Search Result
Results for "
tumor cell lines
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-11005
-
|
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PDK-1
Apoptosis
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Cancer
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BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis .
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-
-
- HY-14807
-
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CHR-2797
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Aminopeptidase
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Cancer
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Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines .
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-
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- HY-12449
-
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LY3039478
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Notch
γ-secretase
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Cancer
|
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Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested .
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-
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- HY-P99931
-
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GEN3013
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CD3
CD20
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Cancer
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Epcoritamab (GEN3013) is an bispecific IgG1 antibody redirecting T-cells toward CD3×CD20 + tumor cells. Epcoritamab induces potent T-cell-mediated cytotoxicity towards B-cell NHL cell lines .
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-
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- HY-132840
-
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AMG 650
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Kinesin
Microtubule/Tubulin
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Cancer
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Sovilnesib (AMG 650) is a potent, orally active kinesin-like protein KIF18A inhibitor with an IC50 value of 0.071 μM. Sovilnesib can be used for the research of cancer .
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-
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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-145899
-
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PKC
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Cancer
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PKN1/2-IN-1 is a potent cell permeabilizer and selective PKN1/2 inhibitor with IC50 values of 16 nM and 210 nM for PKN1 and PKN2, respectively, and Ki values of 8 nM and 108 nM, respectively. PKN1/2-IN-1 exhibits strong intracellular PKN2 binding capacity in NanoBRET assays (IC50 = 2.1 μM). PKN1/2-IN-1 can be used to study physiological processes such as tumor cell migration .
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-
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- HY-B0942
-
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Environmental Pollutants
nAChR
Bacterial
Apoptosis
Caspase
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Infection
Neurological Disease
Cancer
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Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo .
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-
-
- HY-50909
-
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KRX-0401; NSC 639966; D21266
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Akt
Autophagy
Apoptosis
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Cancer
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Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
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-
-
- HY-156112
-
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Ser/Thr Protease
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Cancer
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LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
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-
-
- HY-150617
-
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M4076; ATM Inhibitor-5
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ATM/ATR
STING
PD-1/PD-L1
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
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- HY-P9983
-
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SGN-33; HuM-195; GLK-33 Antibody
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Transmembrane Glycoprotein
Radionuclide-Drug Conjugates (RDCs)
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Inflammation/Immunology
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Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
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- HY-128587
-
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SY-1365
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CDK
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Cancer
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Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .
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-
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- HY-121250
-
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Fatty Acid Synthase (FASN)
Apoptosis
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Cancer
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Fasnall is a selective fatty acid synthase (FASN) inhibitor with an IC50 of 3.71 μM. Fasnall induces apoptosis in HER2 + breast cancer cell lines. Fasnall shows potent anti-tumor activities .
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-
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- HY-119198
-
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Apoptosis
Histone Methyltransferase
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Cancer
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NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers .
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-
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- HY-101870
-
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INCB053914
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Pim
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Cancer
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Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
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-
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- HY-101870B
-
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INCB053914 phosphate
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Pim
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Cancer
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Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
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-
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- HY-100395
-
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Apoptosis
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Cancer
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F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
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-
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- HY-157396
-
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Aurora Kinase
Apoptosis
Caspase
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Cancer
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JAB-2485 is an orally active and selective Aurora kinase A (AURKA) inhibitor with an IC50 value of 0.327 nM. JAB-2485 exhibits inhibitory activity against various tumor cell lines such as neuroblastoma, triple-negative breast cancer, small cell lung cancer, and epithelial ovarian cancer. JAB-2485 can induce cell cycle arrest and apoptosis in tumor cells. JAB-2485 has antitumor activity .
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-
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- HY-154984
-
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Histone Acetyltransferase
PROTACs
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Cancer
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JET-209 is a potent CBP/p300 PROTAC degrader, with DC50 values of 0.05 nM and 0.2 nM for CBP and p300. JET-209 demonstrates remarkable anti-tumor activity against various acute leukemia cell lines and effectively inhibits tumor growth in xenograft tumor models. JET-209 can be used for the study of acute leukemia .
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-
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- HY-144707
-
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Apoptosis
VEGFR
MMP
PTEN
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Cancer
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AK-778-XXMU is a potent DNA binding inhibitor 2 (ID2) antagonist with a KD of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and exhibits significant cancer-suppressing potency. AK-778-XXMU inhibits the ID2-KDR signaling axis, thereby down-regulating the downstream angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9), and up-regulating the tumor suppressor factor (PTEN). AK-778-XXMU can be used for the study of glioma .
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-
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- HY-119529
-
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3,8-Quinolinediol
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Tyrosinase
Bacterial
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Cancer
|
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Jineol is a cytotoxic alkaloid from the centipede Scolopendra subspinipes. Jineol exhibits modest cytotoxic activity in vitro against the growth of human tumor cell lines .
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- HY-P1632
-
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Bacterial
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Infection
Cancer
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Tachyplesin I is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I exhibits cytotoxic properties against various human tumor cell lines acting primarily by impairing the integrity of the outer cell membrane .
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-
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- HY-N6990
-
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Others
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Cancer
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Anhydrosecoisolariciresinol is from the flower of Wedelia biflora, has anti-tumor activities .
Anhydrosecoisolariciresinol decreases the growth of human breast cancer MCF-7 and MDA-MB-231 cell lines .
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-
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- HY-148413
-
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ISIS 3521 sodium
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PKC
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Cancer
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Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .
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-
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- HY-106588
-
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SKI 2053R
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DNA Alkylator/Crosslinker
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Cancer
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Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles .
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- HY-139453
-
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Drug Derivative
DNA Alkylator/Crosslinker
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Cancer
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LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
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- HY-123298
-
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Src
Akt
Apoptosis
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Cancer
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Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research .
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- HY-160843
-
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Apoptosis
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Cancer
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N-ω-chloroacetyl-L-ornithine (NCAO) is a potent reversible competitive ornithine decarboxylase (ODC) inhibitor that exerts cytotoxic and antiproliferative effects on tumor cell lines with EC50 values ranging from 1 to 50.6 µM. NCAO induces tumor cell Apoptosis and inhibits tumor cell migration in vitro. NCAO also exhibits a potent antitumor activity against both solid and ascitic tumors in a mouse model using the myeloma (Ag8) cell line. NCAO is promising for research of antitumor agents .
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- HY-101597
-
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Apoptosis
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Cancer
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NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP .
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- HY-130995
-
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Antibiotic
ADC Payload
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Infection
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Agrochelin, an alkaloid cytotoxic antibiotic, is produced by the fermentation of a marine Agrobacterium sp. Agrochelin has cytotoxic activity in tumor cell lines .
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- HY-125443
-
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Others
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Cancer
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Lucialdehydes A is a lanostante-type triterpene aldehydes, isolated from the fruiting bodies of Ganoderma lucidum. Lucialdehydes A shows cytotoxic effects on tumor cells, including Lewis lung carcinoma (LLC), T-47D, Sarcoma 180, and Meth-A tumor cell lines .
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- HY-N7611
-
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Others
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Cancer
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7-Prenyloxyaromadendrin is a flavonoid from Pterocaulon alopecuroides with antitumor activity. 7-Prenyloxyaromadendrin shows good antiproliferative activity in tumor cell lines .
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- HY-N9339
-
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(+)-Norglaucine
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Others
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Cancer
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Norglaucine ((+)-Norglaucine), a cytotoxic alkaloid, exhibits cytotoxicity towards the tumor cell lines B16-F10, HepG2, K562 and HL-60 cells .
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- HY-N6955
-
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Others
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Cancer
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Eupalinilide B is a guaiane type sesquiterpene lactone that can be found in Eupatorium lindleyanum. Eupalinilide B shows potent cytotoxicity against P-388 and A-549 tumor cell lines .
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- HY-129337
-
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Antibiotic
Fungal
Apoptosis
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Infection
Cancer
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Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity .
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- HY-N7205
-
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Others
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Cancer
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Glaucocalyxin D is a ent-kauranoid-type diterpenoid that can be isolated from Rabdosia japonica. Glaucocalyxin D shows cytotoxicity against various human tumor cell lines. Glaucocalyxin D can be used for cancer research .
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- HY-N11928
-
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Others
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Cancer
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Changnanic acid (schisandrin) is a triterpene compound with potential anti-tumor effects. Changnanic acid exhibits moderate cytotoxic activity against human tumor cell lines Bel-7402, MCF-7 and HL-60, with IC50s of 100 μM, 100 μM and 50.51 μM respectively .
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- HY-N10904
-
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Others
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Cancer
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Broussonol E is a diprenylated flavonol. Broussonol E can be isolated from the leaves of Broussonetia kazinoki. Unlike some dinonylated flavonol derivatives, Broussonol E has no cytotoxicity to human tumor cell lines (A549, HCT-8, KB) .
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- HY-118893
-
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Antibiotic
Bacterial
Fungal
Molecular Glues
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Infection
Cancer
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Asukamycin, a manumycin-type metabolite, could be isolated from Streptomyces nodosus subsp. asukaensis. Asukamycin is an antibiotic and has antimicrobial activity. Asukamycin inhibits growth of various tumor cell lines .
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-
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- HY-14815
-
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Combretastatin A4 phosphate
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Apoptosis
Microtubule/Tubulin
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Cancer
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Fosbretabulin (Combretastatin A4 phosphate) is a vascular disruptor with antitumor activity against atypical thyroid carcinoma (ATC) cell lines and xenografts. Fosbretabulin inhibits tumor growth by inhibiting microtubule polymerization, inducing apoptosis, and suppressing angiogenesis in tumors .
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- HY-N16580
-
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Others
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Cancer
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(+)-Lariciresinol 9′-p-Coumarate is a type of lignan. (+)-Lariciresinol 9′-p-Coumarate exhibits inhibitory activity against leukemia and other tumor cell lines .
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-
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- HY-154797
-
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Topoisomerase
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Cancer
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N,N-Dimethyldoxorubicin is a Doxorubicin (HY-15142A) analogue. N,N-Dimethyldoxorubicin shows cytotoxicity against a panel of tumor cell lines (IC50s < 0.3 μM) .
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-
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- HY-172364
-
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Polo-like Kinase (PLK)
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Cancer
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PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC50 of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research .
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-
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- HY-150753
-
-
-
- HY-122703
-
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Epigenetic Reader Domain
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Cancer
|
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BETi-211 is an orally active BET inhibitor (Ki: <1 nM). BETi-211 inhibits growth of triple-negative breast cancers (TNBC) cell lines with IC50 < 1 μM. BETi-211 degrades BET proteins and suppress tumor growth in xenograft breast tumors .
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-
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- HY-18652A
-
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Ro 5126766 potassium; CH5126766 potassium
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Raf
MEK
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Cancer
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Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC) .
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-
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- HY-125117
-
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DNA/RNA Synthesis
Bacterial
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Infection
Cancer
|
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Simocyclinone D8 is an anthracycline antibiotic with antibacterial and antitumor activity against Gram-positive bacteria. Simocyclinone D8 inhibits DNA gyrase and thus has an inhibitory effect on a variety of tumor cell lines .
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-
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- HY-161096
-
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ROR
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Cancer
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Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
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-
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- HY-12458
-
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DNA/RNA Synthesis
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Infection
Cancer
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Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml .
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- HY-10084
-
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Kinesin
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Cancer
|
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CK0106023 is a potent and specific allosteric inhibitor of KSP with a Ki value of 12 nM, showing antitumor activity. CK0106023 causes mitotic arrest and growth inhibition in several tumor cell lines. CK0106023 exhibits antitumor activity in tumor-bearing mice .
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- HY-114527
-
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Apoptosis
Stearoyl-CoA Desaturase (SCD)
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Cancer
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TPMP-I-2 is an anticancer agent that induces cancer cell lines Apoptosis and decreases protein levels of stearoyl-CoA desaturase. TPMP-I-2 prolongs the survival time of nude rats in a simulated micrometastatic cervical cancer model and reduces tumor growth in a breast cancer model in nude mice combined with immunotoxins .
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- HY-164645
-
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Ras
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Cancer
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pan-KRAS-IN-16 (Compound 3344) is an anti-RAS small molecule derived from an intracellular antibody fragment with pan-RAS-effector protein-protein interaction inhibitor properties. pan-KRAS-IN-16 binds to a hydrophobic pocket near to the effector-binding switch regions of RAS. pan-KRAS-IN-16 prevents endogenous RAS-dependent signaling in tumor cell lines .
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- HY-169078
-
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Histone Methyltransferase
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Cancer
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ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
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- HY-105172A
-
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CAP-232 TFA; TLN-232 TFA
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Somatostatin Receptor
Apoptosis
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Cancer
|
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TT-232 TFA (CAP-232 TFA) is an analogue of somatostatin. TT-232 TFA can induce apoptosis of pancreatic tumor cell lines, inhibit tyrosine kinase activity and stimulate tyrosine phosphatase activity in colon tumor cell lines. TT-232 TFA inhibits the proliferation of tumor cells, induces apoptosis of tumor cells and shows strong anti-tumor effects. TT-232 TFA can be used in the development of anti-tumor drugs and the study of apoptosis mechanism .
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- HY-N14293
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-
- HY-153272
-
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Biochemical Assay Reagents
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Cancer
|
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Antitumor agent-93 (compound 7D) is an anticancer agent that can effectively inhibit the growth of several tumor cell lines, such as MDA-MB-231 and HCT-116 cell lines .
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-
- HY-W848341
-
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NSC 338947; CIEtSoSo
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DNA Alkylator/Crosslinker
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Cancer
|
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Clomesone (NSC 338947) is a compound with antitumor activity. Clomesone induces the formation of cross-links between DNA strands in cell lines. Clomesone is inactive against most human colorectal cancer solid tumor cell lines in vitro, has no significant activity against mouse tumors in vivo, and is accompanied by bone marrow suppression. Its pharmacokinetic behavior indicates that it cannot reach effective concentrations at the tumor site.
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- HY-174512
-
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mRNA
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Cancer
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Human TNFSF8 mRNA encodes the human TNF superfamily member 8 (TNFSF8) protein, a cytokine that belongs to the tumor necrosis factor (TNF) ligand family. TNFSF8 was shown to enhance cell proliferation of some lymphoma cell lines, while to induce cell death and reduce cell proliferation of other lymphoma cell lines.
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- HY-130996
-
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ADC Payload
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Cancer
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Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines .
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- HY-B1714A
-
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Drug Derivative
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Cancer
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NSC 601980 is an anti-tumor compound. In yeast screening experiments, NSC 601980 inhibits cell proliferation in COLO205 and HT29 cell lines with LogGI50 of -6.6 and -6.9, respectively.
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- HY-W773183
-
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Betulonic acid methyl ester; Methyl 3-oxolup-20(29)-en-28-oate
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Drug Intermediate
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Cancer
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Methyl betulonate (Betulonic acid methyl ester) is a triterpenoid. Methyl betulonate inhibits cell growth of eight tumor (including resistant) and two normal fibroblast cell lines with the IC50s >50.0 μM .
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- HY-N10265
-
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Endogenous Metabolite
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Cancer
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Stephacidin B is a fungal metabolite. Stephacidin B shows in vitro cytotoxicity against a panel of human tumor cell lines. Stephacidin B shows the strongest cytotoxicity against testosterone-dependent prostate LNCaP cancer cells .
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- HY-136824
-
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Bacterial
Antibiotic
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Infection
Cancer
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Napyradiomycin A1 is one enantioselective compound of napyradiomycins. napyradiomycins are an intriguing family of halogenated natural products with activity against several tumor cell lines as well as some bacterial strains .
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- HY-123143
-
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MLN576
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Topoisomerase
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Cancer
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XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM) .
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- HY-173515
-
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FAK
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Cancer
|
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FAK-IN-26 is a BBB-penetrable Focal Adhesion Kinase (FAK) inhibitor (IC50: 0.87 nM). FAK-IN-26 significantly suppresses tumor cell viability, cancer stem cell activity, and cell migration in A549 and SKOV-3 cell lines. FAK-IN-26 has potent anti-cancer activity in A549 and SKOV-3 tumor mice models with tumor inhibition rates of 59.15 % and 57.9 % .
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- HY-N3215
-
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Others
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Others
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Nagilactone C is a diterpene dilactone compound isolated from Podocarpus neriifolius. Nagilactone C has potent antiproliferative activity against human fibrosarcoma and murine colon carcinoma tumor cell lines .
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- HY-P1632A
-
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Bacterial
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Infection
Cancer
|
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Tachyplesin I TFA is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I TFA exhibits cytotoxic properties against various human tumor cell lines acting primarily by impairing the integrity of the outer cell membrane .
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- HY-117803
-
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OSI-461 free base
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Apoptosis
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Cancer
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CP 461 free base (OSI-461 free base) is a novel pro-apoptotic compound with the activity of inhibiting cyclic guanosine monophosphate phosphodiesterase. CP 461 free base exhibits growth inhibitory activity against a variety of human tumor cell lines in vitro. CP 461 free base selectively induces apoptosis in cancer cell lines but has no effect on normal cells. CP 461 free base can be used in the study of renal cell carcinoma, prostate cancer and Crohn's disease .
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- HY-P2088
-
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Des-N-tetramethyltriostin A
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Antibiotic
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Cancer
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TANDEM (Des-N-tetramethyltriostin A) is a synthetic antibiotic drug that has the activity of inhibiting the growth of tumor cells. TANDEM can be used in combination with chemotherapy to enhance the inhibitory effect. TANDEM has shown significant inhibitory effects on a variety of cancer cell lines in in vitro experiments. The structure of TANDEM allows it to effectively target tumor cells during the inhibition process. TANDEM's mechanism of action involves interfering with cell proliferation and survival pathways .
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- HY-N12430
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Others
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Cancer
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Marsdenoside A (compound 7) is a Marsdenoside isolated from Alocasia genus. Marsdenoside A has a weak growth inhibitory effect on two tumor cell lines, MGC-803 and HT-29, with IC50 >50 μg/mL.
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- HY-P991555
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TNF Receptor
Apoptosis
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Cancer
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XmAb5485 is an Fc-engineered humanized anti-CD40 monoclonal antibody with high affinity to Fc-γ receptors. XmAb5485 induces potent antibody-dependent cell-mediated cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP) against tumor cells. XmAb5485 inhibits proliferation and induces apoptosis of tumor cells. XmAb5485 shows highly cytotoxic against lymphoma, leukemia and multiple myeloma cell lines as well as primary cancer cells .
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- HY-N14892
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Bacterial
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Infection
Cancer
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Cetoniacytone A has weak activity against Gram-positive and negative bacteria. Cetoniacytone A can inhibit the growth of HEPG2 and MCF7 human tumor cell lines, with GI50 values of 3.2 μM .
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- HY-N14369
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Bacterial
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Infection
Cancer
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9-Hydroxycrisamicin has weak anti-Gram-positive bacteria activity, MIC is 6.25-25 μg/mL. 9-Hydroxycrisamicin has a strong growth inhibitory effect on human tumor cell lines .
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- HY-N15055
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Antibiotic
Bacterial
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Infection
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Propeptin is a peptide antibiotic composed of 19 amino acids. Propeptin has weaker activity against Pseudomonas aeruginosa, Mycobacterium monobacterium, and Xanthomonas oryzae. Propeptin has no effect on KB and L1210 cells of tumor cell lines, but has an inhibitory effect on prolyl endopeptidase .
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- HY-162148
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EGFR
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Cancer
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HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis .
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- HY-148827
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HYBO-165
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PKA
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Cancer
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GEM231 is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
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- HY-148827A
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HYBO-165 sodium
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PKA
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Cancer
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GEM231 sodium is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 sodium induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
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- HY-122315
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NSC-741909
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JNK
Apoptosis
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Cancer
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Oncrasin-60 (NSC-741909) is a compound with antitumor activity that is active against multiple cancer cell lines in vitro and can induce tumor regression in vivo, with its mechanism involving JNK activation and STAT3 inhibition.
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- HY-50909R
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KRX-0401 (Standard); NSC 639966 (Standard); D21266 (Standard)
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Akt
Autophagy
Apoptosis
Reference Standards
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Cancer
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Perifosine (Standard) is the analytical standard of Perifosine. This product is intended for research and analytical applications. Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
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- HY-137831
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Apoptosis
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Cancer
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TLBC, a boronic-chalcone derivative, shows a dose-dependent inhibition with IC50 values of 5.5-25.5 μM in various glioma cell lines. TLBC induces apoptosis independent of changes to the tumor suppressor p53 .
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- HY-170594
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Atg7
Autophagy
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Cancer
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Antitumor agent-192 (Compound 2f) is a β-carboline antitumor agent. Antitumor agent-192 induces autophagy in HCT116 cells via the ATG5/ATG7 pathway. Antitumor agent-192 has an IC50 of less than 5 μM for human tumor cell lines and significantly inhibits tumor development and reduces tumor weight in a mouse colorectal cancer model transplanted with allografts [1].
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- HY-N12128
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Others
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Cancer
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Ophiopogonin R (compound 3) is a steroid saponin. Ophiopogonin R was isolated and purified from natural ophiopogonin. Ophiopogonin R was not cytotoxic to five human tumor cell lines (HepG2, HLE, BEL7402, BEL7403 and Hela) .
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- HY-108352
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VCE 004
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Topoisomerase
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Cancer
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HU 331 (HU 331) is a highly specific Topoisomerase II inhibitor with anticancer activity. HU 331 has shown promising inhibitory effects on human cancer cell lines in vitro and human tumor xenografts in nude mice in vivo .
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- HY-146250
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Microtubule/Tubulin
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Cancer
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Antitumor Agent-71 is an antiproliferative activity antitumor agent and against tumor cell lines with IC50 values ranging from 3.98-15.70 μM. Antitumor Agent-71 is an antitumor agent that can inhibit tubulin polymerization.
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- HY-W854934
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Microtubule/Tubulin
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Cancer
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IKP-104 is a microtubule/tubulin inhibitor (IC50 = 1.31 μM). IKP-104 arrests cells in mitosis and the M phase by inhibiting microtubule polymerization and inducing cytoskeletal microtubule depolymerization. IKP-104 inhibits the growth of mouse and human tumor cell lines. IKP-104 exhibits anti-tumor effects in mouse ascites tumors and lung cancer models. IKP-104 is useful in the research of cancers such as leukemia, lung cancer and melanoma .
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- HY-N12437
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Others
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Cancer
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Marsdenoside B (compound 8) is a Marsdenoside isolated from Alocasia genus. Marsdenoside B inhibits the growth of tumor cell lines MGC-803 and HT-29 with IC50s of 25.6 μg/mL and 32.4 μg/mL, respectively.
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- HY-117520
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Proteasome
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Cancer
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FV-162 is a potent, orally active and irreversible proteasome inhibitor. FV-162 exhibits cytotoxic to human myeloma cell lines and primary myeloma cells. FV-162 inhibits tumor growth in a myeloma xenograft mouse model. FV-162 can be used for myeloma research .
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- HY-174392
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Biochemical Assay Reagents
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Cancer
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Anticancer agent 275 is a natural product that has potent anticancer activity. Anticancer agent 275 shows strong proliferation inhibition activity against BT12 cells. Anticancer agent 275 can be studied in research for rare and aggressive atypical teratoid rhabdoid tumor (ATRT) and other cancer cell lines .
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- HY-N18195
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Others
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Cancer
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Trichilin B is a limonoid compound found in the twigs and leaves of Trichilia connaroides. Trichilin B exhibits no in vitro cytotoxic activity against tumor cell lines .
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- HY-101597R
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Reference Standards
Apoptosis
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Cancer
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NVX-207 (Standard) is the analytical standard of NVX-207 (HY-101597). This product is intended for research and analytical applications. NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP .
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- HY-101870BR
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INCB053914 phosphate (Standard)
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Reference Standards
Pim
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Cancer
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Uzansertib phosphate (Standard) is the analytical standard of Uzansertib phosphate (HY-101870B). This product is intended for research and analytical applications. Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
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- HY-181848
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DNA-PK
Apoptosis
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Cancer
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DNA-PK-IN-16 is an orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 of 10.2 nM. DNA-PK-IN-16 induces the upregulation of γH2A.X, a biomarker of DNA double-strand breaks. DNA-PK-IN-16 exhibits antiproliferative activity in various cancer cell lines. DNA-PK-IN-16 enhances the infiltration of CD8 + T cells in tumor tissues through synergistic action with anti-PD-L1 monoclonal antibody. DNA-PK-IN-16 is applicable for cancer research .
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- HY-114639
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Others
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Others
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Maritinone is a compound with antiproliferative activity and exhibits strong cytostatic activity in various tumor cell lines.
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- HY-181996
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Btk
Caspase
Apoptosis
PARP
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Cancer
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BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies .
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- HY-120187
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Others
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Others
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DDCPPB-Glu (compound 3a) is a compound with anti-tumor activity, which has the activity of inhibiting tumor cell growth and prolonging survival. DDCPPB-Glu has growth inhibition effect on various tumor cell lines, can increase the survival time of leukemia mice, and has inhibitory effect on tumors such as colon cancer and lung cancer.
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- HY-176058
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HDAC
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Cancer
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HDAC6-IN-57 (compound 9c) is an HDAC6 inhibitor with an IC50 value of 7 nM. HDAC6-IN-57 inhibits 60 cancer cell lines with a mean GI50 of 2.64 μM while exhibiting significantly lower cytotoxicity towards non-tumor cell lines .
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- HY-N14893
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Others
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Cancer
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Cetoniacytone B can inhibit the growth of HEPG2 and MCF7 human tumor cell lines, with GI50 values of 4.4 μM .
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- HY-182397
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Cyclophilin
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Cancer
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ZX-J-19L is a CyPJ inhibitor with inhibitory activity against a variety of tumor cell lines. ZX-J-19L inhibits the growth of human liver cancer cells, human breast cancer cells, ovarian cancer cells and prostate cancer cells in vitro. ZX-J-19L can be used for tumor research .
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- HY-181756
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-175164
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Apoptosis
c-Myc
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Cancer
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SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC .
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- HY-N7623
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Drug Derivative
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Cancer
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Ursonic acid methyl ester is an esterified derivative of Ursolic acid (HY-N0140). Ursonic acid methyl ester shows growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela with ED50 values of >100 µg/ml .
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- HY-N12141
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Apoptosis
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Inflammation/Immunology
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Flaccidoside II inhibits proliferation and induces apoptosis in Malignant peripheral nerve sheath tumors (MPNSTs) cell lines. Flaccidoside II ameliorates collagen-induced arthritis in mice. Flaccidoside II is an active triterpenoid saponin constituent from Anemone flaccida rhizome .
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- HY-136910
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USP7-IN-7
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Deubiquitinase
MDM-2/p53
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Cancer
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USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
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- HY-115537
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Apoptosis
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Cancer
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NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo .
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- HY-174341
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Transmembrane Glycoprotein
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Cancer
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CD39-IN-1 is a selective CD39 inhibitor with an IC50 value of 68.7 nM. CD39-IN-1 exerts antiproliferative effects on tumor cells and shows low toxicity to normal cell lines. CD39-IN-1 inhibits CD39-mediated eATP hydrolysis in the ATP-adenosine pathway. CD39-IN-1 is applicable for tumor-related research .
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- HY-150617A
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(Rac)-M4076; (Rac)-ATM Inhibitor-5
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ATM/ATR
STING
PD-1/PD-L1
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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(Rac)-Lartesertib ((Rac)-M4076) is an isoform of Lartesertib (HY-150617). Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
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- HY-146819
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Carbonic Anhydrase
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Cancer
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Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
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- HY-118899
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Endogenous Metabolite
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Cancer
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XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
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- HY-16261
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INNO-206; DOXO-EMCH
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Topoisomerase
ADC Payload
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Cancer
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Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-N6679
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Antibiotic
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Cancer
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(R)-10,11-Dehydrocurvularin is a secondary metabolite isolated from Curvularia sp.. (R)-10,11-Dehydrocurvularin displays concentration-dependent cytotoxicity towards human tumor cell lines
with a mean IC50 value of 1.25 µM .
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- HY-16261C
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INNO-206 hydrochloride; DOXO-EMCH hydrochloride
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Topoisomerase
ADC Payload
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Cancer
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Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-149375
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 37 (Compound 12) is a Tubulin inhibitor that can effectively inhibit Tubulin aggregation (IC50=1.3 µM). Tubulin inhibitor 37 exhibits antiproliferative activity against human tumor cell lines and has potential for studying cancer .
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- HY-136959
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HDAC
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Cancer
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M133 is a HDAC1 and HDAC2 selective inhibitor which shows potent antiproliferative activity against diverse human tumor cell lines with IC50s of 0.75-1.94 μM. M133 can be used for cancer research .
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- HY-125664
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Antibiotic
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Cancer
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Lucialdehyde B is a tetracyclic triterpene isolated from the substrates of Ganoderma lucidum with antiviral and cytotoxic activities. Lucialdehyde B has cytotoxic effects against Lewis lung cancer (LLC), T-47D, Sarcoma 180 and Meth-A tumor cell lines .
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- HY-175857
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HDAC
Apoptosis
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Cancer
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HDAC-IN-92 is a pan-HDAC inhibitor with an IC50 of 12.58 µM in A2780 cells. HDAC-IN-92 demonstrates broad-spectrum, notable cytotoxic activity against a range of human cancer cell lines, including ovarian, liver, and breast carcinomas. HDAC-IN-92 causes apoptosis and demonstrates a notable decrease in tumor cell colony formation. HDAC-IN-92 inhibits the formation of blood vessels in the chick chorioallantoic membrane (CAM). HDAC-IN-92 exhibits anti-tumor effect in a 4T1 tumor-bearing mouse model. HDAC-IN-92 can be used for research targeting solid tumor .
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- HY-18614
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Notch
γ-secretase
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Cancer
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LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibits Notch signalling in tumor cell lines and endothelial cells (IC50=0.005-20 nM). LY900009 can be used for advanced cancer research .
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- HY-115735
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SphK
Apoptosis
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Cancer
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SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines .
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- HY-167880
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Macrophage migration inhibitory factor (MIF)
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Cancer
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BMY-25551 is a Mitomycin A (HY-130332) analogue that is 8 to 20 times more potent than Mitomycin C (HY-13316) in cytotoxicity to murine and human tumor cell lines. BMY-25551 can be utilized in cancer and hematologic depression research .
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- HY-165245
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Transmembrane Glycoprotein
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Cancer
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SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
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- HY-145406
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Adenosine Receptor
HDAC
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Inflammation/Immunology
Cancer
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IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
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- HY-101667
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LTURM34
5 Publications Verification
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DNA-PK
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Cancer
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LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines .
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- HY-146366
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
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- HY-N18186
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Others
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Cancer
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Neojiangyouaconitine is a diterpenoid alkaloid cytotoxin isolated from Aconitum soongaricum var. pubescens. Neojiangyouaconitine exhibits cytotoxic activity against human breast cancer, prostate cancer and lung cancer cells, with weak inhibitory effect on HeLa cells. Neojiangyouaconitine has the ability to kill specific tumor cell lines and can be applied to the research on the mechanisms of related cancers such as breast cancer, prostate cancer and lung cancer .
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- HY-170812
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Aurora Kinase
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Cancer
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BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .
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- HY-173133
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Autophagy
Atg7
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Cancer
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Antitumor agent-199 (Compound 4b) is an antitumor agent. Antitumor agent-199 exhibits significant antiproliferative activity against multiple tumor cell lines. Antitumor agent-199 can induce autophagy in cancer cells via the ATG5/ATG7 pathway and can be used in the study of cancer .
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- HY-122829
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PROTACs
BCL6
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Cancer
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BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research .
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- HY-109583
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4-Oxo-4-HPR
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Apoptosis
Reactive Oxygen Species (ROS)
Drug Metabolite
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Cancer
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4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
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- HY-178941
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Dihydroorotate Dehydrogenase
Apoptosis
Caspase
Reactive Oxygen Species (ROS)
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Cancer
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DHODH-IN-32 (Compound A1) is a DHODH inhibitor. DHODH-IN-32 shows significant cytotoxicity against NCI-60 cell lines, especially being sensitive to breast cancer, prostate cancer and leukemia cell lines. DHODH-IN-32 can induce cell apoptosis by activating the Caspase pathway. DHODH-IN-32 causes G0/G1 phase cell cycle arrest and inhibits cellular metabolism by ROS. DHODH-IN-32 exhibits significant anti-tumor properties in mouse breast cancer models. DHODH-IN-32 can be used for the study of breast cancer .
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- HY-164411
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c-Met/HGFR
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Cancer
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KRC-00715 is an effective oral c-Met inhibitor with an IC50 of 9.0 nM, demonstrating high selectivity in gastric cancer cells. KRC-00715 specifically inhibits the growth of c-Met-highly expressed cell lines by inducing G1/S phase arrest, leading to a reduction in downstream signaling pathways, including Akt and Erk, as well as c-Met activity. KRC-00715, in the gastric cancer cell line Hs746, is characterized by an IC50 of 39 nM, and it selectively inhibits the proliferation of c-Met-highly expressed cell lines. KRC-00715 reduces tumor size in Hs746T xenograft mouse models .
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- HY-N15714
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Drug Derivative
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Cancer
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Acoraminol A is one of the stereoisomers of phenylpropanoids, the other of which is Acoraminol B (HY-N15715), which can be isolated from the methanol extract of the rhizome of Acorus tatarinowii. Acoraminol A has weak cytotoxic effects on several human tumor cell lines (IC50>30 μM) .
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- HY-185347
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- HY-155073
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines,and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines) .
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- HY-P4056
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P15-Tat
|
Casein Kinase
Apoptosis
|
Cancer
|
|
CIGB-300 (P15-Tat) is an anti-casein kinase 2 (CK2) peptide that exhibits anticancer properties by interfering with the phosphorylation of protein kinase CK2. CIGB-300 induces apoptosis in multiple tumor cell lines and can be used in cancer research .
|
-
- HY-N15112
-
|
|
Others
|
Cancer
|
|
Pintulin can inhibit P388, L 1210, HL-60, KB and other tumor cell lines with IC50s (μg/mL) of 0.8, 0.8, 0.8, 0.25, respectively. Pintulin has only very weak antibacterial activity against the microorganisms tested .
|
-
- HY-P4056A
-
|
P15-Tat acetate
|
Casein Kinase
Apoptosis
|
Cancer
|
|
CIGB-300 acetate (P15-Tat acetate) is an anti-casein kinase 2 (CK2) peptide that exhibits anticancer properties by interfering with the phosphorylation of protein kinase CK2. CIGB-300 acetate induces apoptosis in multiple tumor cell lines and can be used in cancer research .
|
-
- HY-162105
-
|
|
Cytochrome P450
|
Endocrinology
Cancer
|
|
Aromatase-IN-3 (compound 7d) is an aromatase inhibitor with an IC50 of 54 nM. Through suppressing the conversion of androstenedione to oestrogen caused by aromatase, Aromatase-IN-3 exerts an appreciable tumor growth inhibitory activities against breast cancer cell lines, suggesting its usage for ER+ cancer research .
|
-
- HY-N15715
-
|
|
Drug Derivative
|
Cancer
|
|
Acoraminol B is one of the stereoisomers of phenylpropanoids, the other of which is Acoraminol A (HY-N15714), which can be isolated from the methanol extract of the rhizome of Acorus tatarinowii. Acoraminol B has weak cytotoxic effects on several human tumor cell lines (IC50>30 μM) .
|
-
- HY-120599A
-
|
VERU-111 hydrochloride; ABI-231 hydrochloride
|
Microtubule/Tubulin
Apoptosis
HPV
Endogenous Metabolite
|
Cancer
|
|
Sabizabulin hydrochloride is a potent orally bioavailable microtubule inhibitor with activity that interacts with the colchicine binding site. Sabizabulin hydrochloride demonstrated significant inhibition of melanoma tumor growth with an average IC50 of 5.2 nM in melanoma and prostate cancer cell lines. Pharmacological screening of Sabizabulin hydrochloride shows it has a low risk of potential side effects .
|
-
- HY-12965B
-
|
|
TAM Receptor
|
Cancer
|
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
|
-
- HY-15096
-
|
FJ-776
|
Fluorescent Dye
HSP
|
Cancer
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-N1691
-
|
3-Epilycoclavanol
|
Others
|
Cancer
|
|
3-Epilycoclavanol (3-Epilycoclavanol) is a triterpenoid antitumor agent that can be extracted from the dried whole plant of Lycopodium japonicum (a plant of the Lycopodium genus in the Lycopodiaceae family). 3-Epilycoclavanol inhibits human tumor A549 and K562 cell lines at concentrations of 10-100 μg/mL .
|
-
- HY-158974
-
|
|
DNA/RNA Synthesis
Apoptosis
PARP
|
Cancer
|
|
YTHDC1-IN-1 is a selective YTHDC1 inhibitor with a Kd of 49 nM and an IC50 of 0.35 μM. YTHDC1-IN-1 can inhibit the proliferation and induce apoptosis of acute myeloid leukemia cell lines. YTHDC1-IN-1 has anti-tumor activity .
|
-
- HY-N14530
-
|
|
Bacterial
|
Infection
Cancer
|
|
Cremeomycin has anti-Gram-positive bacteria activity including methicillin-resistant Staphylococcus aureus (MRSA), MIC is 0.2-0.39 μg/mL. Cremeomycin shows cytotoxicity to mouse tumor cell lines P388, L1210, IMC, S180, B16 and SS3 in vitro .
|
-
- HY-N14144
-
|
|
Bacterial
|
Infection
Cancer
|
|
Cremimycin has anti-Gram-positive bacteria activity including methicillin-resistant Staphylococcus aureus (MRSA), MIC is 0.2-0.39 μg/mL. Cremimycin shows cytotoxicity to mouse tumor cell lines P388, L1210, IMC, S180, B16 and SS3 in vitro .
|
-
- HY-N4201
-
|
|
EGFR
Src
|
Cancer
|
|
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermum erythrorhizon, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells .
|
-
- HY-N2040
-
|
|
Bacterial
Interleukin Related
|
Infection
Inflammation/Immunology
Cancer
|
|
(20R)-Protopanaxadiol is a metabolite of ginsenosides. (20R)-Protopanaxadiol has anti-inflammatory and antibacterial activities, but shows no significant cytotoxicity against tumor cell lines. In addition, (20R)-Protopanaxadiol can inhibit the uptake of 2-deoxy-D-glucose (2-DG) .
|
-
- HY-172795
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-158 (compound 12e) is an orally active EGFR inhibitor with an IC50 of 0.22 nM for EGFR(Del19/T790M). EGFR-IN-158 inhibits phosphorylation and downstream signaling by binding to EGFR, thereby inhibiting the proliferation of tumor cell lines and promoting apoptosis .
|
-
- HY-N6061
-
|
|
Others
|
Cancer
|
|
Ophiopogonin C, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin C shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 19.76 μM and 15.51 μM, respectively .
|
-
- HY-137605
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC50 values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively .
|
-
- HY-120574
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
|
-
- HY-163062
-
|
|
Microtubule/Tubulin
Apoptosis
Complement System
|
Cancer
|
|
Tubulin/NRP1-IN-1 (compound TN-2) is a dual inhibitor of Tubulin and NRP1 with IC50s of 0.71 and 0.85 μM, respectively. Tubulin/NRP1-IN-1 significantly inhibits the viability of prostate tumor cell lines and induces apoptosis .
|
-
- HY-146316
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases .
|
-
- HY-123045
-
|
|
CDK
|
Cancer
|
|
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
|
-
- HY-120275
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
|
-
- HY-P99361
-
|
PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
|
TNF Receptor
|
Cancer
|
|
Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
|
-
- HY-136420
-
|
|
PROTACs
Raf
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
SJF-0628 is a RAF PROTAC degrader. SJF-0628 induces targeted degradation of BRAF in various cancer cell lines (colorectal cancer cell lines (Colo-205, LS-411N, HT-29, RKO) and triple-negative breast cancer cell line DU-4475). SJF-0628 decreases pMEK and pErk levels in DU-4475 cells. SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of colorectal cancer and triple-negative breast cancer. (Pink: RAF ligand (HY-12057), Blue: VHL Ligand ( HY-125845), Black: Linker (HY-B0912)) .
|
-
- HY-146454
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Antiproliferative agent-6 (compound 8a) is a potent antitumor agent. Antiproliferative agent-6 has antiproliferative activity against cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively .
|
-
- HY-175481
-
|
|
Cannabinoid Receptor
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
CB2R agonist 4 is a cannabinoid receptor 2 (CB2R) agonist with an EC50 value of 6.9 μM. CB2R agonist 4 can induce cell apoptosis, ROS production and protein misfolding. CB2R agonist 4 shows cytotoxicity to a panel of tumor cell lines. CB2R agonist 4 can be used for the research of cancer .
|
-
- HY-P11050A
-
|
|
Apoptosis
|
Cancer
|
|
SP94 is a peptide ligand with high specificity for hepatocellular carcinoma cells. SP94 selectively binds to multiple hepatocellular carcinoma cell lines in vitro. SP94 inhibits tumor growth in a mouse model of hepatocellular carcinoma by promoting apoptosis and reducing angiogenesis. SP94 can be used as a specific probe for hepatocellular carcinoma imaging. SP94 is useful for hepatocellular carcinoma research .
|
-
- HY-180158
-
|
|
Parasite
Reactive Oxygen Species (ROS)
|
Infection
Cancer
|
|
Antitrypanosomal agent 28 (Compound 2a) is a trypanocidal agent. Antitrypanosomal agent 28 effectively inhibits Trypanosoma cruzi by inducing the generation of ROS and mitochondrial damage, with an IC₅₀ of 49.4 μM. Antitrypanosomal agent 28 exhibits broad-spectrum anti-tumor activity against various tumor cell lines, especially being sensitive to leukemia, colon cancer, and breast cancer. Antitrypanosomal agent 28 can be used for research on anti-cancer and anti-trypanosome activities .
|
-
- HY-N15636
-
|
(-)-Coccinine
|
Serotonin Transporter
P-glycoprotein
|
Neurological Disease
Cancer
|
|
Coccinine ((-)-Coccinine) is a weak inhibitor of SERT (IC50: 196.3 μM; Ki: 106.8 μM) and P-gp (IC50: 0.96 mM). Coccinine exhibits significant anti-tumor activity against various cancer cell lines, such as breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Coccinine can be used in the research of tumors and neurological diseases .
|
-
- HY-161324
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
|
-
- HY-N10354
-
|
|
Apoptosis
|
Cancer
|
|
27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively .
|
-
- 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-161824
-
|
|
Drug Intermediate
|
Cancer
|
|
Antiproliferative agent-52 (Compound 4a) is an antiproliferative agent that exhibits significant antiproliferative activity against four human tumor cell lines (A549, A2780, SKOV3, HCC827), with IC50 values ranging from 5.83 to 8.63 nM. Antiproliferative agent-52 can be used in cancer research .
|
-
- HY-N12834
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato .
|
-
- HY-182064
-
|
|
EGFR
NO Synthase
COX
NF-κB
Interleukin Related
Apoptosis
|
Cancer
|
|
EGFR-IN-206 is an orally active EGFR inhibitor. EGFR-IN-206 inhibits the phosphorylation of the key tumor growth protein EGFR, and suppresses the proliferation, migration and invasion of EGFR triple-mutant tumor cell lines. EGFR-IN-206 downregulates the expression of inflammation-related proteins iNOS, COX-2 and NF-κB (p65). EGFR-IN-206 promotes the secretion of NO. EGFR-IN-206 reduces the secretion of IL-6. EGFR-IN-206 induces apoptosis (apoptosis) of EGFR triple-mutant tumor cells. EGFR-IN-206 exerts antitumor activity in EGFR triple-mutant mice. EGFR-IN-206 is applicable to the research of non-small cell lung cancer .
|
-
- HY-163435
-
|
|
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
|
Anticancer agent 201 (Compound 2f) has IC50 values in the low micromolar range for multiple tumor cell lines. Anticancer agent 201 is highly cytotoxic to CCRF-CEM cells in vitro, inducing apotosis by activating caspase-3 in the intrinsic mitochondrial pathway and lysis of PARP, as well as reducing the expression of Bcl-2 and Bcl-XL proteins. Anticancer agent 201 can be used in cancer research .
|
-
- HY-W106860
-
|
|
Drug Intermediate
|
Cancer
|
|
9H-Carbazole-3-carbaldehyde is an anticancer agent that can be isolated from the stems of Lansium parasiticum (Lour.) Skeels. 9H-Carbazole-3-carbaldehyde shows significant cytotoxic activity in a variety of tumor cell lines, especially against H1299 and SMMC-7721 lung cancer cells with IC50 values of 6.19-26.84 μg/mL .
|
-
- HY-146462
-
|
|
Apoptosis
ROS Kinase
|
Cancer
|
|
Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
|
-
- HY-146565
-
|
|
DNA-PK
|
Cancer
|
|
DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
|
-
- HY-170905S
-
-
- HY-P99413
-
|
ASP1650
|
HCV
|
Cancer
|
|
IMAB027 (ASP1650) is a specific anti-CLDN6 mAb, while CLDN6 (Claudin 6) is a tight junction membrane protein, aberrantly expressed in various human cancer types, ovarian cancers particularly. IMAB 027 shows anti-tumor activity, and induces apoptosis in CLDN6 + ovarian and testicular cancer cell lines .
|
-
- HY-128910
-
|
|
Drug-Linker Conjugates for ADC
Microtubule/Tubulin
|
Cancer
|
|
MC-VC(S)-PABQ-Tubulysin M is a synthetic ADC drug-linker conjugate composed of the tubulin polymerization inhibitor Tubulysin M (an ADC Cytotoxin) (HY-N7053) and MC-VC(S)- PABQ (an ADC linker) is connected. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors .
|
-
- HY-12447
-
|
|
MEK
Apoptosis
|
Cancer
|
|
SMK-17 is a selective, non-ATP-competitive MEK1/MEK2 inhibitor with IC50s of 62 nM and 56 nM, respectively. SMK-17 binds to the allosteric pocket of MEK1/2. SMK-17 induces apoptosis in tumor cell lines harboring β-catenin mutations .
|
-
- HY-15205
-
Ganetespib
Maximum Cited Publications
42 Publications Verification
STA-9090
|
HSP
Apoptosis
|
Cancer
|
|
Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
|
-
- HY-124083
-
|
|
Microtubule/Tubulin
Apoptosis
Caspase
Mitochondrial Metabolism
|
Cancer
|
MPT0B214 is a microtubule inhibitor that strongly binds to the colchicine binding site of tubulin, preventing tubulin polymerization. MPT0B214 induces apoptosis through a mitochondrial/caspase 9 dependent pathway and shows cytotoxicity across various human tumor cell lines. MPT0B214 can be used for cancer research .
|
-
- HY-19542S1
-
|
C6-Cer-d11; N-Hexanoylsphingosine-d11
|
Apoptosis
Isotope-Labeled Compounds
|
Cancer
|
|
C6 Ceramide-d11 is deuterated labeled C6 Ceramide (HY-19542). C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
|
-
- HY-170965
-
|
|
CDK
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC50 range of 7.5-33.67 μM.
Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines.
Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins.
Anticancer agent 264 can be used for research in the field of cancer-related diseases .
|
-
- HY-101741
-
|
A-289099
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
A-259745 is an orally active antimitotic agent that binds to the colchicine-binding site of tubulin. A-259745 exhibits potent in vitro cytotoxic activity against both multi-drug-resistant and non-multi-drug-resistant cancer cell lines, with ED50 values of 0.018 μM against HCT-15 and 0.028 μM against NCI-H460 cell lines. A-259745 inhibits tubulin polymerization, disrupts the dynamic equilibrium of the mitotic spindle, arrests dividing cells in metaphase, and subsequently induces apoptosis. A-259745 shows dose-dependent antitumor efficacy in murine tumor models. A-259745 can be used for the study of cancer .
|
-
- HY-182349
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bax activator-2 (compound 27c) is a pro-apoptotic agent targeting BAX, with an IC50 of 0.30 μmol/L against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, caspase-3/9 cleavage and PARP cleavage, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against various cancer cell lines, shows reduced cytotoxicity in BAX-knockout A549 cells, and has low cytotoxicity against non-cancerous cell lines. Bax activator-2 can be used in studies related to acute myeloid leukemia and solid tumors .
|
-
- HY-15882
-
|
|
Endogenous Metabolite
|
Cancer
|
|
GNE-783 is a selective CHK1 inhibitor that enhances the activity of gemcitabine. GNE-783 improves the efficacy of anti-metabolite DNA damage drugs by inactivating S-phase and G2-phase cell cycle checkpoints following DNA damage. GNE-783 selectively enhances the chemical synergy of certain drugs in different tumor types, for example, enhancing the activity of temozolomide only in melanoma cell lines .
|
-
- HY-N15614
-
|
|
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 .
|
-
- HY-172449
-
|
|
Hedgehog
|
Cancer
|
|
GLI1-IN-3 (Compound 11a), a triterpenoid analogue, can inhibit Hedgehog signaling in GLI1 overexpression cancer cells. GLI1-IN-3 inhibits the proliferation in NSCLC and prostate cancer cell lines exhibiting hyper-activated Hh signaling. GLI1-IN-3 can also decrease the expression of endogenous GLI1 protein and its target genes associated with tumor progression and proliferation in A549 and DU-145 cancer cells .
|
-
- 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-101849
-
|
|
GLUT
TNF Receptor
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
|
-
- HY-177345
-
|
|
Sigma Receptor
Apoptosis
Caspase
|
Cancer
|
|
SV119 is a selective sigma-2 (σ₂) receptor ligand (Ki ≈ 5-10 nM). SV119 induces apoptosis in various human cancer cell lines by activating caspase-3 and promoting mitochondrial depolarization. SV119 can enhance the effects of chemotherapeutic agents such as Paclitaxel (HY-B0015), increasing their cytotoxicity against tumor cells. SV119 significantly inhibits tumor growth in mouse xenograft models, both alone and in combination. SV119 is useful in the research of cancers such as breast, prostate, and pancreatic cancer .
|
-
- HY-170907
-
|
|
HDAC
DNA/RNA Synthesis
RAD51
|
Cancer
|
|
HDAC-IN-85 (Compound 1) is a BBB-permeable HDAC inhibitor. HDAC-IN-85 has an inhibitory effect on brain tumor cell lines. HDAC-IN-85 can induce acetylation, leading to DNA double-strand breaks, and induce the ubiquitination of RAD51, disrupting the DNA repair process. HDAC-IN-85 can be used in the research of glioblastoma .
|
-
- HY-B1336
-
|
|
Environmental Pollutants
Antibiotic
Bacterial
Apoptosis
Parasite
|
Infection
Cancer
|
|
Furazolidone is a monoamine oxidase (MAO) inhibitor with antiproliferative, apoptosis-inducing and differentiation-promoting activities. Furazolidone may inhibit leukemia fusion protein-mediated bone marrow transformation by upregulating the stability of the tumor suppressor protein p53. Furazolidone exhibits anti-leukemic activity in acute myeloid leukemia (AML) cell lines and can be used for anti-AML research [2].
|
-
- HY-149040
-
|
(S)-OBI-3424; (S)-TH-3424; AST-3424
|
17β-HSD
|
Cancer
|
|
Odafosfamide ((S)-OBI-3424) is a highly selective prodrug bis-alkylating agent activated by aldehyde-keto reductase 1C3 (AKR1C3(). Odafosfamide is highly cytotoxic to cell lines with high AKR1C3 expression. Odafosfamide exhibits antitumor activity in a variety of tumors with high AKR1C3 expression (such as liver cancer, non-small cell lung cancer, and leukemia). Odafosfamide can be used in cancer research .
|
-
- HY-120599
-
|
VERU-111; ABI-231
|
Microtubule/Tubulin
Apoptosis
HPV
|
Cancer
|
|
VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer .
|
-
- HY-180535
-
|
|
Cytochrome P450
|
Cancer
|
|
Aromatase-IN-8 is a selective Aromatase inhibitor against an IC50 of 0.05 µM. Aromatase-IN-8 exhibits selective antiproliferative effects against estrogen receptor-positive breast cancer cell lines, while showing no toxicity toward non-tumoral cells. Aromatase-IN-8 suppresses estrogen active, increases testosterone levels, and downregulates estrogen receptor expression and phosphorylation. Aromatase-IN-8 can be used for triple negative breast cancer research .
|
-
- HY-154949
-
|
|
WDR5
|
Cancer
|
|
WDR5-IN-6 is a WDR5 inhibitor, targeting to WBM site. WDR5-IN-6 inhibits cell proliferation of neuroblastoma cell lines with potent anti-tumor activity. WDR5-IN-6 shows high synergy with OICR-9429 (HY-16993), a WDR5 inhibitor targeting to WIN site. WDR5-IN-6 can be used for reasearch in neuroblastoma .
|
-
- HY-178472
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker) .
|
-
- HY-153067
-
|
|
Drug-Linker Conjugates for ADC
Topoisomerase
|
Cancer
|
|
Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan (Compound 11) is a bioactive compound-linker conjugate for ADC. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can conjugate with antibodies to form ADC (C-11) with anti-tumor activity. Exatecan is a DNA Topoisomerase I inhibitor. Mal-cyclohexane-Gly-Gly-Phe-Gly-Exatecan can be used in the research of squamous cell carcinoma, pancreatic adenocarcinoma and colorectal cancer .
|
-
- HY-18953
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-23 (compound DHM25) is a selective, competitive, irreversible and covalent inhibitor of mTOR. mTOR inhibitor-23 has the mechanism of inhibition occurs mainly through its capacity to covalently interact with a nucleophilic amino acid inside the ATP pocket. mTOR inhibitor-23 exerts potent antitumor activity against triple-negative breast tumor cell lines .
|
-
- HY-W1117786
-
|
|
ADC Payload
NAMPT
|
Cancer
|
|
Nampt-IN-10 (Compound 4) is an efficient inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). Nampt-IN-10 exhibits nanomolar-level inhibitory activity against cell lines such as MDA-MB453, NCI-N87, and NCI-H526. Nampt-IN-10 can be used as an ADC payload, and the ADC constructed with it as the core demonstrates significant anti-tumor activity .
|
-
- HY-N0367
-
|
(E)-Anethole
|
Environmental Pollutants
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Trans-Anethole ((E)-Anethole) is an orally active phenylpropene derivative found in Foeniculum vulgare that is estrogenic at low concentrations and cytotoxic at high concentrations in tumor cell lines. Trans-Anethole also has anti-aflatoxin, anti-thrombotic and anti-diabetic activities. Trans-Anethole is an important odor component in plants such as fennel, myrtle, liquorice, and camphor .
|
-
- HY-15794
-
|
Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
|
G-quadruplex
|
Cancer
|
|
Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
|
-
- HY-151286
-
|
|
STAT
|
Cancer
|
|
Antitumor agent-73 is a Diosgenin (HY-N0177) derivative, which inhibits STAT3 signaling and activates Pdia3/ERp57 exogenously. Antitumor agent-73 shows potent anti-tumor activity against various cancer cell lines, 7.9-341.7-fold stronger than Diosgenin .
|
-
- HY-160597
-
|
|
ADC Payload
Topoisomerase
|
Cancer
|
|
Exatecan-amide-bicyclo[1.1.1]pentan-1-ol (Compound 79) is an exatecan (HY-13631) derivative that can be used as a payload in drug conjugates. Exatecan-amide-bicyclo[1.1.1]pentan-1-ol has significant inhibitory activity against a variety of tumor cell lines .
|
-
- HY-P991982
-
|
|
ADC Antibody
|
Cancer
|
|
ZV0201 Antibody (ZV02) is a monoclonal antibody inhibitor targeting Her2. ZV0201 Antibody can be used to synthesize the antibody-drug conjugate (ADC) ZV0201. ZV0201 Antibody can be used to research related to HER2-positive tumors .
|
-
- HY-179045
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
ERα degrader 14 (Compound B7) is a potent ERα degrader. ERα degrader 14 exhibits significantly potent and selective anti-proliferative activity on two ERα-positive breast cancer cell lines (MCF-7 and T47D). ERα degrader 14 induces cell cycle arrest, inhibits cell migration, and induces cell apoptosis. ERα degrader 14 effectively inhibits tumor growth in mouse models. ERα degrader 14 can be used for the study of breast cancer .
|
-
- HY-Z8644
-
|
N-Formyl-N-deacetylcolchicine
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
N-Deacetyl-N-formylcolchicine (N-Formyl-N-deacetylcolchicine, Compound 11) is a selective inhibitor targeting the colchicine-binding site of tubulin. N-Deacetyl-N-formylcolchicine shows antiproliferative activity against various cancer cell lines with IC50 values of 32.61-100.28 nM. N-Deacetyl-N-formylcolchicine inhibits microtubule polymerization to block cell division, induces cancer cell apoptosis and suppresses migration. N-Deacetyl-N-formylcolchicine is promising for research of cancers such as lung cancer and various solid tumors .
|
-
- HY-13208
-
|
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
|
IAP
Apoptosis
|
Cancer
|
|
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
|
-
- HY-169652
-
|
|
Reactive Oxygen Species (ROS)
AMPK
|
Cancer
|
|
NPC26 is a small molecule mitochondrial disruptor with anti-tumor activity. NPC-26 shows significant anti-proliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 can damage mitochondrial function, leading to the opening of the mitochondrial permeability transition pore (mPTP) and the production of reactive oxygen species, ultimately inducing cell death. NPC-26 can kill CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway .
|
-
- HY-178712
-
|
|
Apoptosis
|
Cancer
|
|
CT 32228 is an inhibitor of lysophosphatidic acid acyltransferase-β (LPAAT-β). CT 32228 inhibits tumor cell growth. CT 32228 exhibits IC50 values of around 0.1-0.8 μM in various leukemia cell lines. CT 32228 induces caspase activation in DHL-4 and Ramos cells. CT 32228 induces apoptosis when combined with Rituximab (HY-P9913). CT 32228 results in a 50% xenograft growth delay in vivo. CT 32228 can be studied in research on acute leukemia .
|
-
- HY-179585
-
|
|
Apoptosis
|
Cancer
|
|
DD-CIP2 is a DNA damage and apoptosis inducer. DD-CIP2 demonstrates effective anti-proliferative activity against multiple cancer cell. DD-CIP2 modulates the DNA damage response pathway, triggering robust DNA damage, cell cycle arrest, and apoptosis in vitro. DD-CIP2 demonstrates significant anti-tumor efficacy in vivo at well-tolerated doses, without substantial toxicity. DD-CIP2 exhibits superior cytotoxic potency against a broad panel of blood-and solid-tumor-derived cancer cell lines independent of their BRCA1/2 status. DD-CIP2 can be used for small-cell lung cancer (SCLC) and non small-cell lung cancer (NSCLC) research .
|
-
- HY-101667R
-
|
|
DNA-PK
Reference Standards
|
Cancer
|
|
LTURM34 (Standard) is the analytical standard of LTURM34 (HY-101667). This product is intended for research and analytical applications. LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines .
|
-
- HY-18979
-
|
|
Flavivirus
Dengue Virus
|
Infection
Cancer
|
|
Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities .
|
-
- HY-162264
-
|
|
Microtubule/Tubulin
Proton Pump
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Tubulin polymerization/V-ATPase-IN-1 (compound F10) is a Tubulin polymerization/V-ATPase inhibitor. Tubulin polymerization/V-ATPase-IN-1 shows robust antiproliferation activity against four human cancer cell lines, and exerts antiproliferative activity by inhibiting tubulin and V-ATPase. Tubulin polymerization/V-ATPase-IN-1 induces immunogenic cell death in addition to apoptosis, and inhibits tumor growth in an RM-1 homograft model with enhanced T lymphocyte infiltration .
|
-
- HY-122038
-
|
|
MDM-2/p53
|
Cancer
|
|
NU-8165 is an inhibitor of the MDM2-p53 protein-protein interaction with anti-tumor activity. Optimization of NU-8165 was guided by MDM2 NMR titrations, which indicated key binding interaction regions. NU-8165 activated MDM2 and p21 transcription in cell-based assays and showed modest selectivity for wild-type p53 cell lines .
|
-
- HY-117991
-
|
|
VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
|
-
- HY-W717425
-
|
|
SHP1
STAT
Caspase
Apoptosis
Bcl-2 Family
CDK
Survivin
Drug Derivative
|
Cancer
|
|
SC-60 is a derivative of Sorafenib (HY-10201). SC-60 exerts its anti-tumor effect by activating the phosphatase activity of SHP-1, thereby inhibiting the STAT3 signaling pathway. SC-60 exhibits strong proliferation inhibitory activity in various hepatocellular carcinoma (HCC) cell lines. SC-60 downregulates the expression of downstream anti-apoptotic proteins (such as Bcl-2, Cyclin D1, Survivin), ultimately inducing caspase-dependent apoptosis. SC-60 significantly inhibits tumor growth in xenograft tumor models. SC-60 can be used for the study of HCC .
|
-
- HY-N0120
-
|
(E/Z)-Piceid
|
Drug Isomer
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
(E/Z)-Polydatin ((E/Z)-Piceid) is a mixture of the E/Z configurations of Polydatin (HY-N0120A). Polydatin can be isolated from Polygonum cuspidatum, grapes, peanuts, red wine, hop pellets, cocoa-containing products and chocolate products. Polydatin exhibits multiple biological properties, such as anti-platelet aggregation, anti-low-density lipoprotein oxidation, cardioprotective activity, anti-inflammatory and immunomodulatory functions. Polydatin shows favorable cytotoxic effects against various tumor cell lines, including cervical cancer cells, liver cancer cells, and nasopharyngeal carcinoma cells .
|
-
- HY-180193
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-86 (Compound B6) is an effective inhibitor of tubulin polymerization. Tubulin polymerization-IN-86 effectively inhibits microtubulin polymerization by binding to the colchicine binding sites on microtubulin, thereby disrupting the microtubule cytoskeleton within the cell. Tubulin polymerization-IN-86 exhibits potent anti-proliferative activity against a variety of cancer cell lines. Tubulin polymerization-IN-86 induces cell cycle arrest, apoptosis, inhibits cell migration, invasion, and long-term survival ability. Tubulin polymerization-IN-86 inhibits tumor growth in mice and can be used for the study of melanoma .
|
-
- HY-175733
-
|
|
RIO Kinase
Apoptosis
|
Cancer
|
|
CQ3196 is an orally active RIOK2 inhibitor with a Kd of 14 nM. CQ3196 effectively inhibits the ATPase activity of RIOK2, with an IC50 value of 72 nM. CQ3196 inhibits cell proliferation and colony formation in gastric cancer cell lines. CQ3196 induces cell apoptosis in HGC-27 and AGS cells. CQ3196 suppresses downstream signal pathway of RIOK2. CQ3196 reduces phosphorylation of mTOR and AKT. CQ3196 modulates ribosome function and protein synthesis. CQ3196 inhibits tumor growth and can be used for gastric cancer invtro and invivo research .
|
-
- HY-109583S
-
|
4-Oxo-4-HPR-d4
|
Isotope-Labeled Compounds
Reactive Oxygen Species (ROS)
Drug Metabolite
Apoptosis
|
Cancer
|
|
4-Oxofenretinide-d4 (4-Oxo-4-HPR-d4) is deuterium labeled 4-Oxofenretinide. 4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
|
-
- HY-P991372
-
|
RN927C antibody
|
TROP2
|
Cancer
|
|
Anti-TROP2 Antibody (RN927C antibody) is a human monoclonal antibody targeting Trop-2. Anti-TROP2 Antibody exerts in vitro inhibitory effects on a variety of tumor cell lines. Anti-TROP2 Antibody exhibits anti-tumor activity in mouse pancreatic PDX, ovarian PDX, lung PDX and triple-negative breast cancer (TNB) PDX models. Anti-TROP2 Antibody can be used for research on pancreatic cancer, ovarian cancer, lung cancer and triple-negative breast cancer .
|
-
- HY-158409
-
|
|
Molecular Glues
Ras
Cyclophilin
PERK
|
Cancer
|
|
Pan-rasin-2 (compound 6A) is an orally active molecular glues that targets RAS. Pan-RAS-IN-2 inhibits pERK (IC50 in AsPC-1 cells: 0.3 nM). Pan-rasin-2 has significant inhibitory activity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor (such as colorectal cancer, pancreatic cancer) effects .
|
-
- HY-146260
-
|
|
PI3K
|
Cancer
|
|
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .
|
-
- HY-176798
-
|
|
Lactate Dehydrogenase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
NCI-006 is an orally active lactate dehydrogenase (LDH) inhibitor (LDHA IC50 = 0.06 μM; LDHB IC50 = 0.03 μM). NCI-006 inhibits intratumoral LDH activity, lactate production, and tumor growth in a mouse pancreatic cancer model. NCI-006 inhibits glycolysis and induces apoptosis in vitro. NCI-006 enhances the radiosensitivity of glycolytic tumor cell lines while sparing non-glycolytic/normal cells (1522, skin fibroblasts) in combination with ionizing radiation (IR). NCI-006 exhibits synergistic antitumor effects in combination with IACS-010759 (HY-112037) against colorectal and gastric cancers. NCI-006 targets glycolysis by inhibiting lactate dehydrogenase impairs tumor growth in an Ewing sarcoma model .
|
-
- HY-15160A
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-15160B
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-121081
-
|
|
CDK
|
Cancer
|
|
BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-958 shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-958 exhibits good metabolic stability. BAY-958 effectively inhibits tumor growth in mouse xenograft models without significant toxicity .
|
-
- HY-N12198
-
|
|
Others
|
Cancer
|
|
Mollicellin H is a secondary metabolite of the fungus C. brasiliense and has a wide range of biological activities, including immunomodulation, cytotoxicity and anti-tumor effects. The growth inhibitory effects (GI50s) of Mollicellin H on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines are 5.1 μg/mL, 6.5 μg/mL and 2.5 μg/mL respectively .
|
-
- HY-177138
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin-IN-52 is a tubulin inhibitor. Tubulin-IN-52 demonstrates significant cytotoxicity toward a variety of
cancer cell types including prostate, lung, and ovarian cancers with strong activity toward highly aggressive cancer lines (IC50 = 0.9-3.8 mM). Tubulin-IN-52 significantly inhibits the growth of established tumors without noticeable toxicity. Tubulin-IN-52 can be used for the study of cancer .
|
-
- HY-100022A
-
|
eFT508 hydrochloride
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib hydrochlorideis a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib hydrochloride treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib hydrochloride also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-P10515
-
|
|
Bacterial
Fungal
|
Infection
Cancer
|
|
AcrAP2 is an antimicrobial peptide present in the venom of the Arabian scorpion (Androctonus crassicauda). AcrAP2 is inhibitory against Gram-positive bacteria and yeast but is essentially inactive against Gram-negative bacteria. A cation-enhanced AcrAP2 analog (AcrAP2a) exhibits significant antiproliferative effects at low concentrations against certain human cancer cell lines. AcrAP2 can be used in antibacterial and anti-tumor research .
|
-
- HY-128601
-
|
|
Checkpoint Kinase (Chk)
|
Cardiovascular Disease
Cancer
|
|
CHK1-IN-3 is a potent and selective CHK1 inhibitor with an IC50 of 0.4 nM. CHK1-IN-3 effectively inhibits the growth of malignant hematopathy cell lines and displays low affinity for hERG (IC50 > 40 μM). CHK1-IN-3 significantly suppresses the tumor growth in vivo. CHK1-IN-3 can be used for the study of hematologic malignancies .
|
-
- HY-15160
-
TAK-960
2 Publications Verification
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-D3432
-
|
|
Fluorescent Dye
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
WazaGaY-1 is an aza-BODIPY derivative, functions as a NIR-I/NIR-II fluorescent contrast agent. WazaGaY-1 undergoes internalization into tumor cells predominantly via clathrin-coated pits. WazaGaY-1 can be used for the research of glioblastoma, ovarian carcinoma and melanoma (Ex/Em = 685/820 nm) .
|
-
- HY-160066
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
SYL3C aptamer sodium is a DNA aptamer that targets epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets a variety of human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd values of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III are 38 nM and 67 nM, respectively. SYL3C aptamer sodium possesses stability, high binding affinity and selectivity, and can be used for targeted cancer cell imaging and circulating tumor cell detection .
|
-
- HY-W231513
-
|
|
MASTL
Ser/Thr Protease
Aurora Kinase
|
Cancer
|
|
MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis .
|
-
- HY-19671
-
|
SR-45023A; SR 9223i; SK&F-99085
|
HMG-CoA Reductase (HMGCR)
Apoptosis
|
Cancer
|
|
Apomine (SR-45023A) is an orally active antineoplastic agent that inhibits the mevalonate/isoprenoid pathway in cholesterol synthesis. Apomine can accelerate the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR). Apomine can also inhibit the growth of various types of cancer cells, including lung cancer, colon cancer, breast cancer, and skin cancer. Apomine is able to induce apoptosis in tumor cell lines derived from leukemia, colon cancer, liver cancer, ovarian cancer, and breast cancer .
|
-
- HY-146461
-
|
|
Apoptosis
Caspase
ROS Kinase
|
Cancer
|
|
Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
|
-
- HY-121382
-
|
|
Cholinesterase (ChE)
Apoptosis
Necroptosis
|
Neurological Disease
Cancer
|
|
Gypsogenin is a selective mixed-type BChE inhibitor (Ki=19.99 μM) that also exhibits significant cytotoxicity against various human cancer cell lines. Gypsogenin inhibits tumor growth by inducing cell cycle arrest and triggering apoptosis. Gypsogenin displays antibacterial activity against bacteria such as Bacillus subtilis and Bacillus thuringiensis, and often serves as a key parent nucleus for the synthesis of anticancer compounds. Gypsogenin is widely used in research on Alzheimer's disease and various cancers including colon cancer, melanoma, and leukemia .
|
-
- HY-179615
-
|
|
Apoptosis
Bcl-2 Family
Survivin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Entadamide A-CO-C12 is an Entadamide A (HY-N12125) derivative with potent anti-cancer activity, particularly against breast cancer cell lines. Entadamide A-CO-C12 promotes apoptosis, suppresses migratory ability, sphere formation, and stem-like cell populations. Entadamide A-CO-C12 inhibits tumor growth in a 4T1 mouse model. Entadamide A-CO-C12 can be used for the research of breast cancer .
|
-
- HY-177497
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
SKLB-03220 is a selective and orally active EZH2 covalent inhibitor with an IC50 of 1.72 nM for EZH2 MUT. SKLB-03220 exhibits weak activities against other tested histone methyltransferases (HMTs) and kinases. SKLB-03220 displays noteworthy potency against ovarian cancer cell lines and induces cell apoptosis. SKLB-03220 significantly inhibits tumor growth in PA-1 xenograft model. SKLB-03220 can be used for the study of ovarian cancer .
|
-
- HY-145729
-
|
AZD9150
|
STAT
Apoptosis
|
Cancer
|
|
Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3. Danvatirsen reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
|
-
- HY-145729A
-
|
AZD9150 sodium
|
STAT
Apoptosis
|
Cancer
|
|
Danvatirsen sodium (AZD9150 sodium) is an antisense oligonucleotide targeting STAT3. Danvatirsen sodium reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen sodium inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen sodium inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen sodium achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen sodium can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
|
-
- HY-175002
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kδ-IN-24 is a selective PI3Kδ inhibitor (IC50 = 0.1 nM). PI3Kδ-IN-24 exhibits significant antiproliferative effects against PI3Kδ-overexpressing cancer cell lines. PI3Kδ-IN-24 reduces p-AKT levels and induces cell cycle arrest and apoptosis in tumor cells. PI3Kδ-IN-24 is useful in cancer research, such as diffuse large B-cell lymphoma (DLBCL) .
|
-
- HY-119272
-
EF24
2 Publications Verification
|
ERK
Caspase
NF-κB
Apoptosis
p38 MAPK
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
|
-
- HY-15205R
-
|
STA-9090 (Standard)
|
HSP
Apoptosis
Reference Standards
|
Cancer
|
|
Ganetespib (Standard) is the analytical standard of Ganetespib. This product is intended for research and analytical applications. Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
|
-
- HY-147165
-
VT02956
1 Publications Verification
|
Ser/Thr Kinase
Large Tumor Suppressor (LATS)
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-164526
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
SH1573 is an orally active mIDH2 inhibitor. SH1573 has a strong and selective inhibitory effect on mIDH2 R140Q protein (IC50=4.78 nmol/L), and can effectively reduce the production of the carcinogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum and tumors. SH1573 can be used for the study of acute myeloid leukemia (AML) .
|
-
- HY-121081A
-
|
BAY-958 hydrochloride
|
CDK
|
Cancer
|
|
BAY-1112054 (BAY-958) hydrochloride is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-1112054 hydrochloride shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-1112054 hydrochloride exhibits good metabolic stability. BAY-1112054 hydrochloride effectively inhibits tumor growth in mouse xenograft models without significant toxicity .
|
-
- HY-147165A
-
|
|
YAP
Large Tumor Suppressor (LATS)
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-185206
-
|
|
PROTACs
Itk
NF-κB
|
Cancer
|
|
BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma .
|
-
- HY-178948
-
|
|
HDAC
|
Cancer
|
HDAC10-IN-3 (Compound 2a) is a potent HDAC10 inhibitor with an IC50s of 0.41, 37, 350 and 4500 nM against HDAC10, HDAC6, HDAC8 and HDAC1. HDAC10-IN-3 exhibits moderate cytotoxicity in KB and SK-OV-3 cells, but does not show significant cytotoxicity against most cancer cell lines. HDAC10-IN-3 can be used for the study of cancers .
|
-
- HY-W053641
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
(E)-2-Nitrocinnamic acid (Compound 1k) is an Acetylcholinesterase inhibitor. (E)-2-Nitrocinnamic acid is applicable to research related to Alzheimer's disease .
|
-
- HY-180836
-
|
|
Molecular Glues
IKZF Family
Apoptosis
|
Cancer
|
|
DIX-01 is a molecular gel degrader that can simultaneously induce the degradation of IKZF1/3 and GSPT1 mediated by CRBN. Its DC50 values are: IKZF1 (19.80 nM), IKZF3 (45.31 nM), and GSPT1 (120.1 nM). DIX-01 exhibits nanomolar-level potent anti-proliferative activity in various cancer cell lines. DIX-01 induces apoptosis in MV4-11 cells and significantly inhibits the growth of leukemia cells in zebrafish. DIX-01 can be used for the study of malignant hematological tumors .
|
-
- HY-146307
-
|
|
TrxR
|
Cancer
|
|
TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins .
|
-
- HY-101849R
-
|
|
Reference Standards
GLUT
TNF Receptor
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Fasentin (Standard) is the analytical standard of Fasentin. This product is intended for research and analytical applications. Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
|
-
- HY-177585
-
|
BLD1102
|
ADC Payload
Topoisomerase
|
Cancer
|
|
BCPT02 (BLD1102) is a Topoisomerase-I inhibitor and ADC payload (ADC Payload). BCPT02 can form the ADC BCG041. BCPT02 is applicable to cancer-related research .
|
-
- HY-160167
-
|
DZD8586
|
Src
Btk
|
Inflammation/Immunology
Cancer
|
|
Birelentinib (DZD8586) is an orally effective, selective, non-covalent inhibitor targeting LYN tyrosine kinase and BTK tyrosine kinase, capable of penetrating the blood-brain barrier. Birelentinib exhibits concentration-dependent antiproliferative effects in RI-1 cells and diffuse large B-cell lymphoma (DLBCL) cell lines carrying BTK resistance mutations (such as C481X, V416L, etc.). Birelentinib blocks both BTK-dependent and independent signaling of the B-cell receptor (BCR), thereby inhibiting tumor cell proliferation and inducing cell death. Birelentinib can be used in research to overcome resistance to existing covalent and non-covalent BTK inhibitors in B-cell non-Hodgkin lymphoma (B-NHL) .
|
-
- HY-128586A
-
|
|
NEDD8-activating Enzyme
Carbonic Anhydrase
Apoptosis
|
Cancer
|
|
TAS4464 hydrochloride is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 hydrochloride against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 hydrochloride targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 hydrochloride exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 hydrochloride has a wide therapeutic window, without obvious toxicity. TAS4464 hydrochloride can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
|
-
- HY-128586
-
|
|
Apoptosis
Carbonic Anhydrase
NEDD8-activating Enzyme
|
Cancer
|
|
TAS4464 is a long-acting, highly selective covalent inhibitor targeting NEDD8-activating enzyme (NAE) (IC50=0.955 nM), and also inhibits CAII with an IC50 of 0.73 μM, which is less potent than MLN4924 (HY-70062). The IC50 values of TAS4464 against other E1 enzymes UAE and SAE are 449 nM and 1280 nM, respectively. TAS4464 targets NEDD8 in an ATP-dependent manner to inhibit NAE, blocks the neddylation pathway, causes accumulation of CRL ubiquitin ligase substrates (such as CDT1, p27, phosphorylated IκBα), and further induces tumor cell apoptosis. TAS4464 exhibits antiproliferative and cytotoxic effects, and has broad-spectrum antitumor activity against various hematologic and solid tumor cell lines as well as patient-derived tumor cells. TAS4464 has a wide selcetive window, without obvious toxicity. TAS4464 can be used in the research of hematologic malignancies (leukemia, lymphoma, multiple myeloma, etc.) and solid tumors (small cell lung cancer, colorectal cancer, sarcoma, endometrial cancer, ovarian cancer, etc.) .
|
-
- HY-113081R
-
|
|
Reference Standards
Endogenous Metabolite
PPAR
Hedgehog
|
Cancer
|
|
1-Methyladenosine (Standard) is the analytical standard of 1-Methyladenosine. This product is intended for research and analytical applications. 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis .
In Vitro:Compared to surrounding tumor tissues, 1-methyladenosine methylation in RNA is aberrantly elevated in hepatocellular carcinoma (HCC) cell lines and liver cancer stem cells (CSCs). Methylated 1-methyladenosine can promote cholesterol synthesis and activate the Hedgehog signaling pathway by enhancing the translation of PPARδ in liver CSCs, ultimately driving the self-renewal and tumorigenesis of liver cancer stem cells .
|
-
- HY-103712
-
|
CT7001; ICEC0942
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib has anti-tumor effects .
|
-
- HY-P10816
-
|
Ac-(DLeu)LLLRVK-Amba
|
Bacterial
|
Infection
Cancer
|
|
PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
|
-
- HY-168899
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-24 (Compound 9f) is a FAK inhibitor (IC50: 0.815 nM). FAK-IN-24 induces DNA damage and apoptosis. FAK-IN-24 has anti-glioblastoma activity. FAK-IN-24 inhibits proliferation of glioblastoma cell lines U87-MG (IC50 = 15 nM) and U251 (IC50 = 20 nM). FAK-IN-24 inhibits tumor growth in U87-MG xenograft model .
|
-
- HY-175465
-
|
|
Interleukin Related
STAT
|
Cancer
|
|
SMI-10B13 is an Oncostatin M (OSM) inhibitor with a KD of 6.6 μM. SMI-10B13 inhibits OSM-mediated STAT3 phosphorylation in T47D and MCF-7 cell lines (IC50 = 136 and 164 nM, respectively). SMI-10B13 shows anti-tumor effect in human breast cancer mice models .
|
-
- HY-100022
-
|
eFT508
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .
|
-
- HY-103712A
-
|
CT7001 hydrochloride; ICEC0942 hydrochloride
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
|
-
- HY-103712C
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-161841
-
|
|
FGFR
|
Cancer
|
|
Antitumor agent-177 (compound 57), a non-steroidal NSC12 derivative, shows potent FGF2 binding affinity with a Kd of 24 μM by SPR. Antitumor agent-177 significantly inhibits the formation of HSPG/FGF2/FGFR1 ternary complexes. Antitumor agent-177 inhibits FGFR activation and exerts a potent anti-tumor activity on multiple myeloma (MM) cell lines in vitro and in vivo .
|
-
- HY-17662
-
|
AK-918/41759663
|
Bcl-2 Family
|
Cancer
|
|
Mol4 (AK-918/41759663) is a highly selective BCL-2 protein inhibitor (IC50=153.3 μM). Mol4 induces mitochondrial outer membrane permeabilization (MOMP) and cytochrome c release, showing significant antiproliferative activity against glioblastoma (U87-MG) cell lines. Mol4 is promising for research of BCL-2-dependent tumors (e.g., chronic lymphocytic leukemia) .
|
-
- HY-15794G
-
|
Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
|
G-quadruplex
|
Cancer
|
|
Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
|
-
- HY-117938
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
T-3861174 is an inhibitor of prolyl-tRNA synthetase (PRS, Aminoacyl-tRNA Synthetase) without completely inhibiting its translation process. T-3861174 activates the GCN2-ATF4 pathway and induces death in multiple tumor cell lines, including SK-MEL-2. T-3861174 demonstrated significant antitumor activity in multiple xenograft models without significantly affecting body weight .
|
-
- HY-15160C
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-172748
-
|
|
Drug Derivative
|
Neurological Disease
Cancer
|
|
9β-Hydroxyhexahydrocannabinol is a synthetic cannabinoid derivative. 9β-Hydroxyhexahydrocannabinol exhibits cytotoxicity against various tumor cell lines, such as HCT-116, MCF-7, K562, MIAPaCa-2, PANC-1, A549, PC-3 and SW-620, with IC50 values ranging from 15.23 to 33.74 μM. 9β-Hydroxyhexahydrocannabinol can be used in the study of cancer .
|
-
- HY-103712B
-
|
CT7001 hydrochloride dihydrate; ICEC0942 hydrochloride dihydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-13312A
-
|
|
IGF-1R
Insulin Receptor
Akt
Apoptosis
|
Cancer
|
|
GTx-134 is a dual insulin-like growth factor 1 receptor/insulin receptor (IGF-1R/IR) inhibitor with an IC50 values for IGF-1R and IR of 97 and 187 nM respectively. GTx-134 inhibits the autophosphorylation of IGF-1R and its downstream signaling pathway (Akt), thereby blocking the proliferation and survival signals of tumor cells. GTx-134 has broad-spectrum inhibitory activity against multiple myeloma cell lines and can induce apoptosis in sensitive cells. GTx-134 significantly inhibits tumor growth in mice with MM1.S cell transplantation. GTx-134 works in synergy with existing therapies (such as protease preparations, immunomodulators). GTx-134 can be used in high-risk myeloma research .
|
-
- HY-169369
-
|
XJZ-06-462
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
TRAP-1 (XJZ-06-462) is a non-covalent regulated induced proximity targeting chimera (RIPTAC) with JQ-1 carboxylic acid (HY-78695) as its target protein ligand. TRAP-1 forms a ternary complex with p53 Y220C and BRD4, potently activates p53 transcription, and inhibits the growth and proliferation of tumor cells. TRAP-1 upregulates p21 and other p53 target genes in pancreatic cell lines carrying p53 Y220C, and induces cellular senescence and apoptosis. TRAP-1 can be used in cancer research involving p53 Y220C-carrying tumors .
|
-
- HY-183623
-
|
|
ADC Payload
Apoptosis
|
Cancer
|
|
ProAlk01 is a protein alkylating agent that serves as a toxin payload for ADCs. ProAlk01 localizes to the cytoplasm and exerts cytotoxic effects mainly by alkylating cytoplasmic proteins rather than binding to DNA. ProAlk01 induces cell cycle arrest, apoptosis, and immunogenic cell death. ProAlk01 can be used in the research of solid tumors .
|
-
- HY-145923
-
|
ABBV-CLS-484
|
Phosphatase
STAT
JAK
|
Cancer
|
|
Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction .
|
-
- HY-145923B
-
|
ABBV-CLS-484 hydrochloride
|
Phosphatase
|
Inflammation/Immunology
Cancer
|
|
Osunprotafib (ABBV-CLS-484) hydrochloride is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib hydrochloride has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib hydrochloride increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib hydrochloride generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction .
|
-
- HY-169096
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax) .
|
-
- HY-147682
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
|
-
- HY-123656
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-61 is a synthetic β-carlinyl chalcone with significant antiproliferative activity. Antiproliferative agent-61 showed significant effects in a range of solid tumor cell lines, with the most prominent effects in breast cancer. Antiproliferative agent-61 showed IC50 values of 2.25 and 3.29 μM in the human breast cancer MCF-7 cell line. Antiproliferative agent-61 significantly induced DNA fragmentation and apoptosis in breast cancer cells. Antiproliferative agent-61 inhibited the interaction of MDM2 with p53 and promoted the degradation of MDM2 .
|
-
- HY-176701
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-4 (Compound 30) is a potent irreversible protein arginine methyltransferase 5 (PRMT5) inhibitor (IC50=8 nM). PRMT5-MTA-IN-4 blocks arginine methylation, inhibiting ribosomal RNA processing and cell cycle-related protein expression. PRMT5-MTA-IN-4 exhibits antiproliferative activity in multiple tumor cell lines (e.g., IC50=0.3 μM in DLD-1 cells). PRMT5-MTA-IN-4 is promising for research of hematological malignancies, such as acute myeloid leukemia, diffuse large B-cell lymphoma .
|
-
- HY-204056
-
|
|
Telomerase
|
Cancer
|
|
Telomerase-IN-8 is an orally active telomerase inhibitor, with an IC50 value of 0.98 μM. Telomerase-IN-8 exhibits potent antiproliferative activity against multiple tumor cell lines, including PC3, Bcap-37, MGC-803 and HepG2. Telomerase-IN-8 demonstrates potent antitumor efficacy in S180 sarcoma or HepG2 hepatoma xenograft mice. Telomerase-IN-8 can be used for the study of telomerase-targeted anticancer .
|
-
- HY-N14722
-
|
|
Bacterial
|
Infection
Cancer
|
|
Lactonamycin had strong activity against Gram-positive bacteria including Staphylococcus, Streptococcus, Enterococcus, MRSA (MIC of 0.39-0.78 μg/mL) and VRE (MIC of 0.39-0.78 μg/mL). Lactonamycin also has inhibitory effect on L-1210, P388, S180, FS-3, Ehrlich, B16-BL5 and other tumor cell lines (IC50s of 0.06-3.3 μg/mL) .
|
-
- HY-N0367R
-
|
(E)-Anethole (Standard)
|
Reference Standards
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
|
Trans-Anethole (Standard) is the analytical standard of Trans-Anethole. This product is intended for research and analytical applications. Trans-Anethole ((E)-Anethole) is an orally active phenylpropene derivative found in Foeniculum vulgare that is estrogenic at low concentrations and cytotoxic at high concentrations in tumor cell lines. Trans-Anethole also has anti-aflatoxin, anti-thrombotic and anti-diabetic activities. Trans-Anethole is an important odor component in plants such as fennel, myrtle, liquorice, and camphor .
|
-
- HY-123981
-
5MPN
3 Publications Verification
|
Phosphatase
|
Cancer
|
|
5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
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-
- HY-N0367S
-
|
(E)-Anethole-d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Endocrinology
|
|
Trans-Anethole-d3 is deuterated labeled Trans-Anethole (HY-N0367). Trans-Anethole ((E)-Anethole) is an orally active phenylpropene derivative found in Foeniculum vulgare that is estrogenic at low concentrations and cytotoxic at high concentrations in tumor cell lines. Trans-Anethole also has anti-aflatoxin, anti-thrombotic and anti-diabetic activities. Trans-Anethole is an important odor component in plants such as fennel, myrtle, liquorice, and camphor .
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-
- HY-100195
-
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Checkpoint Kinase (Chk)
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Cancer
|
|
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents .
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-
- HY-175297
-
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VEGFR
EGFR
|
Cancer
|
|
EGFR T790M/VEGFR-2-IN-1 (Compound 6) is a dual EGFR T790M mutant (IC50=0.26 μM) and VEGFR-2 (IC50=0.95 μM) inhibitor. EGFR T790M/VEGFR-2-IN-1 blocks tumor cell proliferation and angiogenesis signaling pathways. EGFR T790M/VEGFR-2-IN-1 exhibits potent cytotoxicity against multiple cancer cell lines (HCT116, MCF-7, HepG2, A549; IC50=5.35-9.90 μM). EGFR T790M/VEGFR-2-IN-1 is promising for research of non-small cell lung cancer and solid tumors .
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-
- HY-P99974
-
|
Nanoparticle albumin-bound Paclitaxel; Nanoparticle albumin-bound ABI-007
|
Microtubule/Tubulin
Apoptosis
Autophagy
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Cancer
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|
Nab-Paclitaxel (Nanoparticle albumin-bound Paclitaxel) is an albumin-bound nanoparticle formulation of Paclitaxel (HY-B0015). Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel, in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel is a solvent-free taxane with higher response rates and improved tolerability. Nab-Paclitaxel displays less toxicity and greater antitumor activity. Nab-Paclitaxel is more readily available for tumor cell uptake in three rhabdomyosarcoma, seven neuroblastoma cell lines, and one ostersarcoma cell line Nab-Paclitaxel can be studied in cancer research for example breast cancer and solid tumors. (The product specifications below only indicate the effective content of Paditaxel, the actual albumin quality depends on the batch; the ratio of each ingredient in this product is Paditaxel: albumin -1:7~1:11) .
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-
- HY-P1181
-
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|
Toll-like Receptor (TLR)
NO Synthase
IKK
Akt
PKC
NF-κB
p38 MAPK
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
Cancer
|
|
Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
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-
- HY-163510
-
|
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Androgen Receptor
|
Cancer
|
|
AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
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-
- HY-16457
-
|
MST 997
|
Microtubule/Tubulin
Caspase
Apoptosis
|
Cancer
|
|
Simotaxel (MST 997) is an orally active derivative of the taxane class. Simotaxel binds to β-tubulin and promotes tubulin polymerization (EC₅₀ = 0.9 μM), inhibits tubulin depolymerization, and causes cell cycle arrest at the G₂-M phase. Simotaxel disrupts the formation of the mitotic spindle and triggers the caspase-dependent apoptotic pathway (apoptosis). Simotaxel has inhibitory effects on Paclitaxel (HY-B0015) sensitive cell lines and overcomes drug resistance. Simotaxel can be used to study Paclitaxel / Docetaxel (HY-B0011) resistant solid tumors .
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-
- HY-181673
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
Caspase
PARP
|
Cancer
|
|
ICD inducer-2 is a immunogenic cell death inducer. ICD inducer-2 binds to the colchicine binding site on tubulin to inhibit tubulin polymerization. ICD inducer-2 exhibits broad-spectrum antiproliferative activity across multiple cancer cell lines. ICD inducer-2 inhibits cells migration, causes G2/M phase and induces apoptosis. ICD inducer-2 promotes infiltration of CD4+ and CD8+ T cells into the tumor microenvironment. ICD inducer-2 downregulates antiapoptotic protein Bcl-2, upregulates proapoptotic proteins Bax and Bim-1, and increases cleaved caspase 3, cleaved caspase 9, and cleaved PARP levels. ICD inducer-2 overcomes paclitaxel resistance in xenograft models and achieves tumor growth inhibition. ICD inducer-2 can be used for the research of cancer, such as lung carcinoma .
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-
- HY-175298
-
|
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STAT
Src
Apoptosis
|
Cancer
|
|
STAT-3/c-Src-IN-1 (Compound 12d) is a dual STAT-3 (IC50=0.844 μM) and c-Src (IC50=0.268 μM) inhibitor. STAT-3/c-Src-IN-1 blocks tumor cell proliferation, migration, and angiogenesis signaling pathways. STAT-3/c-Src-IN-1 exhibits potent anti-proliferative activity against melanoma (SK-MEL-2) and CNS cancer (SNB-75) cell lines (GI50=-5.75 μM and -5.63 μM), inducing tumor cell apoptosis via G0/G1 and G2/M phase cell cycle arrest. STAT-3/c-Src-IN-1 is promising for research of melanoma and glioblastoma .
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-
- HY-178960
-
|
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Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin-IN-59 (Compound 8g) is an orally active Tubulin inhibitor. Tubulin-IN-59 exhibits potent anti-proliferative activity against HCT116 colorectal cancer, HeLa cervical cancer, and HepG2 liver cancer cell lines, with its IC₅₀ value ranging from 16 to 35 nM. Tubulin-IN-59 arrests HeLa cells in the G2/M phase and induces cell apoptosis. Tubulin-IN-59 demonstrates significant anti-tumor activity in the HT29 human colon cancer mouse xenograft model. Tubulin-IN-59 can be used for the study of colorectal cancer and cervical cancer .
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-
- HY-B0530A
-
|
γ-pipradol hydrochloride
|
Reactive Oxygen Species (ROS)
mAChR
NADPH Oxidase
|
Cancer
|
|
Azacyclonol (γ-pipradol) hydrochloride is a compound with promising anticancer activity, showing effectiveness in inhibiting NOX-derived ROS in A549 human lung cancer cells. Azacyclonol hydrochloride exhibits enhanced proliferation inhibition against androgen-refractory cancer cell lines, specifically DU145 and PC-3. Azacyclonol hydrochloride demonstrates antitumor activity in DU145-xenografted chorioallantoic membrane tumor models. Azacyclonol hydrochloride also acts as a ligand for the M3 muscarinic acetylcholine receptor, which is overexpressed in ARPC. Azacyclonol hydrochloride effectively blocks carbachol-induced proliferation and NOX activity in DU145 cells. Azacyclonol hydrochloride can also be utilized for the treatment of chronic schizophrenia.
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-
- HY-180117
-
|
|
MMP
STAT
Apoptosis
|
Cancer
|
|
MMP-2/9-IN-2 (Compound 6k) is a MMP-2 and MMP-9 inhibitor, with IC50 values of 29.27 and 24.87 μM respectively. MMP-2/9-IN-2 exhibits good selective toxicity against multiple human hepatoma cell lines. MMP-2/9-IN-2 induces cell cycle arrest and apoptosis, significantly inhibits cell migration and invasion. MMP-2/9-IN-2 inhibits the phosphorylation of the STAT3 signaling pathway. MMP-2/9-IN-2 shows strong anti-tumor activity in a nude mouse xenograft model of HepG2 liver cancer cells .
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-
- HY-105369
-
|
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Anaplastic lymphoma kinase (ALK)
Apoptosis
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Cancer
|
|
KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
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-
- HY-180885S
-
|
|
Ras
ERK
|
Cancer
|
|
KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses p-ERK in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer .
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-
- HY-179451
-
|
|
Apoptosis
p38 MAPK
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Apoptosis inducer 53 is an apoptosis inducer. Apoptosis inducer 53 can inhibit proliferation of human tumor cell lines (A549, HeLa, SW1573, T-47D, WiDr) with GI50 values of 2.5-9.1 μM. Apoptosis inducer 53 can induce cancer cells apoptosis and reduce colony formation. Apoptosis inducer 53 can activate p38α MAPK signaling and exerts anti-inflammatory effect. Apoptosis inducer 53 also shows anti-Leishmania donovani activity. Apoptosis inducer 53 can be used for the researches of cancer, infection and inflammation .
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-
- HY-18707
-
|
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Ras
Apoptosis
|
Cancer
|
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K-Ras(G12C) inhibitor 12 is an irreversible inhibitor of K-Ras(G12C). K-Ras(G12C) inhibitor 12 can alter the nucleotide-binding preference of K-Ras and block its interaction with effector proteins. K-Ras(G12C) inhibitor 12 can reduce cell viability and induce apoptosis in lung cancer cell lines with G12C mutations. K-Ras(G12C) inhibitor 12 has anti-tumor activity .
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-
- HY-121382R
-
|
|
Reference Standards
Apoptosis
Cholinesterase (ChE)
Necroptosis
|
Cardiovascular Disease
|
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Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Gypsogenin is a selective mixed-type BChE inhibitor (Ki=19.99 μM) that also exhibits significant cytotoxicity against various human cancer cell lines. Gypsogenin inhibits tumor growth by inducing cell cycle arrest and triggering apoptosis. Gypsogenin displays antibacterial activity against bacteria such as Bacillus subtilis and Bacillus thuringiensis, and often serves as a key parent nucleus for the synthesis of anticancer compounds. Gypsogenin is widely used in research on Alzheimer's disease and various cancers including colon cancer, melanoma, and leukemia .
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-
- HY-149862
-
|
|
PROTACs
Androgen Receptor
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Cancer
|
|
ARD-2051 is a selective and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .
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- HY-164315
-
|
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Ras
PERK
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Cancer
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KRAS G12C inhibitor 67 (Example 35) is an orally active KRAS G12C inhibitor. KRAS G12C inhibitor 67 inhibits pERK and active KRas. KRAS G12C inhibitor 67 selectively inhibits the growth of various KRAS G12C mutant tumor cell lines. KRAS G12C inhibitor 67 exhibits anticancer activity against esophageal cancer, bladder cancer, colorectal cancer, lung cancer, and pancreatic cancer .
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-
- HY-122224
-
|
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Sigma Receptor
|
Cancer
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|
SW43 is a Sigma-2 selective ligand and agonist. SW43 is an ideal molecule for the development of cancer-targeted drug compounds. SW43 conjugated with DOX-L-NETA ( 89Y) exhibits antitumor activity in a VX2 cancer liver tumor allograft rabbit model. SW 43 conjugated with SW IV-52s to form SW III-123 activates the NF-κB pathway, has potent cytotoxicity against ovarian cancer cell lines, and induces apoptosis .
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-
- HY-W587938
-
|
(+)-γ-Eudesmol
|
Apoptosis
|
Cancer
|
|
γ-Eudesmol ((+)-γ-Eudesmol) is a mitochondrial-mediated apoptosis inducer. γ-Eudesmol binds mitochondrial membrane proteins, triggering depolarization of mitochondrial membrane potential and activating caspase cascades. γ-Eudesmol demonstrates cytotoxicity against multiple tumor cell lines (e.g., HepG2, B16-F10) with IC50 values ranging from 8.86-15.15 μg/mL. γ-Eudesmol is promising for research of cancers, such as hepatocellular carcinoma and melanoma .
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-
- HY-143317
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
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-
- HY-139659
-
|
|
PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
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Cancer
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 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-169021
-
|
|
JNK
|
Cancer
|
|
JNK-1-IN-3 (Compound 9e) is an inhibitor of JNK1 that downregulates JNK1 gene expression and inhibits the protein levels of its phosphorylated form, concurrently reducing the expression of its downstream targets, c-Jun and c-Fos, in tumors while restoring p53 activity. JNK-1-IN-3 exhibits broad-spectrum antiproliferative activity, particularly with high inhibitory activity against renal and breast cancer cell lines, demonstrating both in vivo and in vitro anticancer activity .
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-
- HY-N18247
-
|
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Others
|
Cancer
|
|
12-Ethoxynimbolinin F is a nimbolinin-type limonoid found in the fruits of Melia toosendan. 12-Ethoxynimbolinin F shows low cytotoxic activity against cancer cells .
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-
- HY-181687
-
|
|
HSP
CDK
|
Cancer
|
|
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer .
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-
- HY-162098
-
|
|
PROTACs
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
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-
- HY-P1181A
-
|
|
Toll-like Receptor (TLR)
NO Synthase
IKK
Akt
PKC
NF-κB
p38 MAPK
Interleukin Related
|
Cardiovascular Disease
Infection
Inflammation/Immunology
Cancer
|
|
Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
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-
- HY-169921
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
c-Myc inhibitor 15 (Compound A5) is a selective c-Myc inhibitor that exerts anticancer effects by disrupting the interaction between c-Myc and Max, leading to the degradation of c-Myc protein and the induction of apoptosis. Its IC50 values are 4.08 μM and 7.86 μM in A549 and NCI-H1299 lung cancer cell lines, respectively, demonstrating strong cytotoxic activity. In a syngeneic tumor model, c-Myc inhibitor 15 exhibited outstanding antitumor efficacy, achieving a tumor growth inhibition rate of 76.4% and significantly reducing c-Myc protein expression levels. c-Myc inhibitor 15 holds promise for research related to c-Myc-driven lung cancers .
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-
- HY-171955
-
|
|
Lipoxygenase
Apoptosis
Reactive Oxygen Species (ROS)
FAK
|
Cancer
|
|
LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin (HY-15142) resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors .
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-
- HY-178942
-
|
|
VEGFR
EGFR
Apoptosis
Bcl-2 Family
Caspase
MDM-2/p53
|
Cancer
|
|
EGFR/VEGFR2-IN-9 (Compound 9b) is an inhibitor of VEGFR-2 (IC50 = 1.325 μM) and EGFR (IC50 = 1.891 μM). EGFR/VEGFR2-IN-9 significantly inhibits the proliferation of multiple cancer cell lines, particularly leukemia cells. EGFR/VEGFR2-IN-9 upregulates the expression levels of Bax, caspase-3, and p53, while downregulating the expression of Bcl-2. EGFR/VEGFR2-IN-9 induces apoptosis and arrests the cell cycle in the G1 phase. EGFR/VEGFR2-IN-9 can be used to investigate anti-tumor angiogenesis and multi-drug resistant cancers .
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-
- HY-157125
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
|
-
- HY-N17550
-
|
|
Bacterial
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
25-Hydroperoxycycloart-23-en-3β-ol is an anticancer, antibacterial, and antimalarial agent. 25-Hydroperoxycycloart-23-en-3β-ol can be isolated from Blepharodon nitidum. 25-Hydroperoxycycloart-23-en-3β-ol exhibits anti-Mycobacterium tuberculosis and antileishmanial activities. 25-Hydroperoxycycloart-23-en-3β-ol shows significant cytotoxic activity against a panel of tumor cell lines (large cell lung cancer, melanoma, colon adenocarcinoma, chronic myelogenous leukemia) .
|
-
- HY-170620
-
|
|
PROTACs
PARP
|
Cancer
|
|
PARP1 PROTAC 180055 (Compound 180055) is a selective PARP1 PROTAC degrader (DC50 in T47D and MDA-MB-231 cell lines is 180 nM and 240 nM, respectively). PARP1 PROTAC 180055 promotes ubiquitination and degradation of PARP1 as well as inhibits PARP1 enzyme activity without a noticeable DNA trapping effect. PARP1 PROTAC 180055 inhibits tumors carrying BRCA mutations with a minor impact on the growth of normal cells (Pink: PARP1 ligand (HY-10617A); Blue: E3 ligase VHL ligand (HY-125845); Black: linker (HY-W014787)) .
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-
- HY-W106860R
-
|
|
Others
Reference Standards
|
Cancer
|
|
9H-Carbazole-3-carbaldehyde (Standard) is the analytical standard of 9H-Carbazole-3-carbaldehyde (HY-W106860). This product is intended for research and analytical applications. 9H-Carbazole-3-carbaldehyde is an anticancer agent that can be isolated from the stems of Lansium parasiticum (Lour.) Skeels. 9H-Carbazole-3-carbaldehyde shows significant cytotoxic activity in a variety of tumor cell lines, especially against H1299 and SMMC-7721 lung cancer cells with IC50 values of 6.19-26.84 μg/mL .
|
-
- HY-178029
-
|
|
Ribosomal S6 Kinase (RSK)
Topoisomerase
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
|
Cancer
|
|
RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma .
|
-
- HY-103712AR
-
|
CT7001 hydrochloride (Standard); ICEC0942 hydrochloride (Standard)
|
Reference Standards
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib hydrochloride (Standard) is the analytical standard of Samuraciclib hydrochloride (HY-103712A). This product is intended for research and analytical applications. Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
|
-
- HY-181073
-
|
|
Apoptosis
Necroptosis
NF-κB
p38 MAPK
|
Neurological Disease
Cancer
|
|
Apoptosis/necroptosis inducer 1 is an orally active and brain-penetrant apoptosis and necroptosis inducer. Apoptosis/necroptosis inducer 1 induces mitochondria-dependent (intrinsic pathway) apoptosis. Apoptosis/necroptosis inducer 1 induces necroptosis by activating the TNF-α/NF-κB/MAPK signaling pathway. Apoptosis/necroptosis inducer 1 exhibits antiproliferative activity in glioblastoma cell lines and multiple solid tumor types. Apoptosis/necroptosis inducer 1 inhibits growth of orthotopic glioblastoma in animal models and improves survival rate. Apoptosis/necroptosis inducer 1 can be used for the research of glioblastoma .
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-
- HY-169349
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 12 (Compound EF2) is an orally active Androgen receptor (AR) antagonist (IC50: 0.30 μM). Androgen receptor antagonist 12 inhibits transcriptional activity of variant AR mutants and and the proliferation of AR-positive PCa cell lines. Androgen receptor antagonist 12 blocks AR nuclear translocation. Androgen receptor antagonist 12 inhibits tumor growth in a C4-2B xenograft mouse model. Androgen receptor antagonist 12 can be used for prostate cancer (PCa) research .
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-
- HY-N16876
-
-
- HY-P992340
-
|
|
Radionuclide-Drug Conjugates (RDCs)
TNF Receptor
|
Cancer
|
|
CTB006 is a monoclonal antibody targeting a humanized chimeric recombinant anti-DR5. CTB006 specifically binds to and activates DR5, thereby inducing tumor cell apoptosis, inhibiting tumor growth and reducing tumor drug resistance. 177Lu-radiolabeled CTB006 can deliver targeted radiotherapy to tumor cells; while 89Zr- or 177Lu-labeled CTB006 can serve as a PET/CT imaging agent for detecting DR5 expression levels in preclinical tumor models and screening cancers with DR5 overexpression. CTB006 can be applied to research related to gastrointestinal cancer, colorectal cancer and other solid tumors .
|
-
- HY-175541
-
|
|
PROTACs
Btk
|
Cancer
|
|
TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)) .
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-
- HY-174445
-
|
|
PROTACs
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity (Pink: Target protein ligand (HY-111109); Blue: E3 ligase ligand (HY-112078), E3 ligase ligand + linker (HY-174474); black: Linker) .
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- HY-19896
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COTI-2
4 Publications Verification
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MDM-2/p53
Apoptosis
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Cancer
|
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COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation .
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- HY-173488
-
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NF-κB
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
|
Cancer
|
|
NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2 .
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-
- HY-144693
-
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MEK
PI3K
PERK
|
Cancer
|
|
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
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-
- HY-144692
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MEK
PI3K
PERK
|
Cancer
|
|
MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
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-
- HY-153858
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Raf
Discoidin Domain Receptor
MEK
TNF Receptor
Interleukin Related
JAK
STAT
Ras
|
Cancer
|
|
PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma .
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-
- HY-182368
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
PI3Kα-IN-30 is an orally active, selective PI3Kα inhibitor with an IC50 of 2.8 nM. PI3Kα-IN-30 inhibits cancer cell proliferation, as well as the phosphorylation of Akt (S473) and pS6 (S240/244). PI3Kα-IN-30 shows low growth inhibitory activity against normal somatic cell lines at a concentration of 30 μM. PI3Kα-IN-30 induces cancer cell apoptosis and exerts anti-tumor efficacy in xenograft models. PI3Kα-IN-30 can be used for the research of breast cancer .
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-
- HY-153916
-
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T417
|
HOXA
DNA/RNA Synthesis
NEKs
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
TCRS-417 (T417) is a small-molecular inhibitor for PBX1. TCRS-417 can directly block PBX1-binding to DNA (IC50 = 6.58 μM), and affects PBX1 transcription. TCRS-417 is able to hammer out the stemness traits of Carboplatin (HY-17393)-resistant (CR) cells to revert to a differentiated status through tacking PBX1 signaling cascade. TCRS-417 significantly suppresses self-renewal and proliferation of cancer cells expressing high levels of PBX1. TCRS-417 can decrease the mRNA levels of FOXM1, NEK2, and E2F2 in cancer cell lines. TCRS-417 is selectively toxic against chr1q-amp myeloma and solid tumor cells .
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-
- HY-173182
-
|
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Microtubule/Tubulin
P-glycoprotein
|
Cancer
|
|
Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor. By binding to the colchicine site of tubulin, it causes G2/M cell cycle arrest and generates reactive oxygen species (ROS). Antitumor agent-200 exhibits significant inhibitory activity against MCF7/ADR and KBV200 cell lines with overexpression of P-glycoprotein (P-gp), with drug resistance indices (DRI) of 0.83 and 0.58 respectively. In the MCF-7 xenograft model, Antitumor agent-200 (25 mg/kg, intraperitoneal injection) can achieve a tumor growth inhibition rate of 57.2%. Antitumor agent-200 can be used in the research of the anti-cancer field .
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-
- HY-175227
-
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|
STAT
NF-κB
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
STAT3/NF-κB-IN-1 is a potentSTAT3 and NF-κB inhibitor with IC50s of 5.86 (STAT3) and 4.22 μM (NF-κB) in 4T1 cells. STAT3/NF-κB-IN-1 is able to induce apoptosis via its upregulation on key apoptotic regulators; caspases-3/9, Bax and downregulation of Bcl-2. STAT3/NF-κB-IN-1 exerts considerable anticancer activity against breast cancer cell lines and reduces tumor volume in vivo. STAT3/NF-κB-IN-1 can be used for the study of breast cancer .
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-
- HY-155066
-
|
|
PI3K
mTOR
Apoptosis
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
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-
- HY-112296
-
T025
4 Publications Verification
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CDK
Apoptosis
DYRK
|
Cancer
|
|
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
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- HY-B0984A
-
|
|
Calcium Channel
Ras
STING
Autophagy
|
Infection
Cardiovascular Disease
Cancer
|
|
Fendiline, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
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-
- HY-B0984
-
|
|
Calcium Channel
Ras
STING
Autophagy
|
Infection
Cardiovascular Disease
Cancer
|
|
Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
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- HY-175525
-
|
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PROTACs
Aurora Kinase
|
Cancer
|
|
MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors (Pink: Target protein ligand (HY-175526); Blue: E3 ligand (HY-112078); Black: Linker; E3 ligand + Linker (HY-132938)) .
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-
- HY-175253
-
|
|
STAT
Apoptosis
|
Cancer
|
|
YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high
affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer .
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-
- HY-148150A
-
|
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Creatine Kinase
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Cyclocreatine phosphate dilithium is a synthetic intracellular energy buffer. Cyclocreatine phosphate dilithium mediates antiproliferative activity in cells with high creatine kinase levels and inhibits solid tumor growth. Cyclocreatine phosphate dilithium maintains adenosine triphosphate (ATP) levels and protects tissues from hypoxia, cellular damage and inflammation during ischemic events. Cyclocreatine phosphate dilithium accumulates in skeletal muscle, reduces muscle phosphocreatine and total creatine levels, and acts both as a bioenergetic/anti-inflammatory agent and an experimental tool for the assessment of ischemic injury. Cyclocreatine phosphate dilithium can be used in studies related to solid tumors, heart failure and ischemia .
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-
- HY-178964
-
|
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PROTACs
RET
|
Cancer
|
|
PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .
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- HY-186120A
-
|
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Amino Acid Derivatives
|
Cancer
|
|
N-(Aminoiminomethyl)-N-methyl-L-alanine is an Amino acid analog. N-(Aminoiminomethyl)-N-methyl-L-alanine can be used in cancer-related research .
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-
- HY-163434
-
|
|
EGFR
Histone Methyltransferase
|
Cancer
|
|
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
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-
- HY-156158
-
|
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Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH2 R140Q-IN-2 (compound 36) is an an orally active IDH2 R140Q inhibitor (IC50: 29 nM). IDH2 R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2 R140Q (IC50: 10 nM). IDH2 R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2 R140Q-IN-2 can be used for research of acute myeloid leukemia (AML) .
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-
- HY-164202
-
|
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
ORM-5029 is a first-in-class human epidermal growth factor receptor 2 (HER2)-targeted antibody-drug conjugate (ADC) comprised of SMol006, a highly potent GSPT1 degrader, conjugated to Pertuzumab (HY-P9912). ORM-5029 exhibits robust efficacy across 14 HER2-positive breast cancer cell lines, with IC50 values ranging from 0.3 to 14.4 nM.ORM-5029 demonstrates anti-tumor activity in the BT474 xenograft model. ORM-5029 can be used for study of breast cancer .
|
-
- HY-126929
-
|
TXN-B
|
DNA Alkylator/Crosslinker
Apoptosis
Bacterial
Parasite
Fungal
|
Infection
Cancer
|
|
Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma .
|
-
- HY-164530
-
|
|
Src
VEGFR
Raf
p38 MAPK
|
Cancer
|
|
SKLB646 is an orally active multi-target kinase inhibitor. SKLB646 shows significant inhibitory effects on SRC and VEGFR2 with IC50 values ??of 0.002 μmol/L and 0.012 μmol/L, respectively. SKLB646 also shows significant inhibitory effects on B-Raf and C-Raf with IC50 values ??of 0.022 μmol/L and 0.019 μmol/L, respectively. SKLB646 inhibits the activation of the SRC signaling pathway and blocks the MAPK signaling pathway by inhibiting Raf kinase. In addition, SKLB646 can inhibit the proliferation, migration and invasion of human umbilical vein endothelial cells (HUVEC) to inhibit tumor-induced angiopoietic formation. SKLB646 shows significant anti-proliferative and anti-survival activities against triple-negative breast cancer (TNBC) cell lines .
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-
- HY-172878
-
|
|
Small Interfering RNA (siRNA)
HDAC
Apoptosis
|
Cancer
|
|
HDAC/PSMD14-IN-1 (Compound 8B) is a thiolutin derivative. HDAC/PSMD14-IN-1 is a orally active dual-target inhibitor of PSMD14/HDAC1 (IC50 238.7 nM/141.2 nM, respectively). HDAC/PSMD14-IN-1 has good cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). HDAC/PSMD14-IN-1 can induce apoptosis. HDAC/PSMD14-IN-1 has anti-tumor activity in a KYSE30 cell mouse xenograft model. HDAC/PSMD14-IN-1 can be used in anti-esophageal cancer research .
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-
- HY-16491
-
|
DJ-927
|
Microtubule/Tubulin
|
Cancer
|
|
Tesetaxel (DJ-927) is an orally active and brain-penetrant taxane tubulin inhibitor. Tesetaxel inhibits tubulin depolymerization with an IC50 of 0.44 μM. Tesetaxel inhibits cancer cells proliferation and shows potent antitumor activity against P-glycoprotein-positive cancer cells. Tesetaxel can be used for the research of cancer, such as solid tumors, liver metastasis, and advanced breast cancer .
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-
- HY-181947
-
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Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
|
IDO1-IN-33 (Compound YC-16) is a IDO1 inhibitor (with an IC50 of 0.18 μM for IDO1 in HeLa cells). IDO1-IN-33 acts as an apo-IDO1 inhibitor by slowly and competitively displacing heme from mature holo-IDO1 and rapidly binding to the heme-binding site of immature apo-IDO1, without altering the expression level of IDO1. IDO1-IN-33 can be used for the research of hepatocellular carcinoma, non-small cell lung cancer, triple-negative breast cancer, and cervical cancer .
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- HY-179430
-
|
|
Mps1
|
Cancer
|
|
TTK-IN-5 is an orally active covalent threonine tyrosine kinase (TTK) inhibitor with selectivity (IC50 = 8.918 nM). TTK-IN-5 exhibits anti-proliferative potencies against MDA-MB-231, A2780, HCT116, HCC1569 and MKN1 cell lines (IC50 values of 0.113 μM, 0.476 μM, 3.136 μM, 3.649 μM, and 1.856 μM, respectively). TTK-IN-5 potently suppresses tumor growth without notable toxicity in A2780 and MDA-MB-231 xenograft mouse models. TTK-IN-5 can be used for the research of cancer such as breast cancer and ovarian cancer .
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- HY-B0984R
-
|
|
Calcium Channel
Ras
STING
Autophagy
Reference Standards
|
Infection
Cardiovascular Disease
Cancer
|
|
Fendiline (hydrochloride) (Standard) is the analytical standard of Fendiline (hydrochloride). This product is intended for research and analytical applications. Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
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-
- HY-125209A
-
|
|
Apoptosis
PARP
DNA/RNA Synthesis
|
Cancer
|
|
TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
|
-
- HY-P992483
-
|
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Transmembrane Glycoprotein
|
Cancer
|
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VIS832 is an anti-CD138 monoclonal antibody. VIS832 induces antibody-dependent cellular cytotoxicity. VIS832 inhibits the growth of disseminated multiple myeloma tumors in vivo. VIS832 exerts anti-tumor effects on multiple myeloma in combination with Lenalidomide (HY-A0003) or Bortezomib (HY-10227). VIS832 can be used in research related to multiple myeloma .
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-
- HY-172733S
-
|
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Isotope-Labeled Compounds
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
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-
- HY-N12461
-
|
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Bacterial
Caspase
Apoptosis
|
Infection
|
|
Cucurbitacin F is a tetracyclic protostane-type triterpenoid with low toxicity, antibacterial and anti-inflammatory activities, and is also a related compound of Cucurbitacin B (HY-N0416). Cucurbitacin F widely exists in plants such as Cucurbitaceae plants, Quisqualis indica and Sorbaria sorbifolia. Cucurbitacin F acts as an actin aggregator and reduces cell viability in a dose-dependent manner. Cucurbitacin F induces apoptosis by triggering G2/M phase cell cycle arrest and activating the caspase-3-dependent apoptosis .
|
-
- HY-111090
-
|
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Polo-like Kinase (PLK)
NEKs
|
Cancer
|
|
GSK461364 analogue 1 is a thiophene-based PLK1 inhibitor with a PLK1 IC50 of 2 nM and a PLK3 IC50 of 630 nM. GSK461364 analogue 1 also acts as an inhibitor of Nek2 kinase (IC50: 21 nM). GSK461364 analogue 1 has a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%. GSK461364 analogue 1 can be used in studies related to colon cancer, lung cancer, breast cancer and ovarian cancer .
|
-
- HY-181842
-
|
|
PARP
ERK
Apoptosis
|
Cancer
|
|
PARP1/ERK IN-1 is a dual PARP1/ERK inhibitor, with a PARP1 IC50 of 0.9 nM and an ERK2 IC50 of 1.8 nM. PARP1/ERK IN-1 inhibits proliferation and migration of various cancer cell lines, and induces apoptosis and DNA damage. PARP1/ERK IN-1 suppresses tumor growth in mouse models of colorectal cancer, and reduces the expression of Ki‑67, BRCA1 and Rad51. PARP1/ERK IN-1 can be used in the research of colorectal cancer, triple-negative breast cancer and pancreatic cancer .
|
-
- HY-P990905
-
|
SAR-443579
|
Interleukin Related
|
Cancer
|
|
Bexatamig (SAR-443579) is a trifunctional natural killer cell engager targeting IL-3R α/CD123, NKp46/NCR1/CD335 and Fc gamma RIIIA/CD16a. Bexatamig forms a cytolytic synapse between natural killer cells and CD123-positive tumor cells. By activating natural killer cells to induce tumor cell death, Bexatamig effectively reduces the burden of CD123-positive acute myeloid leukemia (AML) blasts. Bexatamig has been granted FDA Fast Track designation, and is primarily investigated for relapsed or refractory acute myeloid leukemia, B-cell acute lymphoblastic leukemia, and high-risk myelodysplastic syndromes .
|
-
- HY-182478
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
MDL-27048, a tubulin inhibitor, binds competitively, reversibly to the Colchicine (HY-16569)-binding site on tubulin heterodimers. MDL-27048 inhibits microtubule assembly, induces slow depolymerization of preassembled microtubules, disrupts microtubule polymerization-depolymerization dynamics, and disrupts cytoplasmic microtubule networks. MDL-27048 exerts growth inhibitory effects on human cancer cells, induces mitotic arrest, and does not disrupt actin filaments at microtubule-depolymerizing concentrations. MDL-27048 can be used for the research of malignant tumors .
|
-
- HY-13774
-
|
|
P-glycoprotein
BCRP
|
Cancer
|
|
WK-X-34 is a low-toxicity, highly effective multidrug resistance reversal agent. By potently inhibiting the transport functions of P-glycoprotein (P-gp, ABCB1) and breast cancer resistance protein (BCRP), WK-X-34 significantly increases the intracellular accumulation of anticancer drugs and radiotracers in drug-resistant cells. WK-X-34 exerts no significant effect on MRP transporters. WK-X-34 not only restores the chemosensitivity of multidrug-resistant ovarian cancer cells, but also significantly enhances the uptake of 99mTc-Sestamibi in P-gp-positive xenograft tumors, brain and intestinal tissues. WK-X-34 exhibits extremely low toxicity and favorable safety profiles both in vitro and in mice (at doses up to 50 mg/kg), and can be used for research on overcoming multidrug resistance in ovarian cancer .
|
-
- HY-157229
-
STX-721
1 Publications Verification
|
EGFR
ERK
|
Cancer
|
|
STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations .
|
-
- HY-B0633D
-
|
|
CD44
Endogenous Metabolite
Bacterial
Akt
PI3K
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Hyaluronic acid sodium (MW 200-1560) is a biopolymer composed of repeating disaccharide units, with a molecular weight of 200-1560. Hyaluronic acid sodium is a major component of the extracellular matrix (ECM). It is synthesized on the plasma membrane. Hyaluronic acid sodium exerts its effects by binding to receptors CD44 and RHAMM. Hyaluronic acid sodium activates PI3K-Akt signaling. Hyaluronic acid sodium also enhances cell invasion and angiogenesis by promoting or stimulating the binding of proteolytic MMP-9 to the cell surface. Elevated hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion, and angiogenesis in digestive system cancers. Hyaluronic acid sodium is involved in tissue remodeling and rapid cell proliferation in several physiological processes, including embryonic morphogenesis and wound healing. Hyaluronic acid sodium can be used as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid sodium can be used as a drug delivery carrier for sodium butyrate, enhancing its anti-proliferative activity against breast cancer cell lines. Hyaluronic acid sodium can lubricate the corneal endothelium. Hyaluronic acid sodium can improve tissue hydration and enhance the resistance of cells to mechanical damage. Hyaluronic acid sodium has been conjugated with antibodies to ensure that the active compound continues to exert its effects at the site of inflammation. Hyaluronic acid sodium can be used in research in the fields of osteoarthritis, ophthalmology, cosmetic dermatology, oncology, and liver diseases .
|
-
- HY-B0633E
-
|
Hyaluronan, low endotoxin; Hyaluronate, low endotoxin
|
Endogenous Metabolite
CD44
Bacterial
Akt
PI3K
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Hyaluronic acid, low endotoxin (Hyaluronan, low endotoxin) is a biopolymer composed of repeating disaccharide units containing low levels of endotoxin. Hyaluronic acid is a major component of the extracellular matrix (ECM). It is synthesized on the plasma membrane. Hyaluronic acid exerts its effects by binding to receptors CD44 and RHAMM. Hyaluronic acid activates PI3K-Akt signaling. Hyaluronic acid also enhances cell invasion and angiogenesis by promoting or stimulating the binding of proteolytic MMP-9 to the cell surface. Elevated hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion, and angiogenesis in digestive system cancers. Hyaluronic acid is involved in tissue remodeling and rapid cell proliferation in several physiological processes, including embryonic morphogenesis and wound healing. Hyaluronic acid can be used as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid can be used as a drug delivery carrier for sodium butyrate, enhancing its anti-proliferative activity against breast cancer cell lines. Hyaluronic acid can lubricate the corneal endothelium. Hyaluronic acid can improve tissue hydration and enhance the resistance of cells to mechanical damage. Hyaluronic acid has been conjugated with antibodies to ensure that the active compound continues to exert its effects at the site of inflammation. Hyaluronic acid can be used in research in the fields of osteoarthritis, ophthalmology, cosmetic dermatology, oncology, and liver diseases .
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- HY-185484
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BMS-936561
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Antibody-Drug Conjugates (ADCs)
Transmembrane Glycoprotein
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Cancer
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MDX-1203 (BMS-936561) is an antibody-drug conjugate targeting CD70. MDX-1203 binds to CD70 and mediates the specific delivery of its conjugated cytotoxic payload to tumors. MDX-1203 delivers a DNA alkylating payload into cells. MDX-1203 can be used in research related to advanced clear cell renal cell carcinoma and relapsed/refractory B-cell non-Hodgkin lymphoma .
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- HY-172159
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HDAC
Apoptosis
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Cancer
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FF2039 (compound 1j) is a specific HDAC1, HDAC6, and HDAC isoforms of class I, IIa and IIb PROTAC degrader. FF2039 demonstrates s significant antiproliferative activity against both hematological and solid cancer cell lines, driven by cell cycle arrest and Apoptosis induction. FF2039 inhibits HDAC isoform of HDAC1, HDAC2, HDAC4 and HDAC6 with IC50s of 1.03, 2.15, 12.4 and 0.053 μM, respectively. FF2039 shows antiproliferative activity against different tumor entities of MM.1S, MDA-MB-231 and U-87MG with EC50s of 2.8, 28 and 30 μM, respectively. (Pink: PRMT5 ligand (HY-168864); Blue: E3 ligase ligand HY-W957284); Black: linker (HY-W881439); E3+linker (HY-172185 )) .
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- HY-172877
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Raf
EGFR
Apoptosis
Bcl-2 Family
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Cancer
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EGFR/BRAFV600E-IN-5 (Compound 7I) is a dual BRAFV600E/EGFR inhibitor with IC50 of 0.048 μM and 0.037 μM, respectively. EGFR/BRAFV600E-IN-5 has significant anti-melanoma activity with IC50 of 3.16 μM and 2.50 μM against MALME-3M and LOX-IMVI cell lines, respectively. EGFR/BRAFV600E-IN-5 exerts anti-tumor effects by inducing G1 arrest, inhibiting DNA synthesis, and activating the mitochondrial apoptosis pathway. EGFR/BRAFV600E-IN-5 can be used for melanoma research, especially for combined inhibition of BRAFV600E mutation and EGFR signaling pathway .
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- HY-186086
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Ras
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Cancer
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RM-041 is a selective, orally active KRAS G13C (ON) inhibitor that forms a covalent complex with KRAS G13C (ON) and Cyclophilin A. RM-041 blocks the binding of RAS effector proteins via steric hindrance, and then covalently binds to Cys-13 to form an irreversible inhibitory complex, thereby inhibiting the proliferation of KRAS G13C mutant cancer cells. RM-041 induces regression of KRAS G13C tumors in cellular and xenograft tumor models. RM-041 exerts a synergistic effect when combined with upstream node inhibitors (such as SHP2 inhibitors). RM-041 can be used for the research of non-small cell lung cancer .
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- HY-172889
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PI3K
HDAC
Apoptosis
mTOR
Akt
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Cancer
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PI3K/HDAC-IN-4 (Compound 31f) is a PI3K/HDAC dual inhibitor (IC50: 0.2μM). PI3K/HDAC-IN-4 shows high selectivity for HDAC1-3 (IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively). PI3K/HDAC-IN-4 is a potent PIK3 inhibitor with IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. PI3K/HDAC-IN-4 significantly induces tumor cell apoptosis by simultaneously inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. PI3K/HDAC-IN-4 exhibits potent antiproliferative activity in a variety of tumor cell lines (e.g., MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively). PI3K/HDAC-IN-4 can be used in the study of lymphoma and leukemia .
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- HY-153468
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TEQ103; Sera2
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Sodium Channel
TRP Channel
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Cancer
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ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer .
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- HY-W750980
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TNF Receptor
Interleukin Related
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Inflammation/Immunology
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β-Bisabolol is a potent anti-inflammatory agent that can be found in cotton gin trash. β-Bisabolol inhibits the production of nitric oxide (NO), pGE2, TNF-α, IL-6, and IL-8 in LPS (HY-D1056)-stimulated macrophages and fibroblast cells. β-Bisabolol can be used for the research on inflammatory conditions .
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- HY-P990716
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AZD7789
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PD-1/PD-L1
Tim3
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Inflammation/Immunology
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Sabestomig (AZD7789) is a monovalent bispecific antibody targeting PD-1 and TIM-3. Sabestomig binds to PD-1 and an epitope in the TIM-3 IgV domain outside the phosphatidylserine-binding cleft, thereby precisely regulating immune responses. Sabestomig promotes IL-2 production, efferocytosis and cross-presentation of tumor antigens, and enhances the release of anti-tumor T cell cytokines, cytotoxicity, and secretion of IFN-γ. Sabestomig inhibits the growth of solid tumors, prolongs the duration of tumor suppression, and significantly enhances anti-tumor responses following anti-PD-1 therapy. Sabestomig has been used in studies related to non-small cell lung cancer and classical Hodgkin lymphoma .
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- HY-182264
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Nordihydroguaiaretic acid tetrapivalate
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IGF-1R
EGFR
Drug Metabolite
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Cancer
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Masoprocol tetrapivalate (Nordihydroguaiaretic acid tetrapivalate) is a catecholic butane metabolite and also a tyrosine kinase activity inhibitor of IGF-1R and EGFR. Masoprocol tetrapivalate regulates tyrosine kinase signaling pathways associated with cell proliferation. Masoprocol tetrapivalate can be used in the research of proliferative diseases, including malignant, precancerous or benign cancers, and solid tumors .
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- HY-W011592
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NO Synthase
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Inflammation/Immunology
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N-Phthaloyl-L-glutamic acid is an orally active anti-inflammatory agent. N-Phthaloyl-L-glutamic acid inhibits Lipopolysaccharides (HY-D1056) (LPS)-induced nitric oxide production in murine spleen cells. N-Phthaloyl-L-glutamic acid does not exhibit significant cytotoxicity in vitro against tumor cells and BALB/c mice spleen cell culture. N-Phthaloyl-L-glutamic acid can be used for the research of inflammation .
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- HY-180416
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Antibiotic
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Cancer
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TMC-169 is a potent antibiotic of the Aspochalasin group that can be isolated from Aspergillus flavipes. TMC-169 exhibits anti-tumor activity against multiple cancer cells. TMC-169 can be used for the research of cancer, such as hematologic malignancies, non-small cell lung cancer, breast cancer, and glioma .
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- HY-136893
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Microtubule/Tubulin
Apoptosis
Caspase
Bcl-2 Family
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Cancer
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SP-6-27 is a tubulin depolymerizing agent that binds to the colchicine site of β-tubulin. SP-6-27 induces G2/M cell cycle arrest in ovarian cancer cells. SP-6-27 enhances intrinsic apoptosis in ovarian cancer cells through upregulation of Bax, Apaf-1, caspase-6, caspase-9, and caspase-3. SP-6-27 reduces ovarian cancer cell migration. SP-6-27 inhibits capillary tube formation by human umbilical vein endothelial cells. SP-6-27 shows minimum cytotoxicity to normal ovarian epithelia. SP-6-27 shows enhanced cytotoxicity in chemo-sensitive/resistant ovarian cancer cells when combined with Cisplatin (HY-17394). SP-6-27 can be used for the research of ovarian cancer .
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- HY-15313B
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Histone Demethylase
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Metabolic Disease
Cancer
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CBB1007 hydrochloride is a reversible and selective LSD1 inhibitor with an IC50 of 5.27 µM for human LSD1. CBB1007 hydrochloride significantly blocks the demethylase activity of LSD1 on H3K4Me2 and H3K4Me. CBB1007 hydrochloride shows selectivity for LSD1 over LSD2 or JARID1A, and induces differentiation-related genes in pluripotent cells. CBB1007 hydrochloride is studied in non-pluripotent cancer research, targeting teratocarcinoma, embryonic carcinoma, and seminoma .
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| Cat. No. |
Product Name |
Type |
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- HY-15096
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FJ-776
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Fluorescent Dyes
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MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
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- HY-15794G
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Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
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Fluorescent Dyes
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Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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- HY-D3432
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Fluorescent Dyes
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WazaGaY-1 is an aza-BODIPY derivative, functions as a NIR-I/NIR-II fluorescent contrast agent. WazaGaY-1 undergoes internalization into tumor cells predominantly via clathrin-coated pits. WazaGaY-1 can be used for the research of glioblastoma, ovarian carcinoma and melanoma (Ex/Em = 685/820 nm) .
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| Cat. No. |
Product Name |
Type |
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- HY-B0633E
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Hyaluronan, low endotoxin; Hyaluronate, low endotoxin
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Biochemical Assay Reagents
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Hyaluronic acid, low endotoxin (Hyaluronan, low endotoxin) is a biopolymer composed of repeating disaccharide units containing low levels of endotoxin. Hyaluronic acid is a major component of the extracellular matrix (ECM). It is synthesized on the plasma membrane. Hyaluronic acid exerts its effects by binding to receptors CD44 and RHAMM. Hyaluronic acid activates PI3K-Akt signaling. Hyaluronic acid also enhances cell invasion and angiogenesis by promoting or stimulating the binding of proteolytic MMP-9 to the cell surface. Elevated hyaluronic acid levels are associated with tumor cell growth, adhesion, migration, invasion, and angiogenesis in digestive system cancers. Hyaluronic acid is involved in tissue remodeling and rapid cell proliferation in several physiological processes, including embryonic morphogenesis and wound healing. Hyaluronic acid can be used as a regulator of cancer-associated lymphangiogenesis. Hyaluronic acid can be used as a drug delivery carrier for sodium butyrate, enhancing its anti-proliferative activity against breast cancer cell lines. Hyaluronic acid can lubricate the corneal endothelium. Hyaluronic acid can improve tissue hydration and enhance the resistance of cells to mechanical damage. Hyaluronic acid has been conjugated with antibodies to ensure that the active compound continues to exert its effects at the site of inflammation. Hyaluronic acid can be used in research in the fields of osteoarthritis, ophthalmology, cosmetic dermatology, oncology, and liver diseases .
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- HY-15794G
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Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
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Biochemical Assay Reagents
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Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1181A
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Toll-like Receptor (TLR)
NO Synthase
IKK
Akt
PKC
NF-κB
p38 MAPK
Interleukin Related
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Cardiovascular Disease
Infection
Inflammation/Immunology
Cancer
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Pam2CSK4 TFA is a TLR2 agonist. Pam2CSK4 TFA induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 TFA activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 TFA expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 TFA acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 TFA can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
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- HY-P10816
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Ac-(DLeu)LLLRVK-Amba
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Bacterial
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Infection
Cancer
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PACE4 Inhibitory peptide C23 (Compound C23; Ac-(DLeu)LLLRVK-Amba)), a potent peptidomimetic inhibitor, is a PACE4 inhibitor. PACE4 Inhibitory peptide C23e shows antiproliferative effects against PCa cell lines (Ki = 5 nM; IC50 = 25 and 40 μM for DU145 and LNCaP, respectively). PACE4 Inhibitory peptide C23 also blocks tumor growth in vivo in LNCaP xenograft-bearing mice .
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- HY-P1181
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Toll-like Receptor (TLR)
NO Synthase
IKK
Akt
PKC
NF-κB
p38 MAPK
Interleukin Related
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Cardiovascular Disease
Infection
Inflammation/Immunology
Cancer
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Pam2CSK4 is a TLR2 agonist. Pam2CSK4 induces the expression of iNOS and NO in macrophage cell lines via TBK1 and MyD88 molecules. Pam2CSK4 activates the NF-κB and Bruton's tyrosine kinase signaling pathways in platelets, and promotes platelet-endothelial cell interactions. TLR2 activation triggered by Pam2CSK4 expands myeloid-derived suppressor cells (MDSCs) and suppresses anti-tumor immune responses in the tumor microenvironment. Pam2CSK4 acts as a Th2-polarizing adjuvant in mouse vaccine models against Leishmania major and Brugia malayi. Pam2CSK4 can be used in the research of various diseases, including thromboinflammatory diseases, sepsis, atherosclerosis, heart failure, influenza, lymphoma, melanoma, cutaneous leishmaniasis and lymphatic filariasis .
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- HY-P1632
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Bacterial
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Infection
Cancer
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Tachyplesin I is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I exhibits cytotoxic properties against various human tumor cell lines acting primarily by impairing the integrity of the outer cell membrane .
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- HY-P4056A
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P15-Tat acetate
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Casein Kinase
Apoptosis
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Cancer
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CIGB-300 acetate (P15-Tat acetate) is an anti-casein kinase 2 (CK2) peptide that exhibits anticancer properties by interfering with the phosphorylation of protein kinase CK2. CIGB-300 acetate induces apoptosis in multiple tumor cell lines and can be used in cancer research .
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- HY-P4056
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P15-Tat
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Casein Kinase
Apoptosis
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Cancer
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CIGB-300 (P15-Tat) is an anti-casein kinase 2 (CK2) peptide that exhibits anticancer properties by interfering with the phosphorylation of protein kinase CK2. CIGB-300 induces apoptosis in multiple tumor cell lines and can be used in cancer research .
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- HY-P11050A
-
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Apoptosis
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Cancer
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SP94 is a peptide ligand with high specificity for hepatocellular carcinoma cells. SP94 selectively binds to multiple hepatocellular carcinoma cell lines in vitro. SP94 inhibits tumor growth in a mouse model of hepatocellular carcinoma by promoting apoptosis and reducing angiogenesis. SP94 can be used as a specific probe for hepatocellular carcinoma imaging. SP94 is useful for hepatocellular carcinoma research .
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- HY-161096
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ROR
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Cancer
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Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
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- HY-P10561
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Peptides
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Cancer
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CPK peptide is a tumor-localizing peptide. CPK peptide specifically binds to the monocarboxylate transporter 1 (MCT1) receptor, which is overexpressed in many human colon cancer cell lines but not in normal cells. CPK peptide can be used in tumor diagnosis research .
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- HY-P1632A
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Bacterial
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Infection
Cancer
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Tachyplesin I TFA is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I TFA exhibits cytotoxic properties against various human tumor cell lines acting primarily by impairing the integrity of the outer cell membrane .
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- HY-P2088
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Des-N-tetramethyltriostin A
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Antibiotic
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Cancer
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TANDEM (Des-N-tetramethyltriostin A) is a synthetic antibiotic drug that has the activity of inhibiting the growth of tumor cells. TANDEM can be used in combination with chemotherapy to enhance the inhibitory effect. TANDEM has shown significant inhibitory effects on a variety of cancer cell lines in in vitro experiments. The structure of TANDEM allows it to effectively target tumor cells during the inhibition process. TANDEM's mechanism of action involves interfering with cell proliferation and survival pathways .
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- HY-P10515
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Bacterial
Fungal
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Infection
Cancer
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AcrAP2 is an antimicrobial peptide present in the venom of the Arabian scorpion (Androctonus crassicauda). AcrAP2 is inhibitory against Gram-positive bacteria and yeast but is essentially inactive against Gram-negative bacteria. A cation-enhanced AcrAP2 analog (AcrAP2a) exhibits significant antiproliferative effects at low concentrations against certain human cancer cell lines. AcrAP2 can be used in antibacterial and anti-tumor research .
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- HY-P11658
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Peptoid 1
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Peptides
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Cancer
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Anticancer peptoid 1 (Peptoid 1) is a peptoid with antitumor activity. Anticancer peptoid 1 exerts cytotoxicity primarily via plasma membrane damage. Anticancer peptoid 1 exerts cytotoxicity against a broad range of cancer cell lines, including those with multidrug resistance. Anticancer peptoid 1 inhibits tumor growth in a human breast cancer xenotransplantation mouse model without noticeable acute adverse effects. Anticancer peptoid 1 can be used for the research of cancer, such as breast cancer, and prostate cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P99974
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Nanoparticle albumin-bound Paclitaxel; Nanoparticle albumin-bound ABI-007
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Microtubule/Tubulin
Apoptosis
Autophagy
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Cancer
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Nab-Paclitaxel (Nanoparticle albumin-bound Paclitaxel) is an albumin-bound nanoparticle formulation of Paclitaxel (HY-B0015). Nab-Paclitaxel is composed of albumin and the active pharmaceutical ingredient Paclitaxel, in which human albumin is used as an excipient to disperse and stabilize particles and carry the main drug. Nab-Paclitaxel is a solvent-free taxane with higher response rates and improved tolerability. Nab-Paclitaxel displays less toxicity and greater antitumor activity. Nab-Paclitaxel is more readily available for tumor cell uptake in three rhabdomyosarcoma, seven neuroblastoma cell lines, and one ostersarcoma cell line Nab-Paclitaxel can be studied in cancer research for example breast cancer and solid tumors. (The product specifications below only indicate the effective content of Paditaxel, the actual albumin quality depends on the batch; the ratio of each ingredient in this product is Paditaxel: albumin -1:7~1:11) .
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(5)
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- HY-P99931
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GEN3013
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CD3
CD20
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Cancer
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Epcoritamab (GEN3013) is an bispecific IgG1 antibody redirecting T-cells toward CD3×CD20 + tumor cells. Epcoritamab induces potent T-cell-mediated cytotoxicity towards B-cell NHL cell lines .
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(5)
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- HY-P99361
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PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
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TNF Receptor
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Cancer
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Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
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(5)
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- HY-P9983
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SGN-33; HuM-195; GLK-33 Antibody
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Transmembrane Glycoprotein
Radionuclide-Drug Conjugates (RDCs)
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Inflammation/Immunology
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Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
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(5)
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- HY-P991372
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RN927C antibody
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TROP2
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Cancer
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Anti-TROP2 Antibody (RN927C antibody) is a human monoclonal antibody targeting Trop-2. Anti-TROP2 Antibody exerts in vitro inhibitory effects on a variety of tumor cell lines. Anti-TROP2 Antibody exhibits anti-tumor activity in mouse pancreatic PDX, ovarian PDX, lung PDX and triple-negative breast cancer (TNB) PDX models. Anti-TROP2 Antibody can be used for research on pancreatic cancer, ovarian cancer, lung cancer and triple-negative breast cancer .
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(5)
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- HY-P99413
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ASP1650
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HCV
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Cancer
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IMAB027 (ASP1650) is a specific anti-CLDN6 mAb, while CLDN6 (Claudin 6) is a tight junction membrane protein, aberrantly expressed in various human cancer types, ovarian cancers particularly. IMAB 027 shows anti-tumor activity, and induces apoptosis in CLDN6 + ovarian and testicular cancer cell lines .
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(5)
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- HY-P990905
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SAR-443579
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Interleukin Related
|
Cancer
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Bexatamig (SAR-443579) is a trifunctional natural killer cell engager targeting IL-3R α/CD123, NKp46/NCR1/CD335 and Fc gamma RIIIA/CD16a. Bexatamig forms a cytolytic synapse between natural killer cells and CD123-positive tumor cells. By activating natural killer cells to induce tumor cell death, Bexatamig effectively reduces the burden of CD123-positive acute myeloid leukemia (AML) blasts. Bexatamig has been granted FDA Fast Track designation, and is primarily investigated for relapsed or refractory acute myeloid leukemia, B-cell acute lymphoblastic leukemia, and high-risk myelodysplastic syndromes .
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(5)
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- HY-P991555
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TNF Receptor
Apoptosis
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Cancer
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XmAb5485 is an Fc-engineered humanized anti-CD40 monoclonal antibody with high affinity to Fc-γ receptors. XmAb5485 induces potent antibody-dependent cell-mediated cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis (ADCP) against tumor cells. XmAb5485 inhibits proliferation and induces apoptosis of tumor cells. XmAb5485 shows highly cytotoxic against lymphoma, leukemia and multiple myeloma cell lines as well as primary cancer cells .
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(5)
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- HY-P990716
-
|
AZD7789
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PD-1/PD-L1
Tim3
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Inflammation/Immunology
|
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Sabestomig (AZD7789) is a monovalent bispecific antibody targeting PD-1 and TIM-3. Sabestomig binds to PD-1 and an epitope in the TIM-3 IgV domain outside the phosphatidylserine-binding cleft, thereby precisely regulating immune responses. Sabestomig promotes IL-2 production, efferocytosis and cross-presentation of tumor antigens, and enhances the release of anti-tumor T cell cytokines, cytotoxicity, and secretion of IFN-γ. Sabestomig inhibits the growth of solid tumors, prolongs the duration of tumor suppression, and significantly enhances anti-tumor responses following anti-PD-1 therapy. Sabestomig has been used in studies related to non-small cell lung cancer and classical Hodgkin lymphoma .
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(5)
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- HY-P991982
-
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ADC Antibody
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Cancer
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ZV0201 Antibody (ZV02) is a monoclonal antibody inhibitor targeting Her2. ZV0201 Antibody can be used to synthesize the antibody-drug conjugate (ADC) ZV0201. ZV0201 Antibody can be used to research related to HER2-positive tumors .
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(5)
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- HY-P992340
-
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Radionuclide-Drug Conjugates (RDCs)
TNF Receptor
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Cancer
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CTB006 is a monoclonal antibody targeting a humanized chimeric recombinant anti-DR5. CTB006 specifically binds to and activates DR5, thereby inducing tumor cell apoptosis, inhibiting tumor growth and reducing tumor drug resistance. 177Lu-radiolabeled CTB006 can deliver targeted radiotherapy to tumor cells; while 89Zr- or 177Lu-labeled CTB006 can serve as a PET/CT imaging agent for detecting DR5 expression levels in preclinical tumor models and screening cancers with DR5 overexpression. CTB006 can be applied to research related to gastrointestinal cancer, colorectal cancer and other solid tumors .
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(5)
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- HY-P992483
-
|
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Transmembrane Glycoprotein
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Cancer
|
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VIS832 is an anti-CD138 monoclonal antibody. VIS832 induces antibody-dependent cellular cytotoxicity. VIS832 inhibits the growth of disseminated multiple myeloma tumors in vivo. VIS832 exerts anti-tumor effects on multiple myeloma in combination with Lenalidomide (HY-A0003) or Bortezomib (HY-10227). VIS832 can be used in research related to multiple myeloma .
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(5)
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- HY-P992414
-
|
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Inhibitory Antibodies
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Cancer
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MS17-38 is a monoclonal antibody targeting PODXL-v2. MS17-38 binds to a specific conformational epitope of PODXL-v2 on gastric cancer cells, modulates target function, inhibits gastric cancer cell growth and migration, and blocks tumor growth and lung metastasis. MS17-38 can be used for the research of gastric cancer .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0367
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- HY-N0120
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(E/Z)-Piceid
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Structural Classification
Stilbenes
Classification of Application Fields
Polygonaceae
Reynoutria japonica Houtt.
Phenols
Polyphenols
Plants
Inflammation/Immunology
Disease Research Fields
Source Classification
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Drug Isomer
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(E/Z)-Polydatin ((E/Z)-Piceid) is a mixture of the E/Z configurations of Polydatin (HY-N0120A). Polydatin can be isolated from Polygonum cuspidatum, grapes, peanuts, red wine, hop pellets, cocoa-containing products and chocolate products. Polydatin exhibits multiple biological properties, such as anti-platelet aggregation, anti-low-density lipoprotein oxidation, cardioprotective activity, anti-inflammatory and immunomodulatory functions. Polydatin shows favorable cytotoxic effects against various tumor cell lines, including cervical cancer cells, liver cancer cells, and nasopharyngeal carcinoma cells .
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- HY-N2040
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- HY-18979
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- HY-121382
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- HY-119529
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- HY-N4201
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- HY-113081R
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Alkaloids
Structural Classification
Microorganisms
Immune System Disorder
Disease markers
Endogenous metabolite
Cancer
Source Classification
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Reference Standards
Endogenous Metabolite
PPAR
Hedgehog
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1-Methyladenosine (Standard) is the analytical standard of 1-Methyladenosine. This product is intended for research and analytical applications. 1-Methyladenosine is an RNA modification that can serve as a tumor marker, with elevated levels in the body associated with cancer development. Following 1-methyladenosine methylation, upregulation of PPARδ expression regulates cholesterol metabolism and activates Hedgehog signaling pathway, driving liver tumorigenesis .
In Vitro:Compared to surrounding tumor tissues, 1-methyladenosine methylation in RNA is aberrantly elevated in hepatocellular carcinoma (HCC) cell lines and liver cancer stem cells (CSCs). Methylated 1-methyladenosine can promote cholesterol synthesis and activate the Hedgehog signaling pathway by enhancing the translation of PPARδ in liver CSCs, ultimately driving the self-renewal and tumorigenesis of liver cancer stem cells .
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- HY-N6990
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- HY-N12461
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- HY-123298
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- HY-130995
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- HY-125443
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Triterpenes
Microorganisms
Terpenoids
Source Classification
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Others
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Lucialdehydes A is a lanostante-type triterpene aldehydes, isolated from the fruiting bodies of Ganoderma lucidum. Lucialdehydes A shows cytotoxic effects on tumor cells, including Lewis lung carcinoma (LLC), T-47D, Sarcoma 180, and Meth-A tumor cell lines .
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- HY-N7611
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- HY-N9339
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- HY-N6955
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- HY-129337
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- HY-N7205
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- HY-N11928
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- HY-N10904
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- HY-W106860
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- HY-118893
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- HY-N16580
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- HY-125117
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-
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- HY-125664
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- HY-W587938
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(+)-γ-Eudesmol
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Terpenoids
Sesquiterpenes
Rutaceae
Plants
Amyris balsamifera L.
Source Classification
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Apoptosis
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γ-Eudesmol ((+)-γ-Eudesmol) is a mitochondrial-mediated apoptosis inducer. γ-Eudesmol binds mitochondrial membrane proteins, triggering depolarization of mitochondrial membrane potential and activating caspase cascades. γ-Eudesmol demonstrates cytotoxicity against multiple tumor cell lines (e.g., HepG2, B16-F10) with IC50 values ranging from 8.86-15.15 μg/mL. γ-Eudesmol is promising for research of cancers, such as hepatocellular carcinoma and melanoma .
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- HY-N14293
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- HY-130996
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- HY-N10265
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- HY-136824
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- HY-N3215
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- HY-N12430
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- HY-N14892
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- HY-N14369
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- HY-N15055
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Natural Products
Microorganisms
Source Classification
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Antibiotic
Bacterial
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Propeptin is a peptide antibiotic composed of 19 amino acids. Propeptin has weaker activity against Pseudomonas aeruginosa, Mycobacterium monobacterium, and Xanthomonas oryzae. Propeptin has no effect on KB and L1210 cells of tumor cell lines, but has an inhibitory effect on prolyl endopeptidase .
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- HY-N12128
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- HY-N12437
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- HY-N12141
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- HY-N6679
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- HY-N15714
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- HY-N15112
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- HY-N14144
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- HY-N6061
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- HY-N15636
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- HY-N12834
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Apocynaceae
Structural Classification
Plants
Urceola rosea (Hook. & Arn.) D. J. Middleton
Steroids
Source Classification
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Others
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Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato .
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- HY-N15614
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Alkaloids
Erythrophleum fordii Oliv.
Leguminosae
Other Alkaloids
Plants
Source Classification
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Others
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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-N12198
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Natural Products
Microorganisms
Source Classification
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Others
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Mollicellin H is a secondary metabolite of the fungus C. brasiliense and has a wide range of biological activities, including immunomodulation, cytotoxicity and anti-tumor effects. The growth inhibitory effects (GI50s) of Mollicellin H on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines are 5.1 μg/mL, 6.5 μg/mL and 2.5 μg/mL respectively .
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- HY-N14722
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Microorganisms
Antibiotics
Other Antibiotics
Source Classification
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Bacterial
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Lactonamycin had strong activity against Gram-positive bacteria including Staphylococcus, Streptococcus, Enterococcus, MRSA (MIC of 0.39-0.78 μg/mL) and VRE (MIC of 0.39-0.78 μg/mL). Lactonamycin also has inhibitory effect on L-1210, P388, S180, FS-3, Ehrlich, B16-BL5 and other tumor cell lines (IC50s of 0.06-3.3 μg/mL) .
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- HY-N0367R
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- HY-121382R
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Triterpenes
Structural Classification
Terpenoids
Plants
Caryophyllaceae
Source Classification
Gypsophila perfoliata Linn.
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Reference Standards
Apoptosis
Cholinesterase (ChE)
Necroptosis
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Cinosulfuron (Standard) is the analytical standard of Cinosulfuron. This product is intended for research and analytical applications. Gypsogenin is a selective mixed-type BChE inhibitor (Ki=19.99 μM) that also exhibits significant cytotoxicity against various human cancer cell lines. Gypsogenin inhibits tumor growth by inducing cell cycle arrest and triggering apoptosis. Gypsogenin displays antibacterial activity against bacteria such as Bacillus subtilis and Bacillus thuringiensis, and often serves as a key parent nucleus for the synthesis of anticancer compounds. Gypsogenin is widely used in research on Alzheimer's disease and various cancers including colon cancer, melanoma, and leukemia .
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- HY-N18195
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- HY-114639
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- HY-N14893
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- HY-N18186
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- HY-N15715
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- HY-N1691
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- HY-N14530
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Natural Products
Microorganisms
Source Classification
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Bacterial
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Cremeomycin has anti-Gram-positive bacteria activity including methicillin-resistant Staphylococcus aureus (MRSA), MIC is 0.2-0.39 μg/mL. Cremeomycin shows cytotoxicity to mouse tumor cell lines P388, L1210, IMC, S180, B16 and SS3 in vitro .
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- HY-N18247
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- HY-N17550
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- HY-W106860R
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- HY-N16876
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- HY-W750980
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-19542S1
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|
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C6 Ceramide-d11 is deuterated labeled C6 Ceramide (HY-19542). C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
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- HY-170905S
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MAT2A-IN-22 (Compound 29-1) is a BBB-penetrable and orally active MAT2A inhibitor with an IC50 of 4 nM. MAT2A-IN-22 shows selectivity and inhibitory activity against MTAP-deficient cancer cell lines. MAT2A-IN-22 has anti-tumor effects .
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- HY-109583S
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4-Oxofenretinide-d4 (4-Oxo-4-HPR-d4) is deuterium labeled 4-Oxofenretinide. 4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
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- HY-N0367S
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Trans-Anethole-d3 is deuterated labeled Trans-Anethole (HY-N0367). Trans-Anethole ((E)-Anethole) is an orally active phenylpropene derivative found in Foeniculum vulgare that is estrogenic at low concentrations and cytotoxic at high concentrations in tumor cell lines. Trans-Anethole also has anti-aflatoxin, anti-thrombotic and anti-diabetic activities. Trans-Anethole is an important odor component in plants such as fennel, myrtle, liquorice, and camphor .
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- HY-172733S
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PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
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- HY-180885S
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KRAS G12D-IN-35 (example 7) is a potent and orally active KRAS G12D inhibitor. KRAS G12D-IN-35 suppresses p-ERK in AGS cells and potently inhibits the proliferation of various KRAS G12D-mutant cancer cell lines. KRAS G12D-IN-35 inhibits tumor growth in HPAC and GP2D mouse models. KRAS G12D-IN-35 can be used for cancer research, such as pancreatic and colorectal cancer .
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| Cat. No. |
Product Name |
|
Classification |
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- HY-139659
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|
|
|
PROTAC Synthesis
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ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 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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| Cat. No. |
Product Name |
|
Classification |
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- HY-50909
-
|
KRX-0401; NSC 639966; D21266
|
|
Phospholipids
|
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Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
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- HY-145729
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AZD9150
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Antisense Oligonucleotides
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Danvatirsen (AZD9150) is an antisense oligonucleotide targeting STAT3. Danvatirsen reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
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- HY-160066
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Aptamers
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SYL3C aptamer sodium is a DNA aptamer that targets epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets a variety of human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd values of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III are 38 nM and 67 nM, respectively. SYL3C aptamer sodium possesses stability, high binding affinity and selectivity, and can be used for targeted cancer cell imaging and circulating tumor cell detection .
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- HY-145729A
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AZD9150 sodium
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Antisense Oligonucleotides
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Danvatirsen sodium (AZD9150 sodium) is an antisense oligonucleotide targeting STAT3. Danvatirsen sodium reduces the viability and promotes apoptosis of leukemia cell lines. Danvatirsen sodium inhibits the expression of endogenous STAT3 and its downstream target genes, and reduces the proliferation and tumorigenicity of neuroblastoma and lymphoma cells. Danvatirsen sodium inhibited tumor growth in mouse models of neuroblastoma, lymphoma, and non-small cell lung cancer. Danvatirsen sodium achieves STAT3 mRNA and protein depletion in a mouse model of epidermoid carcinoma. Danvatirsen sodium can be used in research related to lymphoma, myelodysplastic syndrome, acute myeloid leukemia, neuroblastoma and non-small cell lung cancer .
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- HY-148413
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ISIS 3521 sodium
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Antisense Oligonucleotides
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Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .
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- HY-174512
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mRNA
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Human TNFSF8 mRNA encodes the human TNF superfamily member 8 (TNFSF8) protein, a cytokine that belongs to the tumor necrosis factor (TNF) ligand family. TNFSF8 was shown to enhance cell proliferation of some lymphoma cell lines, while to induce cell death and reduce cell proliferation of other lymphoma cell lines.
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- HY-148827
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HYBO-165
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Antisense Oligonucleotides
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GEM231 is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
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- HY-148827A
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HYBO-165 sodium
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Antisense Oligonucleotides
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GEM231 sodium is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 sodium induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
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| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-15794G
-
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Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
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G-quadruplex
|
Cancer
|
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Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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