Search Result
Results for "
MDA-MB-468、NCI-H1975、HT1080
" in MedChemExpress (MCE) Product Catalog:
8
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
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- HY-100579
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Ferrostatin-1
Maximum Cited Publications
1548 Publications Verification
Fer-1
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Ferroptosis
Fungal
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Cancer
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Ferrostatin-1 (Fer-1), a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1, a synthetic antioxidant, acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibits cell death. Ferrostatin-1 exhibits antifungal activity .
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- HY-B1645
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Ammonium ferric citrate; FAC
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Environmental Pollutants
Ferroptosis
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Cancer
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Ammonium iron(III) citrate (Ammonium ferric citrate), a physiological form of nonetransferrin-bound iron, induces intracellular iron overload to cause ferroptosis . Ammonium iron(III) citrate can enhance protein production .
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- HY-11038
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PU-H71
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HSP
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Cancer
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Zelavespib (PU-H71) is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
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- HY-79256
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Monomethyl auristatin F methyl ester
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ADC Payload
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Cancer
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MMAF-Ome, an antitubulin agent, is also an ADC cytotoxin. MMAF-Ome inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4 -) cell lines, respectively.
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- HY-50908
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MK-8669; Deforolimus; AP23573
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mTOR
Autophagy
Bacterial
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Cancer
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Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells .
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- HY-147098
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dTAG-47
1 Publications Verification
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PROTACs
FKBP
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Cancer
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dTAG-47 is a FKBP12F36V PROTAC degrader. dTAG-47 efficiently degrades FKBP12F36V-MELK(sg3R) in MELK ⁻/⁻ MDA-MB-468-FKBP12F36V-MELK(sg3R) cells. dTAG-47 can be used for the research of basal-like breast cancers (BBC). (Pink: FKBP12F36V ligand (HY-114420), Blue: CRBN Ligand (HY-W087383), Black: Linker (HY-42773), E3 ligase ligand-linker conjugate (HY-175952)) .
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- HY-147858
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PROTACs
EGFR
Apoptosis
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Cancer
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-145669
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Wnt
CDK
GSK-3
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Infection
Cancer
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DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo .
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- HY-153698
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Molecular Glues
Ligands for E3 Ligase
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Cancer
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CC-3060 is a molecular glue modulator targeting Cereblon (CRBN) E3 ubiquitin ligase and ZBTB16 degrader with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 engages structural degrons on ZBTB16’s ZnF1 or ZnF3 domains for fusion protein substrates. CC-3060 can be used for the research of acute promyelocytic leukemia .
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- HY-112338
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CPD188
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STAT
Apoptosis
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Cancer
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C188 (CPD188) is a STAT3 inhibitor with anticancer effects. C188 inhibits STAT3 SH2/pY-peptide binding (IC50 of 20 µM against pY-peptide binding) and IL-6-mediated STAT3 phosphorylation. C188 is selective for STAT3 over STAT1. C188 inhibits nuclear-to-cytoplasmic translocation of Stat3. C188 shows highly active induces apoptosis in breast cancer cell lines with constitutive Stat3 activation (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively) .
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- HY-149236
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- HY-161456
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Phosphoglycerate Dehydrogenase (PHGDH)
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Cancer
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PHGDH-IN-5 (Compound B12) is a covalen inhibitor of PHGDH with an IC50 value of 0.29 μM. PHGDH-IN-5 can inhibit cell proliferation in cancer cell lines overexpressing PHGDH. PHGDH-IN-5 can reduce the production of serine derived from glucose in MDA-MB-468 cells .
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- HY-N9596
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Bacterial
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Infection
Cancer
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Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM .
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- HY-133887
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Antifolate
DNA/RNA Synthesis
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Cancer
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Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent .
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- HY-111844
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PROTACs
SNIPERs
RAR/RXR
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Neurological Disease
Metabolic Disease
Cancer
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PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)) .
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- HY-11038B
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PU-H71 hydrochloride
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HSP
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Cancer
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Zelavespib (PU-H71) hydrochloride is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
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- HY-155787
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CDK
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Cancer
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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) .
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- HY-N8187
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Apoptosis
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Cancer
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Eupalinolide O is a sesquiterpene lactone with anticancer activities. Eupalinolide O induces cell apoptosis in human MDA-MB-468 breast cancer cells .
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- HY-11038D
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PU-H71 formic
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HSP
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Cancer
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Zelavespib formic (PU-H71 formic) is a potent Hsp90 inhibitor with an IC50 value of 51 nM for Hsp90 in MDA-MB-468 cells .
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- HY-175649
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Large Tumor Suppressor (LATS)
YAP
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Cancer
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LATS1/2-IN-1 is a potent and selective LATS1 and LATS2 inhibitor. LATS1/2-IN-1 exhibits potent inhibitory activity against LATS1 and LATS2 with IC50 values of 4.4 nM and 5.5 nM as determined via r 33P functional assay. LATS1/2-IN-1 displays cellular IC50 values of 136 nM for LATS1 and 36.0 nM for LATS2 as determined via NanoBRET assay. LATS1/2-IN-1 reduces phosphorylation of YAP1 in mouse liver. LATS1/2-IN-1 demonstrates wound healing activity in HT-1080 scratch assay and in vivo SKH1 mouse punch biopsy model. LATS1/2-IN-1 can be used for the study of regenerative medicine indications such as wound healing .
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- HY-176772
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- HY-176869
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Drug Derivative
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Cancer
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EMC-AANL-DOX is a legumain-activated prodrug conjugate of Doxorubicin (DOX) (HY-15142A). EMC-AANL-DOX shows antitumor activity in mouse models of neuroblastoma (NB), breast cancer (4T1), fibrosarcoma (HT1080), and colorectal cancer liver metastases (CT26). EMC-AANL-DOX can be used for cancer research .
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- HY-164384
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PI3K
Akt
mTOR
Apoptosis
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Cancer
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DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
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- HY-158170
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CDK
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Cancer
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CDK7-IN-28 (CDK7-1276) is a potent CDK7 inhibitor(IC50<5 nM). CDK7-IN-28 can inhibit proliferation of MDA-MB-468 cell line by blocking cell cycle and inhibiting DNA replication .
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- HY-115605
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EGFR
p38 MAPK
ERK
Phosphatase
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Cancer
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CN009543V is an epidermal growth factor receptor (EGFR) agonist. CN009543V enhances tyrosine phosphorylation of EGFR at Tyr1068 and Tyr1173, thereby activating the MAPK/ERK cascade. CN009543V inhibits the activity of PTP-1B in MDA MB468 cells. CN009543V can be used in cancer research .
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- HY-173002
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DNA Methyltransferase
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Cancer
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MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM .
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- HY-116505
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JAK
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Cancer
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JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM) .
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- HY-143293
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VEGFR
Apoptosis
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Cancer
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VEGFR-IN-3 (compound 3f) is a VEGFR inhibitor. VEGFR-IN-3 inhibits OVCAR-4 and MDA-MB-468 cancer cells growth with IC50s of 0.29 and 0.35 μM, respectively. VEGFR-IN-3 can be used for the research of cancer .
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- HY-169133
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PROTACs
Glutathione Peroxidase
Ferroptosis
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Cancer
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GDCNF-11 is a HIM-PROTAC GPX4 degrader based on the chaperone protein HSP90. GDCNF-11 promotes the ubiquitination and degradation of GPX4 through the HSP 90 chaperone complex, reduces endogenous GPX4 expression to induce ferroptosis in HT-1080 cells, and the DC50 value is 0.08 μM (Pink: Target protein ligand (HY-153748); Blue: HSP90 ligand (HY-10212); Black: Linker (HY-W169526)) .
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- HY-145860
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Phosphoglycerate Dehydrogenase (PHGDH)
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Cancer
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PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells .
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- HY-176549
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RAD51
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Cancer
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(Rac)-IBR120 is the racemate of IBR120 (HY-176549A). IBR120 is a RAD51 inhibitor that has significant growth inhibition activity against MDA-MB-468 cells. (Rac)-IBR120 can be used for the research of difficult-to-treat cancers like triple negative breast cancer .
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- HY-N10158
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Drug Derivative
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Cancer
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1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one (compound 39), a diarylheptanoid, exhibits antiproliferative activity towards human HT-1080 fibrosarcoma and murine colon 26-L5 carcinoma cells .
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- HY-172957
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JAK
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Cancer
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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) .
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- HY-159990
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Glutathione Peroxidase
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Cancer
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GPX4-IN-15 (Compound C1) is an inhibitor for GPX4, that inhibits 19.8% GPX4 at 1 μM. GPX4-IN-15 inhibits the proliferation of cancer cell MDA-MB-468, BT-549 and MDA-MB-231 with IC50 of 0.86, 0.96 and 0.48 μM .
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- HY-174828
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PARP
ATM/ATR
Apoptosis
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Cancer
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ATR/PARP1-IN-1 is a potent ATR and PARP1 dual inhibitor with IC50s of 17.3 nM and 0.38 nM, respectively. ATR/PARP1-IN-1 effectively reduces cell viability, induces apoptosis and DNA damage. ATR/PARP1-IN-1 significantly impairs triple-negative breast cancer (TNBC) colony formation, migration, and invasion. ATR/PARP1-IN-1 suppresses tumor growth effectively in MDA-MB-468 xenografted mice, with no significant body weight change .
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- HY-171958
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PROTACs
EGFR
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Cancer
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PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFR L858R-T790M (NCI-H1975 cells), EGFR L858R (NCI-H3255 cells), and EGFR L858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM .
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- HY-101447
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EPH 116
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Src
Apoptosis
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Cancer
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SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg) .
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- HY-178242
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PROTACs
EGFR
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Cancer
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PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand (HY-178313); Blue: CRBN ligand (HY-W1128702); Black: Linker; EGFR ligand + Linker (HY-178311)) .
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- HY-10062
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EBP-921
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Akt
Farnesyl Transferase
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Cancer
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AZD3409 is a prenyl inhibitor that exhibits inhibitory activity against both farnesyl transferase and geranylgeranyl transferase I. AZD3409 inhibits the growth of breast cancer cells, with IC50s of 220 nM (MDA-MB-468), 180 nM (MDA-MB-361), and 290 nM (SK-Br-3). AZD3409 significantly reduces the activation level of AKT in breast cancer cell lines. AZD3409 induces G0/G1 phase arrest in MDA-MB-468 cells, causes G2/M phase arrest in MDA-MB-361 cells. AZD3409 can be used for the study of breast cancer .
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- HY-173029
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Ferroptosis
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Cancer
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UAMC-4821 is an inhibitor for ferroptosis with an IC50 of 5.2 nM. UAMC-4821 scavenges free radicals, blocks the lipid peroxidation, inhibits ML162 (HY-100002)-induced ferroptosis, and exhibits protective effect in HT-1080 cell. UAMC-4821 exhibits good pharmacokinetics characteristics in mouse with an oral bioavailability of 63%. UAMC-4821 can cross blood-brain barrier .
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- HY-114459
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Isocitrate Dehydrogenase (IDH)
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Cancer
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Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells .
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- HY-178370
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Ferroptosis
Reactive Oxygen Species (ROS)
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Cancer
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Ferroptosis inducer-12 is a potent and selective ferroptosis inducer. Ferroptosis inducer-12 exhibits potent antiproliferative activity against HT1080 and OS-RC-2, with IC50 values of 3 nM and 5 nM, respectively. Ferroptosis inducer-12 strongly inhibits GPX4 enzymatic activity, induces intracellular ROS and elevates intracellular Fe 2+ levels in OS-RC-2 cells. Ferroptosis inducer-12 significantly inhibits tumor growth in BALB/c nude mice bearing OS-RC-2 xenografts. Ferroptosis inducer-12 can be used for the study of cancer .
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- HY-P10760
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Peptide-Drug Conjugates (PDCs)
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Cancer
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PhAc-ALGP-Dox, a peptide-drug conjugate, is a novel anticancer prodrug, with IC50 values ranged from 311 nM to 34.25 μM for TNBC (E0771), normal murine epithelium (HC-11), human TNBC (MDA-MB-231 and MDA-MB-468), human CrC (LS 174T), normal human epithelium (HME-1) cells .
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- HY-160899A
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Drug-Linker Conjugates for ADC
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Cancer
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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 .
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- HY-170995
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PROTACs
ROR
Apoptosis
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Cancer
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PROTAC ROR1 degrader-1 is a ROR1 PROTAC degrader with DC50 values of 40.88 nM (NCI-H23), 69.0 nM (NCI-H460), 83.35 nM (NCI-H1299) and 42.07 nM (NCI-H1975), respectively. PROTAC ROR1 degrader-1 inhibits the proliferation of lung cancer cells and induces apoptosis. PROTAC ROR1 degrader-1 can be used in research related to non-small cell lung cancer .
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- HY-175041
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Glutathione Peroxidase
Reactive Oxygen Species (ROS)
Cannabinoid Receptor
Ferroptosis
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Cancer
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GPX4-IN-18 (Compound 17) is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4). GPX4-IN-18 is also an inducer of ferroptosis. GPX4-IN-18 can increase the production of ROS and malondialdehyde (MDA) levels in OS-RC-2 clear cell renal cell carcinoma cells. GPX4-IN-18 induces ferroptosis in HT-1080 cells with IC50s of 0.007 μM (absence of ferrostatin-1) and 1.486 μM (presence of ferrostatin-1). GPX4-IN-18 reduces in vivo tumor volume and intratumoral GPX4 levels in OS-RC-2 xenograft murine model .
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- HY-160598
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ADC Payload
Topoisomerase
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Cancer
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Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol (compound 45) is a camptothecin compound that can inhibit cell proliferation, with an IC50 of 2.92 ng/mL for MDA‑MB‑468 cells. Exatecan-amide-bicyclo[1.1.1]pentan-1-ylmethanol can be used for the research of cancer .
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- HY-156879
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Drug Derivative
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Cancer
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Antiproliferative agent-40 (Compound 9) inhibits proliferation of HT1080 and MCF-7 with IC50s of 52 and 8.2 μM respectively .
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- HY-175213
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Isocitrate Dehydrogenase (IDH)
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Cancer
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Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells .
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- HY-149359
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Isocitrate Dehydrogenase (IDH)
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Cancer
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IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
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- HY-161930
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PROTACs
Ferroptosis
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Cancer
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PROTAC GPX4 degrader-3 is a potent PROTAC GPX4 degrader with a DC50 (24h) of 0.019 μM and an IC50 of 0.024 μM in HT1080 cell .
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- HY-162718
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Ferroptosis
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Cancer
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GPX4-IN-12 (compound I22) is a non-covalent GPX4 inhibitor. GPX4-IN-12 induces ferroptosis and inhibits cell growth of HT1080 cells .
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- HY-162716
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Ferroptosis
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Cancer
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GPX4-IN-10 (compound I20) is a non-covalent GPX4 inhibitor. GPX4-IN-10 induces ferroptosis and inhibits cell growth of HT1080 cells .
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- HY-159771
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FAP
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Cancer
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FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a Kd of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.
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- HY-164392
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EGFR
Apoptosis
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Cancer
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TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .
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- HY-156878
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Others
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Cancer
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Antiproliferative agent-39 (Compound 12) inhibits proliferation of A549, SNU-638, Col2, HT1080, MCF-7 with IC50s of 11, 25, 14, 11, 6.3 μM respectively .
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- HY-121085
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Microtubule/Tubulin
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Cancer
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CID-663143 targets microtubule-associated proteins, not tubulin itself, to inhibit the polymerization process within cells. CID-663143 inhibits cancer cell growth (IC50: <100 nM for HT-1080, BJeLR, MCF10A cells) .
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- HY-159567
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Ferroptosis
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Cardiovascular Disease
Neurological Disease
|
|
Ferroptosis-IN-11 (compound 43) is a ferroptosis inhibitor. Ferroptosis-IN-11 can inhibit Erastin (HY-15763) induced ferroptosis in HT-1080 human fibroblasts (EC50=36 nM). Ferroptosis-IN-11 can be used in the study of cardiovascular disease and neurodegeneration .
|
-
- HY-159576
-
|
O-Me B1939; O-Me E7389; O-Me ER-086526
|
ADC Payload
|
Cancer
|
O-Me Eribulin is a derivative of Eribulin and is an ADC cytotoxin that can be used for ADC synthesis. O-Me Eribulin can inhibit the cell viability of SKBR3, MDA-MB-468, and A549 cells, with IC50 values of 0.2052, 0.1827, and 0.5151 nM, respectively. O-Me Eribulin can be used for tumor research .
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-
- HY-N15614
-
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Others
|
Cancer
|
|
Cassamine is a diterpenoid compound that can be isolated from the bark of Erythrophleum fordii. Cassamine exhibits certain cytotoxicity against non-small cell lung cancer cell lines, with IC50 values of 3.4, 2.1, and 1.9 μM against A549, NCI-H1975, and NCI-H1299, respectively. Cassamine has antitumor activity and can be used in the research of lung cancer and other tumors .
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-
- HY-139248
-
|
|
Drug Derivative
|
Cancer
|
|
Paclitaxel octadecanedioate (compound PTX-FA18) is comprised of Paclitaxel (HY-B0015) conjugated to 1,18-octadecanedioic acid (HY-W005178). Paclitaxel octadecanedioate mixed with human serum albumin (HAS) is cytotoxic to HT-1080, PANC-1, HT-29 and Hela cells (IC50s = 12, 2.48, 8.62, and 64.42 nM, respectively) .
|
-
- HY-146132
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFR WT and EGFR L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .
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-
- HY-161948
-
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|
Ferroptosis
|
Cancer
|
|
Ferroptosis inducer-4 (Compound 5) is a ferroptosis (Ferroptosis) inducer with a structure featuring terminal double bonds introduced at the sn-2 position of phospholipids. Ferroptosis inducer-4 exhibits significant cytotoxicity towards HT-1080 cells, with an IC50 of 18 μM. This cytotoxic mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane triggered by the terminal double bonds. Ferroptosis inducer-4 can be used for research on ferroptosis regulation .
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-
- HY-168093
-
|
|
Ferroptosis
|
Cancer
|
|
Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
|
-
- HY-170959
-
|
|
Ferroptosis
|
Neurological Disease
Metabolic Disease
|
|
NYY-6a is a Ferroptosis inhibitor. NYY-6a shows significant inhibitory activity against RSL3-induced ferroptosis across 786-O and HT-1080 cells with EC50s of 52 and 50 nM, respectively. NYY-6a functions as a radical trapping antioxidant (RTA) with efficacy of diminishing lipid peroxidation comparable to ferrostatin-1 and liproxtatin-1. NYY-6a is potential for ferroptosis related pathologies reasearch .
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-
- HY-173038
-
|
|
EGFR
ERK
STAT
Apoptosis
|
Cancer
|
|
EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. EGFR-IN-151 inhibits the proliferation of a variety lung cancer cells (IC50s for NCI-H1781, HCC827, NCI-H3255 and NCI-H1975 is 11.7, 5.19, 7.32 and 1.53 μM, respectively), inhibits the colony formation and migration of H1975, arrests the cell cycle at G1 phase, and induces apoptosis in H1975 .
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-
- 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-143234
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .
|
-
- HY-147858A
-
|
|
PROTACs
|
Cancer
|
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
|
-
- HY-147670
-
|
|
Hedgehog
Smo
Gli
Apoptosis
|
Cancer
|
|
TPB15 is an orally active and potent Hh (Hedgehog) signaling inhibitor. TPB15 markedly induces cell cycle arrest and apoptosis in MDA-MB-468 cells. TPB15 blocks Smo (Smoothened) translocation into the cilia and reduced Smo protein and mRNA expression. TPB15 inhibits the expression of the downstream regulatory factor glioma-associated oncogene 1 (Gli1). TPB15 shows good anti-tumor activity with low toxicity .
|
-
- 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-162751
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC50 of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC50 of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice .
|
-
- HY-152945
-
|
|
NF-κB
|
Cancer
|
|
Antiproliferative agent-22 (compound 2) is an anticancer agent. Antiproliferative agent-22 shoes anti-proliferative activities against MCF-7, MDA-MB-231 and MDA-MB-468 cells with IC50 values of 6.2 μM, 3.3 μM and 3.3 μM, respectively .
|
-
- HY-173330
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-89 is an inhibitor of HDAC1 (IC50: 0.95 nM), HDAC2 (IC50: 0.86 nM), HDAC3 (IC50: 1.06 nM) and HDAC8 (IC50: 4.24 nM). HDAC-IN-89 blocks the cell cycle and induces apoptosis. HDAC-IN-89 has anti-tumor activity .
|
-
- HY-169382
-
|
|
Melatonin Receptor
|
Cancer
|
|
Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.
|
-
- 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-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-N9596S
-
|
|
Isotope-Labeled Compounds
Bacterial
|
Cancer
|
|
Stigmasta-4,22-dien-3-one-d5 is the deuterium labeled Stigmasta-4,22-dien-3-one (HY-N9596). Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM .
|
-
- HY-175011
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFR L858R/T790M and EGFR WT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma .
|
-
- HY-173060
-
|
|
ERK
Apoptosis
Autophagy
|
Cancer
|
|
ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
|
-
- HY-N0998
-
|
|
Melanocortin Receptor
|
Cancer
|
|
1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 μM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders .
|
-
- HY-157319
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
|
-
- 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-101517A
-
|
|
PI3K
|
Cancer
|
|
(S)-PI3K-IN-2, an enantiomer of PI3K-IN-2 (HY-101517), is a ΡΙ3Κβ/δ inhibitor, with IC50s of 0.198 and 0.282 μΜ, respectively. (S)-PI3K-IN-2 can inhibit phospho AKT (ser473) in MDA-MB-468 cells (IC50=27 nM) .
|
-
- 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-179044
-
|
|
p38 MAPK
JNK
Caspase
Apoptosis
|
Cancer
|
|
MKK7-JNK activator 1 (Compound 10) is a MKK7-JNK pathway activator. MKK7-JNK activator 1 effectively inhibits the proliferation and migration of MDA-MB-468 cells, induces G2/M phase arrest and caspase -dependent apoptosis (independent of ROS production). MKK7-JNK activator 1 significantly increases the levels of p-MKK7 and p-JNK, but does not affect p-ERK or p-p38. MKK7-JNK activator 1 can be used for the study of triple-negative breast cancer (TNBC) .
|
-
- HY-157432
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
|
-
- HY-161972
-
|
|
HyT
Ferroptosis
Glutathione Peroxidase
|
Cancer
|
|
ZX782 is a HyT GPX4 degrader and a ferroptosis inducer, which induces GPX4 degradation and significantly increases lipid ROS accumulation in HT1080 cells. ZX782 can be used to treat AD by reducing the size and/or number of brain amyloid plaques and by inhibiting the spread of IL-1beta-positive microglial-like cells around amyloid plaques. ZX782 is labeled with hydrophobic benzyl alcohol (HBA) and appears bright blue under acidic conditions, which can be used for quantitative determination . ZX782 is composed of target protein ligand (red part) ML-210 (HY-100003), PROTAC linker (black part) Bromo-PEG2-CH2-Boc (HY-141371) and Hty molecule (blue part) Adamantan-1-ylmethanamine (HY-W037848). The conjugate consisting of Hyt and linker parts is Adamantan-C-amide-PEG2-C-Br (HY-161974), and the activity control of the target protein ligand is Hydroxyl-ML-210 (HY-161973).
|
-
- HY-120015
-
|
|
MMP
|
Cancer
|
|
BE-16627B is a metalloproteinase inhibitor. BE-16627B can be isolated from microbial cultures. BE-16627B can inhibit metalloproteinases in enzyme assays. BE-16627B reduces the number and size of HT1080 cell nodules on lung surface in mouse models. BE-16627B inhibits growth of HT1080 cells in mice. BE-16627B can be studied in anti-cancer research .
|
-
- HY-149670
-
|
|
Ferroptosis
|
Inflammation/Immunology
|
|
Ferroptosis-IN-3 (Compound 25) is a ferroptosis inhibitor. Ferroptosis-IN-3 inhibits RSL3-induced ferroptosis (EC50: 8.6?nM in HT-1080?cells). Ferroptosis-IN-3 scavenges DPPH and ABTS radicals (EC50: 3.94?and 6.3 μM respectively). Ferroptosis-IN-3 decreases lipid peroxidation .
|
-
- HY-100579R
-
|
Fer-1 (Standard)
|
Ferroptosis
Reference Standards
Fungal
|
Cancer
|
|
Ferrostatin-1 (Standard) is the analytical standard of Ferrostatin-1 (HY-100579). This product is intended for research and analytical applications. Ferrostatin-1 (Fer-1), a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1, a synthetic antioxidant, acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibits cell death. Ferrostatin-1 exhibits antifungal activity .
|
-
- HY-181598
-
|
|
HyT
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GPX4 degrader-1 (Compound RS-1) is a hydrophobic tagging (HyT)-mediated GPX4 degrader (DC50: 8.9 nM in HT1080 cells) GPX4 degrader-1 induces GPX4 degradation. GPX4 degrader-1 induces Ferroptosis. GPX4 degrader-1 increases lipid ROS. GPX4 degrader-1 demonstrates potent antitumor efficacy in a murine mammary carcinoma model .
|
-
- HY-115465
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Rev1-CT/RIR PPI-IN-1 (Compound 1) is a thiophene-based compound. Rev1-CT/RIR PPI-IN-1 can specifically disrupt the protein-protein interaction between Rev1-CT and RIR, with an IC50 value of 2.5 µM. Rev1-CT/RIR PPI-IN-1 can enhance chemosensitivity and reduce the mutation rate in Cisplatin (HY-17394)-sensitive HT-1080 cells. Rev1-CT/RIR PPI-IN-1 can be used for tumor research .
|
-
- HY-168236
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC50 of 3 nM in HiBiT A549 cells. (Pink: Ligand for target protein (HY-168237); Black: Linker (HY-168238); Blue: Ligand for E3 ligase (HY-W087383))
|
-
- HY-109113
-
|
GPX-150
|
Topoisomerase
|
Cancer
|
|
Camsirubicin (GPX-150) is a non-cardiotoxic Doxorubicin (HY-15142) analog that selectively targets topoisomerase IIβ. Camsirubicin reduces cell viability and clone formation of MDA-MB-468 breast cancer cells. Camsirubicin increases the exposure of CALR and HSP90 on the cell surface. Camsirubicin can be used for the study of breast cancer .
|
-
- HY-170349
-
-
- HY-181502
-
|
|
EGFR
ERK
PARP
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
|
EGFR-IN-197 is an EGFR inhibitor with IC50 values of 19.5 nM and 12.0 nM against EGFR L858R/T790M and EGFR L858R/T790M/C797S, respectively. EGFR-IN-197 arrests the cell cycle of NCI-H1975 cells at the G2/M phase, while inhibiting their proliferation, colony formation and migration; it also inhibits mitochondrial translocation and upregulates mitochondrial H2S levels. EGFR-IN-197 disrupts anti-apoptotic signaling pathways by regulating apoptosis-related proteins; it induces DNA damage and activates pro-apoptotic pathways to trigger apoptosis. EGFR-IN-197 can be used in studies related to non-small cell lung cancer (NSCLC) .
|
-
- HY-181035
-
|
|
PROTACs
CDK
|
Cancer
|
|
DN1679 is a potent, selective and orally active CRBN-dependent CDK12/13 PROTAC dual degrader. DN1679 shows DC50 of 8.8/9.8 nM (MDA-MB-231), 5.1/6.4 nM (MDA-MB-157) and 17.2/15.8 nM (MDA-MB-468) for CDK12/13. DN1679 can downregulate DNA damage response gene mRNA levels, such as ATM, ATR, BRCA1 and RAD51. DN1679 demonstrates a potent synergistic anti-tumor effect companied with Olaparib (HY-10162). DN1679 can be used for research of triple-negative breast cance .
|
-
- HY-180850
-
|
|
PROTACs
Estrogen Receptor/ERR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer .
|
-
- HY-170352
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
E3 Ligase Ligand-linker Conjugate 150 is the conjugate of the ligand for E3 ligase VHL and the linker, that can be used for synthesis of PROTAC SMARCA2 degrader-32 (HY-170343) .
|
-
- HY-170343
-
|
|
PROTACs
SWI/SNF Complex
|
Cancer
|
|
PROTAC SMARCA2 degrader-32 (Compound 27) is the degrader for SMARCA2 with a DC50 of 1.3 nM. PROTAC SMARCA2 degrader-32 inhibits the proliferation of lung cancer cell NCI-H838 with a GI50 of 34 nM . (Pink: ligand for target protein SMARCA2 ligand-11 (HY-170349); Black: linker (HY-W895794); Blue: ligand for E3 ligase VHL (HY-170348))
|
-
- HY-162449
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
GIC-20 is a dual inducer for apoptosis and ferroptosis. GIC-20 exhibits antitumor efficacy against fibrosarcoma .
|
-
- HY-162717
-
-
- 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-162413
-
|
|
Src
|
Cancer
|
|
(R)-LW-Srci-8 is a selective covalent inhibitor of c-Src (IC50= 35.83 nM) that disrupts the autophosphorylation of c-Src by targeting its autophosphorylation site (Y419) .
|
-
- HY-W749442
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
7a-Hydroxyfrullanolide has anticancer properties. 7a-Hydroxyfrullanolide reduces polymerization of α-, β-tubulin. 7a-Hydroxyfrullanolide preferrs to bind to β-tubulin over α-tubulin. 7a-Hydroxyfrullanolide also triggers DNA damage response arrests cells in the G2/M-phase. 7a-Hydroxyfrullanolide is an eudesmanolide sesquiterpene lactone (SL) and can be isolated from the flowering plants of the Asteraceae family .
|
-
- HY-161764
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-67 (compound 5k) is a potent α-Glucosidase inhibitor with IC50 values of 0.31, 4.51 µM for alpha-glucosidase and alpha-amylase, respectively. α-Glucosidase-IN-67 has the potential for the research of type-2 diabetes .
|
-
- HY-N2117
-
-
- HY-162106
-
|
|
Ferroptosis
PROTACs
Glutathione Peroxidase
|
Cancer
|
|
PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .
|
-
- HY-N2117R
-
|
|
Reference Standards
MMP
Akt
NF-κB
Proteasome
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy .
|
-
- HY-162131
-
-
- 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-151888
-
|
|
Others
|
Cancer
|
|
Anticancer agent 92 (Compound 5f) is an anticancer agent that is nontoxic against noncancerous cells .
|
-
- HY-131493
-
|
PRMT5-IN-3
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PF-06939999 (PRMT5-IN-3) is a SAM-competitive, orally active PRMT5 inhibitor that inhibits the expression of SDMA protein (IC50 in A427 is 1.1 nM). PF-06939999 exhibits antitumor effect .
|
-
- HY-147173
-
|
|
FAP
|
Cancer
|
|
FAPI-74 is a PET (positron emission tomography) tracer targeting the fibroblast activation protein (FAP). FAPI-74 can be used for FAP-positive tumor research .
|
-
- HY-155602
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-18 (compound 8q) is a potent inhibitor of CDK2/E and CDK4/D1, with IC50s of 8 nM and 46 nM, respectively. CDK2-IN-18 inhibits the proliferation of tumor cells .
|
-
- HY-149923
-
-
- HY-157788
-
|
|
PROTACs
Reactive Oxygen Species (ROS)
Ferroptosis
Glutathione Peroxidase
|
Cancer
|
|
ZX703 (compound 5I) is a PROTAC that significantly degrades GPX4 in a dose- and time-dependent manner through the ubiquitin-proteasome and autophagy-lysosome pathways (DC50=0.315 µM). ZX703 induces ferroptosis by inducing Reactive Oxygen Species (ROS) accumulation in cells. ZX703 can be used for cancer research .
|
-
- HY-168879
-
|
|
Glutathione Peroxidase
|
Cancer
|
|
GPX4-IN-16 ((R)-9i) is a potent GPX4 inhibitor with an Kd value of 20.4 nM. GPX4-IN-16 shows cytotoxicity. GPX4-IN-16 shows anticancer activity .
|
-
- HY-100914
-
|
Ophobolin A
|
Calmodulin
|
Cancer
|
|
A-7 hydrochloride (Ophobolin A) is a calmodulin antagonist and can be used for the research of cancer .
|
-
- HY-117192
-
|
|
HSP
Fungal
|
Infection
|
|
NSC145366 monohydrochloride is a Hsp90 C-terminal inhibitor. NSC145366 monohydrochloride directly interacts with the C-terminus of Hsp90 and inhibits its chaperone activity. NSC145366 monohydrochloride strongly inhibits the growth of Saccharomyces cerevisiae cog7Δ and cog8Δ strains .
|
-
- HY-149959
-
|
|
Mps1
|
Cancer
|
|
Mps1-IN-6 is a potent Mps1 inhibitor with an IC50 value of 2.596 nM. Mps1-IN-6 shows antiproliferative activity. Mps1-IN-6 shows antitumor activity .
|
-
- HY-151632
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-15 is a potent hCA IX inhibitor with a Ki value of 38.8 nM. hCAIX-IN-15 shows good broad-spectrum anticancer activity and can be used for cancer research .
|
-
- HY-N0364
-
|
|
Apoptosis
Autophagy
PPAR
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ and increases the expression of the cholesterol transporter ABCA1 in cells. Falcarindiol induces apoptosis and autophagy. Falcarindiol has anti-inflammatory, antifungal, anticancer and antidiabetic properties . Falcarindiol 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-147994
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-174384
-
|
|
c-Met/HGFR
Apoptosis
G-quadruplex
|
Cancer
|
|
MET Transcription-IN-1 (Compound C3) is an orally active MET transcription inhibitor. MET Transcription-IN-1 can efficiently bind and stabilize the G-quadruplex in the MET promoter region, thereby inhibiting c-Met expression. MET Transcription-IN-1 can also overcome drug resistance caused by specific c-Met mutations. MET Transcription-IN-1 is capable of inhibiting tumor cell proliferation, migration, and invasion, as well as inducing cell cycle arrest and apoptosis. MET Transcription-IN-1 has antitumor activity, and can be used in the research of tumors such as non-small cell lung cancer .
|
-
- HY-147992
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research .
|
-
- HY-119944
-
JND3229
1 Publications Verification
|
EGFR
|
Cancer
|
|
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .
|
-
- HY-137175
-
|
|
mTOR
|
Cancer
|
|
TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+ .
|
-
- HY-181447
-
|
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
GPX4 (S)-9i is a GPX4 inhibitor and ferroptosis inducer, with its (R) enantiomer exhibiting stronger activity. GPX4 (S)-9i can be used for the study of fibrosarcoma .
|
-
- HY-175770
-
|
|
Isocitrate Dehydrogenase (IDH)
PDK-1
Apoptosis
|
Cancer
|
|
mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma .
|
-
- HY-169350
-
|
|
Glutathione S-transferase
|
Cancer
|
|
EA-B2L is a potent degrader of glutathione S-transferase (GSTP), with the DC50 of 48 μM. EA-B2L is a kind of Boc2Lys-linked Ethacrynic acid (HY-B1640). EA-B2L plays an important role in cancer research .
|
-
- HY-123524
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-4 (compound B9) is a STAT3 inhibitor with Kd values for STAT3 (I634S/Q635G) and WT are 22.75 and 4.59 μM, respectively. STAT3-IN-4 can inhibit the proliferation of tumor cells .
|
-
- HY-174826
-
|
|
EGFR
c-Kit
|
Cancer
|
|
EGFR-IN-164 (Compound 4) is a selective and covalent allosteric EGFR inhibitor. EGFR-IN-164 significantly inhibits the activity of EGFR L858R/T790M/C797S kinase (IC50: 48.1 nM) and proliferation of of EGFR-mutant cells. EGFR-IN-164 can be used for drug resistance of cancer research .
|
-
- HY-173619
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-160 (Compound R12) is an EGFR inhibitor (IC50 values are 1.62, 0.49 and 0.98 μM for EGFR WT, EGFR T790M and EGFR L858R/T790M/C797S, respectively). EGFR-IN-160 induces G2/M and S phase arrest and apoptosis in NCI-H522 cells, and has anticancer activity. EGFR-IN-160 has antioxidant effects against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM) .
|
-
- HY-N2497R
-
|
|
Reference Standards
NF-κB
MMP
p38 MAPK
|
Cancer
|
|
Isoliquiritin apioside (Standard) is the analytical standard of Isoliquiritin apioside. This product is intended for research and analytical applications. Isoliquiritin apioside significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells .
|
-
- HY-B1465R
-
|
Palmityl alcohol (Standard)
|
Reference Standards
Endogenous Metabolite
|
Others
|
|
1-Hexadecanol (Standard) is the analytical standard of 1-Hexadecanol. This product is intended for research and analytical applications. 1-Hexadecanol is a fatty alcohol, a lipophilic substrate. 1-Hexadecanol can be used for the research of ferroptosis .
|
-
- HY-124922
-
|
|
NF-κB
MDM-2/p53
Apoptosis
|
Cancer
|
|
CBLC100 is an anticancer compound that targets FACT, while inhibiting NF-κB and activating p53. CBLC100 induces cytotoxicity through p53-dependent apoptotic and non-apoptotic pathways. CBLC100 is applicable to the research of cancers such as fibrosarcoma .
|
-
- HY-172896
-
|
|
Ferroptosis
|
Cancer
|
|
FSP1-IN-1 (compound 39) is a potent FSP1 inhibitor with an IC50 of 35 nM. FSP1-IN-1 enhances RSL3 (HY-100218A)-induced lipid peroxide accumulation and sensitizes cancer cells to ferroptosis .
|
-
- HY-B1465
-
-
- HY-N2497
-
|
|
NF-κB
MMP
p38 MAPK
|
Cancer
|
|
Isoliquiritin apioside significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells .
|
-
- HY-129800
-
|
|
ERK
|
Cancer
|
|
CGP78850 is a potent and selective competitor of Grb2 SH2-phosphopeptide interactions. CGP78850 can be used for the research of cancer .
|
-
- HY-168951
-
|
|
Annexin A
Apoptosis
|
Cancer
|
|
(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 .
|
-
- HY-P990859
-
|
|
Transmembrane Glycoprotein
|
Others
|
|
Anti-CD44 Antibody (Hermes-1) is a kind of rat IgG2a κ chimeric antibody, targeting to human CD44. Anti-CD44 Antibody (Hermes-1) blocks the binding of hyaluronan to CD44. Anti-CD44 Antibody (Hermes-1) restores (Platelet-derived Growth Factor-BB)-induced β-receptor activation and motility in fibroblasts. Anti-CD44 Antibody (Hermes-1) causes partial loss of the anti-aging effect of hyaluronic .
|
-
- HY-155339
-
|
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 168 (compound d16) is a inhibitor of DNA2. Anticancer agent 168 induces apoptosis and cell-cycle arrest mainly at S-phase, and exhibits anticancer activities and overcomes chemotherapy resistance in mutp53-bearing cancers .
|
-
- 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-148570
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC50 value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer .
|
-
- 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-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-153992
-
|
|
STAT
|
Inflammation/Immunology
|
|
STAT6-IN-3 is a phosphopeptide mimic targeting the SH2 domain of STAT6 and has a high affinity for STAT6 (IC50: 0.04 μM). STAT6-IN-3 can be used in the research of inflammation such as asthma .
|
-
- 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-125964
-
|
|
Survivin
|
Cancer
|
|
LLP-3 is a potent Survivin inhibitor that disrupts the Survivin-Ran interaction in cancer cells. LLP-3 can be used in the research of Glioblastoma multiforme (GBM) .
|
-
- HY-13016R
-
|
XL184 (Standard); BMS-907351 (Standard)
|
Reference Standards
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
|
-
- HY-122862
-
|
|
Ras
|
Cancer
|
|
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .
|
-
- HY-13016A
-
|
XL184 hydrochloride; BMS-907351 hydrochloride
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
|
-
- HY-176488
-
|
|
Porcupine
Wnt
β-catenin
c-Myc
|
Cancer
|
|
Y-99 is a PORCN inhibitor with an IC50 of 155.4 nM against the Wnt/β-catenin signaling pathway. Y-99 inhibits the expression of p-LRP6, β-catenin, and c-Myc .
|
-
- HY-101761A
-
|
|
PAI-1
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-13016
-
|
XL184; BMS-907351
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
|
-
- HY-N10229
-
|
|
Fungal
|
Infection
|
|
Harzianum A is a trichothecene compound. Harzianum A has no antibacterial activity against Gram-negative and Gram-positive bacteria, but has antifungal activity. In addition, Harzianum A is cytotoxic to tumor cells .
|
-
- HY-103692R
-
|
|
Reference Standards
STAT
|
Cancer
|
|
STX-0119 (Standard) is the analytical standard of STX-0119 (HY-103692). This product is intended for research and analytical applications. STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM .
|
-
- HY-103692
-
|
|
STAT
|
Cancer
|
|
STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM .
|
-
- 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-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-141478
-
|
|
ATM/ATR
|
Cancer
|
|
Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity .
|
-
- HY-146666
-
|
|
Apoptosis
STAT
|
Cancer
|
|
STAT3-IN-9 is a potent STAT3 inhibitor. STAT3-IN-9 inhibits the activation of STAT3 (Tyr705) without influencing the phosphorylation of STAT1 (Tyr701). STAT3-IN-9 induces apoptosis and cell cycle arrest at the G2/M phase .
|
-
- HY-132135
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity .
|
-
- 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-178211
-
|
|
Ras
MEK
ERK
Akt
|
Cancer
|
|
SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer .
|
-
- HY-147185
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT7-IN-1 (Compound 14) is a PRMT7 inhibitor with an IC50 of 2.1 μM. PRMT7-IN-1 shows anticancer activity against different cancer cells .
|
-
- HY-178194
-
|
|
Ras
MEK
ERK
Akt
|
Cancer
|
|
SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer .
|
-
- 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-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-B0581
-
|
ICRF-187; ADR-529; NSC-169780
|
Ferroptosis
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Dexrazoxane, as an intracellular iron chelating agent, reduces the formation of superoxide radicals and has cardioprotective, anti-inflammatory, antioxidant, anti-tumor and neuroprotective activities. Dexrazoxane inhibits ferroptosis of H9c2 cells by inhibiting HMGB1. Dexrazoxane induces DNA damage and apoptosis in human fibrosarcoma cells .
|
-
- HY-148595
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1A1-IN-2 (Compound 14) is a competitive inhibitor of CYP1A1 (Ki: 1.4 μM). CYP1A1-IN-2 exhibits potent antimitotic activity and arrests cell in the G2/M phase. CYP1A1-IN-2 disrupts the microtubule and the cytoskeleton in CYP1A1-expressing breast cancer cells .
|
-
- HY-139361
-
|
PIN1-3
|
PIN1
|
Cancer
|
|
Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors .
|
-
- HY-179231
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK2-IN-50 is a CDK2 inhibitor (IC50 = 0.77 nM). CDK2-IN-50 can induce G1 phase arrest, indicating that it has an effective CDK2/cyclin E targeting mechanism. CDK2-IN-50 also has a significant pro-apoptotic effect. CDK2-IN-50 can be used for the study of breast cancer .
|
-
- HY-113831
-
|
|
CDK
SRPK
|
Cancer
|
|
LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC50 values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs .
|
-
- HY-133120A
-
|
|
PROTACs
Akt
|
Cancer
|
|
INY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
|
-
- 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-P99041B
-
|
ABX-EGF (powder)
|
EGFR
|
Cancer
|
|
Panitumumab (ABX-EGF) (powder) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (powder) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (powder) can be used in the research of cancers, such as colon cancer .
|
-
- HY-P99041
-
|
ABX-EGF
|
EGFR
|
Cancer
|
|
Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer .
|
-
- HY-P992146
-
|
MYTX-011 Antibody; Q-397
|
ADC Antibody
c-Met/HGFR
|
Cancer
|
|
Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-P99041A
-
|
|
EGFR
|
Cancer
|
|
Panitumumab (anti-EGFR) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (anti-EGFR) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (anti-EGFR) can be used in the research of cancers, such as colon cancer .
|
-
- HY-14299D
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Indacaterol acetate is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol acetate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol acetate can also be used in cardiovascular disease research .
|
-
- HY-14299
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research .
|
-
- HY-14299A
-
|
QAB149
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research .
|
-
- HY-14299AR
-
|
QAB149 (Standard)
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Indacaterol (maleate) (Standard) is the analytical standard of Indacaterol (maleate). This product is intended for research and analytical applications. Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research .
|
-
- HY-14299R
-
|
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Indacaterol (Standard) is the analytical standard of Indacaterol. This product is intended for research and analytical applications. Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research .
|
-
- HY-153339
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .
|
-
- HY-181548
-
|
|
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
|
|
YL3147 is a ferroptosis inhibitor. YL3147 also acts as a radical-trapping antioxidant that directly prevents the spread of lipid peroxidation and blocks ferroptosis. YL3147 exerts significant cardioprotective effects in mouse cardiomyopathy models. YL3147 can be used in studies related to cardiomyopathy .
|
-
- HY-183304
-
|
|
Cytochrome P450
|
Cancer
|
|
Anticancer agent 318 (Compound 8 (6)) is a selective anticancer agent. Anticancer agent 318 can be metabolized by CYP1A1, CYP1A2 and CYP1B1. After bioactivation, Anticancer agent 318 exerts antiproliferative activity in breast cancer cells expressing CYP1. Anticancer agent 318 can be used in the research of breast cancer .
|
-
- HY-145655
-
|
|
CDK
|
Cancer
|
|
CDK7-IN-11 is an orally active CDK7 inhibitor. CDK7-IN-11 exhibits high CDK7 inhibitory activity with IC50 value of 4.2 nM. CDK7-IN-11 can be effectively used for the research of diseases associated with CDK7 .
|
-
- HY-10395
-
|
|
Bcr-Abl
Src
|
Cancer
|
|
PD173955 is an orally active inhibitor of Src (IC50= 22 nM), Yes, Abl, ATP and MAP kinases. PD173955 can effectively prevent the mitotic process and has anticancer activity .
|
-
- 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-10395R
-
|
|
Reference Standards
Bcr-Abl
Src
|
Cancer
|
|
PD173955 (Standard) is the analytical standard of PD173955 (HY-10395). This product is intended for research and analytical applications. PD173955 is an orally active inhibitor of Src (IC50= 22 nM), Yes, Abl, ATP and MAP kinases. PD173955 can effectively prevent the mitotic process and has anticancer activity .
|
-
- HY-P991049
-
|
ATM-001
|
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Atrosimab is an Fv-Fc1K fusion protein with an EC50 value of 0.37 nM against humans. Atrosimab inhibits TNF-induced TNFR1 activation, release of IL-6 and IL-8, and cell death, and alleviates neuroinflammation. Atrosimab is applicable to research related to inflammatory diseases, neurodegenerative diseases, acute and chronic inflammation, experimental arthritis, non-alcoholic steatohepatitis, and experimental autoimmune encephalomyelitis .
|
-
- HY-163760
-
|
|
HuR
MMP
|
Cancer
|
|
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 .
|
-
- 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-156515
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) is a drug-linker conjugate for ADC, formed by conjugation of 7ethanol-10NH2-11F-Camptothecin (HY-156517) with the protease-cleavable MC-GGFG linker. MC-GGFG-(7ethanol-10NH2-11F-Camptothecin) is applicable for cancer research .
|
-
- HY-115589
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity .
|
-
- HY-101982R
-
|
Lys-Nε-MCC-DM1 (Standard)
|
Reference Standards
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Lys-SMCC-DM1 (Standard) is the analytical standard of Lys-SMCC-DM1 (HY-101982). This product is intended for research and analytical applications. 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-175633
-
|
|
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
ML210-ansaFc (Compound III-13) is a covalent GPX4 inhibitor with a -ferrocenophane group (IC50 of 3.4 μM). ML210-ansaFc potently induces ferroptosis by increasing the level of ROSand promoting lipid peroxidation (LPO) in cancers cells. ML210-ansaFc has an anticancer activity and suppresses tumor growth in tumor 3D spheroids. ML210-ansaFc can be used for cancer therapy resistance research .
|
-
- HY-112806
-
|
|
Drug-Linker Conjugates for ADC
HDAC
EGFR
Microtubule/Tubulin
|
Cancer
|
|
ST8155AA1 is a part of antibody agent conjugates (ADCs) charged with HDAC inhibitor. ST8155AA1 induces α-tubulin, histone H3/H4 acetylation via direct enzymatic inhibition. ST8155AA1 recognizes and binds EGFR, undergoes internalization into EGFR-expressing tumor cells. ST8155AA1 inhibits cancer cell proliferation and exerts activity in mouse tumor models. ST8155AA1 can be used for the research of non-small cell lung cancer .
|
-
- HY-P99237
-
|
MMUC 1206A
|
Mucin
|
Cancer
|
|
Sofituzumab (MMUC 1206A) is an anti-MUC16 antibody with a Kd of 0.3-0.9 nM. Sofituzumab can bind multiple adjacent antibody molecules to the repeat sequences of the same MUC16 molecule. Sofituzumab exhibits no anti-tumor activity in the HPAC pancreatic adenocarcinoma xenograft model .
|
-
- 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-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-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-181068
-
|
|
PARP
Apoptosis
Microtubule/Tubulin
|
Cancer
|
|
2'-Nitroflavone is a PARP1 inhibitor. 2'-Nitroflavone inhibits the proliferation, induces cell cycle arrest and apoptosis of triple-negative breast cancer cells. 2'-Nitroflavone also inhibits the migration of triple-negative breast cancer cells and endothelial cells. 2'-Nitroflavone exhibits antitumor activity and can be used in the research of tumors such as triple-negative breast cancer .
|
-
- HY-149209
-
|
|
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)) .
|
-
- HY-123242
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity .
|
-
- HY-123242A
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FTI-2153 TFA is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 TFA is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity .
|
-
- HY-161780
-
|
|
Drug-Linker Conjugates for ADC
CDK
|
Cancer
|
|
Maleimide-Val-Ala-PAB-SNS032 is a conjugate of ADC toxin and linker. SNS032 is an inhibitor for CDK, inhibiting the cell cycle at G1/S phase and cell viability of cancer cells. Maleimide-Val-Ala-PAB is a cleavable ADC linker. Maleimide-Val-Ala-PAB-SNS032 can be utilized for the synthesis of ADC molecules .
|
-
- HY-116107
-
|
|
Necroptosis
|
Cancer
|
|
AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines .
|
-
- HY-155113
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC Hsp90α degrader 1 is a selective PROTAC Hsp90α degrader with a DC50 of 0.295 μM. PROTAC Hsp90α degrader 1 exhibits antitumor activity with low toxic side effects. PROTAC Hsp90α degrader 1 can be used for the research of breast cancer .
|
-
- HY-N2959
-
|
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
|
Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50=?10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
|
-
- 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-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-N2959R
-
|
|
Reference Standards
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
|
Brevilin A (Standard) is the analytical standard of Brevilin A. This product is intended for research and analytical applications. Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy .
|
-
- HY-12807
-
FIPI
5 Publications Verification
5-Fluoro-2-indolyl deschlorohalopemide
|
Phospholipase
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
FIPI is a phospholipase D (PLD) inhibitor with an IC50 for PLD1 and PLD2 of about 25 nM. FIPI regulates cytoskeletal recombination, cell diffusion and chemotaxis. FIPI can be used in cancer research. In addition, FIPI can enhance the secretion and aggregation of platelet dense particles, inhibit thrombosis, reduce ischemic stroke infarct volume and improve nerve function .
|
-
- 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-N2707
-
|
|
Reactive Oxygen Species (ROS)
|
Neurological Disease
Cancer
|
|
6-Deoxyjacareubin is a natural xanthone, that can be isolated from the leaves of Vismia latifolia. 6-Deoxyjacareubin protects against non-apoptotic cell death by inhibiting ROS production. 6-Deoxyjacareubin ameliorates neurodegeneration in a mouse model of familial amyotrophic lateral sclerosis (ALS) .
|
-
- HY-181581
-
|
|
PI3K
|
Cancer
|
|
IMM-H012 is a specific PI3K inhibitor with an IC50 of 0.80 nM against PI3Kα. IMM-H012 combined with [ 177Lu]Lu-P4 shows synergistic antitumor effects against stomach cancer and lung cancer .
|
-
- HY-D2869
-
|
|
Fluorescent Dye
Drug Intermediate
|
Others
|
|
Ac-H-FluNox is an acetylated cell-compatible prodrug of H-FluNox (HY-D2339). Ac-H-FluNox undergoes intracellular hydrolysis of its acetyl group by esterases to generate H-FluNox, which then undergoes a deoxygenation reaction with labile heme to form a fluorescent product. Ac-H-FluNox detects fluctuations of labile heme in living cells, acute labile heme release upon nitric oxide stimulation, and accumulation of labile heme following inhibition of heme export proteins .
|
-
- HY-14454
-
TPh A
2 Publications Verification
Triphenyl Compound A
|
Biochemical Assay Reagents
|
Cancer
|
|
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells .
|
-
- HY-181392
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
PROTAC EZH2 Degrader-35 (compound U3i (44)) is a PROTAC protein degrader targeting EZH2 with a human EZH2 Ka of 16.19 nM. PROTAC EZH2 Degrader-35 exhibits antiproliferative activity in triple-negative breast cancer cells and minimal cytotoxicity in normal human epithelial, hepatic, renal cells.PROTAC EZH2 Degrader-35 can be used for the research of triple-negative breast cancer .
|
-
- HY-P11844
-
|
|
Cathepsin
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
NOTA-FZCD-3 is a NOTA (HY-134418)-labeled FZCD-3 polypeptide precursor that targets cathepsin D (CTSD) with a KD of 0.65 μM. NOTA-FZCD-3 binds specifically to the active site of CTSD, exhibits rapid in vivo clearance properties, and remains stable in blood for more than 2 h. NOTA-FZCD-3 can be used in studies monitoring CTSD-positive tumors .
|
-
- HY-D1236
-
|
|
Parasite
Deubiquitinase
PARP
|
Cancer
|
|
Fluorescent brightener 71 (FB71) is an inhibitor targeting deubiquitinases UCHL5 and USP14, as well as a CD40 ligand. Fluorescent brightener 71 blocks enzymatic activity, induces apoptosis, inhibits cell growth and triggers reactive oxygen species production. Meanwhile, Fluorescent brightener 71 upregulates the expression of oxidative stress-related genes gpx-4 and sod-4, and reversibly increases the protein levels of UCHL5 and USP14 through a feedback response. Fluorescent brightener 71 inhibits the growth, movement and reproductive capacity of Caenorhabditis elegans, and also exhibits concentration-dependent toxic effects. Fluorescent brightener 71 can be applied to scientific research in related fields such as breast cancer .
|
-
- HY-176848
-
|
|
YTHDF
Apoptosis
MMP
Caspase
|
Cancer
|
|
SKLB-Y13 is a selective YTHDF1 inhibitor with an IC50 of 0.76 μM and a KD of 5.097 μM. SKLB-Y13 binds to the Tyr397 and Trp470 residues in the m 6A-binding pocket of YTHDF1, disrupting the interaction between YTHDF1 and m 6A-modified mRNA. SKLB-Y13 inhibits cancer cell proliferation and promotes apoptosis. SKLB-Y13 is applicable to breast cancer-related research .
|
-
- HY-135699
-
TD52
2 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-163468
-
|
|
Src
|
Cancer
|
|
SRC-3-IN-1 (compound SI-10) is a steroid receptor coactivator 3 (SRC-3) inhibitor (IC50=3.3 μM). SRC-3-IN-1 has good water solubility, oral bioavailability, and improved selectivity profile. SRC-3-IN-1 can be used in prostate cancer research .
|
-
- HY-133120
-
|
|
PROTACs
Akt
|
Cancer
|
|
INY-03-041 is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003, Cereblon ligand). INY-03-041 inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively .
|
-
- 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-181629
-
|
|
Aryl Hydrocarbon Receptor
Apoptosis
Caspase
Cytochrome P450
|
Cancer
|
|
ZSTK3744 is an aryl hydrocarbon receptor (AhR) agonist. ZSTK3744 directly binds to AhR, upregulates the expression of AhR target genes including CYP1A1, CYP1B1 and TIPARP, and mediates cell growth inhibitory activity in triple-negative breast cancer cells. ZSTK3744 induces apoptosis in triple-negative breast cancer cells. ZSTK3744 exhibits anti-tumor activity and can be used in the research of chemoresistant triple-negative breast cancer .
|
-
- HY-173119
-
|
|
ERK
Autophagy
Apoptosis
p62
mTOR
Reactive Oxygen Species (ROS)
Ferroptosis
|
Cancer
|
|
SKLB-D18 is an orally active ERK1/2/ERK5 inhibitor, with an IC50 of 38.69 nM and a Kd of 126.9 nM against human ERK1, an IC50 of 40.12 nM and a Kd of 209.8 nM against ERK2, and an IC50 of 59.72 nM and a Kd of 468.2 nM against ERK5. SKLB-D18 inhibits cancer cell proliferation, induces G0/G1 cell cycle arrest and apoptosis. SKLB-D18 reduces the levels of p-ERK5, p-RSKp90, p-c-Myc and c-Myc, and upregulates the level of p-ERK1/2, thereby inhibiting the ERK1/2/5 pathway in cells. SKLB-D18 increases LC3B-II accumulation, and decreases the levels of p62, p-mTOR and p-p70S6K. SKLB-D18 elevates the levels of ROS, lipid peroxidation and free ferrous ions, reduces the levels of NCOA4 and GPX4, and induces ferritin autophagy-dependent ferroptosis in cancer cells. SKLB-D18 exhibits antitumor activity in a triple-negative breast cancer xenograft mouse model. SKLB-D18 can be used in research related to triple-negative breast cancer .
|
-
- HY-N2460
-
-
- HY-113825
-
|
|
CDK
|
Cancer
|
|
CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 16 nM and 45 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities [1] .
|
-
- HY-183013
-
|
|
PROTACs
PARP
Apoptosis
|
Cancer
|
|
PROTAC PARP2 degrader-1 is an orally active PARP2 PROTAC degrader with a DC50 of 2 μM. PROTAC PARP2 degrader-1 potently inhibits the enzymatic activities of PARP1 (IC50 = 2.74 nM) and PARP2 (IC50 = 0.32 nM), with approximately 10-fold higher selectivity for PARP2. PROTAC PARP2 degrader-1 induces cell cycle arrest and apoptosis, and exhibits significant anti-tumor efficacy in mouse models. PROTAC PARP2 degrader-1 can be used for the research of triple-negative breast cancer .
|
-
- HY-16031A
-
|
NSC710464
|
Aryl Hydrocarbon Receptor
Integrin
Drug Intermediate
DNA/RNA Synthesis
|
Cancer
|
|
AFP464 (NSC710464) is a prodrug of Aminoflavone (HY-132974) and an agonist of the aryl hydrocarbon receptor (AhR). AFP464 downregulates the expression of α6-integrin (α6-integrin), inhibits breast tumor growth, reduces the population of tumor-initiating cells, disrupts mammosphere structure, induces the formation of mucin lake clusters, triggers DNA damage, and exerts antiproliferative activity. AFP464 is rapidly converted to Aminoflavone by nonspecific esterases in plasma and cell culture media. AFP464 is applicable to research related to breast cancer .
|
-
- HY-113670
-
|
|
CDK
|
Cancer
|
|
CLK1/2-IN-2 is CLK1 and CLK2 inhibitor with IC50 values of 1.1 nM and 2.4 nM, respectively. CLK1/2-IN-2 exhibits potent anti-cancer activities [1] .
|
-
- HY-177414
-
|
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Inflammation/Immunology
Cancer
|
|
BB-1701 is an anti-HER2 antibody-drug conjugate (ADC). BB-1701 is composed of a humanized anti-HER2 antibody (Trastuzumab) (HY-P9907), a linker (Mal-PEG2-VCP), a microtubule inhibitor (Eribulin) (HY-13442), and the drug-linker conjugate for ADC is Mal-PEG2-VCP-Eribulin (HY-128870). BB-1701 has a potent cytotoxicity and bystander effects on tumors with heterogeneous target expression. BB-1701 significantly induces immunogenic cell death and the activation of the immune .
|
-
- HY-183007
-
|
|
PROTACs
SWI/SNF Complex
|
Cancer
|
|
LJM133 is a SMARCA2/PBRM1/SMARCA4 PROTAC degrader with DC50 values of 3.5 nM, 7 nM, and 6.4 nM. LJM133 induces ternary complex formation with VHL E3 ligase to drive proteasome-mediated degradation of target proteins. LJM133 suppresses cell proliferation and exhibits significant antitumor efficacy in a SMARCA4 mutant cancer xenograft model. LJM133 can be used for the research of cancer, such as SMARCA4 mutant non-small cell lung cancer . (Pink: SMARCA2/PBRM1/SMARCA4 ligand (HY-182987); E3 ubiquitin ligase ligand-linker conjugate (HY-183619)).
|
-
- 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-12784
-
|
Chlorguanide triazine
|
Antifolate
DNA/RNA Synthesis
STAT
Parasite
|
Infection
Cancer
|
|
Cycloguanil (Chlorguanide triazine) is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
- HY-181999
-
|
|
PARP
CDK
Protease Activated Receptor (PAR)
Wnt
β-catenin
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Cancer
|
|
PC8 is a selective dual inhibitor of PARP1/CDK6, with an IC50 of 0.126 μM for PARP1 and 0.197 μM for CDK6. PC8 does not alter PARP1 expression, but reduces the expression of its downstream target PAR. PC8 inhibits the canonical Wnt/β-catenin signaling pathway. PC8 induces intracellular ROS accumulation and exacerbates DNA damage. PC8 inhibits the proliferation of triple-negative breast cancer (TNBC) cells. PC8 can be used for the research of triple-negative breast cancer .
|
-
- HY-185310
-
|
|
MASTL
c-Myc
DNA/RNA Synthesis
|
Cancer
|
|
MKI-2 is a selective MASTL inhibitor with an IC50 of 37.44 nM. MKI-2 induces mitotic catastrophe resulting from the modulation of the MASTL-PP2A axis in breast cancer cells. MKI-2 reduces phospho-ENSA, total, phospho-c-Myc levels. MKI-2 inhibts cancer cells proliferation, migration and induces DNA damage. MKI-2 inhibits germinal vesicle breakdown in mouse oocytes. MKI-2 can be used for the research of cancer, such as breast cancer .
|
-
- HY-12784A
-
|
Chlorguanide triazine hydrochloride
|
Antifolate
Parasite
DNA/RNA Synthesis
STAT
|
Infection
Cancer
|
|
Cycloguanil (Chlorguanide triazine) hydrochloride is a dihydrofolate reductase (DHFR) inhibitor with an IC50 of 10.8 μM against human DHFR. Cycloguanil hydrochloride blocks the folate metabolic pathway, thereby affecting nucleotide synthesis and interfering with DNA replication. Cycloguanil inhibits DHFR in Plasmodium and is thus used in malaria research. Cycloguanil hydrochloride also potently inhibits DHFR in human cancer cells and blocks the transcriptional activity of STAT3, thereby exhibiting anticancer activity .
|
-
- HY-10261A
-
|
BIBW 2992MA2
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261
-
|
BIBW 2992
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261D
-
|
BIBW 2992 oxalate
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
|
Cancer
|
|
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261R
-
|
BIBW 2992 (Standard)
|
Reference Standards
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261AR
-
|
BIBW 2992MA2 (Standard)
|
Reference Standards
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
|
Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-164056
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-8 (Compound 9) is a selective EGFR T790M/L858R mutant kinase inhibitor with a IC50 of 56.8 μM, and it shows no inhibitory activity against wild-type EGFR. EGFR T790M/L858R-IN-8 can be used for the research of non-small cell lung cancer .
|
-
- HY-161929
-
|
|
Glutathione Peroxidase
Ferroptosis
|
Cardiovascular Disease
|
|
GPX4 activator 2 is a GPX4 activator with a Ka value of 0.426 μM for human GPX4. GPX4 activator 2 reduces lipid hydroperoxide levels, prevents lipid peroxide accumulation, and inhibits ferroptosis. GPX4 activator 2 rescues cell death induced by Erastin (HY-15763). GPX4 activator 2 exerts cardioprotective effects in a mouse model of doxorubicin (HY-15142A)-induced myocardial injury .
|
-
- HY-12475
-
|
Agios 135
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Mutant IDH1-IN-1 (Agios 135) is a selective mutant IDH1 inhibitor with activity against both IDH1 R132H and IDH1 R132C. Mutant IDH1-IN-1 reduces the level of 2-hydroxyglutarate (2-HG), stabilizes mutant IDH1 protein, and restores blocked monocyte differentiation. Mutant IDH1-IN-1 can be used in tumor-related research .
|
-
- HY-D3447
-
|
|
Fluorescent Dye
Ferroptosis
|
Others
|
|
LPd peroxida probe-2 (Compound I-1) is a lipid peroxidation fluorescent indicator (Ex = 488 nm, Em = 535 nm). LPd peroxida probe-2 undergoes fluorescence spectral changes in response to lipid hydroperoxides and can be used for Ferroptosis detection and cell imaging.
|
-
- HY-181954
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer .
|
-
- HY-181928
-
|
|
c-Met/HGFR
PARP
Apoptosis
|
Cancer
|
|
PARP1/c-Met-IN-3 (Compound L19) is a selective c-Met and PARP1 inhibitor, with an IC50 of 5.4 nM against c-Met and an IC50 of 3.7 nM against PARP1. PARP1/c-Met-IN-3 inhibits PARP2 enzymatic activity with an IC50 of 4.52 nM, and shows no specificity for PARP1 and PARP2. PARP1/c-Met-IN-3 induces cell cycle arrest and apoptosis. PARP1/c-Met-IN-3 exhibits anti-tumor activity against triple-negative breast cancer .
|
-
- HY-P992488
-
|
ZV0501 Antibody
|
Transmembrane Glycoprotein
ADC Antibody
|
Cancer
|
|
ZV05 (ZV0501 Antibody) is an anti-5T4 monoclonal antibody with an EC50 of 4.3 ng/mL against h5T4. ZV05 does not induce apoptosis or interfere with cell cycle progression. ZV05 accumulates specifically in 5T4-positive tumor xenografts. ZV05 can serve as the antibody component of antibody-active molecule conjugates (ADCs) to bind the 5T4 glycoprotein, thereby enabling targeted delivery of toxins. ZV05 is used in studies of 5T4-positive cancers, including triple-negative breast cancer .
|
-
- HY-170027
-
|
|
HIF/HIF Prolyl-Hydroxylase
AMPK
|
Cancer
|
|
LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model .
|
-
- HY-164346
-
|
|
Microtubule/Tubulin
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Amine-PEG8-Val-Cit-PAB-MMAE is a potent drug-linker conjugate for antibody-drug conjugates (ADCs).Amine-PEG8-Val-Cit-PAB-MMAE consists of the linker amine-PEG8-Vali-Cit-PAB and the payload MMAE (HY-15162), and can be used to synthesize ADCs. Amine-PEG8-Val-Cit-PAB-MMAE can be used for the research of gastric cancer, colon cancer, lung adenocarcinoma .
|
-
- HY-148104
-
-
- HY-181756
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
LGF308 is a PROTAC degrader of BRD4 that exhibits selective cytotoxicity toward cancer cells over normal cells. LGF308 mediates the formation of a ternary complex between BRD4 and DCAF11 to achieve BRD4 degradation. LGF308 induces tumor cell apoptosis by upregulating apoptosis-related proteins. LGF308 inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines. LGF308 can be used for the research of breast cancer .
|
-
- HY-181460
-
|
|
HyT
PARP
|
Cancer
|
|
PARP1 degrader-2 (Compound 11e) is a potent, selective PARP1 HYT degrader (DC50: 2.16 μM). PARP1 degrader-2 selectively binds to and degrades PARP1 but not PARP2. PARP1 degrader-2 mediates the degradation of PARP1 via the ubiquitin-proteasome system (UPS). PARP1 degrader-2 exhibits anticancer activity against triple-negative breast cancer and colon cancer (hydrophobic tag: (HY-W022007); PARP1 ligand: (HY-75706); Linker: (HY-W015300)) .
|
-
- HY-116474
-
|
|
ERK
JNK
MMP
p38 MAPK
STAT
Fungal
Bacterial
NO Synthase
PGE synthase
NF-κB
Wnt
β-catenin
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Viridicatol is a quinolone alkaloid with anti-inflammatory, antibacterial, antifungal, osteogenic and chondrogenic activities. Viridicatol reduces the phosphorylation levels of ERK, JNK, p38 and STAT6; inhibits MMP-2, MMP-9, NF-κB signaling pathway and PTP1B; downregulates genes related to mast cell activation; and binds to SHN3 to activate the Wnt/SHN3 signaling pathway. Viridicatol inhibits the expression of pro-inflammatory mediators and cytokines, and promotes osteogenic/chondrogenic differentiation. Viridicatol can be used in studies related to fibrosarcoma, allergy, bacterial infection, fungal infection and osteoporosis .
|
-
- HY-171658
-
|
|
PROTACs
Ser/Thr Kinase
TNF Receptor
Toll-like Receptor (TLR)
NF-κB
p38 MAPK
|
Inflammation/Immunology
Cancer
|
|
R1-ICR-5 is a highly selective RIPK1 PROTAC degrader. Mediated by VHL, R1-ICR-5 induces the degradation of RIPK1, which in turn dysregulates the TNFR1 and TLR3/4 signaling hubs, enhances the signaling outputs of NF-κB, MAPK and IFN, and simultaneously promotes RIPK3 activation and necroptosis (necroptosis). R1-ICR-5 can be used in the research of triple-negative breast cancer and skin inflammation .
|
-
- HY-182378
-
|
|
|
Cancer
|
|
Vps34-IN-5 is an orally active VPS34 inhibitor, 98% target inhibition, and an IC50 categorized as B. Vps34-IN-5 induces additive or synergistic anti-proliferative activity with EGFR inhibitors in cancer cells. Vps34-IN-5 is administered orally alone or with Erlotinib (HY-50896) in mouse xenograft models. Vps34-IN-5 can be used for the research of non-small cell lung cancer .
|
-
- 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-N18190
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
N-Desmethyldauricine is a NF-κB p65 inhibitor and apoptosis inducer. N-Desmethyldauricine reduces the protein expression level of p65, induces apoptosis, arrests the cell cycle at the G0/G1 phase, attenuates intercellular adhesion, and inhibits the growth of 3D spheroids of triple-negative breast cancer. N-Desmethyldauricine can be used in studies related to triple-negative breast cancer .
|
-
- HY-181626
-
|
|
HSP
Aurora Kinase
Apoptosis
|
Cancer
|
|
NN-01-195 is a HSP90 and AURKA inhibitor. NN-01-195 binds tightly to and inhibits AURKA and HSP90, with an IC50 of 3.1 nM against AURKA and an IC50 of 8.7 nM against HSP90α. NN-01-195 induces mitotic arrest and spindle abnormality in tumor cells, and triggers cell apoptosis. NN-01-195 can be used in the research of solid tumors .
|
-
- HY-185056
-
|
|
Ferroptosis
Fluorescent Dye
|
Cardiovascular Disease
Neurological Disease
|
|
Ferfluor-1 is a Ferroptosis inhibitor (EC50 of 57 nM in HT108 cells; EC50 of 75 nM in OS-RC-2 cells; EC50 of 2.3 nM in SH-SY5Y neuroblastoma cells), and ratiometric photoluminescent probe with blood-brain barrier permeability. Ferfluor-1 is a specific indicator for the fluctuation of Ferroptosis. Ferfluor-1 alleviates brain disorder diseases of in vivo stroke and PD models .
|
-
- HY-162250
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer .
|
-
- HY-173117
-
|
|
CaMK
|
Cardiovascular Disease
Cancer
|
|
RA306 is an orally active CaMKIIδ/γ inhibitor with IC50 values of 15, 25, 61, and 420 nM against CaMKIIδ, γ, α, and β isoforms, respectively. RA306 reduces the serine/threonine phosphorylation level of PEAK1, inhibits PEAK1-mediated cancer cell migration and invasion, and attenuates the growth and metastasis of cancer xenografts. RA306 can be used in research related to triple-negative breast cancer and dilated cardiomyopathy .
|
-
- HY-146127
-
|
|
MEK
|
Cancer
|
|
Grb2 SH2 domain inhibitor 1 is an inhibitor of the Grb2 SH2 domain with an IC50 of 0.40 μM. Grb2 SH2 domain inhibitor 1 is also a cell-permeable cyclic peptide that can enter the cytosol of mammalian cells. Grb2 SH2 domain inhibitor 1 downregulates the expression level of p-MEK. Grb2 SH2 domain inhibitor 1 can be used in the research of breast cancer .
|
-
- HY-181833
-
|
|
ADC Payload
PI3K
|
Cancer
|
|
PI3K/PIKK-IN-1 is a PI3K and PIKK inhibitor that serves as a payload for antibody-drug conjugates (ADC) to prepare ADC. PI3K/PIKK-IN-1 is applicable to research related to breast cancer, multiple myeloma, Burkitt lymphoma, diffuse large B-cell lymphoma, and non-small cell lung cancer .
|
-
- HY-183294
-
|
|
Glutathione Peroxidase
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GPX4-IN-24 is an orally active glutathione peroxidase 4 (GPX4) inhibitor with a human IC50 of 10.90 μM, human Kd of 10.04 μM. GPX4-IN-24 suppresses GPX4 enzymatic activity, disrupts redox homeostasis, drives lipid peroxidation, promotes lipid peroxidation, and induces ferroptosis. GPX4-IN-24 can be used for the research of triple-negative breast cancer .
|
-
- HY-178749
-
|
|
ClpP
Mitochondrial Metabolism
Apoptosis
Caspase
PARP
|
Cancer
|
|
MS6076 is a mitochondrial protease ClpP agonist. MS6076 specifically activates the ClpP protease in the mitochondrial matrix, significantly disrupting mitochondrial Electron Transport Chain (ETC) function by accelerating the degradation of unfolded proteins. MS6076 exhibits potent cytotoxicity against a variety of cancer cell lines. MS6076 induces cell apoptosis, increasing cleavage of caspase 3 and PARP. MS6076 can be used for the research of breast cancer .
|
-
- HY-P11143A
-
|
|
Interleukin Related
Liposome
|
Cancer
|
|
IL4RPep-1 acetate is an interleukin-4 receptor (IL-4R) binding agent. IL4RPep-1 acetate preferentially binds to cells with high levels of IL-4R expression compared to those with low levels of expression. IL4RPep-1-labeled liposomes containing Doxorubicin (HY-15142A) are internalized by cells more efficiently. IL4RPep-1-labeled liposomes accumulate more effectively within H226 tumors .
|
-
- HY-NP163A
-
|
WGA-AF488
|
Fluorescent Dye
|
Cancer
|
Wheat germ agglutinin-AF488 (WGA-AF488) is a cell membrane-specific staining agent prepared by conjugating wheat germ agglutinin with the Alexa Fluor 488 (HY-D1304) fluorescent dye, and it binds to cell surface glycoproteins with high affinity. Wheat germ agglutinin-AF488 is applied in fluorescence microscopy and confocal imaging techniques, and it can clearly label the membrane structures of various cells including breast cancer cells, enabling high-resolution visual observation. Wheat germ agglutinin-AF488 is used in studies of breast cancer and triple-negative breast cancer to observe cell morphology and membrane dynamic changes .
|
-
- HY-120031
-
|
|
STAT
PARP
Apoptosis
|
Cancer
|
|
NSC-368262 is a STAT3 inhibitor. NSC-368262 selectively alkylates and covalently modifies STAT3 Cys468 at the DNA-binding interface of STAT3, blocks the DNA-binding activity of STAT3, and inhibits the phosphorylation of STAT3. NSC-368262 blocks the accumulation of activated STAT3 in the nucleus of cancer cells, induces PARP cleavage and apoptosis in cells, and inhibits tumor growth in mouse models. NSC-368262 can be used in research related to breast cancer and cervical cancer .
|
-
- HY-P991969
-
|
|
EGFR
|
Cancer
|
|
LR004 is an EGFR monoclonal antibody, with a Kd of 2.80×10 -9 M against human EGFR. LR004 shows extremely weak inhibitory effect on the viability of EGFR-positive tumor cells in vitro, but inhibits the growth of EGFR-positive tumor xenografts as a single agent. LR004 is applicable to research related to advanced colorectal cancer, solid tumors, esophageal squamous cell carcinoma, epidermoid carcinoma, colon cancer and breast cancer .
|
-
- HY-132885
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-1 is a first-in-class dual PARP-1/EZH2 inhibitor with IC50 values of 6.87 nM and 36.51 nM, respectively. PARP/EZH2-IN-1 induces autophagy in cancer cells and shows potent antiproliferative activity in BRCA wild-type triple-negative breast cancer cells .
|
-
- HY-151704
-
|
|
Fluorescent Dye
|
Cancer
|
|
ICG-alkyne is a short-wave infrared (SWIR)-emitting cyanine fluorescent probe based on alkyne-derivatized indocyanine green. ICG-alkyne can undergo click chemistry reaction to conjugate with antibody molecules via binding to the azide groups introduced into antibodies. ICG-alkyne enables SWIR fluorescent molecular imaging of breast tumors in living mice. ICG-alkyne can be used in breast cancer-related research .
|
-
- HY-174929A
-
|
DBCO-PEG5000-NH2
|
Biochemical Assay Reagents
|
Others
|
|
DBCO-PEG5000-Amine (DBCO-PEG5000-NH2) is a polyethylene glycol derivative containing dibenzocyclooctyne. DBCO-PEG-Amine is a universal, modular "bridge molecule": it forms stable covalent linkage with target materials (e.g., MSN or polymers) via the amino group at one end, while the DBCO group at the other end enables efficient, specific, and biocompatible click chemical conjugation with any azide-bearing biological entities (e.g., bacteria, cells) in subsequent steps .
|
-
- HY-168037A
-
|
|
PIN1
|
Cancer
|
|
PROTAC PIN1 degrader-1 TFA is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer .
|
-
- HY-168037
-
|
|
PROTACs
PIN1
|
Cancer
|
|
PROTAC PIN1 degrader-1 is a PIN1-target PROTAC degrader. PROTAC PIN1 degrader-1 TFA can be used for the research of triple-negative breast cancer, pancreatic cancer, and liver cancer .
|
-
- HY-W1123936D
-
|
DBCO-PEG3400-Folate
|
Folate Receptor (FR)
|
Others
|
|
DBCO-PEG-FA (DBCO-PEG-Folate) (MW 3400) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-W1123936H
-
|
DBCO-PEG10000-Folate
|
Folate Receptor (FR)
|
Others
|
|
DBCO-PEG10000-FA (DBCO-PEG10000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-W1123936B
-
|
DBCO-PEG1000-Folate
|
Folate Receptor (FR)
|
Cancer
|
|
DBCO-PEG1000-FA (DBCO-PEG1000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-W1123936C
-
|
DBCO-PEG2000-Folate
|
Folate Receptor (FR)
|
Others
|
|
DBCO-PEG2000-FA (DBCO-PEG2000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-W1123936E
-
|
DBCO-PEG5000-Folate
|
Folate Receptor (FR)
|
Others
|
|
DBCO-PEG5000-FA (DBCO-PEG5000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-P10775A
-
|
|
MMP
|
Cancer
|
|
BT1769 acetate is a conjugate and antitumor agent targeting MT1-MMP, with a Kd value of 3.35 nM against human targets. BT1769 acetate exhibits favorable pharmacokinetic properties. BT1769 acetate specifically binds to MT1-MMP via its bicyclic peptide component, delivering the cytotoxic agent MMAE (HY-15162) to antigen-expressing cells. It effectively inhibits tumor growth, induces complete responses, and significantly prolongs event-free survival in osteosarcoma patient-derived xenograft models. BT1769 acetate shows extremely low activity in Ewing sarcoma models and can be used in osteosarcoma-related research .
|
-
- HY-173561A
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
MS115 TFA is a selective PRMT5/MEP50 PROTAC degrader, with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and MEP50, respectively. MS115 TFA promotes PRMT5/MEP50 ubiquitination and degradation. MS115 TFA shows anticancer activity against breast cancer .
|
-
- HY-175201
-
|
|
LPL Receptor
STAT
|
Cancer
|
|
pro-FTY, a FTY720 (HY-12005) anticancer prodrug, is a sphingosine-1-phosphate (S1P) (HY-108496) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel (HY-B0015) or Doxorubicin (HY-15142A). pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia .
|
-
- HY-183716
-
|
|
Drug Derivative
|
Cancer
|
|
Mito-TP-2 is a triptolide (HY-32735) derivative. Mito-TP-2 exhibits concentration-dependent cytotoxicity in cancer cells. Mito-TP-2 is selectively driven and accumulated into the mitochondria of tumor cells by mitochondrial transmembrane potential and exerts specific mitochondrial toxicity. Mito-TP-2 can be used for the research of liver cancer, breast cancer, and non-small cell lung cancer .
|
-
- HY-175245
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCA-IN-1 (Compound 5u) is an hCA inhibitor with Ki values of 159.2, 4.8, 15.5, and 2 nM against hCA I, hCA II, hCA IX, and hCA XII, respectively. hCA-IN-1 exhibits broad-spectrum anticancer activity against melanoma, breast, and colon cancer cells. ADME predictions indicate that hCA-IN-1 has good solubility and oral bioavailability. hCA-IN-1 can be used in tumor research .
|
-
- HY-W1123937C
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Biotin-PEG-CHO (with a molecular weight of 5000) is a biotin-attached PEG derivative that can be used for biotinylation of biological molecules or other material surfaces. Biotin can be easily detected through the biotin/streptavidin binding test, and is widely used in molecular targeted detection.
|
-
- HY-181940
-
|
|
Proteasome
|
Cancer
|
|
Berberine-amide-m-PhBA chloride (Compound 8b) is a selective anti-breast cancer agent. Berberine-amide-m-PhBA chloride may inhibit the proteasome by interacting with the 20S proteasome β5 subunit. Berberine-amide-m-PhBA chloride can be used in the research of breast cancer .
|
-
-
- HY-D2869
-
|
|
Fluorescent Dyes
|
|
Ac-H-FluNox is an acetylated cell-compatible prodrug of H-FluNox (HY-D2339). Ac-H-FluNox undergoes intracellular hydrolysis of its acetyl group by esterases to generate H-FluNox, which then undergoes a deoxygenation reaction with labile heme to form a fluorescent product. Ac-H-FluNox detects fluctuations of labile heme in living cells, acute labile heme release upon nitric oxide stimulation, and accumulation of labile heme following inhibition of heme export proteins .
|
-
- HY-177414
-
|
|
Fluorescent Dyes
|
|
BB-1701 is an anti-HER2 antibody-drug conjugate (ADC). BB-1701 is composed of a humanized anti-HER2 antibody (Trastuzumab) (HY-P9907), a linker (Mal-PEG2-VCP), a microtubule inhibitor (Eribulin) (HY-13442), and the drug-linker conjugate for ADC is Mal-PEG2-VCP-Eribulin (HY-128870). BB-1701 has a potent cytotoxicity and bystander effects on tumors with heterogeneous target expression. BB-1701 significantly induces immunogenic cell death and the activation of the immune .
|
-
- HY-151704
-
|
|
Fluorescent Dyes
|
|
ICG-alkyne is a short-wave infrared (SWIR)-emitting cyanine fluorescent probe based on alkyne-derivatized indocyanine green. ICG-alkyne can undergo click chemistry reaction to conjugate with antibody molecules via binding to the azide groups introduced into antibodies. ICG-alkyne enables SWIR fluorescent molecular imaging of breast tumors in living mice. ICG-alkyne can be used in breast cancer-related research .
|
-
- HY-D1236
-
|
|
Fluorescent Dyes
|
|
Fluorescent brightener 71 (FB71) is an inhibitor targeting deubiquitinases UCHL5 and USP14, as well as a CD40 ligand. Fluorescent brightener 71 blocks enzymatic activity, induces apoptosis, inhibits cell growth and triggers reactive oxygen species production. Meanwhile, Fluorescent brightener 71 upregulates the expression of oxidative stress-related genes gpx-4 and sod-4, and reversibly increases the protein levels of UCHL5 and USP14 through a feedback response. Fluorescent brightener 71 inhibits the growth, movement and reproductive capacity of Caenorhabditis elegans, and also exhibits concentration-dependent toxic effects. Fluorescent brightener 71 can be applied to scientific research in related fields such as breast cancer .
|
-
- HY-NP163A
-
|
WGA-AF488
|
Biochemical Assay Reagents
|
Wheat germ agglutinin-AF488 (WGA-AF488) is a cell membrane-specific staining agent prepared by conjugating wheat germ agglutinin with the Alexa Fluor 488 (HY-D1304) fluorescent dye, and it binds to cell surface glycoproteins with high affinity. Wheat germ agglutinin-AF488 is applied in fluorescence microscopy and confocal imaging techniques, and it can clearly label the membrane structures of various cells including breast cancer cells, enabling high-resolution visual observation. Wheat germ agglutinin-AF488 is used in studies of breast cancer and triple-negative breast cancer to observe cell morphology and membrane dynamic changes .
|
-
- HY-W1123936B
-
|
DBCO-PEG1000-Folate
|
Biochemical Assay Reagents
|
|
DBCO-PEG1000-FA (DBCO-PEG1000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-174929A
-
|
DBCO-PEG5000-NH2
|
Biochemical Assay Reagents
|
|
DBCO-PEG5000-Amine (DBCO-PEG5000-NH2) is a polyethylene glycol derivative containing dibenzocyclooctyne. DBCO-PEG-Amine is a universal, modular "bridge molecule": it forms stable covalent linkage with target materials (e.g., MSN or polymers) via the amino group at one end, while the DBCO group at the other end enables efficient, specific, and biocompatible click chemical conjugation with any azide-bearing biological entities (e.g., bacteria, cells) in subsequent steps .
|
-
- HY-W1123936C
-
|
DBCO-PEG2000-Folate
|
Biochemical Assay Reagents
|
|
DBCO-PEG2000-FA (DBCO-PEG2000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-W1123936D
-
|
DBCO-PEG3400-Folate
|
Biochemical Assay Reagents
|
|
DBCO-PEG-FA (DBCO-PEG-Folate) (MW 3400) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-W1123936H
-
|
DBCO-PEG10000-Folate
|
Biochemical Assay Reagents
|
|
DBCO-PEG10000-FA (DBCO-PEG10000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-W1123936E
-
|
DBCO-PEG5000-Folate
|
Biochemical Assay Reagents
|
|
DBCO-PEG5000-FA (DBCO-PEG5000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-W1123937C
-
|
|
Biochemical Assay Reagents
|
|
Biotin-PEG-CHO (with a molecular weight of 5000) is a biotin-attached PEG derivative that can be used for biotinylation of biological molecules or other material surfaces. Biotin can be easily detected through the biotin/streptavidin binding test, and is widely used in molecular targeted detection.
|
| Cat. No. |
상품명 |
Target |
Research Area |
-
- 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-146127
-
|
|
MEK
|
Cancer
|
|
Grb2 SH2 domain inhibitor 1 is an inhibitor of the Grb2 SH2 domain with an IC50 of 0.40 μM. Grb2 SH2 domain inhibitor 1 is also a cell-permeable cyclic peptide that can enter the cytosol of mammalian cells. Grb2 SH2 domain inhibitor 1 downregulates the expression level of p-MEK. Grb2 SH2 domain inhibitor 1 can be used in the research of breast cancer .
|
-
- HY-P10760
-
|
|
Peptide-Drug Conjugates (PDCs)
|
Cancer
|
PhAc-ALGP-Dox, a peptide-drug conjugate, is a novel anticancer prodrug, with IC50 values ranged from 311 nM to 34.25 μM for TNBC (E0771), normal murine epithelium (HC-11), human TNBC (MDA-MB-231 and MDA-MB-468), human CrC (LS 174T), normal human epithelium (HME-1) cells .
|
-
- HY-159771
-
|
|
FAP
|
Cancer
|
|
FAP6-19 is a fibroblast activation protein (FAP) targeting radioligand with a Kd of 18.2 nM. FAP6-19 selectively delivers therapeutic radioactive nuclides (such as 177Lu) to the tumor site by targeting the overexpressed FAP protein in the tumor microenvironment, achieving precise killing of cancer cells while minimizing radiation damage to healthy tissues. FAP6-19 exhibits extremely high total cellular uptake and good intracellular retention ability in HT1080 cells. After being labeled with 111In, FAP6-19 produced extremely high tumor/kidney and tumor/liver dose ratios in the mouse model with 4T1 tumors. FAP6-19 can be used in the research of solid tumors expressing FAP.
|
-
- HY-P10775A
-
|
|
MMP
|
Cancer
|
|
BT1769 acetate is a conjugate and antitumor agent targeting MT1-MMP, with a Kd value of 3.35 nM against human targets. BT1769 acetate exhibits favorable pharmacokinetic properties. BT1769 acetate specifically binds to MT1-MMP via its bicyclic peptide component, delivering the cytotoxic agent MMAE (HY-15162) to antigen-expressing cells. It effectively inhibits tumor growth, induces complete responses, and significantly prolongs event-free survival in osteosarcoma patient-derived xenograft models. BT1769 acetate shows extremely low activity in Ewing sarcoma models and can be used in osteosarcoma-related research .
|
-
- HY-P11844
-
|
|
Cathepsin
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
NOTA-FZCD-3 is a NOTA (HY-134418)-labeled FZCD-3 polypeptide precursor that targets cathepsin D (CTSD) with a KD of 0.65 μM. NOTA-FZCD-3 binds specifically to the active site of CTSD, exhibits rapid in vivo clearance properties, and remains stable in blood for more than 2 h. NOTA-FZCD-3 can be used in studies monitoring CTSD-positive tumors .
|
-
- HY-P11143A
-
|
|
Interleukin Related
Liposome
|
Cancer
|
|
IL4RPep-1 acetate is an interleukin-4 receptor (IL-4R) binding agent. IL4RPep-1 acetate preferentially binds to cells with high levels of IL-4R expression compared to those with low levels of expression. IL4RPep-1-labeled liposomes containing Doxorubicin (HY-15142A) are internalized by cells more efficiently. IL4RPep-1-labeled liposomes accumulate more effectively within H226 tumors .
|
| Cat. No. |
상품명 |
Target |
Research Area |
Image |
-
- HY-P99041
-
|
ABX-EGF
|
EGFR
|
Cancer
|
|
Panitumumab (ABX-EGF) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab can be used in the research of cancers, such as colon cancer .
|
-
(5)
-
- HY-P991049
-
|
ATM-001
|
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Atrosimab is an Fv-Fc1K fusion protein with an EC50 value of 0.37 nM against humans. Atrosimab inhibits TNF-induced TNFR1 activation, release of IL-6 and IL-8, and cell death, and alleviates neuroinflammation. Atrosimab is applicable to research related to inflammatory diseases, neurodegenerative diseases, acute and chronic inflammation, experimental arthritis, non-alcoholic steatohepatitis, and experimental autoimmune encephalomyelitis .
|
-
(5)
-
- HY-P99041A
-
|
|
EGFR
|
Cancer
|
|
Panitumumab (anti-EGFR) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (anti-EGFR) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (anti-EGFR) can be used in the research of cancers, such as colon cancer .
|
-
(5)
-
- HY-P99237
-
|
MMUC 1206A
|
Mucin
|
Cancer
|
|
Sofituzumab (MMUC 1206A) is an anti-MUC16 antibody with a Kd of 0.3-0.9 nM. Sofituzumab can bind multiple adjacent antibody molecules to the repeat sequences of the same MUC16 molecule. Sofituzumab exhibits no anti-tumor activity in the HPAC pancreatic adenocarcinoma xenograft model .
|
-
(5)
-
- HY-P990859
-
|
|
Transmembrane Glycoprotein
|
Others
|
|
Anti-CD44 Antibody (Hermes-1) is a kind of rat IgG2a κ chimeric antibody, targeting to human CD44. Anti-CD44 Antibody (Hermes-1) blocks the binding of hyaluronan to CD44. Anti-CD44 Antibody (Hermes-1) restores (Platelet-derived Growth Factor-BB)-induced β-receptor activation and motility in fibroblasts. Anti-CD44 Antibody (Hermes-1) causes partial loss of the anti-aging effect of hyaluronic .
|
-
(5)
-
- HY-P99041B
-
|
ABX-EGF (powder)
|
EGFR
|
Cancer
|
|
Panitumumab (ABX-EGF) (powder) is a fully human IgG2 anti-EGFR monoclonal antibody with anti-tumor activity. Panitumumab (powder) inhibits tumor cell proliferation, survival and angiogenesis. Panitumumab (powder) can be used in the research of cancers, such as colon cancer .
|
-
(5)
-
- HY-P992146
-
|
MYTX-011 Antibody; Q-397
|
ADC Antibody
c-Met/HGFR
|
Cancer
|
|
Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P992488
-
|
ZV0501 Antibody
|
Transmembrane Glycoprotein
ADC Antibody
|
Cancer
|
|
ZV05 (ZV0501 Antibody) is an anti-5T4 monoclonal antibody with an EC50 of 4.3 ng/mL against h5T4. ZV05 does not induce apoptosis or interfere with cell cycle progression. ZV05 accumulates specifically in 5T4-positive tumor xenografts. ZV05 can serve as the antibody component of antibody-active molecule conjugates (ADCs) to bind the 5T4 glycoprotein, thereby enabling targeted delivery of toxins. ZV05 is used in studies of 5T4-positive cancers, including triple-negative breast cancer .
|
-
(5)
-
- HY-P991969
-
|
|
EGFR
|
Cancer
|
|
LR004 is an EGFR monoclonal antibody, with a Kd of 2.80×10 -9 M against human EGFR. LR004 shows extremely weak inhibitory effect on the viability of EGFR-positive tumor cells in vitro, but inhibits the growth of EGFR-positive tumor xenografts as a single agent. LR004 is applicable to research related to advanced colorectal cancer, solid tumors, esophageal squamous cell carcinoma, epidermoid carcinoma, colon cancer and breast cancer .
|
-
(5)
| Cat. No. |
상품명 |
Category |
Target |
Chemical Structure |
-
- HY-B1645
-
-
-
- HY-N2117
-
-
-
- HY-B1465
-
-
-
- HY-N2959
-
-
-
- HY-N2460
-
-
-
- HY-N0364
-
-
-
- HY-N2497
-
-
-
- HY-N9596
-
-
-
- HY-116474
-
|
|
Infection
Alkaloids
Structural Classification
Monophenols
Microorganisms
Classification of Application Fields
Phenols
Quinoline Alkaloids
Disease Research Fields
Source Classification
|
ERK
JNK
MMP
p38 MAPK
STAT
Fungal
Bacterial
NO Synthase
PGE synthase
NF-κB
Wnt
β-catenin
|
|
Viridicatol is a quinolone alkaloid with anti-inflammatory, antibacterial, antifungal, osteogenic and chondrogenic activities. Viridicatol reduces the phosphorylation levels of ERK, JNK, p38 and STAT6; inhibits MMP-2, MMP-9, NF-κB signaling pathway and PTP1B; downregulates genes related to mast cell activation; and binds to SHN3 to activate the Wnt/SHN3 signaling pathway. Viridicatol inhibits the expression of pro-inflammatory mediators and cytokines, and promotes osteogenic/chondrogenic differentiation. Viridicatol can be used in studies related to fibrosarcoma, allergy, bacterial infection, fungal infection and osteoporosis .
|
-
-
- HY-N8187
-
-
-
- HY-138071
-
-
-
- HY-B1465R
-
-
-
- HY-N10229
-
-
-
- HY-N15614
-
|
|
Alkaloids
Erythrophleum fordii Oliv.
Leguminosae
Other Alkaloids
Plants
Source Classification
|
Others
|
|
Cassamine is a diterpenoid compound that can be isolated from the bark of Erythrophleum fordii. Cassamine exhibits certain cytotoxicity against non-small cell lung cancer cell lines, with IC50 values of 3.4, 2.1, and 1.9 μM against A549, NCI-H1975, and NCI-H1299, respectively. Cassamine has antitumor activity and can be used in the research of lung cancer and other tumors .
|
-
-
- HY-N2117R
-
-
-
- HY-W749442
-
|
|
Natural Products
Sphaeranthus indicus L.
Asteraceae
Plants
Source Classification
|
Microtubule/Tubulin
|
|
7a-Hydroxyfrullanolide has anticancer properties. 7a-Hydroxyfrullanolide reduces polymerization of α-, β-tubulin. 7a-Hydroxyfrullanolide preferrs to bind to β-tubulin over α-tubulin. 7a-Hydroxyfrullanolide also triggers DNA damage response arrests cells in the G2/M-phase. 7a-Hydroxyfrullanolide is an eudesmanolide sesquiterpene lactone (SL) and can be isolated from the flowering plants of the Asteraceae family .
|
-
-
- HY-N2497R
-
-
-
- HY-N2959R
-
-
-
- HY-N2707
-
-
-
- HY-N18190
-
-
| Cat. No. |
상품명 |
Chemical Structure |
-
- HY-N9596S
-
|
|
|
Stigmasta-4,22-dien-3-one-d5 is the deuterium labeled Stigmasta-4,22-dien-3-one (HY-N9596). Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM .
|
-
| Cat. No. |
상품명 |
|
Classification |
-
- HY-147858
-
|
|
|
Alkynes
PROTAC Synthesis
|
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 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-115997
-
|
|
|
PROTAC Synthesis
|
|
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-135699
-
TD52
2 Publications Verification
|
|
Alkynes
|
|
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-W1123936B
-
|
DBCO-PEG1000-Folate
|
|
DBCO
|
|
DBCO-PEG1000-FA (DBCO-PEG1000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
|
-
- HY-135699A
-
|
|
|
Alkynes
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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.
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- HY-174929A
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DBCO-PEG5000-NH2
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DBCO
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DBCO-PEG5000-Amine (DBCO-PEG5000-NH2) is a polyethylene glycol derivative containing dibenzocyclooctyne. DBCO-PEG-Amine is a universal, modular "bridge molecule": it forms stable covalent linkage with target materials (e.g., MSN or polymers) via the amino group at one end, while the DBCO group at the other end enables efficient, specific, and biocompatible click chemical conjugation with any azide-bearing biological entities (e.g., bacteria, cells) in subsequent steps .
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- HY-178370
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Alkynes
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Ferroptosis inducer-12 is a potent and selective ferroptosis inducer. Ferroptosis inducer-12 exhibits potent antiproliferative activity against HT1080 and OS-RC-2, with IC50 values of 3 nM and 5 nM, respectively. Ferroptosis inducer-12 strongly inhibits GPX4 enzymatic activity, induces intracellular ROS and elevates intracellular Fe 2+ levels in OS-RC-2 cells. Ferroptosis inducer-12 significantly inhibits tumor growth in BALB/c nude mice bearing OS-RC-2 xenografts. Ferroptosis inducer-12 can be used for the study of cancer .
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- HY-W1123936C
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DBCO-PEG2000-Folate
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DBCO
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DBCO-PEG2000-FA (DBCO-PEG2000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
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- HY-168093
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Alkynes
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Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
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- HY-175633
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Alkynes
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ML210-ansaFc (Compound III-13) is a covalent GPX4 inhibitor with a -ferrocenophane group (IC50 of 3.4 μM). ML210-ansaFc potently induces ferroptosis by increasing the level of ROSand promoting lipid peroxidation (LPO) in cancers cells. ML210-ansaFc has an anticancer activity and suppresses tumor growth in tumor 3D spheroids. ML210-ansaFc can be used for cancer therapy resistance research .
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- HY-151704
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Alkynes
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ICG-alkyne is a short-wave infrared (SWIR)-emitting cyanine fluorescent probe based on alkyne-derivatized indocyanine green. ICG-alkyne can undergo click chemistry reaction to conjugate with antibody molecules via binding to the azide groups introduced into antibodies. ICG-alkyne enables SWIR fluorescent molecular imaging of breast tumors in living mice. ICG-alkyne can be used in breast cancer-related research .
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- HY-W1123936D
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DBCO-PEG3400-Folate
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DBCO
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DBCO-PEG-FA (DBCO-PEG-Folate) (MW 3400) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
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- HY-168879
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Azide
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GPX4-IN-16 ((R)-9i) is a potent GPX4 inhibitor with an Kd value of 20.4 nM. GPX4-IN-16 shows cytotoxicity. GPX4-IN-16 shows anticancer activity .
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- HY-157411
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Alkynes
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anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
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- HY-W1123936H
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DBCO-PEG10000-Folate
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DBCO
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DBCO-PEG10000-FA (DBCO-PEG10000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
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- HY-W1123936E
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DBCO-PEG5000-Folate
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DBCO
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DBCO-PEG5000-FA (DBCO-PEG5000-Folate) is a multifunctional bioconjugation reagent, which is a copolymer of DBCO and Folic acid (FA) (HY-16637) and can target folate receptors (FR). Folate receptors are highly overexpressed on the surface of many cancer cells (such as lung cancer, nasopharyngeal cancer, ovarian cancer, etc.), but exhibit extremely low expression levels in normal tissues. DBCO-PEG-FA can be used for click chemistry conjugation via its DBCO terminal, and thus applies to various bioconjugation and drug delivery applications .
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- HY-175201
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Azide
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pro-FTY, a FTY720 (HY-12005) anticancer prodrug, is a sphingosine-1-phosphate (S1P) (HY-108496) inhibitor. pro-FTY specifically inhibits S1P signaling in cancer cells using a drug delivery system (DDS) that reacts with acrolein. pro-FTY significantly inhibits the survival of breast cancer cells, including multidrug-resistant cells and its organoids resistant to Paclitaxel (HY-B0015) or Doxorubicin (HY-15142A). pro-FTY potently suppresses tumor growth in 4T1 cells or organoids xenograft tumors mice model while avoiding lymphocytopenia .
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- HY-181447
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Alkynes
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GPX4 (S)-9i is a GPX4 inhibitor and ferroptosis inducer, with its (R) enantiomer exhibiting stronger activity. GPX4 (S)-9i can be used for the study of fibrosarcoma .
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상품명 |
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Classification |
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- HY-B1465
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Palmityl alcohol
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Emulsifiers
Surfactants
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1-Hexadecanol is a fatty alcohol, a lipophilic substrate. 1-Hexadecanol can be used for the research of ferroptosis .
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