Search Result
Results for "
MCF‐7
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-137099A
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Others
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Endocrinology
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Genistein 7-sulfate sodium is a metabolite of genistein that can reduce the activity of estrogen agonists in MCF-7 cells. Genistein 7-sulfate sodium can promote the growth of MCF-7 cells at concentrations of 10 μM and above .
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- HY-N10871
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Others
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Cancer
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Neocryptomerin, a biflavonoid, shows inhibitory activity against U251, MCF-7, HeLa cell .
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- HY-169122
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Others
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Cancer
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LLC1 is an amiloride (HY-B0285) derivative with cytotoxicity against breast cancer cells, particularly those resistant to treatment. The IC50 values of LLC1 for MCF7, MCF7 MX-100, MCF7 TS, MCF7 TR-1, and MCF7 TR-5 are 13, 12, 25, 26, and 19 mM, respectively. LLC1 shows potential for research in the field of cancer therapy .
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- HY-137099
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Others
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Endocrinology
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Genistein 7-sulfate is a metabolite of genistein that can reduce the activity of estrogen agonists in MCF-7 cells. Genistein 7-sulfate can promote the growth of MCF-7 cells at concentrations of 10 μM and above .
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-
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- HY-W016794
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Reactive Oxygen Species
Apoptosis
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Cancer
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NSC3852 exhibits anti-proliferative activity against cancer cell MCF-7. NSC3852 promotes the ROS generation, DNA damage, and apoptosis in MCF-7. NSC3852 exhibits anti-tumor against leukemia in mouse model
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- HY-N11973
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Others
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Cancer
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5,7-Dimethoxy-2,3-phenanthrenediol is a compound with estrogenic activity. 5,7-Dimethoxy-2,3-phenanthrenediol increases the proliferation of MCF-7 cell and the expression of ERβ in the MCF-7 cell line .
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- HY-153700
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Estrogen Receptor/ERR
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Endocrinology
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Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM .
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- HY-144637
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Apoptosis
Autophagy
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Cancer
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Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
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- HY-144306
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Estrogen Receptor/ERR
Apoptosis
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Cancer
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ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
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- HY-161858
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PI3K
Akt
Apoptosis
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Cancer
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EpskA21 is an inhibitor for PI3K/AKT signaling pathway, and inhibits the proliferation of cancer cells MCF-7, A549, MIA-PaCa-2, Panc-1 and HepG2, with IC50 of 1.3-7.24 μM. EpskA21 inhibits the cell migration, arrests the cell cycle at G2/M (MCF-7) and S (MIA-PaCa-2) phase, and induces apoptosis in MCF-7 and MIA-PaCa-2. EpskA21 causes the mitochondrial dysfunction .
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- HY-145866
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Others
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Cancer
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Antiproliferative agent-3 (comp 4) shows the highest potency for MCF-7 cells (IC50 = 0.19 nM) .
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- HY-163281
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Fluorescent Dye
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Cancer
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FSY-OSO2F shows an uptake in MCF-7 cells through the regulation of L-Tyr, ASC, and ASC2 transporters. FSY-OSO2F can be used as a PET tracer, when labeled with 18F, and exhibits good uptake and good contrast in MCF-7 and 22Rv1 subcutaneous tumors .
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- HY-153469
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ADC Cytotoxin
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Cancer
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Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .
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- HY-155841
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-46 (compound 9q) is a microtubule/Tubulin inhibitor that inhibits tubulin polymerization and induces apoptosis. Tubulin polymerization-IN-46 inhibits mitosis and arrests MCF-7 cells in the G2/M phase. Tubulin polymerization-IN-46 has anti-proliferative activity against MCF-7 breast cancer cells with an IC50 of 10 nM .
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- HY-163126
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Cholinesterase (ChE)
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Cancer
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AChE-IN-52 (compound A6) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-52 shows antitumor efficacy, especially against breast cancer MCF-7 cells. AChE-IN-52 significantly disrupts the amino acid metabolism and inhibits migration of MCF-7. AChE-IN-52 plays anticancer role by regulating Best1 and HIST1H2BJ .
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- HY-134964
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- HY-163679
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Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
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Cancer
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PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
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- HY-N5103
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Others
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Endocrinology
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Genistein 7,4'-di-O-β-D-glucoside is a natural product with significantly estrogenic proliferative effect in MCF-7 cells .
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- HY-147967
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EGFR
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Cancer
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EGFR-IN-63 is an EGFR inhibition (IC50: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC50: 2.49 μM).
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- HY-N3042
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Platyphyllone
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Others
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Cancer
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Platyphyllonol (Platyphyllone) can be isolated from A. japonica. Platyphyllonol shows cytotoxic effects on MCF-7 cells with IC50 values of 46.9 μg/mL .
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- HY-N4010
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Others
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Cancer
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Iriflophenone, isolated from Aquilaria sinensis, stimulates MCF-7 and T-47D human breast cancer cells proliferation .
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- HY-132247B
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Others
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Cancer
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(S)-ErSO is the dextrorotatory enantiomer of ErSO. (S)-ErSO is inactive in MCF-7 cells (from patent WO2020009958A1, compound (s)-105) .
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- HY-N8679
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Endogenous Metabolite
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Cancer
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Physalin C is a natural product that can be found in physalis angulata. Physalin C shows cytotoxic activities against MCF-7 and HepG2 cells .
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- HY-103452
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Estrogen Receptor/ERR
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Endocrinology
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RU58668 is a steroidal antiestrogen that can be used as a potent antiproliferative agent on MCF-7 cells. RU58668 has the potential for the breast cancer research .
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- HY-W747516
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Antibiotic
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Infection
Cancer
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Butylcycloheptylprodigiosin is the secondary metabolite produced by some bacteria, such as Streptomyces. Butylcycloheptylprodigiosin is a red-pigmented antibiotic and exhibits cytotoxicity against cancer cell MCF-7 and HDF .
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- HY-13686
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PQ401
2 Publications Verification
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IGF-1R
Apoptosis
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Cancer
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PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis .
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- HY-118129
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Ganwuweizic acid
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PARP
Apoptosis
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Cancer
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Schisandronic acid is a triterpenoid antioxidant and anticancer agent extracted from Schisandra chinensis, which has potent cytotoxicity against human breast cancer cells, especially MCF-7. Schisandronic acid induces apoptosis and reduces cell viability in a time-dependent manner (MCF-7, IC50=8.06 μM). Schisandronic acid can upregulate active caspase-3 expression and cleave PARP, reduce the generation of reactive oxygen species and exhibit antioxidant effects .
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- HY-13668
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PaTrin-2
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DNA Methyltransferase
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Cancer
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Lomeguatrib is a O 6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ~6?nM in MCF-7 cells.
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- HY-N2887
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Others
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Cancer
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Araliadiol is a polyacetylenic compound isolated from the leaves of Aralia cordata Thunb. Araliadiol inhibits MCF-7 cells growth with an IC50 value of 6.41 μg/mL .
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- HY-156879
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Others
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Cancer
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Antiproliferative agent-40 (Compound 9) inhibits proliferation of HT1080 and MCF-7 with IC50s of 52 and 8.2 μM respectively .
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- HY-N2198
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Topoisomerase
Apoptosis
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Cancer
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Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .
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- HY-N10305
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Autophagy
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Cancer
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Clionamine B is an autophagy stimulating aminosteroid isolated from the sponge Cliona celata. Clionamine B strongly stimulates autophagy in human breast cancer MCF-7 cells .
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- HY-158388
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Topoisomerase
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Cancer
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Anticancer agent 215 (1) is a Camptothecin compound, with IC50 values of 5.2 nM and 8.2 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
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- HY-158389
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Topoisomerase
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Cancer
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Anticancer agent 216 (34A) is a Camptothecin compound, with IC50 values of 9.6 nM and 11.6 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
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- HY-158387
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Topoisomerase
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Cancer
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Anticancer agent 214 (2) is a Camptothecin compound, with IC50 values of 2.6 nM and 15.7 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
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- HY-156114
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EGFR
CDK
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Cancer
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EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor of EGFR and CDK-2 with IC50s of 19.6 and 87.9 nM, respectively. EGFR/CDK2-IN-2 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-2 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 0.39 μM .
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- HY-156115
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EGFR
CDK
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Cancer
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EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC50s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 3.16 μM .
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- HY-156116
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EGFR
CDK
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Cancer
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EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC50s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 2.74 μM .
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- HY-158390
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Topoisomerase
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Cancer
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Anticancer agent 217 (35B) is a Camptothecin compound, with IC50 values of 6.2 nM and 7.1 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
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- HY-N2863
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Others
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Cancer
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Goniothalenol is a styryl lactone that can be isolated from Goniothalamus griffithii. Goniothalenol exhibits cytatoxic activity against A2780, HCT-8, KB and MCF-7 cell lines .
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- HY-N7464
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Others
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Others
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Jolkinolide E is a casbane diterpenoid from the roots of Euphorbia rapulum. Jolkinolide E shows weak selective activity against HepG2, MCF-7, and C6 cell lines .
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- HY-168644
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- HY-168589
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Apoptosis
Cytochrome P450
Caspase
Reactive Oxygen Species
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Cancer
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Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
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- HY-147887
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells .
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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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- HY-N7589
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Carolignan M
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Others
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Cancer
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Demethylcarolignan E is a phenylpropanoid ester that can be isolated from the stems of Hibiscus taiwanensi. Demethylcarolignan E has cytotoxicity against human cancer lines A549 and MCF-7 (IC50: <10 μg/mL) .
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- HY-14307
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Others
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Cancer
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Necrocide 1 (compound (S)-38) a potent anticancer agent. Necrocide 1 has antiproliferative activity with an IC50 value of 0.48 and 2 nM for MCF-7 and PC3, respectively .
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- HY-162035
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MDM-2/p53
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Cancer
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MDM2-IN-23 (compound 5d) is an inhibitor of MDM2. MDM2-IN-23 has an IC50 of 60.09 μM on MCF-7 cells .
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- HY-161692
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Estrogen Receptor/ERR
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Cancer
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ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC50 value of 0.15 μM .
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- HY-N3722
-
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Others
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Cancer
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O-Demethylmurrayanine is a natural phenol with anticancer effects. O-Demethylmurrayanine exhibits strong cytotoxicity against MCF-7 and SMMC-7721 with IC50 values in the range 4.42-7.59 μg/mL .
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- HY-155167
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Antibiotic
Fungal
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Cancer
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Anticancer agent 151 (compound 6C) is an anticancer agent. Anticancer agent 151 exhibits excellent in vitro cytotoxic activity against MCF-7 cells with an IC50 value of 6.3 μM .
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- HY-158743
-
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Others
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Cancer
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Indium (III) thiosemicarbazone 5b (compound 5b) is an Indium (III) thiosemicarbazone agent. Indium (III) thiosemicarbazone 5b effectively inhibits MCF-7 and DDP tumor cells growth .
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- HY-147504
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Apoptosis
Caspase
Bcl-2 Family
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Cancer
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Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity .
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- HY-22024
-
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Others
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Cancer
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5-Hydroxyflavone, a flavonoid ligand, shows no cytotoxic activity against MCF-7, FaDU, MDA-MB-435S, U87, RPE-1, and HEK293 cells .
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- HY-N8859
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16-Hydroxyiridal
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Others
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Others
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Isoiridogermanal can be isolated from the extract of rhizomes of Iris tectorum Maxim. Isoiridogermanal is cytotoxic with IC50 values of 11 μM and 23 μM against MCF-7 and C32 cell lines.
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- HY-P5956
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Caspase
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Cancer
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Ac-AAVALLPAVLLALLAP-LEHD-CHO is an inhibitor of caspases 4, 5 and 9. Ac-AAVALLPAVLLALLAP-LEHD-CHO shows protective effects upon Neocarzinostatin (HY-111183)-treated MCF-7 cells .
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- HY-100219
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VD/VDR
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Cancer
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CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM .
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- HY-115948
-
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Others
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Cancer
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Antitumor agent-46 (Compound 2h) is an anti-tumor agent. Antitumor agent-46 demonstrates markedly higher antiproliferative activity on MCF-7 cells with an IC50 value of 2.08 µM .
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- HY-148453
-
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Others
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Cancer
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Antiproliferative agent-16 is an indolyl hydrazide-hydrazone compound with anticancer activity. Antiproliferative agent-16 exhibits specificity toward breast cancer cells (IC50 of 6.94 μM for MCF-7 cells) .
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- HY-163812
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Molecular Glues
Estrogen Receptor/ERR
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Cancer
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ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .
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- HY-135584
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Estrogen Receptor/ERR
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Endocrinology
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Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6 .
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- HY-135590
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Estrogen Receptor/ERR
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Endocrinology
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Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6 .
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- HY-N9391
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Apoptosis
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Cancer
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7,3′,5′-Trihydroxyflavanone, a flavanoid derivative, induces the apoptotic cell death of MCF-7 cells by increasing Bax expression level. 7,3′,5′-Trihydroxyflavanone also exhibits antioxidant activity .
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- HY-107550
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HDAC
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Cancer
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TCS HDAC6 20b is a HDAC6-selective inhibitor. TCS HDAC6 20b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells .
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- HY-N10846
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Others
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Others
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Neotriptonoterpene, a compound isolated from T. regelii, shows weak cytotoxic activity against A2780, HepG2 and MCF-7 cells with IC50 values of 65.80, 35.45 and 64.80 µM respectively .
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- HY-163308
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Bcl-2 Family
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Cancer
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Bcl-2-IN-18 (Compound 23) is a breast cancer Bcl-2 inhibitor with a IC50 value of 4.7 μM for MCF-7. Bcl-2-IN-18 has antitumor activity .
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- HY-13762
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Cytochrome P450
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Cancer
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Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
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- HY-147781
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Apoptosis
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Cancer
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Anticancer agent 66 (Compound 13e) is an anti-cancer agent. Anticancer agent 66 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 66 is a ciprofloxacin analog .
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- HY-147782
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Apoptosis
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Cancer
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Anticancer agent 67 (Compound 13g) is an anti-cancer agent. Anticancer agent 67 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 67 is a ciprofloxacin analog .
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- HY-147882
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Bacterial
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Infection
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Anti-MRSA agent 6 (compound 3q6) is a potent anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) agent. Anti-MRSA agent 6 shows low cytoxicity for MCF-7, A549 cells .
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- HY-112721
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FDI-6
2 Publications Verification
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DNA/RNA Synthesis
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Cancer
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FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.
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- HY-N11438
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Estrogen Receptor/ERR
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Cancer
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3'-Hydroxymirificin (compound 3) is a naural compound that can be isolated from Pueraria lobata roots. 3'-Hydroxymirificin (compound 3) possesses estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
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- HY-162239
-
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Others
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Cancer
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Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
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- HY-B0812
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SSA dihydrate
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Biochemical Assay Reagents
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Cancer
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5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
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- HY-160811
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VEGFR
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Cancer
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hVEGF-IN-3 (compound 9) is a potent hVEGF inhibitor. hVEGF-IN-3 inhibits HT-29, MCF-7, and HEK-293 cells proliferation with IC50s of 61, 142, and 114 μM .
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- HY-161641
-
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
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- HY-161852
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PI3K
Apoptosis
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Cancer
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PI3K-IN-55 (Compound 6a) is a potent inhibitor for PI3K. PI3K-IN-55 affects PI3K/Akt/p53 signaling pathway, inhibits the proliferation of cancer cells A549, Hela, HepG2, MCF-7 and HT-29, with IC50s of 1.03-6.78 μM. PI3K-IN-55 induces apoptosis in cell MCF-7 .
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- HY-146162
-
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Others
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Cancer
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Colletotrichalactones A is a polyketide that display moderate-to-potent cytotoxic activities against MCF7 cells with an IC50 of 35.06 µM .
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- HY-13734
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IV-2
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Others
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Cancer
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PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
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-
- HY-N3443
-
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Others
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Cancer
|
Jolkinol A is a natural product that can be found in Euphorbia pubescens. Jolkinol A inhibits cell growth with GI50s of 95.3, 57.3, >100 µM for MCF-7, NCI-460, SF-268 cells, respectively .
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- HY-N3261
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AP-1
ERK
STAT
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Inflammation/Immunology
Cancer
|
Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis .
|
-
- HY-N11919
-
|
Others
|
Cancer
|
Anticancer agent 149 (compound 3) is an anticancer agent isolated from the rhizome of Dioscorea dioscorea (DM). Anticancer agent 149 exhibits selective cytotoxic activity against MCF-7 cells (IC50=31.41 μM) .
|
-
- HY-156878
-
|
Others
|
Cancer
|
Antiproliferative agent-39 (Compound 12) inhibits proliferation of A549, SNU-638, Col2, HT1080, MCF-7 with IC50s of 11, 25, 14, 11, 6.3 μM respectively .
|
-
- HY-N4227
-
|
Others
|
Cancer
|
Conicasterol is a 4-mercaptosteroid with significant cytotoxic activity. Conicasterol showed an IC50 value of 6.23 μg/mL in a test on a human breast adenocarcinoma cell line (MCF-7). Conicasterol's antitumor activity makes it a potential bioactive lead molecule .
|
-
- HY-111524
-
|
HSP
Apoptosis
|
Cancer
|
CPUY201112 is a potent heat shock protein Hsp90 inhibitor with Kd of 27 nM. CPUY201112 induces p53-mediated apoptosis in MCF-7 cells, resulting in cell cycle arrest, which can be used in cancer research .
|
-
- HY-N7302
-
|
Others
|
Cancer
|
Anthracophyllone is an aristolane sesquiterpene that can be isolated from the mushroom Anthracophyllum. Anthracophyllone has cytotoxicity against MCF-7, KB, NCI-H187, Vero cells (IC50: 32.97, 18.02, 15.17, 18.06 μM) .
|
-
- HY-153697
-
|
FAK
|
Cancer
|
FAK-IN-10 is an inhibitor of FAK with an IC50 of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC50s of 4.23 and 0.78 μM,respectively .
|
-
- HY-113796
-
|
Others
|
Cancer
|
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
|
-
- HY-N13213
-
|
Others
|
Cancer
|
Fenugreek Seed Extract is a fenugreek extract. Fenugreek Seed Extract has potential antibacterial and anticancer activities, can inhibit Staphylococcus aureus and Pseudomonas aeruginosa, and inhibit the proliferation of MCF-7 breast cancer cells (no significant effect on liver cancer cells). .
|
-
- HY-163947
-
|
VD/VDR
|
Cancer
|
UG-480 is a gemini analog that effectively stabilizes the active VDR conformation. UG-480 has antiproliferative effects in estrogen receptor-positive MCF-7 breast adenocarcinoma cells. UG-480 can be used in cancer research .
|
-
- HY-161769
-
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
|
-
- HY-121149
-
3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
|
-
- HY-N3000
-
|
Others
|
Cancer
|
6-Methoxydihydrosanguinarine is an lkaloid isolated from the fruits of M.cordata. 6-Methoxydihydrosanguinarine shows strong cytotoxicity against MCF-7 and SF-268 cell lines with IC50 values of 0.61 μM and 0.54 μM, respectively .
|
-
- HY-N10959
-
|
Others
|
Cancer
|
4,15-Isoatriplicolide methylacrylate is a germacrane-type sesquiterpene lactone. 4,15-Isoatriplicolide methylacrylate also is a cytotoxic agent. 4,15-Isoatriplicolide methylacrylate has cytotoxic activity for MCF-7 human breast cancer cell line .
|
-
- HY-144337
-
|
DNA Alkylator/Crosslinker
|
Cancer
|
DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
|
-
- HY-135309
-
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM .
|
-
- HY-13847
-
|
mTOR
|
Cancer
|
GNE-555 is a selective, metabolically stable mTOR inhibitor (Ki=1.5 nM) that also has good oral bioavailability. GNE-555 exhibits antiproliferative activity on PC3 and MCF-7 cells and can be used in cancer research .
|
-
- HY-N1252
-
|
Others
|
Cancer
|
Scillascillin (compound 10) is a homoisoflavanone. Scillascillin can be isolated from S. scilloides. Scillascillin shows anticancer activity towards MCF-7 (breast cancer) and DU-145 (prostate cancer) cells with the IC50 of 9.59 and 11.32 ug/ml, respectively .
|
-
- HY-18351A
-
LMP-400 hydrochloride; NSC-724998 hydrochloride
|
Topoisomerase
|
Infection
Cancer
|
Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-144792
-
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-144791
-
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-N7654
-
|
Apoptosis
|
Cancer
|
(-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro .
|
-
- HY-144314
-
|
Estrogen Receptor/ERR
|
Cancer
|
PSDalpha is an ERα degrader conjugating photosensitizer (PS), triphenylamine benzothiadiazole (TB) and 17β-estradiol via an acetylene bond. PSDalpha shows excellent anti-proliferation performance on MCF-7 cells. The maximum absorption wavelength of PSDalpha in the visible region is located at 465 nm .
|
-
- HY-161146
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-100 (compound 3f) is a EGFR inhibitor with IC50 range of 0.137-0.507 μM. EGFR-IN-100 has antiproliferative activity and induces the apoptosis pathway. EGFR-IN-100 arrests the MCF-7 cell cycle at the S phase .
|
-
- HY-126803
-
|
Antibiotic
|
Infection
Cancer
|
Saquayamycin B (compound 3) is a new angucycline antibiotic. Saquayamycin B has antitumor activities against a human lung (H-460) and a human breast cancer cell line (MCF-7) with GI50 values of 12.2 and 15.2 µM respectively .
|
-
- HY-W560574
-
|
Xanthine Oxidase
|
Cancer
|
Xanthine oxidase-IN-14 (Compound 3f) is an inhibitor for xanthine oxidase, with IC50 >100 μM. Xanthine oxidase-IN-14 inhibits proliferations of cancer cells MCF-7, NCI-H460 and SF-268, with IC50 greater than 150 μM .
|
-
- HY-N6885
-
|
Others
|
Cancer
|
Puerarin-4'-O-β-D-glucopyranoside (compound 8) is a isoflavone from Pueraria lobata root (PLR). Puerarin-4'-O-β-D-glucopyranoside has estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
|
-
- HY-N3316
-
|
Others
|
|
Martynoside protects ex vivo bone marrow cells from 5-fluorouracil (5-FU)-induced cell death and inflammation response by down-regulating the TNF signaling pathway .Martynoside is a potent antiestrogen in MCF-7 cells, increasing IGFBP3 levels
|
-
- HY-118474
-
NSC 721648
|
Aryl Hydrocarbon Receptor
Cytochrome P450
|
Cancer
|
GW 610 (NSC 721648), an antitumor agent, is a potent AhR ligand with a Ki of 6.8 nM. GW 610 induces CYP1A1 expression in MCF-7 cells. GW 610 shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines .
|
-
- HY-146988
-
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
hCAIX/XII-IN-1 is a potent CAIX/XII inhibitor with the KI values of 0.48 µM and 0.83 µM for CAIX and CAXII, respectively. hCAIX/XII-IN-1 shows antiproliferative activity in vitro. hCAIX/XII-IN-1 induces apoptosis in MCF-7 cells .
|
-
- HY-P5033
-
|
Bacterial
|
Cancer
|
Cyclo(Gly-His) is a liposome-encapsulated cyclic dipeptide with antimicrobial and anticancer activity. Cyclo(Gly-His) has cytotoxicity for HeLa and MCF-7 cell with IC50 values of 1.699 mM and 0.358 mM, respectively. Cyclo(Gly-His) can be used for the research of drug delivery systems .
|
-
- HY-N3615
-
|
Others
|
Cancer
|
Confluentin can be isolated from Rhododendron dauricum. Confluentin shows weak cytotoxicity against human tumor cells (IC50: 15.05, 17.08, 18.48, and 23.01 μM for HL-60, SMMC-7712, A-549, and MCF-7) .
|
-
- HY-156378
-
|
Aurora Kinase
|
Cancer
|
Aurora A inhibitor 3 (Compound 5h) inhibits Aurora-A kinase with an IC50 value of 0.78 μM. Aurora A inhibitor 3 is cytotoxic, with GI50 values of 0.12 μM and 0.63 μM for MCF-7 and MDA-MB-231 cells, respectively .
|
-
- HY-161770
-
|
Ligands for E3 Ligase
|
Cancer
|
HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-162695
-
|
Microtubule/Tubulin
|
Cancer
|
Antitumor agent-168 (compound 21b) disrupts the microtubule network in tumor cells leading to G2/M cell cycle arrest and apoptosis induction. Antitumor agent-168 inhibits MCF-7 growth with an IC50 value of 1.4 nM .
|
-
- HY-135607
-
|
Apoptosis
|
Cancer
|
Tingenin B is an anticancer agent with cytotoxic activity against breast cancer stem cells. Tingenin B is cytotoxic to MCF-7 cells (IC50=2.38 μM) by inducing apoptosis. Tingenin B has also been found to induce endoplasmic reticulum stress .
|
-
- HY-169253
-
|
Reactive Oxygen Species
Apoptosis
|
Cancer
|
ROS inducer 5 (compound 6e) can induce intracellular ROS accumulation and subsequent nuclear fragmentation. ROS inducer 5 can induce apoptosis in MCF-7 cells, with an IC50 value of 3.85 μM. ROS inducer 5 can be used in anticancer research .
|
-
- HY-144733
-
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
|
-
- HY-147788
-
|
Dihydroorotate Dehydrogenase
|
Cancer
|
hDHODH-IN-9 (Compound 3k) is a potent inhibitor of hDHODH with an IC50 of 0.34 μM. hDHODH-IN-9 demonstrates high cytotoxic activity against MCF-7 and A375 cells and good selectivity. hDHODH-IN-9 has the potential for the research of cancer diseases .
|
-
- HY-18351
-
LMP-400; NSC-724998
|
Topoisomerase
|
Infection
Cancer
|
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-N10351
-
|
Apoptosis
|
Cancer
|
27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells .
|
-
- HY-N11651
-
|
Others
|
Others
|
Peganumine A is a natural product that can be found in Peganum harmala. Peganumine A shows cytotoxicity with IC50s of5.8, 38.5, 40.2, 55.4 µM for HL-60, MCF-7, PC-3, and HepG2 cells ,respectively .
|
-
- HY-155239
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-35 (compound 7) is a potent VEGFR-2 inhibitor with IC50=37 nM. VEGFR-2-IN-35 inhibits MCF-7 and HCT 116 cancer cells with IC50 values of 10.56 and 7.07 μM, respectively .
|
-
- HY-N12299
-
Quercetin 3-O-β-D-glucuronide butyl ester
|
Others
|
Cancer
|
Parthenosin (Quercetin 3-O-β-D-glucuronide butyl ester) is a flavonoid, that can be isolated from the aerial parts of Calligoum polygonoides. Parthenosin shows cytotoxic activity against HepG2 and MCF-7 cell lines with IC50 values of 60.46 and 61.4 μg/mL, respectively .
|
-
- HY-157402
-
|
Topoisomerase
EGFR
|
Cancer
|
Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer .
|
-
- HY-N12607
-
|
Others
|
Cancer
|
Garcilatelic acid (Compound 5) is a compound that can be isolated from Garcinia lateriflora. Garcilatelic acid has antiproliferative activity against tumor cell lines (A549, MDA-MB-231, MCF-7, KB and KB-VIN), with IC50 values of 0.5-1.3 μM .
|
-
- HY-147888
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site .
|
-
- HY-13636
-
Fulvestrant
Maximum Cited Publications
85 Publications Verification
ICI 182780; ZD 9238; ZM 182780
|
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- HY-115994
-
|
Carbonic Anhydrase
|
Cancer
|
Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research .
|
-
- HY-N10777
-
|
Others
|
Cancer
|
1-Ketoaethiopinone is an abietane-diterpenoid. 1-Ketoaethiopinone has an α, β-unsaturated carbonyl function. 1-Ketoaethiopinone shows cytotoxic activity against human cancer cell lines MOLT-4 (human lymphoblastic leukemia) and MCF-7 (human breast adenocarcinoma) .
|
-
- HY-N11928
-
|
Others
|
Cancer
|
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 .
|
-
- HY-157487
-
|
Others
|
Cancer
|
Anticancer agent 185 (compound 9d) is a glycohybrid derivative of pyrazolopyrimidine [1,5-a]. Anticancer agent 185 has good anti-breast cancer activity. Anticancer agent 185 shows good cytotoxic activity against MCF-7 cells with IC50 value of 15.3 μM .
|
-
- HY-159605
-
|
Autophagy
JNK
Reactive Oxygen Species
|
Cancer
|
Autophagy inducer 5 (compound 21o) is a potent MCF-7 inhibitor (IC50: 2 μM), and a potential breast cancer inhibitor. Autophagy inducer 5 induces cellular autophagy by activating the ROS/JNK signaling pathway, which increases ROS generation and JNK phosphorylation, exerting cytotoxic effects .
|
-
- HY-168128
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin polymerization-IN-69 (compund 6c) significantly inhibits microtubule/tubulin polymerization in vitro (78.3% inhibition) with an IC50 value of 6.53 μM, and rapidly induces apoptotic cell death and G2/M cell cycle arrest in MCF-7 cells .
|
-
- HY-114310
-
|
VD/VDR
Apoptosis
|
Cancer
|
VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC50 of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2 .
|
-
- HY-112811
-
|
PROTACs
CDK
|
Cancer
|
PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC .
|
-
- HY-N2298
-
|
Apoptosis
|
Cancer
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population .
|
-
- HY-N1833
-
|
Others
|
Cancer
|
3'-Geranyl-3-prenyl-2',4',5,7-tetrahydroxyflavone displays cytotoxicity of 1.32, 3.92 and 5.22 μm against the human cervical carcinoma HeLa, human breast carcinoma MCF-7, and human hepatocarcinoma Hep3B cells .
|
-
- HY-145379
-
|
Parasite
Endogenous Metabolite
|
Infection
|
Miaosporone A, an angucyclic quinone, exhibits antimalarial activity against Plasmodium falciparum K1 and antibacterial activity against Mycobacterium tuberculosis with respective IC50 values of 2.5 and 2.4 μM and displays cytotoxic activities against both cancerous (MCF-7 and NCI-H187) and nonmalignant (Vero) cells .
|
-
- HY-151519
-
|
Sirtuin
|
Cancer
|
SIRT2-IN-9 (compound 12) is a selective inhibitor of SRIT2 with an IC50 value of 1.3 μM. SIRT2-IN-9 inhibits proliferative activity of MCF-7 breast cancer cells. SIRT2-IN-9 can be used for the research of cancer .
|
-
- HY-N10023
-
|
NO Synthase
|
Inflammation/Immunology
|
Physalin O is a physalin that can be isolated from Physalis angulata. Physalin O shows cytotoxicity to Hep G2 and MCF-7 cancer cells with IC50 values of 31.1 and 11.4 µM, respectively. Physalin O inhibits the production of nitric oxide (NO) and shows anti-inflammatory activities .
|
-
- HY-113319
-
|
Endogenous Metabolite
|
Cancer
|
β-D-Fructose is a β-fruit sugar that can be produced by the hydrolysis of sucrose. β-D-Fructose can be used as a sweetness potentiator. β-D-Fructose can be designed as a units of antiproliferative agents against breast (MCF-7) and colon (MDST8) cancer cell lines .
|
-
- HY-155969
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-83 (Compound 9) is an EGFR inhibitor (IC50: 2.53 nM). EGFR-IN-83 has antiproliferative activity against MCF-7 and MDA-MB-231 cells, with IC50 of 2.50 μM and 1.96 μM. EGFR-IN-83 can induce cell apoptosis .
|
-
- HY-N9505
-
Kadsulactone acid
|
Others
|
Cancer
|
Schisanlactone E is a triterpenoids that can be isolated from Kadsura heteroclita. Schisanlactone E exhibits moderate cytotoxic activity against Bel-7402, BGC-823, MCF-7 and HL-60 cell line with IC50s of 68.33, 100, >100, 73.37 μM,respectively .
|
-
- HY-155348
-
|
PARP
|
Cancer
|
Ru3 is a poly(ADP-ribose) polymerase 1 inhibitor. Ru3 induces apoptosisin MCF-7 cells by multiple modes, inclusive of inducing DNA damage, suppressing DNA damage repair, disturbing cell cycle distribution, decreasing the mitochondrial membrane potential, and increasing the intracellular reactive oxygen species levels .
|
-
- HY-117872
-
20-O-Acetylsartorypyrone D
|
Fungal
|
Infection
|
Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
|
-
- HY-13762S
-
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cancer
|
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-167694
-
|
Others
|
Cancer
|
Antiproliferative agent-62 is a functionalized benzylidene-indolin-2-one with notable antiproliferative activity, particularly in inducing NQO1 expression in murine Hepa1c1c7 cells and demonstrating effectiveness against human cancer cell lines, including MCF-7 and HCT116.
|
-
- HY-147913
-
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
PI3K/Akt/mTOR-IN-3 (compound 3d) is a potent PI3K/AKT/mTOR inhibitor. PI3K/Akt/mTOR-IN-3 displays the inhibitory activity in MCF-7, HeLa and HepG2 cells, with IC50 values of 0.77, 1.23, and 4.57μM, respectively. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 and HeLa cells at the concentration of 4 μM. PI3K/Akt/mTOR-IN-3 induces cell apoptosis and S phase arrest .
|
-
- HY-144335
-
|
DNA Alkylator/Crosslinker
|
Cancer
|
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .
|
-
- HY-147921
-
|
Pim
|
Cancer
|
PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor, with an IC50 of 0.67 μM. PIM1-IN-7 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively .
|
-
- HY-147920
-
|
Pim
|
Cancer
|
PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor, with an IC50 of 0.60 μM. PIM1-IN-6 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 1.51 and 15.2 μM, respectively .
|
-
- 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-144070
-
|
Others
|
Cancer
|
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model .
|
-
- HY-151624
-
|
PARP
Apoptosis
|
Cancer
|
PARP-2-IN-2 (compound 27) is a PARP‑2 inhibitor with an IC50 value of 0.057 µM. PARP-2-IN-2 induces cell cycle arrest and apoptosis of MCF-7 breast cancer cells. PARP-2-IN-2 can be used for the research of cancer .
|
-
- HY-14585
-
Estrone 3-O-sulfamate
|
Steroid Sulfatase
|
Cancer
|
Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS) inhibitor. Estrone O-sulfamate has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer .
|
-
- HY-152945
-
|
NF-κB
|
Cancer
|
Antiproliferative agent-22 (compound 2) is an anticancer agent. Antiproliferative agent-22 shoes anti-proliferative activities against MCF-7, MDA-MB-231 and MDA-MB-468 cells with IC50 values of 6.2 μM, 3.3 μM and 3.3 μM, respectively .
|
-
- HY-W080443
-
|
Others
|
Others
Cancer
|
O-allylvanillin is O-allylchalcone derivative with anti-cancer effects . O-allylvanillin inhibits THP-1, HL60, Hep-G2, MCF-7 cells growth with IC50 values of 74.76 μM, 63.52 μM, 90.99 μM, and 90.11 μM, respectively .
|
-
- HY-134008
-
|
Others
|
Cancer
|
Protoapigenone is an antineoplastic agent isolated from ferns. Protoapigenone has significant inhibitory activity against Hep G2, Hep 3B, MCF-7, A549 and MDAMB-231, with IC50s values of 1.60, 0.23, 0.78, 3.88 and 0.27 μg/mL respectively .
|
-
- HY-126618
-
|
Tyrosinase
|
Cancer
|
Aspochalasin I exhibits cytotoxicity against cancer cells NCIH460, MCF-7 and SF-268, with IC50s of 22.1, 33.4 and 19.9 μM. Aspochalasin I inhibits melanogenesis (IC50 of 22.4 μM) through inhibition of tyrosinase, and can thus be used as whitening agent .
|
-
- HY-161755
-
|
Others
|
Cancer
|
Anticancer agent 232 (compound 12f) is a glycohybrid designed using 1-azidoglycosides derived from d-glucose, d-galactose, and d-mannose. The IC50 values of anticancer agent 232 against MCF-7 and MDA-MB231 cells are 1.05 μM and 18.03 μM, respectively .
|
-
- HY-160563
-
-
- HY-146467
-
|
Others
|
Cancer
|
Anticancer agent 62 (compound 4c) is a potent anticancer agent. Anticancer agent 62 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. Anticancer agent 62 shows effective tumor growth inhibition .
|
-
- HY-149081
-
|
Estrogen Receptor/ERR
Cytochrome P450
|
Cancer
|
ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
|
-
- HY-Y0598
-
|
Fatty Acid Synthase (FASN)
Apoptosis
Fungal
|
Inflammation/Immunology
Cancer
|
trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7. trans-Chalcone has antifungal and anticancer activity .
|
-
- HY-115947
-
|
Others
|
Cancer
|
Anticancer agent 33 (compound 3), a Squamocin and Bullatacin derivative, is a potent anticancer agent. Anticancer agent 33 shows high potency to inhibit 4T1 breast cancer cell line (A549, HeLa, HepG2 and MCF-7 cells) growth with IC50s of 1.9-5.4 µM .
|
-
- HY-150692
-
|
Estrogen Receptor/ERR
|
Cancer
|
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .
|
-
- HY-152774
-
|
Akt
PI3K
|
Cancer
|
Antitumor agent-86 (compound 5a) inhibits MCF-7 breast cancer cells with an IC50 value of 2.62 µM. Antitumor agent-86 induces cell apoptosis and cell cycle arrest, and shows antineoplastic activity by targeting RAS/PI3K/Akt/JNK signaling cascades .
|
-
- HY-155441
-
|
CDK
|
Cancer
|
CDK2-IN-20 (compound 3b) is an inhibitor of CDK2. CDK2-IN-20 has cytotoxicity on tumor cells presenting an IC50 range of 5.52-17.09 µM. CDK2-IN-20 arrests the MCF-7 cell cycle at the S phase and induces apoptosis .
|
-
- HY-157138
-
|
Others
|
Cancer
|
MMP-9-IN-8 (Compound 3) is an MMP-9 inhibitor with inhibitory activities of 42.16% and 58.28% at 10 μM and 50 μM concentrations, respectively. MMP-9-IN-8 has anti-cancer activity and can induce apoptosis in MCF-7 cells with an IC50 value of 23.42 μM .
|
-
- HY-130431
-
|
Parasite
|
Infection
|
Vinclozolin M2 is an active metabolite of vinclozolin. It is formed from vinclozolin by successive esterase activity and decarboxylation of vinclozolin in C. elegans and by decarboxylation in human liver microsomes. Vinclozolin M2 is an antagonist of the mineralocorticoid receptor (IC50=1,400 nM) and androgen receptor (IC50=0.17 nM) in reporter assays using MCF-7 cells.
|
-
- HY-161866
-
|
EGFR
|
Cancer
|
EGFR-IN-118 (Compound 4a) is an inhibitor for the tyrosine kinase EGFR. EGFR-IN-118 demonstrates anti-cancer property, inhibiting the proliferation of MCF-7 and PC3 with IC50 of 2.53 and 3.25 µg/ml. EGFR-IN-118 exhibits antioxidant efficacy, inhibiting the DPPH free radicals with IC50 of 10.04 µg/ml .
|
-
- HY-N13162
-
|
Others
|
Cancer
|
Hemsleyadin D is a triterpenoid compound derived from Hemsleya penxianensis with antitumor activity. Its IC50 values against K562, MGC-803, U118, HepG2, A549, and MCF-7 cells are 93.9, 47.1, 25.9, 56.1, 66.3, and 67.6 μM, respectively .
|
-
- HY-124403
-
|
Estrogen Receptor/ERR
|
Cancer
|
D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 -7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .
|
-
- HY-146810
-
-
- HY-W179181
-
|
GLUT
|
Metabolic Disease
|
MSNBA is a specific inhibitor of GLUT5 fructose transport in proteoliposomes. MSNBA competitively inhibits GLUT5 fructose uptake with a KI of 3.2±0.4?μM in MCF7 cells .
|
-
- HY-164421
-
|
Others
|
Cancer
|
PhpC is a G-clamp analogue. PhpC shows antiproliferative activity against MCF7 cells, with an IC50 of 387.9 μM. PhpC modulates G-quadruplex-RNA landscapes in human cells .
|
-
- HY-146466
-
|
Others
|
Cancer
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition .
|
-
- HY-101989
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-24 (compound HMBA) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-24 inhibits MCF-7 cells proliferation. Tubulin polymerization-IN-24 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-24 increase the GTP hydrolysis rate and inhibits microtubule assembly .
|
-
- HY-158090
-
|
Others
|
Cancer
|
Triptolide palmitate is the derivative of Triptolide (HY-32735). Triptolide palmitate exhibits cytotoxicity against cancer cell MCF-7 and A549, with IC50 of 7.5 and 6.4 μM. Triptolide palmitate exhibits a half-time T1/2 of 50.4 min in Sprague Dawley rats. Triptolide palmitate can be utilizd as drug carrier .
|
-
- HY-119358
-
|
Reactive Oxygen Species
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
Traumatic Acid is a wound healing agent and a cytokinin (phytohormone). Traumatic Acid enhances the biosynthesis of collagen in cultured human skin fibroblasts. Traumatic Acid inhibits MCF-7 breast cancer cells viability and enhances apoptosis and oxidative stress. Traumatic Acid can be used in studies of cancer, circulatory disorders (including arterial hypertension), and skin diseases associated with oxidative stress and impaired collagen biosynthesis .
|
-
- HY-13636S
-
ICI 182780-d3; ZD 9238-d3; ZM 182780-d3
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].
|
-
- HY-147174
-
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker .
|
-
- HY-143301
-
|
Topoisomerase
|
Cancer
|
Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer .
|
-
- HY-N2741
-
|
Bcl-2 Family
|
Cancer
|
Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively .
|
-
- HY-W317408
-
|
Biochemical Assay Reagents
|
Others
|
(+)-Menthyl acetate is a compound isolated from natural Cunila angustifolia Benth essential oil. The selectivity of (+)-Menthyl acetate is higher than that of MCF-7 cell line, IC50=34.0 μg?mL -1, and lower than that of SK-Mel-28 cell line, IC50=279.9 μg?mL -1, on A549 cell without fatal .
|
-
- HY-N12586
-
|
Reactive Oxygen Species
|
Endocrinology
|
Pheophytin a is a chlorophyll that can be isolated from S. vermiculata extracts. Pheophytin a has antioxidant activity with IC50 values of? 200.5 and 137.7 μg/mL for SOD, and NO respectively. Pheophytin a has reducing power with an IC50 value of 4.2 μg/mL . Pheophytin a has a cytotoxic effect on the MCF-7 cell line(IC50= 35.9 μg/mL)[1].
|
-
- HY-138210
-
|
Fungal
|
Infection
|
N,O-Diacetyltyramine is a compound with antibacterial activity and cytotoxicity that can be isolated from the actinomycete Pseudonocardia endophytica VUK-10. N,O-Diacetyltyramine has antibacterial activity against Gram-positive and Gram-negative bacteria and fungi. N,O-Diacetyltyramine is cytotoxic to MDA-MB-231, HeLa, MCF-7 and OAW-42 cells .
|
-
- HY-162227
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis .
|
-
- HY-151564
-
|
Others
|
Cancer
|
Anticancer agent 85 (compound 6j) is an anticancer agent that shows good cytotoxicity against MCF7 cells. Anticancer agent 85 can be used in breast cancer and other cancer studies .
|
-
- HY-161267
-
-
- HY-149995
-
|
Pim
|
Cancer
|
Pim-1 kinase inhibitor 5 (Compound 4c) is a Pim-1 kinase inhibitor (IC50: 0.61 μM). Pim-1 kinase inhibitor 5 shows cytotoxicity against cancer cells, with IC50s of 6.95-20.19 μM for HepG2, MCF-7, PC3, and HCT-116 cells .
|
-
- HY-115950
-
|
Others
|
Cancer
|
Antitumor agent-48 (Compound 4a) is a 2,3-dehydrosilybin derivative with an antitumor activity. Antitumor agent-48 shows cytotoxic activity against MCF-7, NCI-H1299, HepG2 and HT29 cells with IC50 values of 8.06 µM, 13.1 µM, 16.51 µM and 12.44 µM, respectively .
|
-
- HY-145865
-
|
Apoptosis
|
Cancer
|
Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase .
|
-
- HY-139434
-
|
Histone Demethylase
|
Cancer
|
JMJD6-IN-1 (Compound 1-3) is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC50s of 19.2 μM and 25.2 μM. JMJD6-IN-1 can be used for research of cancers .
|
-
- HY-13636R
-
ICI 182780(Standard); ZD 9238(Standard); ZM 182780 (Standard)
|
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
Fulvestrant (Standard) is the analytical standard of Fulvestrant. This product is intended for research and analytical applications. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- HY-155105
-
|
Glucosidase
|
Metabolic Disease
|
α-Glucosidase-IN-30 (compound 8c) is a potent, orally active, competitive inhibitor against α-glucosidase, with Ki of 40.0 µM and IC50 value of 49.0 µM. α-Glucosidase-IN-30 is non-cytotoxic against the cancer and normal cell lines MCF-7 and HDF, and can be used for Type 2 diabetes study .
|
-
- HY-149480
-
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- HY-149149
-
|
Bacterial
|
Infection
Metabolic Disease
Cancer
|
Incadronic acid inhibits growth of Dictyostelium discoideum with an IC50 of 1.6 μM. Incadronic acid binds the farnesyl diphosphate synthase (FPPS) in Leishmania major with the Ki of 23 nM. Incadronic acid inhibits the bone resorption and reduces bone loss, that can be used in osteoporosis research. Incadronic acid inhibits the proliferation of cells RAW264.7, PC-3 and MCF-7 with IC50 of 48 to 228.6 µM .
|
-
- HY-162593
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 45 (compound 5) is an inhibitor of tubulin protein active sites. Tubulin inhibitor 45 against MCF7 and HePG2 cancer cells with IC50 values of 11 μM and 13 μM .
|
-
- HY-169019
-
|
PI3K
Apoptosis
|
Cancer
|
XJTU-L453 is a PI3Kα inhibitor with an IC50 value of 0.4 nM. XJTU-L453 can inhibit the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. XJTU-L453 can inhibit the PI3K pathway, induce cell cycle arrest, and trigger cell apoptosis (apoptosis). XJTU-L453 also has antitumor activity in MCF7 xenograft mice .
|
-
- HY-146454
-
|
Others
|
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-B0543
-
Thiosinamine; N-Allylthiourea
|
Reactive Oxygen Species
|
Cancer
|
Allylthiourea can selectively inhibit the oxidation of ammonia. Allylthiourea is commonly used to inhibit nitrification by targeting ammonia monooxygenase and chelating copper in the active site to suppress its activity. Allylthiourea also exhibits anticancer activity, showing cytotoxicity against the MCF-7 cell line with an IC50 of 5.22 mM. Allylthiourea can be utilized in research related to micropollutant biodegradability and cancer studies .
|
-
- HY-144774
-
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
|
-
- HY-150968
-
|
Apoptosis
|
Cancer
|
Antiproliferative agent-11 (compound 7) is an antiproliferative and selective Ruthenium(II)-Tris-pyrazolylmethane complex. Antiproliferative agent-11 shows antiproliferative activity towards MCF-7, HeLa, 518A2, HCT116 and RD with IC50s of 6, 10, 6.8, 6.7 and 6 μM, respectively. Antiproliferative agent-11 can be used for the research of cancer .
|
-
- HY-N3210
-
|
Others
|
Cancer
|
Nb-Demethylechitamine is an alkaloid isolated from the methanol extract of Alstonia rostrata twigs. Nb-Demethylechitamine has in vitro cytotoxic activity against several human cancer cell lines, including human myeloid leukemia HL-60, liver cancer SMMC-7721, lung cancer A-549, breast cancer MCF-7, and colon cancer SW480 cells .
|
-
- HY-160264
-
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader (DC50: <10 nM), and inhibits MCF-7 proliferation (DC50: <10 nM). PROTAC ER Degrader-12 has anticancer effect. Pink: ER ligand (HY-169978); Blue: E3 ligase ligand (HY-138793); Black: linker (HY-30756) .
|
-
- HY-162312
-
|
Deubiquitinase
Apoptosis
|
Cancer
|
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
|
-
- HY-158371
-
|
HDAC
Casein Kinase
|
Cancer
|
HDAC/CK2-IN-1 (compound 38) is a HDAC1 (IC50 = 1.46 μM), HDAC6 (IC50 = 0.66 μM), and CK2 (IC50 = 3.67 μM) inhibitor. HDAC/CK2-IN-1 exhibits promising antproliferative activity against Jurkat, MCF-7, HCT-116, and HL-60 cell lines .
|
-
- HY-163632
-
|
EGFR
|
Cancer
|
EGFR-IN-112 (SPP10) is an EGFR kinase inhibitor which exhibits IC50s of 2.31 ± 0.3, 3.16 ± 0.8, and 4.2 ± 0.2 μM, against MCF-7, H69AR, and PC-3 cancer cells, respectively. EGFR-IN-112 also demonstrates selective cytotoxicity against cancer cells .
|
-
- HY-119539
-
|
Phosphatase
|
Endocrinology
Cancer
|
Limocitrin is a natural product that can be isolated from the buds of P. acerifolia and P. orientalis. Limocitrin suppresses estradiol-dependent proliferation of MCF7 cells weakly but estradiol-induced AlkP (alkaline phosphatase) expression only marginally .
|
-
- HY-128600
-
ERD-308
1 Publications Verification
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
ERD-308 is a highly potent von Hippel-Lindau-based PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment. ERD-308 induces >95% of ER degradation at concentrations as low as 5 nM in both cell lines (DC50 (concentration causing 50% of protein degradation) of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells, respectively) .
|
-
- HY-143232
-
|
Fungal
Bacterial
|
Infection
Cancer
|
Antibacterial agent 73 (compound 7a) is a potent antimicrobial agent. Antibacterial agent 73 exhibits very good antitubercular activity (MIC=0.65 µg/mL) against Mtb H37Rv. Antibacterial agent 73 shows good activity against fungal and bacterial. Antibacterial agent 73 also shows cytotoxicity in MCF-7 breast cancer cell lines, with IC50 of 8.20 μM .
|
-
- HY-148368
-
|
Bcl-2 Family
Apoptosis
|
Cancer
|
CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .
|
-
- HY-153789
-
|
Others
|
Cancer
|
PI5P4Kγ-IN-1 (compound 2) is a selective PI5P4Kγ inhibitor. PI5P4Kγ-IN-1 can be used to signal mTORC1 in MCF-7 breast cancer cells and further characterize PI5P4Kγ in the cells .
|
-
- HY-155118
-
|
EGFR
|
Cancer
|
EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC50s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively .
|
-
- HY-N1107
-
NSC 119993; NSC 277290; Odorigeni
|
Others
|
Cancer
|
Uzarigenin (NSC 119993; NSC 277290; Odorigeni) is a carnolide can be isolated from Pergularia tomentosa and exhibits antiproliferative activity. Uzarigenin resists the proliferation of PC3 cells, HeLa cells, Calu-1 cells, MCF-7 cells and U251MG cells, with IC50 values of 0.3 μM, 3.0 μM, 8.0 μM, 6.0 μM and 6.0 μM respectively .
|
-
- HY-163125
-
|
VEGFR
|
Cancer
|
BHEPN is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). BHEPN has inhibition of VEGFR-2 with an IC50 value of 0.320 μM. BHEPN also exhibits remarkable cytotoxic effects against HepG2 and MCF-7 cancer cell lines, with IC50 values of 0.19 μM and 1.18 μM, respectively. BHEPN can be used for anticancer research .
|
-
- HY-157419
-
7-(4-Ethylphenyl)-FL118
|
Apoptosis
|
Cancer
|
FL77-24, a FL118 analog and apoptosis inducer, possesses antitumor activity, with IC50 values of 99.4 nM, 118 nM, <6.4 nM, 28.5 nM and <6.4 nM in HCT116, HepG2, MCF-7, A549 and HeLa cells, respectively. FL77-24 mainly causes cell cycle arrest in S and G2/M phases .
|
-
- HY-116377
-
|
Steroid Sulfatase
|
Neurological Disease
|
DU-14 is a potent steroid sulfatase inhibitor with an IC50 of 55.8 nM. DU-14 inhibits the MCF-7 cell proliferation (IC50 = 38.7 nM). DU-14 has neuroprotective effects against neurotoxic Aβ, suggesting that up-regulation of endogenous DHEAS by DU-14 could be beneficial to the alleviation of Aβ-induced impairments in spatial memory and synaptic plasticity .
|
-
- HY-156452
-
|
VEGFR
|
Cancer
|
T-1-MCPAB is a VEGFR-2 inhibitor (IC50=0.135 µM) that effectively inhibits MCF7 migration. T-1-MCPAB can be used in cancer research .
|
-
- HY-157960
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-42 (compound 8c) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-42 shows anti-proliferative effect against MCF7 cells with the IC50 of 25 µM .
|
-
- HY-145864
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent VEGFR-2 inhibitor with an IC50 of 0.037 µM. VEGFR-2-IN-12 shows high growth inhibition against MCF-7 cells (GI50=1.6 µM). VEGFR-2-IN-12 has antitumor activity .
|
-
- HY-146819
-
|
Carbonic Anhydrase
|
Cancer
|
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.
|
-
- HY-147853
-
|
Raf
|
Cancer
|
B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC50 of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC50 values of 9.78, 13.78, 18.52 and 29.85 µM .
|
-
- HY-P4523
-
|
Endogenous Metabolite
|
Endocrinology
|
FA-Ala-Arg is a dipeptide with furylacryloyl group. FA-Ala-Arg breaks down to produce arginine. While cell-surface Carboxypeptidase-D (CPD) also increases intracellular Arg, which is converted to nitric oxide (NO). FA-Ala-Arg enhances NO production in MCF-7 cells. FA-Ala-Arg also increases the cell survival of prolactin (PRL)-treated cells, PRL regulates CPD mRNA levels in cells .
|
-
- HY-N10481
-
|
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
Aviculin, a lignan glycoside, is a potent anticancer agent. Aviculin reduces metabolic activity on MCF-7 cells below 50%, with an IC50 of 75.47 μM. Aviculin induces breast cancer cell apoptosis through the intrinsic apoptosis pathway. Aviculin increases expression of initiator caspase-9, executioner caspase-7, and poly (ADP-ribose) polymerase (PARP). Aviculin shows an increase in the Bax/Bcl-2 ratio .
|
-
- HY-155337
-
|
Others
|
Cancer
|
eIF4E-IN-6(compound 4b) is a GMP analogs synthesized to targeteIF4Eand restrain its binding to cap mRNA.eIF4E-IN-6shows cell cytotoxicity against Caco-2, HepG-2,and MCF-7 cells, withIC50values of 31, 27, and 21 μM, respectively .
|
-
- HY-162006
-
|
PKC
Pim
|
Cancer
|
Pim-1 kinase inhibitor 8 (compound 12) is a potent inhibitor of Pim-1 kinase with an IC50 of 14.3 nM. Pim-1 kinase inhibitor 8 has potent cytotoxicity against MCF-7 and HepG2 cells with IC50s of 0.5 and 5.27 μM, respectively. Pim-1 kinase inhibitor 8 can used in study breast cancer .
|
-
- HY-157516
-
|
CDK
|
Cancer
|
CDK2-IN-22 (compound 7I) is a potent CDK2 inhibitor with an IC50 of 64.42 nM. CDK2-IN-22 presents a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC50 values of 0.83 μM, 2.12 μM, 3.12 μM, and 8.61 μM, respectively .
|
-
- HY-163566
-
|
Apoptosis
|
Cancer
|
Apoptosis inducer 18, a potent inducer of apoptosis, shows significant cytotoxicity to the breast cancer cell line MCF-7 (IC50=0.559 μM). Apoptosis inducer 18 inhibits cell cycle progression and promotes apoptosis by binding to DNA and causing damage, and by binding to the active site of CDK-2, interfering with its kinase activity. Apoptosis inducer 18 can be used in anti-breast cancer research .
|
-
- HY-N12208
-
|
Others
|
Cancer
|
Neohelmanthicin B is a phenylpropanoid that can be isolated from Thapsia garganica. Neohelmanthicin B exhibits cytotoxicity against EL4, S180 and MCF7 cell lines with IC50s of 10, 5 and12 μM, respectively .
|
-
- HY-153588
-
|
HSP
|
Cancer
|
HSP90-IN-22 (Compound 35) is an Hsp90 inhibitor with antiproliferative properties on cells with IC50 values of 3.65 μM for MCF7 breast cancer cells and 2.71 μM for SKBr3 breast cancer cells, respectively.
|
-
- HY-156919
-
|
MDM-2/p53
|
Cancer
|
p53 Activator 8 (compound 5) is a p53 activator. p53 Activator 8 has potent anti-proliferative activity against MCF7 breast cancer cell lines with an IC 50 value of 0.5 μM .
|
-
- HY-147852
-
|
Raf
|
Cancer
|
B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC50 of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC50 values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM .
|
-
- HY-147839
-
|
Topoisomerase
Apoptosis
|
Cancer
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
|
-
- HY-50936S
-
Ecteinascidin 743-d3; ET-743-d3
|
Isotope-Labeled Compounds
Reactive Oxygen Species
Apoptosis
|
Inflammation/Immunology
Cancer
|
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
|
-
- HY-155242
-
|
VEGFR
Bcl-2 Family
Apoptosis
|
Cancer
|
VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM) .
|
-
- HY-160062
-
|
Mucin
|
Cancer
|
S2.2 aptamer sodium is a nucleic acid aptamer targeting the mucin MUC1 and can be used for targeted imaging of MCF-7 cancer cells. S2.2 aptamer sodium was labeled with Cy5, and when fluorescent silicon nanodots (SiND) were present, the fluorescence was quenched; when MUC1 was also present, the fluorescence was restored. S2.2 aptamer sodium detects MUC1 with a linear range of 3.33-250 nM .
|
-
- HY-155956
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
GM-90257 is a microtubule acetylation inhibitor that binds directly to α-tubulin. GM-90257 prevents the recruitment of α-tubulin acetyltransferase 1 (αTAT1) to the K40 residue in α-tubulin. GM-90257 causes the apoptosis of MDA-MB-231 cells with weaker effects on MCF-10A or MCF-7 cells, which have a relatively low level of microtubule acetylation .
|
-
- HY-157942
-
|
Cytochrome P450
|
Cancer
|
CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
|
-
- 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-P10426
-
|
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC50 of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .
|
-
- HY-161868
-
|
PARP
HDAC
Apoptosis
|
Cancer
|
DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC50 of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase .
|
-
- HY-161855
-
|
VEGFR
Apoptosis
|
Cancer
|
VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer, with an IC50 value of 0.33 μM. VEGFR-2-IN-50 (Compound 10f) has growth inhibitory activity on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, which is expected to be used in the study of breast cancer diseases .
|
-
- HY-N13115A
-
(E)-21-Angeloyl-protoaescigenin
|
Others
|
Cancer
|
Protoescigenin 21-tiglate (compound 10) is a glycosidic oleanane-type triterpenoid (BAT) that can be isolated from the acid hydrolysis product (AHP) of the crude extract of Aesculus chinensis seeds. Aesculus-derived triterpenoids (BAT) generally exhibit good antitumor, anti-inflammatory, and anti-Alzheimer's activities. However, the antitumor activity of Protoescigenin 21-tiglate is relatively weak, with IC50 values of >80 μM and 80 μM against MCF-7 and HeLa cells, respectively .
|
-
- HY-N13115
-
(Z)-Protoescigenin 21-tiglate
|
Others
|
Cancer
|
21-Angeloyl-protoaescigenin (compound 11) is a glycosidic oleanane-type triterpenoid (BAT) that can be isolated from the acid hydrolysis product (AHP) of the crude extract of Aesculus chinensis seeds. Aesculus-derived triterpenoids (BAT) generally exhibit good antitumor, anti-inflammatory, and anti-Alzheimer's activities. Protoescigenin 21-tiglate has antitumor activity, with IC50 values of 38.2 μM and 33 μM against MCF-7 and HeLa cells, respectively .
|
-
- HY-116904
-
|
Apoptosis
Akt
|
Cancer
|
Anticancer agent 253 (Compound 26) has anti-cancer activity against breast cancer cells, with IC50s of 6 μM (MCF-7), 10 μM (MDA-MB-231) and 6.4 μM (4T1 cells). Anticancer agent 253 arrests cell cycle and induces mitochondria-mediated apoptosis in cancer cells. Anticancer agent 253 inhibits Akt phosphorylation in human breast and prostate cancer .
|
-
- HY-168164
-
|
Others
|
Cancer
|
4-Methoxycinnamyl alcohol is an anticancer compound with cytotoxic activity against MCF-7, HeLa, and DU145 cancer cell lines with IC50 values of 14.24, 7.82, and 22.10 μg/mL, respectively. 4-Methoxycinnamyl alcohol showed the ability to induce cell necrosis, rather than apoptosis, after a 48-hour DNA fragmentation assay. 4-Methoxycinnamyl alcohol was isolated from Foeniculum vulgare .
|
-
- HY-156470
-
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
|
Cancer
|
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
|
-
- 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 .
|
-
- HY-147710
-
|
MicroRNA
|
Cancer
|
PIN1 inhibitor 2 (compound 12) is a potent PIN1 inhibitor. PIN1 inhibitor 2 shows antitumor activity with an IC50 of 9.55 µM for MCF7 cells. PIN1 inhibitor 2 has the potential for the research of breast cancer .
|
-
- HY-N7340
-
|
Others
|
Cancer
|
Withaperuvin C is a withanolide that can be isolated from Physalis Minima. Withaperuvin C has moderate cytotoxicity against cancer cells such as HepG2, SK-LU-1, and MCF7 cells (IC50: 19.5, 14.65, 11.74 μg/mL) .
|
-
- HY-146103
-
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis .
|
-
- HY-144749
-
|
Aldose Reductase
|
Cancer
|
AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
|
-
- HY-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-146228
-
|
HSP
Apoptosis
Topoisomerase
EGFR
VEGFR
|
Cancer
|
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
|
-
- HY-151158
-
|
EGFR
|
Cancer
|
EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM) .
|
-
- HY-155061
-
|
Cytochrome P450
Aryl Hydrocarbon Receptor
|
Cancer
|
hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM),as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells .
|
-
- HY-155203
-
|
Apoptosis
Reactive Oxygen Species
Ferroptosis
|
Cancer
|
Anticancer agent 154 (Compound 8h) increases the levels of reactive oxygen species and leads to mitochondrial damage. Anticancer agent 154 induces cell apoptosis and DNA damage. Anticancer agent 154 also induces ferroptosis by reducing the GSH level and GPX4 expression and increasing the lipid peroxidation level. Anticancer agent 154 inhibits cancer cell (HT29, H1975, A549, and MCF-7) proliferation with IC50s of 1.0-1.9 μM .
|
-
- HY-163615
-
|
Bacterial
|
Infection
|
Antimicrobial agent-32 (Compound 4g) is an antimicrobial agent that exhibits significant activity against various bacteria, including Staphylococcus aureus, Bacillus subtilis, Bacillus cereus (MIC=1000 µg/mL), Klebsiella pneumonia, and Staphylococcus aureus (MRSA) (MIC=500 µg/mL), as well as Escherichia coli (MIC=250 µg/mL). Additionally, Antimicrobial agent-32 inhibits the proliferation of MCF-7, HCT-116, and HepG-2 cells, demonstrating anticancer activity .
|
-
- HY-118761
-
5,6-epoxy atRA; 5,6-epoxy RA
|
Others
|
Metabolic Disease
|
all-trans-5,6-epoxy Retinoic acid (5,6-epoxy RA) is an agonist of all isoforms of the retinoic acid receptor (RAR; EC50s=77, 35, and 4 nM for RARα, RARβ, and RARγ, respectively). 5,6-epoxy RA (1 μM) also induces growth arrest of MCF-7 and NB4 cells in vitro. It is a natural metabolite of all-trans retinoic acid, which is a metabolite of vitamin A.
|
-
- HY-163616
-
|
Apoptosis
|
Cancer
|
Anticancer agent 221 (Compound 4h) is an orally active anticancer agent and an antioxidant agent. Anticancer agent 221 exhibits cytotoxicity to cancer cells A549 (IC50=22.09 µg/mL) and MCF-7 (IC50=6.40 µg/mL), and induces apoptosis. Anticancer agent 221 exhibits antioxidant efficacy with an IC50 of 42.46 μM in DPPH experiment. Anticancer agent 221 exhibits antitumor efficacy against breast cancer in mouse models .
|
-
- HY-162751
-
|
HSP
Apoptosis
|
Cancer
|
Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC50 of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC50 of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice .
|
-
- HY-162000
-
|
Apoptosis
|
Cancer
|
hCAIX/XII-IN-13 is an inhibitor of human carbonic anhydrases (hCA). hCAIX/XII-IN-13 shows good inhibitory activity against the tumor-related CA subtypes IX and XII, with Ki values of 0.08 µM and 0.06 µM, respectively. Under hypoxic conditions, hCAIX/XII-IN-13 can restore the cytotoxicity of Doxorubicin (HY-15142A) on MCF-7 cells, increasing G2/M phase cell cycle arrest and apoptosis .
|
-
- HY-B0543R
-
|
Reactive Oxygen Species
|
Cancer
|
Allylthiourea (Standard) is the analytical standard of Allylthiourea. This product is intended for research and analytical applications. Allylthiourea can selectively inhibit the oxidation of ammonia. Allylthiourea is commonly used to inhibit nitrification by targeting ammonia monooxygenase and chelating copper in the active site to suppress its activity. Allylthiourea also exhibits anticancer activity, showing cytotoxicity against the MCF-7 cell line with an IC50 of 5.22 mM. Allylthiourea can be utilized in research related to micropollutant biodegradability and cancer studies [4].
|
-
- HY-162887
-
|
VEGFR
Apoptosis
|
Cancer
|
VEGFR-2-IN-53 (Compound 15w) is a VEGFR-2 inhibitor with an IC50 of 4.34 μM. VEGFR-2-IN-53 induces apoptosis by inhibiting VEGFR-2 activity and preventing cell migration, thereby exhibiting anti-angiogenic effects. The IC50 value of VEGFR-2-IN-53 for inhibiting MCF-7 cell growth is 3.87 μM. VEGFR-2-IN-53 can be used in cancer research .
|
-
- HY-114770
-
|
Others
|
Cancer
|
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .
|
-
- HY-157151
-
|
Histone Methyltransferase
|
Cancer
|
iPRMT1 is a potent and selective PRMT1 inhibitor for breast cancer research. iPRMT1 inhibits breast cancer cell growth in vitro and in vivo with EC50 values of 90, 70, and 9 nM in MCF7, T47D, and MDA-MB-231 cells, respectively .
|
-
- HY-146440
-
|
Histone Demethylase
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM .
|
-
- HY-146169
-
|
Reactive Oxygen Species
Microtubule/Tubulin
|
Cancer
|
Antitumor agent-68 is a potent tubulin inhibitor. Antitumor agent-68 shows potent anticancer activity with IC50s of 3.6 and 3.8 μM for HeLa and MCF-7 cells, respectively. Antitumor agent-68 exhibits good scavenging activity of ROS and DPPH radical in a dose-dependent manner . Antitumor agent-68 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-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-149390
-
|
TrxR
|
Cancer
|
TrxR1-IN-1 (Compound 5j) is a TrxR1 inhibitor (IC50: 8.8 μM). TrxR1-IN-1 has anticancer activity, with IC50s of MCF-7 (1.5 μM), HeLa (1.7 μM), BGC-823 (2.4 μM), SW-480 (2.8 μM), A549 (2.1 μM). TrxR1-IN-1 has antioxidant activity, and scavenges DPPH radical .
|
-
- HY-155113
-
|
PROTACs
HSP
|
Cancer
|
PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively .
|
-
- HY-155177
-
|
CDK
|
Cancer
|
CDK9-IN-27 (Compound 6a) is a CDK9 inhibitor (IC50s: 0.424 μM). CDK9-IN-27 induces apoptosis and cell cycle arrest at S stage. CDK9-IN-27 has cytotoxic action against HepG2, HCT-116 and MCF-7 cell lines, with IC50s of 10.31-40.34 μM. CDK9-IN-27 can be used for cancer research .
|
-
- HY-124053
-
|
HDAC
|
Cancer
|
BRD2492 (compound 6d) is a potent, selective HDAC1 and HDAC2 inhibitor with IC50s of 13.2 nM and 77.2 nM, respecrtively. BRD2492 exhibits >100-fold selectivity for HDAC1/2 over selectivity over HDAC3 and HDAC6. BRD2492 inhibits breast cancer cell lines growth with IC50s of 1.01 μM and 11.13 μM for T-47D and MCF-7 cells, respectively .
|
-
- HY-161776
-
|
P-glycoprotein
CDK
|
Cancer
|
P-gp/CDK2-IN-1 (Compound 4j) is an inhibitor for is inhibitor for P-glycoprotein (P-gp) and for cyclin-dependent kinase-2 (CDK2). P-gp/CDK2-IN-1 inhibits the proliferation of cancer cells SW-480 and MCF-7 wit IC50 of 38.6 μM and 26.6 μM. P-gp/CDK2-IN-1 exhibits antioxidant efficacy with EC50 of 580 μM in DPPH experiment .
|
-
- HY-163747
-
|
VEGFR
|
Cancer
|
VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma .
|
-
- HY-149132
-
DDA
|
LXR
|
Cancer
|
Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
|
-
- HY-169058
-
|
Glutathione S-transferase
|
Cancer
|
GSTP1-1 inhibitor 2 (Compound 5g) is an hGSTP1-1 (glutathione S-transferase P1-1) inhibitor with an IC50 value of 12.2 μM. GSTP1-1 inhibitor 2 exhibits significant cytotoxicity against DU-145, PC3, and MCF-7 cell lines, with CC50 values of 36.6 μM, 11.9 μM, and 17.4 μM, respectively. It can be used in cancer research .
|
-
- HY-N12209
-
|
Others
|
Cancer
|
Neohelmanthicin A (compound 3A) is a phenylpropanoid compound with antitumor activity. The IC50s of Neohelmanthicin A for inhibiting leukemia cell line EL4, breast cancer cell line S180 and breast cancer cell line MCF7 are 0.13 μM, 7 μM and 23 μM respectively .
|
-
- HY-162670
-
|
CDK
|
Cancer
|
Anticancer agent 238 (compound 5) is an anticancer agent with a notably strong binding affinity towards the CDK-5 enzyme. Anticancer agent 238 shows a strong efficacy agains HCT116 and MCF7 cells, with IC50 values of 13.46 µM and 16.43 µM, respectively .
|
-
- HY-147202
-
|
Epigenetic Reader Domain
|
Cancer
|
BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A) .
|
-
- HY-151573
-
|
EGFR
CDK
|
Cancer
|
EGFR/CDK2-IN-1 (Compound 3b) is an EGFR/CDK2 inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research .
|
-
- HY-129152
-
|
Influenza Virus
|
Infection
|
Ganoderic acid T-N, a triterpenoid, is a H5N1 and H1N1 influenza neuraminidase (NA) inhibitor with IC50s of 2.7 μM and 42 μM, respectively. Ganoderic acid T-Q shows cytotoxicity against MCF7 cells (CC50=24.4 μM) .
|
-
- HY-129672
-
25-Dihydrostichorrenoside E
|
Others
|
Cancer
|
Thelenotoside B (25-Dihydrostichorrenoside E) shows strong cytotoxicities against five cancer cell lines as HepG2, KB, LNCaP, MCF7 and SK-Mel2 with the IC50 values from 0.95 ± 0.08 to 1.90 ± 0.13 μM. Thelenotoside B is a triterpene tetraglycoside .
|
-
- HY-117102
-
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
|
-
- HY-151154
-
|
EGFR
|
Cancer
|
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .
|
-
- HY-156912
-
|
EGFR
|
Cancer
|
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC50s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC50s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .
|
-
- HY-149636
-
|
EGFR
CDK
VEGFR
|
Cancer
|
Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
|
-
- HY-N8470
-
NSC 204855; U 40615
|
Bacterial
|
Infection
|
Steffimycin B is an anthracycline bacterial metabolite originally isolated from Streptomyces. It binds to DNA, preferentially intercalating at sites containing cytosine and guanine.2 Steffimycin B is cytotoxic to MCF-7, KB, NCI-H187, and Vero cells (IC50s=3.5, 6.75, 3.28, and 10.5 μM, respectively). It is active against M. tuberculosis (MIC=5.2 nM), B. cereus (MIC=1.56 μg/mL), and P. falciparum (IC50=2.19 μM).
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-
- HY-124456
-
|
Others
|
Infection
|
Unguinol is a depsidone originally isolated from A. unguis. It is an inhibitor of pyruvate phosphate dikinase (PPDK; IC50=42.3 μM). It inhibits the growth of plants utilizing C4, but not C3, carbon fixation. Unguinol also inhibits the growth of the bacteria S. aureus and V. harveyi (GI50s=8.7 and 69.5 μM, respectively) and H460, MCF-7, and SF-268 cancer cells (GI50s=28.2, 50.8, and 44.3 μM, respectively).
|
-
- HY-124509
-
|
Bacterial
|
Infection
|
Pyrocoll is a bacterial metabolite originally isolated from Streptomyces. It inhibits the growth of A. aurescens, A. globiformis, A. oxydans, A. pascens, and R. erythropolis bacteria (MICs=10, 1, 10, 3, and 10 μg/mL, respectively) and HMO2, HepG2, and MCF-7 cancer cells (GI50s=0.28, 0.42, and 2.2 μg/mL, respectively) in vitro. Pyrocoll is also active against P. falciparum and T. rhodesiense (IC50s=1.19 and 1.97 μg/mL, respectively).
|
-
- HY-161773
-
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
HL389-NHC2-PEG3-C2NH inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389-NHC2-PEG3-C2NH can be utilized as a conjugate of an E3 ligase ligand and a linker, for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-W348485
-
|
mTOR
|
Cancer
|
WRX606 is an inhibitor for mTOR complex 1 (mTORC1). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 S6K1 (IC50=10 nM), and the phosphorylation of the eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50=0.27 μM) in MCF-7. WRX606 exhibits cytotoxicity to HepG2 with IC50 of 17 nM. WRX606 exhibits antitumor efficacy in mouse models .
|
-
- HY-162885
-
|
Proteasome
JAK
STAT
Interleukin Related
|
Cancer
|
YSY01A is a proteasome inhibitor that can suppress cancer cell survival by inducing apoptosis (Apoptosis). Its IC50 values are 51.0 nM for HEK293T, 9.2 nM for A549, 5.2 nM for MCF-7, 8.9 nM for MGC-803, and 35.4 nM for PC-3M cells. Additionally, YSY01A eliminates constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A holds promise for research in the field of cancer therapy .
|
-
- HY-W131302
-
N,N-Ethylenediglycine
|
Others
|
Cancer
|
Ethylenediaminediacetic acid (N,N-Ethylenediglycine) is an important ligand that enhances the antiproliferative activity of metal complexes. The complexes formed by ethylenediacetic acid and metal ions exhibited significant antiproliferative properties in MCF-7 cancer cell line. The metal complexes of ethylenediacetic acid were able to interact with DNA and were studied by CD and EPR spectroscopy techniques. Ethylenediaminediacetic acid and its metal complexes were able to induce cell cycle arrest at the G(0)/G(1) phase. The crystal structure analysis of ethylenediacetic acid provided important structural information for understanding its biological activity .
|
-
- HY-132294A
-
|
Estrogen Receptor/ERR
|
Cancer
|
(1S,3R)-GNE-502 (compound 179) is a potent ERα degrader with an EC50 value of 13 nM against ERα in MCF7 HCS. (1S,3R)-GNE-502 can be used to research cancer related with estrogen receptor .
|
-
- HY-148789
-
OP-1250
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER +/HER2 + cancer .
|
-
- HY-138098
-
|
Others
|
Cancer
|
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
|
-
- HY-115997
-
|
PROTACs
HSP
|
Cancer
|
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-155965
-
|
VEGFR
PARP
Apoptosis
|
Cancer
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
|
-
- HY-155197
-
|
Microtubule/Tubulin
Estrogen Receptor/ERR
|
Cancer
|
ER degrader 7 (Compound 35t) is an ERα and ERβ degrader. ER degrader 7 inhibits tubulin polymerization. ER degrader 7 inhibits cell viability with IC50s of 0.06, 2.56, 15.84, 1.59, 1.67, 1.37 μM for MCF-7, T47D, MCF-10A, LCC2, T47D D538G, and T47D Y537S cells respectively. ER degrader 7 also inhibits breast cancer tumor growth .
|
-
- HY-N10621
-
|
Others
|
Cancer
|
3,5-Dimethoxy-2,7-phenanthrenediol (compound 2) is a phenanthrene compound isolated from the roots of Combretum laxum. 3,5-Dimethoxy-2,7-phenanthrenediol is cytotoxic to human cancer cell lines 786-0, MCF-7 and NCI/ADR-RES, with IC50s of 73.26 μM, 118.40 μM and 83.99 μM respectively. 3,5-Dimethoxy-2,7-phenanthrenediol also has free radical scavenging activity with an IC50 of 20.4 μM .
|
-
- HY-134997
-
4-oxo DHA
|
Others
|
Cancer
|
4-oxo Docosahexaenoic acid (4-oxo DHA) is a putative metabolite of Docosahexaenoic acid (HY-B2167) with antiproliferative and PPARγ agonist activity. It inhibits the growth of several triple negative breast cancer cell lines (MCF-10F, trMCF, bsMCF, MDA-MB-231, and BT549) at 50-100 μM, however it increased proliferation of MCF-7 cells. 4-oxo DHA binds covalently to PPARγ and activates gene transcription in luciferase reporter assays and in dendritic cells with EC50 values of approximately 8-16 μM.
|
-
- HY-117649
-
|
Estrogen Receptor/ERR
|
Cancer
|
RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
|
-
- HY-168102
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC50 of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .
|
-
- HY-146080
-
|
Apoptosis
|
Cancer
|
Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC50s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways .
|
-
- HY-156444
-
|
HDAC
CDK
Apoptosis
|
Cancer
|
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells .
|
-
- HY-157161
-
|
11β-HSD
|
Cancer
|
11β-HSD2-IN-1 (compound CDSN) is a potent inhibitor of 11β-HSD2, inhibiting the metabolism of Cholestane-3β,5α,6β-triol (CT) in cells by 11β-HSD2 into the tumor promoter, carcinosterone. 11β-HSD2-IN-1 inhibits testosterone biosynthesis, thereby inhibiting MCF-7 cell proliferation. 11β-HSD2-IN-1 has immune activity and antiviral infection effects .
|
-
- HY-162805
-
|
NO Synthase
Topoisomerase
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM) .
|
-
- HY-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-146238
-
|
EGFR
Thymidylate Synthase
Apoptosis
|
Cancer
|
EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis .
|
-
- HY-125620
-
|
Antibiotic
Bacterial
|
Infection
Cancer
|
Rubiginone D2 is an antibiotic, which exhibits antimicrobial activities against Bacillus subtilis, Staphylococcus aureus and Escherichia coli. Rubiginone D2 exhibits antitumor efficacy, inhibits proliferations of cancer cells HM02, Kato III, HepG2 and MCF7, with GI50s of 0.1, 0.7, <0.1 and 7.5 μM, respectively .
|
-
- HY-155382
-
|
Monocarboxylate Transporter
|
Others
Cancer
|
Lactate transportor 1 (compound 1) is an active lactate transporter in living cells. Lactate transportor 1 displays the cytotoxic effect, with IC50 values of 3.36, 3.27,5.58 and 7.66 μM in Hela, CAL27, MCF7 and MCF10A, respectively. Lactate transportor 1 has an additive effect with Cisplatin (HY-17394) observed in HeLa cells .
|
-
- HY-143233
-
|
Pim
HDAC
Apoptosis
|
Cancer
|
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase .
|
-
- HY-147081
-
AGRO-100
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
|
-
- HY-N9174
-
|
Others
|
Cancer
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
- HY-121255
-
(R)-Cryptopleurine; NSC 19912
|
Others
|
Cancer
|
(–)-Cryptopleurine is an alkaloid that has been found in Lauraceae and has diverse biological activities. It inhibits the growth of human A375 melanoma, A431 epidermoid carcinoma, A549 lung, MES-SA uterine sarcoma, and MCF-7 breast cancer cells (IC50=3 nM for all).2 (–)-Cryptopleurine inhibits hypoxia-induced gene expression in a hypoxia response element (HRE) reporter assay (IC50=8.7 nM).3 (–)-Cryptopleurine (500 μg/mL) prevents lesion formation in tobacco (N. tabacum) plants infected with tobacco mosaic virus (TMV). It also inhibits protein synthesis by yeast and mammalian ribosomes.
|
-
- HY-P10393
-
ERα (295-311)
|
Apoptosis
|
Cancer
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-130624
-
|
HSP
Apoptosis
|
Cancer
|
Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549 .
|
-
- HY-135453
-
|
Bacterial
|
Infection
|
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines .
|
-
- HY-156018
-
|
PI3K
|
Cancer
|
PI3Kα-IN-13 (Compound 18a) is a PI3Kα inhibitor (IC50: 2.5 nM). PI3Kα-IN-13 induces tumor cell apoptosis. PI3Kα-IN-13 inhibits cancer cell proliferation with IC50s of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), 9.85 μM (SW620), respectively. PI3Kα-IN-13 inhibits tumor cell colony formation, migration and invasion .
|
-
- HY-149376
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM,24 h) mediates mitotic arrest,blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa,MCF7,and U87 MG cells .
|
-
- HY-N12887
-
|
Mitochondrial Metabolism
|
Others
Cancer
|
Mycothiazole is an inhibitor for mitochondrial electron transport chain (ETC) complex I. Mycothiazole exhibits cytotoxicity in cancer cells Huh7 (IC50 is 55.8 μM), U87 and MCF7. Mycothiazole induces apoptosis in Huh7. Mycothiazole utilizes the unfolded protein response (UPR) and heat shock response (HSR) pathway involved transcription factors ATFS-1 and HSF1, to extend the lifespan of C. elegans .
|
-
- HY-147825
-
|
EGFR
Raf
Apoptosis
|
Cancer
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
|
-
- HY-N10778
-
|
Others
|
Others
|
(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol is a cucurbitane-type triterpenoid. (19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol has been tested to no effect against 5 cancer cell lines, MCF-7, HepG2, Du145, Colon205 and HL-60 by MTT assay .
|
-
- HY-149407
-
|
VEGFR
CDK
EGFR
Necroptosis
Apoptosis
|
Cancer
|
Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer .
|
-
- HY-157319
-
|
PI3K
|
Cancer
|
PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
|
-
- HY-161786
-
|
Bcl-2 Family
Apoptosis
Reactive Oxygen Species
|
Cancer
|
Bcl-2-IN-20 (Compound 81) is an inhibitor for Bcl-2 with IC50 <10 μM (79.1% inhibition at 9 μM). Bcl-2-IN-20 exhibits cytotoxicity in SK-MEL-28 (IC50>10 μM), A549 (IC50=6.1 μM), HepG2 (IC50>10 μM), MCF-7 (IC50=8.9 μM), HCT116 (IC50>10 μM) and HEK-293 (IC50=14.1 μM). Bcl-2-IN-20 promotes the ROS production, induces apoptosis and DNA damage .
|
-
- HY-168608
-
|
TRP Channel
Apoptosis
PI3K
Akt
|
Cancer
|
TRPM7-IN-1 (compound SUD), a benzoylurea derivative, is an effective TRPM7 inhibitor. TRPM7-IN-1 induces cell cycle arrest and apoptosis, decreases the migration of MCF-7 and BGC-823 cells. TRPM7-IN-1 decreases vimentin expression and increases E-cadherin expression. TRPM7-IN-1 potentially reduces the TRPM7-like current and decreases TRPM7 expression through the PI3K/Akt signaling pathway. TRPM7-IN-1 is a potential agent to suppress the metastasis of breast and gastric cancer by inhibiting TRPM7 expression and function .
|
-
- HY-111846
-
|
SNIPERs
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ERα Degrader-2 comprises a IAP ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs) .
|
-
- HY-164619
-
|
CDK
SARS-CoV
|
Infection
Cancer
|
CDK9-IN-34 (Compound 1b) is an inhibitor for CDK9 with an IC50 of 0.25 μM. CDK9-IN-34 exhibits cytotoxicity to cancer cell HCT116, MCF7 and K652 with IC50 of 1.43, 3.01 and 50.27 μM, respectively. CDK9-IN-34 exhibits antiviral activity against coronavirus 229E with an IC50 of 145.92 μM .
|
-
- HY-158328A
-
-
- HY-161687
-
|
Src
|
Cancer
|
Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
|
-
- HY-162721
-
|
Others
|
Cancer
|
Anticancer agent 242 (7) possesses anticancer activity in A2780 (IC50 = 0.24 μM, ovarian adenocarcinoma), A2780cis (IC50 = 0.45 μM, resistant derivative of A2780), CCD18Co (IC50 = 0.59 μM, non-malignant human fibroblasts), A549 (IC50 = 0.32 μM, lung carcinoma), HT29 (IC50 = 0.26 μM, colorectal adenocarcinoma), and MCF7 (IC50 = 0.55 μM, breast adenocarcinoma) .
|
-
- HY-103455
-
|
Others
|
Others
|
ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.
|
-
- HY-151459
-
|
VEGFR
Bacterial
Dihydrofolate reductase (DHFR)
Fungal
|
Infection
Cancer
|
VEGFR-2/DHFR-IN-2 (compound 5b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.623 and 9.085 μM, respectively. VEGFR-2/DHFR-IN-2 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 3.59-8.38 μM. VEGFR-2/DHFR-IN-2 can be used for the research of cancer .
|
-
- HY-149633
-
|
EGFR
Dihydrofolate reductase (DHFR)
Apoptosis
|
Cancer
|
EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells .
|
-
- HY-111640
-
|
HIV
Reverse Transcriptase
|
Infection
|
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells . 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-159122
-
|
Carbonic Anhydrase
Reactive Oxygen Species
Apoptosis
|
Cancer
|
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
|
-
- HY-110193
-
SPP-86
1 Publications Verification
|
RET
|
Cancer
|
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 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-155180
-
|
PI3K
|
Cancer
|
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth .
|
-
- HY-N12135
-
|
Others
|
Cancer
|
15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2) is an enantio-kaurene diterpenoid (ent -kaurene diterpenoid), which can be isolated from Rubescens rubescens. 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide has cellular activity against EC-1, U87, A549, MCF-7 and HeLa cell lines Toxicity, IC50s are 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, 462.13 μM, and 180.09 μM respectively .
|
-
- HY-139090
-
28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin
|
Others
|
Infection
|
3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor Betulin (HY-N0083). It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50=0.12 μg/mL), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s=8, 10.6, 5.2, and 12.7 μg/mL, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s=>10 μg/mL for both).2 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50=13.4 μM). It is also active against L. donovani amastigotes when used at a concentration of 50 μM.
|
-
- HY-123715
-
|
Others
|
Cancer
|
Anticancer agent 255 is a monocarbonylated curcumin-1,2,3-oxazole conjugate with significant anticancer activity. The IC50 values of Anticancer agent 255 in prostate cancer cells PC-3 and DU-145 are 8.8μM and 9.5μM respectively. The IC50 values of Anticancer agent 255 against breast cancer cells MCF-7, MDA-MB-231 and 4T1 are 6μM, 10μM and 6.4μM, showing good anti-cancer activity Effect. Anticancer agent 255 can induce mitochondria-mediated apoptosis in cancer cells and prevent cell cycle progression. Anticancer agent 255 down-regulated the cell proliferation marker PCNA and inhibited the activation of cell survival proteins. Anticancer agent 255 up-regulated the pro-apoptotic protein Bax and down-regulated the anti-apoptotic protein Bcl-2 .
|
-
- HY-154978
-
|
Others
|
Cancer
|
Cisplatin-resistant cells-IN-1 (Compound 8) has high cytotoxicity against Cisplatin (HY-17394)-resistant cells. Cisplatin-resistant cells-IN-1 reduces the metabolic activity effectively in the low nanomolar range (IC50: 0.14–1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells) .
|
-
- HY-N12589
-
|
Others
|
Cancer
|
8-epi-Helenalin is a semitterpene lactone with anti-tumor activity that can be isolated from Inula britannicaL. var. chinensis (Rupr.) Reg. and the ED50 values of 8-epi-Helenalin for HL-60, A549, MCF7, HCT-15, SK-OV-3 and Malme-3M are 12.2 μM, 53.8 μM, 9.1 μM, 8.7 μM, 18.7 μM and 8.3 μM, respectively. 8-epi-Helenalin can be used for anti-tumor studies .
|
-
- HY-114803
-
-
- HY-161995
-
|
Apoptosis
Necroptosis
FGFR
VEGFR
PDGFR
|
Cancer
|
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells .
|
-
- HY-10812
-
|
PI3K
mTOR
|
Cancer
|
GNE-490, a (thienopyrimidin-2-yl)aminopyrimidine, is a potent pan-PI3K inhibitor with IC50s of 3.5 nM, 25 nM, 5.2 nM, 15 nM for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ, respectively. GNE-490 has >200 fold selectivity for mTOR (IC50=750 nM). GNE-490 shows potent suppression efficacy profile against MCF7.1 breast cancer xenograft model .
|
-
- HY-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-162447
-
|
P-glycoprotein
Apoptosis
|
Cancer
|
P-gp inhibitor 22 is a P-glycoprotein (P-gp) inhibitor that effectively inhibits P-pg and efflux function. P-gp inhibitor 22 induces apoptosis and accumulation of MCF-7/ADR cells processed in the S phase .
|
-
- HY-149632
-
|
EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
|
EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .
|
-
- HY-138074
-
5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
|
Parasite
|
Infection
|
Milbemycin A4 oxime is a derivative of milbemycin A4 (Item No. 17155) and a component of Milbemycin Oxime (HY-B0778), compounds that both have insecticidal and nematocidal activity. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae of the heartworm D. immitis in naturally infested dogs. It inhibits the growth of clinical isolates of C. glabrata with MIC80 values ranging from 16 to greater than 32 μg/mL.1 Milbemycin A4 oxime (2.5 μg/mL) blocks efflux of Fluconazole (HY-B0101) from a clinical isolate of C. glabrata, but not from a strain lacking the efflux pumps CgCDR1 and PDH1, and reduces the MICs of fluconazole and 4-nitroquinoline 1-oxide in wild-type C. glabrata. It enhances adriamycin-induced inhibition of cell growth, as well as increases the intracellular accumulation of adriamycin and the P-glycoprotein substrate Rhodamine 123 (HY-D0816), in adriamycin-resistant, but not -sensitive, MCF-7 breast cancer cells in a concentration-dependent manner.
|
-
- HY-113062
-
20-OH-P
|
Endogenous Metabolite
Cytochrome P450
|
Endocrinology
Cancer
|
20α-Dihydroprogesterone is the metabolite of Progesterone (HY-N0437). 20α-Dihydroprogesterone inhibits cell proliferation and migration in breast tissue. 20α-Dihydroprogesterone inhibits aromatase in cell MCF-7aro with IC50 about 5 μM .
|
-
- HY-151458
-
|
VEGFR
Bacterial
Dihydrofolate reductase (DHFR)
Fungal
|
Infection
Cancer
|
VEGFR-2/DHFR-IN-1 (compound 8b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.384 and 7.881 μM, respectively. VEGFR-2/DHFR-IN-1 shows good antibacterial activities against Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA and MRSA with MIC values of 16, 16, 16, 8, and 16 μg/mL, respectively. VEGFR-2/DHFR-IN-1 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 2.97-7.12 μM. VEGFR-2/DHFR-IN-1 can be used for the research of cancer .
|
-
- HY-10815
-
|
Sigma Receptor
Apoptosis
|
Neurological Disease
Cancer
|
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
|
-
- HY-W010713
-
Fimaporfin free base
|
Others
|
Cancer
|
Meso-tetraphenylchlorin (TPCS2a) is a photosensitizer with poor water solubility, which limits its use in the blood circulation. However, TPCS2a@NPs nanoparticles can be prepared based on polylactic-co-polyethylene glycol acid (PLGA) polymer core loaded with TPCS2. Such nanoparticles can be coated with mesenchymal stem cell-derived plasma membranes (mMSCs) to form mMSC-TPCS2a@NPs, which prolongs blood circulation time and improves tumor targeting ability. Compared with uncoated TPCS2a@NPs, mMSC-TPCS2a@NPs can reduce macrophage uptake by 54% to 70% under different conditions. Both nanoparticle forms are effectively accumulated in MCF7 and MDA-MB-231 breast cancer cells, while uptake in normal breast epithelial cells MCF10A is significantly lower .
|
-
- HY-161260
-
|
P-glycoprotein
|
Cancer
|
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
|
-
- HY-161171
-
|
Parasite
Ephrin Receptor
|
Cancer
|
Antimalarial agent 37 (compound 33) is a selective inhibitor against Type Ⅱ kinase with antiplasmodial activity. Antimalarial agent 37 exhibited cytotoxicity and selectivity towards cancer cells HepG2 and MCF 7 .
|
-
- HY-149360
-
|
P-glycoprotein
|
Cancer
|
P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells .
|
-
- HY-136552
-
|
Others
|
Cancer
|
β-Bisabolene is a sesquiterpene isolated from opoponax (Commiphora guidotti). β-Bisabolene, an anti-cancer agent, can be used for the study of breast cancer .
|
-
- HY-163981
-
|
P-glycoprotein
|
Cancer
|
ABCB1-IN-2 (compound 16q) is a functional inhibitor that can directly bind to the ABCB1 protein and stabilize its structure without affecting the expression and subcellular localization of ABCB1. ABCB1-IN-2 can increase the sensitivity of MCF-7/ADR cells to paclitaxel (PTX), increase the accumulation of PTX, and prevent the accumulation and excretion of luciferin Rh123 mediated by ABCB1. ABCB1-IN-2, as an ABCB1-mediated multidrug resistance (MDR) reversal agent, shows a strong ability to reverse MDR .
|
-
- HY-144666
-
|
Glutaminase
|
Cancer
|
GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells .
|
-
- HY-N12606
-
|
Fungal
|
Infection
|
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-B0812
-
SSA dihydrate
|
Chelators
|
5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
|
-
- HY-113319
-
|
Carbohydrates
|
β-D-Fructose is a β-fruit sugar that can be produced by the hydrolysis of sucrose. β-D-Fructose can be used as a sweetness potentiator. β-D-Fructose can be designed as a units of antiproliferative agents against breast (MCF-7) and colon (MDST8) cancer cell lines .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5956
-
|
Caspase
|
Cancer
|
Ac-AAVALLPAVLLALLAP-LEHD-CHO is an inhibitor of caspases 4, 5 and 9. Ac-AAVALLPAVLLALLAP-LEHD-CHO shows protective effects upon Neocarzinostatin (HY-111183)-treated MCF-7 cells .
|
-
- HY-P5033
-
|
Bacterial
|
Cancer
|
Cyclo(Gly-His) is a liposome-encapsulated cyclic dipeptide with antimicrobial and anticancer activity. Cyclo(Gly-His) has cytotoxicity for HeLa and MCF-7 cell with IC50 values of 1.699 mM and 0.358 mM, respectively. Cyclo(Gly-His) can be used for the research of drug delivery systems .
|
-
- HY-P4523
-
|
Endogenous Metabolite
|
Endocrinology
|
FA-Ala-Arg is a dipeptide with furylacryloyl group. FA-Ala-Arg breaks down to produce arginine. While cell-surface Carboxypeptidase-D (CPD) also increases intracellular Arg, which is converted to nitric oxide (NO). FA-Ala-Arg enhances NO production in MCF-7 cells. FA-Ala-Arg also increases the cell survival of prolactin (PRL)-treated cells, PRL regulates CPD mRNA levels in cells .
|
-
- HY-P10426
-
|
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC50 of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .
|
-
- HY-P10393
-
ERα (295-311)
|
Apoptosis
|
Cancer
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N10871
-
-
-
- HY-N4010
-
-
-
- HY-N2198
-
-
-
- HY-N11973
-
-
-
- HY-N5103
-
-
-
- HY-N3042
-
-
-
- HY-N8679
-
-
-
- HY-W747516
-
-
-
- HY-N2887
-
-
-
- HY-N10305
-
-
-
- HY-N2863
-
-
-
- HY-N7464
-
-
-
- HY-N6990
-
-
-
- HY-N7589
-
-
-
- HY-N3722
-
-
-
- HY-22024
-
-
-
- HY-N8859
-
-
-
- HY-N9391
-
-
-
- HY-N10846
-
-
-
- HY-N11438
-
-
-
- HY-N3443
-
-
-
- HY-N3261
-
-
-
- HY-N11919
-
-
-
- HY-N4227
-
-
-
- HY-N7302
-
-
-
- HY-113796
-
-
-
- HY-N3000
-
-
-
- HY-N10959
-
-
-
- HY-N1252
-
-
-
- HY-N7654
-
-
-
- HY-126803
-
-
-
- HY-N6885
-
-
-
- HY-N3316
-
-
-
- HY-N3615
-
-
-
- HY-N10351
-
-
-
- HY-N12299
-
-
-
- HY-N12607
-
-
-
- HY-N10777
-
-
-
- HY-N11928
-
-
-
- HY-N2298
-
-
-
- HY-N1833
-
-
-
- HY-145379
-
-
-
- HY-N10023
-
-
-
- HY-113319
-
-
-
- HY-N9505
-
-
-
- HY-117872
-
-
-
- HY-134008
-
-
-
- HY-126618
-
-
-
- HY-Y0598
-
-
-
- HY-N13162
-
|
Triterpenes
Structural Classification
Terpenoids
Source classification
Cucurbitaceae
Plants
Hemsleya pengxianensis W. J. Chang
|
Others
|
Hemsleyadin D is a triterpenoid compound derived from Hemsleya penxianensis with antitumor activity. Its IC50 values against K562, MGC-803, U118, HepG2, A549, and MCF-7 cells are 93.9, 47.1, 25.9, 56.1, 66.3, and 67.6 μM, respectively .
|
-
- HY-119358
-
-
- HY-N2741
-
-
- HY-N12586
-
-
- HY-138210
-
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Fungal
|
N,O-Diacetyltyramine is a compound with antibacterial activity and cytotoxicity that can be isolated from the actinomycete Pseudonocardia endophytica VUK-10. N,O-Diacetyltyramine has antibacterial activity against Gram-positive and Gram-negative bacteria and fungi. N,O-Diacetyltyramine is cytotoxic to MDA-MB-231, HeLa, MCF-7 and OAW-42 cells .
|
-
- HY-N3210
-
-
- HY-119539
-
-
- HY-N1107
-
-
- HY-N10481
-
-
- HY-N12208
-
-
- HY-N13115A
-
(E)-21-Angeloyl-protoaescigenin
|
Aesculus chinensis Bunge
Triterpenes
Structural Classification
Terpenoids
Hippocastanaceae
Source classification
Plants
|
Others
|
Protoescigenin 21-tiglate (compound 10) is a glycosidic oleanane-type triterpenoid (BAT) that can be isolated from the acid hydrolysis product (AHP) of the crude extract of Aesculus chinensis seeds. Aesculus-derived triterpenoids (BAT) generally exhibit good antitumor, anti-inflammatory, and anti-Alzheimer's activities. However, the antitumor activity of Protoescigenin 21-tiglate is relatively weak, with IC50 values of >80 μM and 80 μM against MCF-7 and HeLa cells, respectively .
|
-
- HY-N13115
-
(Z)-Protoescigenin 21-tiglate
|
Aesculus chinensis Bunge
Triterpenes
Structural Classification
Terpenoids
Hippocastanaceae
Source classification
Plants
|
Others
|
21-Angeloyl-protoaescigenin (compound 11) is a glycosidic oleanane-type triterpenoid (BAT) that can be isolated from the acid hydrolysis product (AHP) of the crude extract of Aesculus chinensis seeds. Aesculus-derived triterpenoids (BAT) generally exhibit good antitumor, anti-inflammatory, and anti-Alzheimer's activities. Protoescigenin 21-tiglate has antitumor activity, with IC50 values of 38.2 μM and 33 μM against MCF-7 and HeLa cells, respectively .
|
-
- HY-N7340
-
-
- HY-149132
-
DDA
|
Triterpenes
Structural Classification
Terpenoids
Source classification
Endogenous metabolite
|
LXR
|
Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
|
-
- HY-N12209
-
-
- HY-129672
-
-
- HY-138098
-
-
- HY-N10621
-
|
Structural Classification
Combretaceae
Phenols
Polyphenols
Plants
Quisqualis indica Linn.
|
Others
|
3,5-Dimethoxy-2,7-phenanthrenediol (compound 2) is a phenanthrene compound isolated from the roots of Combretum laxum. 3,5-Dimethoxy-2,7-phenanthrenediol is cytotoxic to human cancer cell lines 786-0, MCF-7 and NCI/ADR-RES, with IC50s of 73.26 μM, 118.40 μM and 83.99 μM respectively. 3,5-Dimethoxy-2,7-phenanthrenediol also has free radical scavenging activity with an IC50 of 20.4 μM .
|
-
- HY-125620
-
-
- HY-N9174
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Structural Classification
Flavonoids
Flavones
Source classification
Plants
Moraceae
Broussonetia papyrifera (Linnaeus) L'Heritier ex Ventenat
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Others
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5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
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- HY-135453
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- HY-N12887
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- HY-N10778
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Triterpenes
Structural Classification
Terpenoids
Source classification
Cucurbitaceae
Plants
Momordica charantia Linn.
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Others
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(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol is a cucurbitane-type triterpenoid. (19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol has been tested to no effect against 5 cancer cell lines, MCF-7, HepG2, Du145, Colon205 and HL-60 by MTT assay .
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- HY-N12135
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Structural Classification
Terpenoids
Labiatae
Source classification
Diterpenoids
Plants
Cyrtocymura cincta var. cincta
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Others
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15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2) is an enantio-kaurene diterpenoid (ent -kaurene diterpenoid), which can be isolated from Rubescens rubescens. 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide has cellular activity against EC-1, U87, A549, MCF-7 and HeLa cell lines Toxicity, IC50s are 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, 462.13 μM, and 180.09 μM respectively .
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- HY-N12589
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- HY-114803
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- HY-113062
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- HY-136552
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- HY-N12606
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-13636S
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Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy[1].
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- HY-50936S
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Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
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- HY-13762S
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Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
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Cat. No. |
Product Name |
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Classification |
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- HY-111640
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Azide
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3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells . 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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Cat. No. |
Product Name |
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Classification |
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- HY-160062
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Aptamers
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S2.2 aptamer sodium is a nucleic acid aptamer targeting the mucin MUC1 and can be used for targeted imaging of MCF-7 cancer cells. S2.2 aptamer sodium was labeled with Cy5, and when fluorescent silicon nanodots (SiND) were present, the fluorescence was quenched; when MUC1 was also present, the fluorescence was restored. S2.2 aptamer sodium detects MUC1 with a linear range of 3.33-250 nM .
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- HY-147081
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AGRO-100
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Aptamers
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AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
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