor 8 (compound 56) is a c-Myc inhibitor. c-Myc inhibitor 8 effectively inhibits cell viability of a variety of cancer cells. c-Myc inhibitor 8 inhibits human prostate and lung cancer growth in mouse models. c-Myc inhibitor 8 can be used for cancer research .
|
-
- HY-F0002
-
|
Sodium NADP
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
NADP sodium salt is the sodium salt form of NADP (HY-113325). NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes .
|
-
- HY-116248
-
|
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity .
|
-
- HY-P10472
-
|
|
GnRH Receptor
|
Endocrinology
|
|
Azaline B is an antagonist for gonadotropin-releasing hormone (GnRH) with IC50 of 1.37 nM, Azaline B can be used in research of sex hormone-related pathological states, ovulation induction and male contraception .
|
-
- HY-152189
-
|
|
Others
|
Cancer
|
|
S19-1035 is a highly potent and specific aldo-keto reductase 1C3 (AKR1C3) inhibitor. S19-1035 inhibits AKR1C3 with an IC50 value of 3.04 nM. S19-1035 can be used for the research of tumor .
|
-
- HY-101089
-
RHPS4
2 Publications Verification
|
Telomerase
Apoptosis
|
Cancer
|
|
RHPS4 is a potent telomerase inhibitor (IC50 = 0.33 μM). RHPS4 is a DNA damage inducer .
|
-
- HY-113325A
-
|
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
NADP sodium hydrate is the sodium salt hydrate form of NADP (HY-113325). NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes .
|
-
- HY-110201
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors .
|
-
- HY-N0104R
-
|
|
Apoptosis
|
Cancer
|
|
Curcumol (Standard) is the analytical standard of Curcumol. This product is intended for research and analytical applications. Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers .
|
-
- HY-W276106
-
|
|
Others
|
Cancer
|
|
KM02894 is an inhibitor of glutamate release. Cancer cells release high levels of glutamate, which disrupts normal bone turnover and may lead to cancer-induced bone pain. KM02894 can be used for cancer related research .
|
-
- HY-163119
-
|
|
Pim
|
Cancer
|
|
Pim-1 kinase inhibitor 9 (compound 8b) is a selective inhibitor against Pim-1 kinase with IC50 value of 0.24 µM. Pim-1 kinase inhibitor 9 inhibits cell cycle of T47D at S phase. Pim-1 kinase inhibitor 9 reveals antitumor activity .
|
-
- HY-N2058
-
|
|
Bacterial
Apoptosis
|
Infection
Cancer
|
|
Neogambogic acid, an active ingredient in garcinia, induces apoptosis and has anticancer effect. Neogambogic acid has significant inhibitory activity toward methicillin-resistant Staphylococcus aureus (MRSA) .
|
-
- HY-18285
-
|
|
Wnt
Casein Kinase
ERK
CDK
|
Cancer
|
|
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of 5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively .
|
-
- HY-103439
-
|
|
EGFR
|
Cancer
|
|
GW 583340 dihydrochloride is a potent dual EGFR/ErbB2 tyrosine kinase inhibitor (IC50: 0.01 and 0.014 μM respectively). GW 583340 dihydrochloride reverses ABCG2- and ABCB1-mediated drug resistance. GW 583340 dihydrochloride has anti-cancer activity .
|
-
- HY-16023
-
|
EM-652 hydrochloride; SCH 57068 hydrochloride
|
Estrogen Receptor/ERR
|
Cancer
|
|
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties .
|
-
- HY-F0002A
-
|
Disodium NADP
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
NADP disodium salt is the disodium salt form of NADP (HY-113325). NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes .
|
-
- HY-N0104
-
|
(-)-Curcumol
|
Apoptosis
|
Cancer
|
|
Curcumol ((-)-Curcumol), a bioactive sesquiterpenoid, possesses numerous pharmacological activities like anticancer, antimicrobial, antifungal, antiviral, and antiinflammatory. Curcumol is a potent inducer of apoptosis in numerous cancer cells via targeting key signaling pathways as MAPK/ERK, PI3K/Akt and NF-κB which are generally deregulated in several cancers .
|
-
- HY-163721
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-29 (compound 20) is an inhibitor of CDK7 with an IC50 value of 1.4 nM. CDK7-IN-29 has oral activity and good pharmacokinetic (PK) properties .
|
-
- HY-113325
-
|
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
NADP is a coenzyme involved in cellular electron transfer reactions in biological metabolism, which is alternately oxidized (NADP+) and reduced (NADPH), and can maintain cellular redox homeostasis and regulate many biological events, including cellular metabolism. NADPH is a universal electron donor that provides reducing ability for synthetic metabolic reactions and redox balance. NADPH plays a multifunctional role in regulating inflammation, redox homeostasis, and synthetic metabolism processes .
|
-
- HY-139066
-
|
Trichosanic acid
|
TNF Receptor
GLUT
Proteasome
Tau Protein
PKC
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways .
|
-
- HY-W087187
-
|
|
Radionuclide-Drug Conjugates (RDCs)
EGFR
|
Cancer
|
|
DOTAGA-anhydride is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide drug conjugates (RDCs). DOTAGA-anhydride can be used to label monoclonal antibodies (mAbs) such as trastuzumab (targeting HER2/neu receptor with an affinity of 5.5 nM) under mild conditions (PBS pH 7.4, 25 °C, 30 minutes) after chelation with indium-111. [111In-DOTAGA]-trastuzumab showed a tumor uptake of 65% ID/g in mice bearing breast cancer BT-474 xenografts 72 hours after injection, which is valuable for SPECT/CT imaging and biodistribution studies.
|
-
- HY-164388
-
Z-VAD
4 Publications Verification
|
Caspase
Apoptosis
Autophagy
Necroptosis
|
Cardiovascular Disease
Cancer
|
|
Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation .
|
-
- HY-16950A
-
|
Afimoxifene; 4-OHT
|
Estrogen Receptor/ERR
Adhesion G Protein-coupled Receptors (AGPCRs)
Drug Metabolite
|
Metabolic Disease
Cancer
|
|
(E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity .
|
-
- HY-40136
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
cis-4-Hydroxy-L-proline is an orally active proline analog and collagen production inhibitor. cis-4-Hydroxy-L-proline inhibits cell growth by preventing the deposition of triple helical collagen on the cell layer. cis-4-Hydroxy-L-proline inhibits N-nitrosomethylurea-induced breast tumor growth. cis-4-Hydroxy-L-proline improves lung compliance and reduces prostate weight. cis-4-Hydroxy-L-proline can be used in the study of hypoxic pulmonary hypertension .
|
-
- HY-155763
-
|
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
|
hCA/VEGFR-2-IN-4 (compound 15b) is an indolinylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-4 inhibits VEGFR-2 (IC50=0.811 μM) and has high binding activity to hCAs, with Ki of 3.8 nM (hCA XII), 6.2 nM (hCA IX), 19.8 nM (hCA II), and 35.5 nM (hCA I), respectively. hCA/VEGFR-2-IN-4 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
|
-
- HY-155758
-
|
|
VEGFR
Carbonic Anhydrase
|
Cancer
|
|
hCA/VEGFR-2-IN-2 (compound 8g) is an indolinonylbenzenesulfonamide and a potential dual inhibitor of cancer-associated hCA IX/XII and VEGFR-2. hCA/VEGFR-2-IN-2 inhibits VEGFR-2 (IC50=204 nM) and has high binding activity to hCAs, with Kis of 3.6 nM (hCA IX), 16.1 nM (hCA II), 16.7 nM (hCA XII), and 75.3 nM (hCA I), respectively. hCA/VEGFR-2-IN-2 has antiproliferative activity on VEGFR-2-overexpressing breast cancer cells .
|
-
- HY-156123
-
|
|
Dihydrofolate reductase (DHFR)
Bacterial
|
Infection
Cancer
|
|
DHFR-IN-9 (compound 8A) is a dihydrofolate reductase (DHFR) inhibitor that affects purine and thymidylate biosynthesis in cell proliferation and growth. DHFR-IN-9 inhibits methicillin-resistant Staphylococcus aureus (MRSA) ATCC 43300 (IC50=0.25 μg/mL) and has anti-infective effects in mouse models of systemic infection and thigh infection caused by it (dose: 2.5 mg /kg, 5 mg/kg; ip). DHFR-IN-9 has stronger anticancer activity than paclitaxel (Y-B0015) in a mouse model of breast cancer (dose: 2.5 mg/kg; ip; once every 3 days) .
|
-
- HY-164979
-
|
|
Kinesin
|
Cancer
|
|
KIF18A-IN-15 (Compound Example 36) is a KIF18A inhibitor, available in two forms, EX36-A and its enantiomer EX36-B, with IC50s of 0.01-0.1 μM, respectively. EX36-A and EX36-B inhibit OVCAR-3 cells viability with IC50s of 0.01-0.1 μM and 0-0.01 μM, respectively. KIF18A-IN-15 can be used in tumor (e.g. colon, breast, lung) studies .
|
-
- HY-162460
-
|
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations .
|
-
- HY-103490
-
|
EDHS-206
|
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
|
-
- HY-121149B
-
|
(E/Z)-3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
(E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
|
-
- HY-138071
-
|
8αTGH
|
STAT
Pyroptosis
Apoptosis
Reactive Oxygen Species (ROS)
c-Myc
Bcl-2 Family
TrxR
|
Cancer
|
|
8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo .
|
-
- HY-158684
-
|
|
PROTACs
MDM-2/p53
|
Cancer
|
|
YX-02-030M is a PROTAC MDM2 degrader. YX-02-030M inhibits MDM2-p53 binding and VHL-HIF1α binding with IC50s of 63 nM and 1.35 μM respectively. YX-02-030M binds MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, and effectively kills p53 mutant or deleted Triple-negative breast cancers (TNBC) cells. (Blue: VHL ligand; Black: linker; Pink: MDM2 inhibitor) .
|
-
- HY-P10833
-
|
|
VEGFR
PI3K
Akt
mTOR
ERK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
C-VGB3 is a selective vascular endothelial growth factor receptor 2 (VEGFR2) antagonist, which inhibits VEGFR2-mediated PI3K/AKT/mTOR and PLCγ/ERK1/2 signaling pathways. C-VGB3 binds to the extracellular domain of VEGFR2, blocking ligand-receptor interaction and inducing apoptosis in endothelial and tumor cells through both intrinsic (involving Bcl2 family and caspases) and extrinsic (death receptor-mediated) pathways. C-VGB3 is promising for research of angiogenesis-related cancers, such as breast cancer .
|
-
- HY-121255
-
|
(R)-Cryptopleurine; NSC 19912
|
TMV
|
Cancer
|
|
(–)-Cryptopleurine is an alkaloid that has been found in Lauraceae and has diverse biological activities. It inhibits the growth of human A375 melanoma, A431 epidermoid carcinoma, A549 lung, MES-SA uterine sarcoma, and MCF-7 breast cancer cells (IC50=3 nM for all).2 (–)-Cryptopleurine inhibits hypoxia-induced gene expression in a hypoxia response element (HRE) reporter assay (IC50=8.7 nM).3 (–)-Cryptopleurine (500 μg/mL) prevents lesion formation in tobacco (N. tabacum) plants infected with tobacco mosaic virus (TMV). It also inhibits protein synthesis by yeast and mammalian ribosomes.
|
-
- HY-B0693A
-
|
|
Histamine Receptor
SARS-CoV
Bacterial
|
Infection
Metabolic Disease
Cancer
|
|
Ranitidine bismuth citrate is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine bismuth citrate antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine bismuth citrate has selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate also has anti-Helicobacter pylori infection. Ranitidine bismuth citrate inhibits breast tumor development and spread in mice .
|
-
- HY-141877
-
MS4322
1 Publications Verification
YS43-22
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-154919
-
|
|
YTHDF
FOXO
MMP
Pyroptosis
Interleukin Related
|
Endocrinology
Cancer
|
|
DC-Y13-27 is a DC-Y13 derivative and YTHDF2 inhibitor (KD: 37.9 μM). DC-Y13-27 inhibits YTHDF2, restores FOXO3 and TIMP1 protein levels, and reduces MMP1/3/7/9 expression. DC-Y13-27 induces Pyroptosis and increases IL-1β secretion. DC-Y13-27 reduces intervertebral disc degeneration and enhances the response to radiotherapy in colon cancer and melanoma. DC-Y13-27 has antitumor activity against breast cancer .
|
-
- HY-121605
-
|
|
Apoptosis
|
Cancer
|
|
RL71 is a curcuminoid anticancer agent that exhibits potent cytotoxicity against a variety of ER-negative breast cancer cells. RL71 (1 μM) induces cell cycle arrest in the G2/M phase and induces apoptosis in SKBr3 cells. RL7 also decreases HER2/neu phosphorylation and increases p27. RL71 also significantly reduced the phosphorylation of Akt and transiently increased the stress kinases JNK1/2 and p38 MAPK. Furthermore, RL71 exhibited anti-angiogenic potential in vitro, inhibiting the migration of HUVEC cells and the ability of these cells to form tubular networks .
|
-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-149486
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor 7 (compound 5) is an inhibitor of FGFR1 Tyrosine Kinase with IC50 value of 0.33 nM. FGFR1 inhibitor 7 shows broad-spectrum cytotoxicity agasinst human cancer cell lines, and inhibits MOLT3 cells with IC50 of 2.1 μM .
|
-
- HY-10619E
-
|
MK-4827 tosylate hydrate
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib (MK-4827) tosylate hydrate is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib tosylate hydrate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-168518
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-9 (compound 29) is a highly selective and efficient CDK9 degrader based on PROTAC technology. PROTAC CDK9 degrader-9 can be used in anti-cancer research .
|
-
- HY-169994
-
-
- HY-10619
-
|
MK-4827
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-10619A
-
|
MK-4827 hydrochloride
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib hydrochloride (MK-4827 hydrochloride) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib hydrochloride leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-163680
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
|
Cancer
|
|
ERα degrader 9 is a dual targeting ligand for estrogen receptor α (ERα) and aromatase (ARO). ERα degrader 9 can be utilized for synthesis of PROTAC ERα Degrader-9 (HY-163679) .
|
-
- HY-157298
-
|
|
Apoptosis
|
Cancer
|
|
anti-TNBC agent-4 (compound 7) exhibits highly inhibitory activity against different TNBC cells with IC50s from 0.37 μM to 1.52 μM. anti-TNBC agent-4 inhibits IKKβ mediated phosphorylation of IκB and p65. anti-TNBC agent-4 induces TNBC cells apoptosis .
|
-
- HY-W402682
-
|
|
Amino acid Transporter
|
Neurological Disease
Cancer
|
|
SXC2023 is an inhibitor for solute carrier family 7 member 11 (SLC7A11). SXC2023 exhibits antitumor efficacy, and ameliorates central nervous system disorder through downregulation of glutamate export .
|
-
- HY-111253
-
|
|
LPL Receptor
|
Neurological Disease
|
|
CYM-5478 is a potent and highly selective S1P2 agonist with an EC50 of 119 nM in a TGFα-shedding assay. CYM-5478 protects neural-derived cell lines against Cisplatin toxicity .
|
-
- HY-15244
-
|
BYL-719
|
PI3K
|
Cancer
|
|
Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity .
|
-
- HY-164619
-
|
|
CDK
SARS-CoV
|
Infection
Cancer
|
|
CDK9-IN-34 (Compound 1b) is an inhibitor for CDK9 with an IC50 of 0.25 μM. CDK9-IN-34 exhibits cytotoxicity to cancer cell HCT116, MCF7 and K652 with IC50 of 1.43, 3.01 and 50.27 μM, respectively. CDK9-IN-34 exhibits antiviral activity against coronavirus 229E with an IC50 of 145.92 μM .
|
-
- HY-13502B
-
|
Mitozantrone diacetate; NSC 301739 diacetate
|
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity . Mitoxantrone diacetate also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-172957
-
|
|
JAK
|
Cancer
|
|
JNN-5 is a potent and selective JAK2 inhibitor with an IC50 of 0.41 nM. JNN-5 shows strong antiproliferative activities in the TNBC cell lines (MDA-MB-468, MDA-MB-213, HCC70, MDA-MB-157) .
|
-
- HY-100789
-
|
|
Apoptosis
Polo-like Kinase (PLK)
Mitosis
|
Cancer
|
|
ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 μM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity .
|
-
- HY-P9985
-
|
RC48
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
|
Disitamab vedotin (RC48) is an antibody-drug conjugate (ADC) comprising a monoclonal antibody against human epidermal growth factor receptor 2 (HER2) conjugated via a cleavable linker to the cytotoxic agent Monomethyl auristatin E (MMAE). Disitamab vedotin enhances antitumor immunity .
|
-
- HY-P4073
-
|
GRN1005; Paclitaxel trevatide
|
Peptide-Drug Conjugates (PDCs)
LDLR
|
Cancer
|
|
ANG1005 (Paclitaxel trevatide) is a brain-penetrating peptide-drug conjugate. ANG1005, a taxane derivative, consists of three paclitaxel (HY-B0015) molecules covalently linked to Angiopep-2, designed to cross the blood-brain and blood-cerebrospinal barriers and to penetrate malignant cells via low density lipoprotein receptor-related protein (LRP1) transport system .
|
-
- HY-10358
-
|
MK-2206 (2HCl)
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy .
|
-
- HY-159798
-
|
|
PROTACs
p38 MAPK
|
Cancer
|
|
NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)) .
|
-
- HY-162034
-
|
|
FAK
|
Cancer
|
|
FAK-IN-17 is a focal adhesion kinase (FAK) inhibitor. FAK-IN-17 possesses anticancer activity against A549 and MDA-MB-231 cell lines with IC50 values of 130 nM and 94 nM .
|
-
- HY-N6611
-
|
|
IGF-1R
|
Infection
Inflammation/Immunology
Cancer
|
|
Chimaphilin is an IGF-1R inhibitor (IC50: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola .
|
-
- HY-110147A
-
|
|
Furin
|
Infection
|
|
SSM3 tetraTFA is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro .
|
-
- HY-163679
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
|
-
- HY-10619R
-
|
|
PARP
Apoptosis
|
Cancer
|
|
Niraparib (Standard) is the analytical standard of Niraparib. This product is intended for research and analytical applications. Niraparib (MK-4827) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively. Niraparib leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
|
-
- HY-15888
-
|
|
BMI1
Autophagy
|
Cancer
|
|
PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment .
|
-
- HY-15888A
-
|
|
BMI1
Autophagy
|
Cancer
|
|
PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment .
|
-
- HY-162239
-
|
|
Others
|
Cancer
|
|
Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
|
-
- HY-170620
-
|
|
PROTACs
PARP
|
Cancer
|
|
PROTAC PARP1 degrader-4 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PROTAC PARP1 degrader-4 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PROTAC PARP1 degrader-4 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)) .
|
-
- HY-148789
-
|
OP-1250
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
|
Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER +/HER2 + cancer .
|
-
- HY-147515
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-11 (Compound 30) is a potent, selective, covalent FGFR4 inhibitor with an IC50 of 2.1 nM. FGFR4-IN-11 significantly inhibits the FGF19/FGFR4 signaling pathway and shows antitumor activity .
|
-
- HY-172605
-
|
|
Steroid Sulfatase
|
Cancer
|
|
Steroid sulfatase-IN-9 (compound 54E) is a steroid sulfatase (STS) inhibitor with the inhibition rates of 87.03% at 10 μM. Steroid sulfatase-IN-9 shows no detectable toxic effects in zebrafish larvae model .
|
-
- HY-136270
-
|
VX-803; M4344; ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity .
|
-
- HY-N7678
-
|
|
Others
|
Cancer
|
|
Gypenoside LXXV, isolated from Gynostemma pentaphyllum, is one of the deglycosylated shapes of ginsenoside Rb1. Gypenoside LXXV significantly reduces cancer cell viability and displays an anti-cancer effect .
|
-
- HY-164349
-
|
|
STAT
|
Cancer
|
|
WZ-2-033 is a potent STAT3 inhibitor. WZ-2-033 inhibits MDA-MB-231, HCC70, and MDA-MB231-4175 cells proliferation, colony survival, migration, and invasion with IC50s of 0.7, 1.3, and 1.3 μM, respectively .
|
-
- HY-132842A
-
|
(S)-DZD9008
|
EGFR
Btk
|
Cancer
|
|
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK .
|
-
- HY-162037
-
|
|
CDK
FLT3
|
Cancer
|
|
CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation .
|
-
- HY-110147B
-
|
|
Furin
|
Infection
|
|
SSM3 tetraTFA hydrate is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA hydrate is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro .
|
-
- HY-P99969
-
|
|
EGFR
|
Cancer
|
|
Inetetamab is a monoclonal antibody binding to domain IV of HER2 receptor. Inetetamab alone or together with tyrosine kinase inhibitors has antitumor activities .
|
-
- HY-170842
-
|
|
Apoptosis
|
Cancer
|
|
TDK-HCPT is a small-molecule conjugate that links glutathione-sensitive thiamine disulfide to the chemotherapy drug 10-Hydroxycamptothecin (HY-N0095) via a thioketal bond. TDK-HCPT can target tumor cells and prolong the retention of chemotherapy agents within tumor cells. TDK-HCPT can inhibit tumor growth, induce apoptosis of tumor cells, and has anti-tumor activity .
|
-
- HY-14507
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
YK-4-279 blocks RNA Helicase A (RHA) binding with EWS-FLI1 (oncogenic protein). YK-4-279 induces apoptosis and shows anti-proliferation activities towards various cancer cells. YK-4-279 has a chiral center and it can be separated into two enantiomers. YK-4-279 can be used for the research of cancer .
|
-
- HY-170942
-
|
|
CDK
PARP
|
Cancer
|
|
CDK9/PARP-IN-1 (compound 37) is a CDK9/PARP inhibitor. CDK9/PARP-IN-1 inhibits CDK9 and PARP1 with IC50s of 118 and 107 nM, respectively. CDK9/PARP-IN-1 exhibits broad-spectrum antiproliferative effects across multiple cancer cell lines .
|
-
- HY-161852
-
|
|
PI3K
Apoptosis
|
Cancer
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PI3K-IN-55 (Compound 6a) is a potent inhibitor for PI3K. PI3K-IN-55 affects PI3K/Akt/p53 signaling pathway, inhibits the proliferation of cancer cells A549, Hela, HepG2, MCF-7 and HT-29, with IC50s of 1.03-6.78 μM. PI3K-IN-55 induces apoptosis in cell MCF-7 .
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- HY-110002
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LFM-A13
1 Publications Verification
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Polo-like Kinase (PLK)
Btk
JAK
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Cancer
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LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research
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- HY-124611
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HSP
Apoptosis
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Cancer
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JG-231 is an allosteric inhibitor of heat shock protein 70 (Hsp70). JG - 231 inhibits the binding of Hsp70 and BAG family proteins, including inhibition of Hsp70 and BAG1 with a Ki of 0.11 μM. JG-231 inhibits proliferation of tumor cells and induces apoptosis. JG-231 has antitumor activity .
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- HY-155686
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Microtubule/Tubulin
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Cancer
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Tubulinpolymer-in-44 (compound 7w) is a strong and effective Tubulin inhibitor, with an IC50 value of 0.21 μM. Tubulinpolymer-in-44 induces apoptosis by arresting G2/M phase, which can be used for cancer research.
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- HY-10619B
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MK-4827 tosylate
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PARP
Apoptosis
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Cancer
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Niraparib tosylate (MK-4827 tosylate) is a highly potent and orally bioavailable PARP1 and PARP2 inhibitor with an IC50 of 3.8 and 2.1 nM, respectively. Niraparib tosylate leads to inhibition of repair of DNA damage, activates apoptosis and shows anti-tumor activity .
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- HY-13757AS1
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ICI 47699-d3; (Z)-Tamoxifen-d3; trans-Tamoxifen-d3
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Isotope-Labeled Compounds
Estrogen Receptor/ERR
Apoptosis
Autophagy
HSP
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Cancer
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Tamoxifen-d3 is the deuterium labeled Tamoxifen . Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells . Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively . Tamoxifen activates autophagy and induces apoptosis . Tamoxifen also can induce gene knockout of CreER(T2) transgenic mouse .
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- HY-172551
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Apoptosis
Cadherin
MMP
Bcl-2 Family
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Cancer
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anti-TNBC agent-9 (Compound 3as) is an anti-cancer agent for triple-negative breast cancer (TNBC). anti-TNBC agent-9 exhibits significant inhibitory activity against MDA-MB-453 cells with an IC50 value of 8.5 μM. anti-TNBC agent-9 inhibits tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. anti-TNBC agent-9 induces apoptosis by increasing the expression of the pro-apoptotic protein BAX and decreasing the expression of the anti-apoptotic protein BCL-2, thereby inhibiting tumor cell proliferation .
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- HY-N0726R
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![4-(Benzo[d]oxazol-2-yl)aniline](http://file.medchemexpress.com/product_pic/hy-w029411.gif)
