Search Result
Results for "
MCF 7 cells
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-134964
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- HY-112721
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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-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-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-W016794
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Reactive Oxygen Species (ROS)
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-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-113319
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Drug Intermediate
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Cancer
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β-D-Fructose is a monosaccharide. Derivatives synthesized using β-D-Fructose as the sugar backbone exhibit potent and selective antiproliferative activity against breast cancer MCF-7 cells .
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- HY-153469
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ADC Payload
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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-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-137099A
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Fluorescent Dye
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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-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-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-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-137099
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Fluorescent Dye
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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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- 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-132247B
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Estrogen Receptor/ERR
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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-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-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-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-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-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-148453
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Drug Derivative
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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-170402
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Sirtuin
Apoptosis
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Cancer
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SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC50 of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC50 of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models .
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- HY-178774
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Isopentyl-deoxynboquinone
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Quinone Reductase
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Cancer
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IP-DNQ is an efficient NQO1 dependent cytotoxic agent. IP-DNQ has a potent killing effect on MCF-7 cells (IC50 = 0.18 µM). IP-DNQ can be used for cancer research .
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- HY-107550
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HDAC
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Cancer
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NCT-14b is a HDAC6-selective inhibitor. NCT-14b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells .
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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-W288480
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Apoptosis
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Cancer
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Trihexyl phosphate is an organophosphate flame retardant. Trihexyl phosphate causes mitochondrial impairment and induces cell apoptosis in CHO cells. Trihexyl phosphate promotes the proliferation of human breast cancer cells (MCF-7) in a dose-dependent manner and exerts estrogenicity via ERα-independent pathways .
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- HY-178099
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Apoptosis
Caspase
PARP
Bcl-2 Family
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Cancer
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Apoptosis inducer 45 is an apoptosis inducer. Apoptosis inducer 45 is cytotoxically active against the MCF-7 cell line. Apoptosis inducer 45 elicits MCF-7 cell apoptosis via the mitochondrial pathway (increases the Bax/Bcl-2 ratio) by activating cleavage of caspase-9, thereby inducing the fragmentation of DNA repair protein PARP. Apoptosis inducer 45 also can induce caspase-8 cleavage, subsequently initiating cleavage of caspase-3 and its downstream protein PARP to culminate in the extrinsic apoptosis. Apoptosis inducer 45 can be used in the research of breast cancer .
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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-169122
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Drug Derivative
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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-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-170590
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VEGFR
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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VEGFR-2-IN-61 (Compound 7b) is an inhibitor for VEGFR-2 with an IC50 of 2.83 µM. VEGFR-2-IN-61 inhibits the proliferation of multi cancer cells (IC50 for MCF-7 is 2.12 μM). VEGFR-2-IN-61 inhibits the cell migration, induces oxidative stress and apoptosis in MCF-7 .
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- HY-145866
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Drug Intermediate
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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-155841
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Microtubule/Tubulin
Mitosis
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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-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-N14603
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Fungal
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Infection
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Chandrananimycin A has anti-mucor activity, as well as anti-tumor cell activity such as CCL HT29, MFXF 529L, MACL McF-7 .
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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-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-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-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-175567
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Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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Apoptosis inducer 41 is an apoptosis inducer that induces apoptosis through the mitochondrial pathway. Apoptosis inducer 41 exhibits remarkable inhibitory effects against MCF-7 cells (IC50 = 6.2 μM). Apoptosis inducer 41 significantly arrests MCF-7 cells in the G2/M phase, increases ROS accumulation, induces mitochondrial membrane potential depolarization. Apoptosis inducer 41 can used for the study of breast cancer .
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- HY-N4010R
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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-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-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-168589
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Apoptosis
Cytochrome P450
Caspase
Reactive Oxygen Species (ROS)
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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-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-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-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-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-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-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-173040
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Apoptosis
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Cancer
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Anticancer agent 266 (Compound 3B) is an anticancer agent that can inhibit the proliferation of tumor cells. Anticancer agent 266 has an IC50 of 0.13 μM for MCF-7 breast cancer cell line .
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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-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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Biochemical Assay Reagents
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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-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-162239
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Drug Intermediate
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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-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-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-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-175638
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Carbonic Anhydrase
Apoptosis
Bcl-2 Family
CDK
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Cancer
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Carbonic anhydrase-IN-35 is a selective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase-IN-35 potently inhibits tumor-associated hCA IX (Ki = 0.6 nM) and hCA XII (Ki = 2.2 nM). Carbonic anhydrase-IN-35 induces apoptosis in MCF-7 cells by elevating Bax, reducing Bcl-2, and downregulating CDK4/6. Carbonic anhydrase-IN-35 exhibits potent cytotoxicity against MCF-7 (IC50 = 0.3975 μM normoxic/0.6575 μM hypoxic), MCF-7-ADR (IC50> = 0.3975 μM normoxic/4.488 μM hypoxic), MDA-MB-231, and 4T1 breast cancer cells. Carbonic anhydrase-IN-35 can be used for the study of breast cancer .
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- HY-N3443
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Others
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Cancer
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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-100219
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VD/VDR
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Cancer
|
|
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 .
|
-
- HY-134964R
-
-
- HY-115948
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- HY-163812
-
|
|
Molecular Glues
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .
|
-
- HY-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-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-13762
-
|
|
Cytochrome P450
|
Cancer
|
|
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-135584
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
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 .
|
-
- HY-161641
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
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 .
|
-
- HY-161852
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-147882
-
|
|
Bacterial
|
Infection
|
|
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 .
|
-
- HY-N16642
-
|
|
Others
|
Cancer
|
|
Rabdoternin D is an Ent-Kaurane diterpenoid found in Rabdosia rubescens. Rabdoternin D shows no significant cytotoxicity to Hep G2, COLO 205, MCF-7 and HL-60 cancer cells with IC50 values >100 μM .
|
-
- HY-N11438
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
3'-Hydroxymirificin (compound 3) is a naural compound that can be isolated from Pueraria lobata roots. 3'-Hydroxymirificin (compound 3) possesses estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
|
-
- HY-173368
-
|
|
PI3K
|
Cancer
|
|
Antiproliferative agent-67 (Compound 5g) is a PI3K inhibitor with a selectivity index SI of 7.72 for breast cancer cells (MCF-7). Antiproliferative agent-67 inhibits the activity of PI3K protein by forming hydrogen bonds and intermolecular hydrophobic forces with it, exerting anti - proliferative activity against breast cancer cells (MCF-7), and can be used in the research of breast cancer .
|
-
- HY-180827
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-79 (Compound 17) is a VEGFR-2 inhibitor with an IC50 of 2.32 μM. VEGFR-2-IN-79 exhibits potent and broad-spectrum cytotoxicity and can induce apoptosis in MCF-7 cells. VEGFR-2-IN-79 does not cause a significant decrease in the mitochondrial membrane potential of MCF-7 cells. VEGFR-2-IN-79 can be used for research on breast cancer .
|
-
- HY-N14604
-
|
|
Fungal
|
Infection
|
|
Chandrananimycin B has anti-mucor activity, as well as anti-tumor cell activity such as CCL HT29, MFXF 529L, MACL McF-7 .
|
-
- HY-159994
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
AUPF02, a 5-arylurea uracil derivative, is a potent anti-breast cancer agent, with an IC50 of 23.4 µM for MCF-7 cells .
|
-
- HY-186161
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-77 is an anticancer cell proliferation agent that exerts significant antiproliferative effects on HCT116, HepG2, H1299 and MCF-7 .
|
-
- HY-N15306
-
|
|
Apoptosis
|
Cancer
|
|
Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
|
-
- HY-179103
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PLK4-IN-5 (compound 5f) is a PLK4 (IC50 = 0.8 nM) inhibitor. PLK4-IN-5 can inhibit MCF-7 cell clone formation, induce cell cycle arrest (S/G2 phase), and apoptosis. PLK4-IN-5 has anti proliferative activity against MCF-7 cells (IC50 = 0.48 μM). PLK4-IN-5 can be used in the research of cancer such as breast cancer .
|
-
- HY-168644
-
-
- HY-176956
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 13 (Compound 37) is an estrogen receptor (ER) degrader. ER degrader 13 has a significant inhibitory effect on the proliferation of ER-positive breast cancer MCF-7 cells .
|
-
- HY-N16759
-
|
|
Others
|
Cancer
|
|
Apparicine is a monoterpene indole alkaloid that can be naturally extracted from the stems of Tabernaemontana divaricata. Apparicine shows no cytotoxicity against MCF-7 human breast cancer cells and A-549 human lung cancer cells .
|
-
- HY-W702106
-
|
|
Endogenous Metabolite
|
Cancer
|
2-Methyl estradiol, an endogenous metabolite of Estradiol (HY-B0141), inhibits cell proliferation and angiogenesis, with IC50 values of 3 and 2.39 μM for HUVEC and MCF-7 human breast cancer cell proliferation, respectively .
|
-
- HY-183197
-
|
|
Drug Derivative
|
Cancer
|
|
SR 13915 is a structural analog of EGCG (HY-13653), a green tea polyphenol, and exhibits an IC50 greater than 100 μM against both MCF‑7 and MDA‑MB‑231 cell lines .
|
-
- HY-13762A
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene hydrochloride is an antihistamine agent and a chemical sensitizer. Tesmilifene hydrochloride targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene hydrochloride overcomes multidrug resistance .
|
-
- HY-N3318
-
|
|
HIV
|
Infection
|
|
Marsdenoside F is a polyoxygenated pregnane glycoside isolated from the stems of Marsdenia tenacissima. Marsdenoside F showed no significant cytotoxicity against A549 and MCF-7 cell lines, nor did it exhibit significant anti-HIV activity .
|
-
- 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-144791
-
|
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-144792
-
|
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-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-164923
-
|
Hemiasterlin methyl ester
|
Microtubule/Tubulin
|
Cancer
|
|
SPA107 (Hemiasterlin methyl ester) is a Hemiasterlin (HY-117371) analog. SPA107 inhibits the polymerization of tubulin, exhibits antimitotic activity (IC50 of 0.5 nM) and cytotoxicity in p53 mutated MCF-7 cell with IC50 of 0.5 nM .
|
-
- HY-13734
-
|
IV-2
|
Apoptosis
|
Cancer
|
|
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.
|
-
- HY-N3261
-
|
|
AP-1
ERK
STAT
|
Inflammation/Immunology
Cancer
|
|
Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis .
|
-
- HY-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-N4227
-
|
|
Endogenous Metabolite
|
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-B1029
-
Danazol
4 Publications Verification
|
PKC
Apoptosis
Tyrosinase
|
Endocrinology
Cancer
|
|
Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
|
-
- 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-175591
-
|
|
Photosensitizer
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Photosensitizer-7 is a endoplasmic reticulum (ER)-targeted photosensitizer (PS) (λab = 610 nm, λem = 622 nm). Photosensitizer-7shows an IC50 of 4.006 μM in HeLa cells and 3.28 μM in MCF-7 cells under light irradiation. Photosensitizer-7 exhibits dose-dependent cellular uptake and predominant colocalization with ER. Photosensitizer-7 induces dose-dependent intracellular ROS generation, reduces mitochondrial membrane potential, and increases apoptosis upon light irradiation in cells. Photosensitizer-7 significantly inhibits tumor growth in MCF-7 tumor-bearing mice. Photosensitizer-7 can be used for the study of photodynamic anticancer applications .
|
-
- 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-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-N5052
-
|
|
Others
|
Cancer
|
|
Asiaticoside B is a 9,19-cycloartane triterpene glycoside found in Actaea asiatica. Asiaticoside B has cytotoxicity against HepG2 and MCF-7 cancer cells with IC50 values of 9.74 µM and 8.32 µM, respectively .
|
-
- HY-146162
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Colletotrichalactones A is a polyketide that display moderate-to-potent cytotoxic activities against MCF7 cells with an IC50 of 35.06 µM .
|
-
- 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-B1029R
-
-
- HY-N1366
-
|
Methylumbelliferone
|
Apoptosis
Bacterial
|
Infection
Cancer
|
|
Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer .
|
-
- 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-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-W038396
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Ferrotrace (Compound dppt) is a ligand. Ferrotrace can bind to DNA and BSA (Kb = 0.14 x 10 4 M -1). Ferrotrace shows an IC50 of 17.35 μM for MCF-7 cells. Ferrotrace can be used for the research of breast cancer .
|
-
- 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-N15584
-
|
Isoheraclenin
|
Others
|
Cancer
|
|
Pabularinone is a compound found in the plant Clausena lansium. Pabularinone has potent cytotoxic activity, and its activity showed inhibitory effects in human breast cancer (MCF-7) cells (IC50: 33.74 μg/mL). Pabularinone can be used in anti-tumor research .
|
-
- HY-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-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-178143
-
|
|
KLF
|
Cancer
|
|
Sp1-IN-1 is a selective specificity protein 1 (Sp1) inhibitor. Sp1-IN-1 inhibits the proliferation of Hela cells and MCF-7 cells. Sp1-IN-1 can be used to the studies of cervical cancer and breast cancer .
|
-
- 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-N10871
-
|
|
SARS-CoV
|
Cancer
|
|
Neocryptomerin, a biflavonoid, shows inhibitory activity against U251, MCF-7, HeLa cell. Neocryptomerin has favorable binding affinities in the active pocket of SARS-CoV-2. Neocryptomerin is the leading compound of rational compounds against COVID-19 .
|
-
- 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-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-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-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-172932
-
|
|
YAP
|
Cancer
|
|
TEAD-IN-20 is a TEAD inhibitor. The IC50 values of TEAD-IN-20 in TEAD4 FRET and TEAD4 MCF7-Tead cell lines are 0.021 and 0.044 μM, respectively. TEAD-IN-20 can be used in cancer research .
|
-
- 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-170580
-
|
|
Topoisomerase
|
Cancer
|
|
Topo I/II-IN-1 (compound 7t) is a potent Topo I and Topo II dual inhibitor. Topo I/II-IN-1 exhibits significant cytotoxicity against MCF-7 breast cancer cell line with an IC50 of 7.45 μM .
|
-
- HY-173528
-
|
|
Bacterial
Fungal
|
Infection
Cancer
|
|
Antimicrobial agent-40 (Compound 5a) has antimicrobial activity against fungi, Gram-negative and Gram-positive bacteria. Antimicrobial agent-40 has good cytotoxicity against MCF-7 cells (IC50: 33.52 μM) and exhibits anticancer activity .
|
-
- 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-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-173060
-
|
|
ERK
Apoptosis
Autophagy
|
Cancer
|
|
ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
|
-
- HY-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-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-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-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-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-173182
-
|
|
Microtubule/Tubulin
P-glycoprotein
|
Cancer
|
|
Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor. By binding to the colchicine site of tubulin, it causes G2/M cell cycle arrest and generates reactive oxygen species (ROS). Antitumor agent-200 exhibits significant inhibitory activity against MCF7/ADR and KBV200 cell lines with overexpression of P-glycoprotein (P-gp), with drug resistance indices (DRI) of 0.83 and 0.58 respectively. In the MCF-7 xenograft model, Antitumor agent-200 (25 mg/kg, intraperitoneal injection) can achieve a tumor growth inhibition rate of 57.2%. Antitumor agent-200 can be used in the research of the anti-cancer field .
|
-
- HY-175177
-
|
|
Apoptosis
Caspase
β-catenin
|
Cancer
|
|
Xiap-casp7 PPI-IN-1 is a reversible XIAP: CASP7 inhibitor with specifically disrupting the interaction between XIAP and CASP7. XIAP-CASP7 PPI-IN-1 selectively induce MCF-7 and other caspase-3 down-regulation (CASP3/DR) triple-negative breast cancer cell apoptosis. XIAP-CASP7 PPI-IN-1 overcomes chemoresistance via down-regulating β-catenin and its associated ABC transporters in Paclitaxel (HY-B0015)-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 can be used for the study of breast cancer .
|
-
- 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-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-169253
-
|
|
Reactive Oxygen Species (ROS)
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-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-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-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-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-N16645
-
|
|
Cholinesterase (ChE)
|
Cancer
|
|
Plasiaticine B (Compound 2) is an indole alkaloid found in Plantago asiatica. Plasiaticine B shows no significant cytotoxicity to HL-60, A-549 and MCF-7 cells with IC50 >40 μM. Plasiaticine B shows no significant inhibitory effect on AChE, with an inhibition rate <60% .
|
-
- 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-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-N14378
-
|
|
Bacterial
|
Infection
|
|
Parimycin has activity against Gram-positive bacteria, negative bacteria and tumors, and no effect on fungal. Parimycin can inhibit tumor cells including GXF 251L, H640, LXFA 629L, MCF-7, MEXF 514L with IC70s of 0.9-6.7 μg/mL .
|
-
- 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-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-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-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-W106688
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Triisopropyl phosphate inhibits TFF1 and EGR3 gene expression, exhibits anti-estrogenic activity that inhibits Estradiol (HY-B0141)-induced MCF-7 cell proliferation with an EC50 of 341 μM. Triisopropyl phosphate inhibits the estrogen response element (ERE)-stimulated luciferase activity in MVLN cells with an EC50 of 900 μM .
|
-
- 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-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-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-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-168901
-
|
|
Src
|
Cancer
|
|
Hck-IN-2 (Compound 8e) is an HCK inhibitor. Hck-IN-2 is cytotoxic to tumor cells, with IC50 values of 19.58 μM and 1.42 μM against MDA-MB231 and MCF-7, respectively. Hck-IN-2 has anti-tumor activity .
|
-
- 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-13636
-
Fulvestrant
Maximum Cited Publications
133 Publications Verification
ICI 182780; ZD 9238; ZM 182780
|
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Inflammation/Immunology
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-157487
-
|
|
Drug Derivative
|
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-173151
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
BRCA2-IN-1 (Compound 3j) is a potential BRCA2 inhibitor that exhibits antiproliferative activity against the breast cancer MCF-7 cell lines. BRCA2-IN-1 also demonstrates DPPH radical scavenging ability, with an IC50 of 12.36 µM .
|
-
- HY-N14893
-
|
|
Others
|
Cancer
|
|
Cetoniacytone B can inhibit the growth of HEPG2 and MCF7 human tumor cell lines, with GI50 values of 4.4 μM .
|
-
- 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-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-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-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-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-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-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-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-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-170975
-
|
|
VD/VDR
|
Cancer
|
|
UG-650 is a non-Gemini analog of UVB1 that combines the structural features of UVB1 and MC 1288. UG-650 can bind to the vitamin D receptor (VDR) and inhibit the proliferation of MCF-7 cells and the migration of MC3T3-E1 cells .
|
-
- 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-161755
-
|
|
Endogenous Metabolite
|
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-W080443
-
|
|
Endogenous Metabolite
|
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-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-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-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-167694
-
|
|
Quinone Reductase
|
Cancer
|
|
Antiproliferative agent-62 (compound 5) is a functionalized benzylidene-indolin-2-one with notable antiproliferative activity and NQO1 activity induciton funciton, particularly in inducing NQO1 expression in murine Hepa1c1c7 cells and demonstrating effectiveness against human cancer cell lines, including MCF-7 and HCT116.
|
-
- 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-N14255
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Memnobotrin A is an antibiotic found in Memnoniella echinata (JS6308). Memnobotrin A has inhibitory effect on NCI-460, MCF7 and SF-268 cell lines .
|
-
- 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-N1366S
-
|
7-Methoxycoumarin-d3; Methyl umbelliferyl ether-d3
|
Isotope-Labeled Compounds
Apoptosis
Bacterial
|
Infection
Cancer
|
|
Herniarin-d3 is the deuterium labeled Herniarin (HY-N1366). Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer .
|
-
- HY-173361
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 270 (Compound 8e) is an inhibitor that acts on tubulin. Its IC50 value against MCF-7 breast cancer cells is 1.02 μM. Through a dual mechanism of action, namely inducing Apoptosis and destabilizing microtubules, it exerts significant anti-proliferative activity against breast cancer cells. Anticancer agent 270 can be applied to research in the field of cancer .
|
-
- HY-172783
-
|
|
Cytochrome P450
Apoptosis
|
Cancer
|
|
Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. Aromatase-IN-5 effectively blocks estrogen production. Aromatase-IN-5 inhibits the proliferation of breast cancer cell lines like MCF-7, arrests the cell cycle at the G1 phase, and induces apoptosis. Aromatase-IN-5 is promising for research of breast cancer .
|
-
- 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-179150
-
|
|
EGFR
Tyrosinase
|
Cancer
|
|
EGFR-TK-IN-6 (compound 10B) is an EGFR-TK inhibitor (IC50 = 0.65 μM). EGFR-TK-IN-6 has anti proliferative activity against MCF-7 cells (IC50 = 37.7 μM). EGFR-TK-IN-6 has low toxicity to normal cells. EGFR-TK-IN-6 can be used for cancer research .
|
-
- HY-157138
-
|
|
MMP
|
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-Y0598
-
|
Benzylideneacetophenone
|
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-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-176955
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 12 (Example 1) is an estrogen receptor (ER) degrader with IC50 values for ERα and ERβ of 2.3 and 80.2 nM respectively (TR-FRET experiment). ER degrader 12 inhibits the proliferation of MCF-7 cells, with an IC50 of 1.53 nM. ER degrader 12 can be used for research on breast cancer .
|
-
- 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-162002A
-
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ATM/ATR
|
Cancer
|
|
(S)-WSD0628 (Compound 28) is the S-isomer of WSD0628 (HY-162002). (S)-WSD0628 is the inhibitor for ATM that inhibits the phosphorylation of ATM in MCF-7 cell with IC50 <100 nM. (S)-WSD0628 exhibits radiosensitizing activity. (S)-WSD0628 can cross blood-brain barrier .
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-
- HY-146467
-
|
|
Drug Derivative
|
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-W587738
-
|
|
Apoptosis
|
Cancer
|
|
Viridiflorol is an active natural molecule with anti-cancer effect. Viridiflorol induces anti-neoplastic effects on breast (MCF-7, IC50 = 10 µM), lung (A549, IC50 = 30 µM), and brain (Daoy, IC50 = 0.1 µM) cancer cells through apoptosis. Viridiflorol can be used for breast, lung, and brain cancer research .
|
-
- 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-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.
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-
- HY-N10949
-
|
|
Others
|
Cancer
|
|
Viscosalactone B is a withanolide found in Withania somnifera. Viscosalactone B shows potent inhibitory activities to NCI-H460, HCT-116, MCF-7 and SF-268 cancer cells with IC50 values of 0.32, 0.47, 0.4 and 0.45 μg/mL. Viscosalactone B can be used for the research of cancer .
|
-
- 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-175173
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-166 (Compound 2) is a EGFR inhibitor. EGFR-IN-166 has potent anticancer activity against breast cancer cells with IC50s of 69.63 and 22.84 μM for MCF-7 and MDA-MB-231 cells, respectively. EGFR-IN-166 significantly inhibits cell migration and EGFR expression. EGFR-IN-166 can be used for breast cancer research .
|
-
- HY-169477
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
PAMAM Dendrimer G0.5 Carboxylate sodium is a polyamidoamine (PAMAM) dendrimer with carboxylate termini. PAMAM Dendrimer G0.5 Carboxylate sodium conjugated with DACHPt is cytotoxic to A2780 ovarian cancer cells, MCF-7 breast cancer cells, Caco-2 colon cancer cells and BJ fibroblasts with IC50 values of 0.03, 1.6, 0.18 and 3 µM, respectively .
|
-
- HY-N0435
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Isorhamnetin 3-gentiobioside is a flavonoid with activity of promoting cancer cell proliferation. Isorhamnetin 3-gentiobioside is an activator of DNA synthesis in MCF-7 human breast cancer cells with an EC50 of 3.1 μg/mL. Isorhamnetin 3-gentiobioside exhibits ABTS radical scavenging activity with an IC50 of 33.43 μg/mL. The compound can be used to study the bidirectional regulatory mechanism of cancer .
|
-
- 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-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-N1366R
-
|
Methylumbelliferone (Standard)
|
Reference Standards
Apoptosis
Bacterial
|
Cancer
|
|
Herniarin (Standard) (Methylumbelliferone (Standard)) is the analytical standard of Herniarin (HY-N1366). This product is intended for research and analytical applications. Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer.
|
-
- HY-146454
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Antiproliferative agent-6 (compound 8a) is a potent antitumor agent. Antiproliferative agent-6 has antiproliferative activity against cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively .
|
-
- HY-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-N13709
-
|
|
Others
|
Cancer
|
|
12β-Acetoxy-7β-hydroxy-3,11,15,23-tetraoxo-5a-lanosta-8,20-dien-26-oic acid, a lanostanoid triterpene that can be isolated from Ganoderma lingzhi, exhibits an IC50 of 80.8 μM in MCF-7 cells .
|
-
- 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-180541
-
|
|
COX
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-190 (Compound 3o) is an inhibitor that targets both EGFR (IC₅₀ = 0.028 μM) and COX-2 (IC₅₀ = 0.208 μM). EGFR-IN-190 exhibits potent inhibitory activity against MCF-7 cells and induces apoptosis (apoptosis). EGFR-IN-190 can be used for research on breast cancer .
|
-
- 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-111846
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ERα Degrader-2 (Compound 11) is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)) .
|
-
- HY-N12232
-
|
|
Parasite
Bacterial
|
Infection
Cancer
|
|
Carbazomycin D exhibits antituberculosis and antimalarial activities, that inhibits Plasmodium falciparum with an IC50 > 10 μg/mL, inhibits Mycobacterium tuberculosis with MIC of 25 μg/mL. Carbazomycin D exhibits cytotoxicity in cell MCF-7, KB, NCI-H187 and Vero, with IC50s of 21.3, 33.2, 12.9, and 34.3 μg/mL, respectively .
|
-
- 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-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 .
|
-
- HY-158090
-
|
|
Drug Derivative
|
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 (ROS)
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Traumatic Acid is a wound healing agent and a cytokinin (phytohormone). Traumatic Acid enhances the biosynthesis of collagen in cultured human skin fibroblasts. Traumatic Acid inhibits MCF-7 breast cancer cells viability and enhances apoptosis and oxidative stress. Traumatic Acid can be used in studies of cancer, circulatory disorders (including arterial hypertension), and skin diseases associated with oxidative stress and impaired collagen biosynthesis .
|
-
- HY-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-13734R
-
|
IV-2 (Standard)
|
Apoptosis
Reference Standards
|
Cancer
|
|
PX-12 (Standard) is the analytical standard of PX-12. This product is intended for research and analytical applications. 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.
|
-
- HY-N15479
-
|
|
Bacterial
|
Infection
Cancer
|
|
Nanangenine F is a drimane sesquiterpenoid with weak antibacterial and anticancer activities. Nanangenine F inhibits Bacillus subtilis (ATCC 6633) with an IC50 of 78 µg/mL. Nanangenine F inhibits NS-1, DU-145, MCF-7 and human fibroblast NFF cells with IC50s of 49 µg/mL, 95 µg/mL, 49 µg/mL, and 84 µg/mL, respectively .
|
-
- HY-N15652
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Versimide (Compound 15) can be isolated from the insect pathogenic fungus Gibellula sp. BCC36964. Versimide exhibits cytotoxicity in cell lines including MCF-7, KB, NCI-H187, and Vero with IC50s of 3.59, 4.83, 1.89, and 3.49 μg/mL, respectively, demonstrating its anticancer activity .
|
-
- 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-N14280
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Memnobotrin B is an antibiotic found in Memnoniella echinata (JS6308). Memnobotrin B has inhibitory effect on NCI-460, MCF7 and SF-268 cell lines .
|
-
- HY-160563
-
-
- 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-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-W177546
-
|
|
Phosphodiesterase (PDE)
Apoptosis
Caspase
DNA/RNA Synthesis
|
Cancer
|
|
CD00509 is a tyrosyl-DNA phosphodiesterase (PDE) Tdp1 inhibitor with an IC50 of 0.71 μM. CD00509 increases DNA damage and promotes apoptosis of MCF-7 cells. CD00509 can sensitize breast cancer cells and wild-type murine embryonic fibroblasts (MEFs) to Camptothecin (CPT) (HY-16560). CD00509 can be used for the study of cancers such as breast cancer .
|
-
- 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-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-113319R
-
|
|
Reference Standards
Drug Intermediate
|
Cancer
|
|
β-D-Fructose, (Standard) is the analytical standard of β-D-Fructose (HY-113319R). This product is intended for research and analytical applications. β-D-Fructose is a monosaccharide. Derivatives synthesized using β-D-Fructose as the sugar backbone exhibit potent and selective antiproliferative activity against breast cancer MCF-7 cells .
|
-
- HY-155105
-
|
|
Glycosidase
|
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-N14056
-
|
|
Bacterial
|
Infection
Cancer
|
|
Chrolactomycin is found in the strain of Streptomyces sp. 569N-3. The IC50 of Chrolactomycin for ACHN, A431, McF-7 and T24 cells are 1.2 μM, 1.6 μM, 0.69 μM and 0.45 μM, respectively. Chrolactomycin has only anti-Gram-positive bacteria activity with the MIC of 5.2-10.4 μg/mL .
|
-
- HY-115950
-
|
|
Drug Derivative
|
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-13636R
-
|
ICI 182780(Standard); ZD 9238(Standard); ZM 182780 (Standard)
|
Reference Standards
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-144070
-
|
|
Estrogen Receptor/ERR
|
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 (HY-132247). ErSO-DFP displays antitumor activity against MCF-7 in mice. ErSO-DFP can cross the blood brain barrier .
|
-
- 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-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-174870
-
|
|
PROTACs
Estrogen Receptor/ERR
Apoptosis
Fluorescent Dye
|
Cancer
|
|
PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .
|
-
- HY-161267
-
-
- 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-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-174336
-
|
|
Survivin
Apoptosis
|
Cancer
|
|
Survivin-IN-1 (Compound II₃) is a potent Survivin (a member of the Inhibitor of Apoptosis Protein family) inhibitor with an IC50 value of 8.1 μM against human lung cancer A549 cells and 9.0 μM against breast cancer MCF-7 cells. Survivin-IN-1 reduces Survivin protein levels and induces tumor cell apoptosis. Survivin-IN-1 is promising for research of malignant tumors such as lung cancer and breast cancer .
|
-
- 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-155337
-
|
|
Eukaryotic Initiation Factor (eIF)
|
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-150108
-
|
|
mTOR
Apoptosis
Caspase
|
Cancer
|
|
RMC-4745 is a selective dual-site inhibitor of mTORC1, with a selectivity of 35 times for mTORC1 and mTORC2. RMC-4745 inhibits the proliferation of MCF-7 cells and upregulates Caspase-3/7 activity to induce cell apoptosis. RMC-4745 does not cause the upregulation of HER3 due to the inhibition of mTORC2. RMC-4745 can be used for the study of breast cancer .
|
-
- 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-173232
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 value of 0.509 µM and an IC50 value of 7.48 μM for inhibiting the proliferation of MCF-7 cells. VEGFR-2-IN-66 exerts its anti-cancer activity by arresting the cell cycle, inducing apoptosis, and regulating gene expression, and can be used in the research of the breast cancer field .
|
-
- HY-B0543
-
|
Thiosinamine; N-Allylthiourea
|
Reactive Oxygen Species (ROS)
|
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-W016887
-
|
H-Gly-Pro-OH; Gly-Pro
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
Cancer
|
|
Glycyl-L-proline (H-Gly-Pro-OH) is a dipeptide. Glycyl-L-proline can induce MCF-7 cells apoptosis. Glycyl-L-proline can enhance the inhibitory effect of the PRODH/POX knockout on collagen and DNA biosynthesis. Glycyl-L-proline can inhibit Gly-Sar and L-proline transport. Glycyl-L-proline can be used for the researches of cancer and metabolic disease, such as breast cancer .
|
-
- 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-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-134997
-
|
4-oxo DHA
|
PPAR
|
Cancer
|
|
4-oxo Docosahexaenoic acid (4-oxo DHA) is a putative metabolite of Docosahexaenoic acid (HY-B2167) with antiproliferative and PPARγ agonist activity. It inhibits the growth of several triple negative breast cancer cell lines (MCF-10F, trMCF, bsMCF, MDA-MB-231, and BT549) at 50-100 μM, however it increased proliferation of MCF-7 cells. 4-oxo DHA binds covalently to PPARγ and activates gene transcription in luciferase reporter assays and in dendritic cells with EC50 values of approximately 8-16 μM.
|
-
- HY-168720
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, showing anti-tumor activity. Apoptosis inducer 32 caused significant cellular morphological changes in MDA-MB-231 cells, including membrane bubbling, nuclear fragmentation, and apoptotic body formation. The IC50 of Apoptosis inducer 32 in MCF-7, MDA-MB-231, and HEK cells is 4.77, 6.56 and 337.8 μM respectively .
|
-
- 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-170382
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
|
-
- HY-50936S
-
|
Ecteinascidin 743-d3; ET-743-d3
|
Isotope-Labeled Compounds
Reactive Oxygen Species (ROS)
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-168164
-
|
|
Histone Methyltransferase
|
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-169476
-
|
|
Drug Derivative
|
Cancer
|
|
Pyrrolidine linoleamide is a derivative of linoleic acid amide with anticancer activity. Pyrrolidine linoleamide exhibits antiproliferative activity against a range of cancer cell lines, with IC50 values of 12.0, 27.5, 7.7, 21.9, 36.6, 32.6, and 33.9 μg/mL against U251, MCF-7, NCI-ADR/RES, 786-0, NCI-H460, PC-3, and OVCAR-3 cell lines, 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-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-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-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-170910
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
|
-
- HY-W082856A
-
|
|
BCRP
|
Cancer
|
|
Butein tetramethyl ether (Compound 20) is a potent and selective breast cancer resistance protein/ATP-binding cassette subfamily G member 2 (BCRP/ABCG2) inhibitor. Butein tetramethyl ether has inhibitory potencies against MCF-7 MX and MDCK BCRP cells with IC50 values of 2.2 and 1.03 μM, respectively. Butein tetramethyl ether is promising for research of cancers .
|
-
- HY-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-N14892
-
|
|
Bacterial
|
Infection
Cancer
|
|
Cetoniacytone A has weak activity against Gram-positive and negative bacteria. Cetoniacytone A can inhibit the growth of HEPG2 and MCF7 human tumor cell lines, with GI50 values of 3.2 μM .
|
-
- HY-175019
-
|
|
VEGFR
Apoptosis
Caspase
MDM-2/p53
Bcl-2 Family
|
Cancer
|
|
VEGFR-2-IN-70 is a potent VEGFR-2 inhibitor with an IC50 of 18.04 nM. VEGFR-2-IN-70 exhibits cytotoxicity against A549 and MCF-7 cancer cells with IC50 values of 0.43 μM and 3.8 μM, respectively. VEGFR-2-IN-70 induces G1 cell cycle arrest and apoptosis in lung cancer cells. VEGFR-2-IN-70 is useful in cancer research .
|
-
- 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-173075
-
|
|
RIP kinase
Mixed Lineage Kinase
Necroptosis
|
Cancer
|
|
Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC50 for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models .
|
-
- HY-138089
-
|
|
Androgen Receptor
Estrogen Receptor/ERR
LDLR
|
Metabolic Disease
Cancer
|
|
17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats .
|
-
- HY-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-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-174131
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC50=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC50=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer .
|
-
- HY-170483
-
|
|
HSV
HIV
|
Infection
Cancer
|
|
Antitumor agent-191 (Compound 7) exhibits antiviral activity against HSV-1 and HIV with EC50 of 0.03 μM and 0.81 μM. Antitumor agent-191 exhibits potential antitumor efficacy, that inhibits cancer cell HepG2, WI-38, Vero and MCF-7, with IC50s of 19.6, 39.3, 18.3 and 28 μM, respectively .
|
-
- 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-171777
-
|
ErPC3; Erucylphosphohomocholine
|
PI3K
Akt
Ras
Raf
p38 MAPK
|
Cancer
|
|
Erufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC50: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia .
|
-
- HY-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-12520
-
|
|
Dopamine Receptor
|
Neurological Disease
Cancer
|
|
SKF 38393 is a selective dopamine D1 receptor agonist. SKF 38393 activates the cAMP signaling pathway and promotes dopamine release in the developing rat striatum. SKF 38393 inhibits MCF-7 breast cancer cell proliferation (IC50=0.1 μM). SKF 38393 is promising for research of neurodevelopmental disorders, dopamine-related diseases (e.g., Parkinson’s, dopamine deficiency), and cancers .
|
-
- 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-13636S1
-
|
ICI 182780-d5; ZD 9238-d5; ZM 182780-d5
|
Isotope-Labeled Compounds
|
Others
|
|
Fulvestrant-d5 (ICI 182780-d5) is a isotope of Fulvestrant (HY-13636) . 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-175779
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
TDP1-IN-4 (Compound 33) is a Tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 0.90 μM. TDP1-IN-4 has a strong synergistic effect with Camptothecin (HY-16560) in SK-Mel-2 cells, but not in cancer cells (A549, HCT-116 and MCF-7 cells) and non-cancerous Ges-1 cells. TDP1-IN-4 can be used for cancer chemotherapy and radiotherapy research .
|
-
- 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-174414
-
|
|
EGFR
|
Cancer
|
EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC50 values of 0.09 (EGFR) and 0.08 μM (HER2) respectively. EGFR/HER2-IN-18 exhibits broad-spectrum anti-cancer activity. EGFR/HER2-IN-18 induces MCF-7 cells apoptosis and inhibits the cell cycle. EGFR/HER2-IN-18 can be used for the study of breast cancer .
|
-
- HY-177966
-
|
|
Drug Metabolite
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
ETM-305 is a degradation product of the anticancer agent ET-743 (HY-50936). ET-743 (Ecteinascidin 743; Trabectedin) is a tetrahydroisoquinoline alkaloid that binds to the minor groove of DNA, blocks the transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cell apoptosis, and increases ROS production in MCF-7 and MDA-MB-453 cells. Trabectedin is used in the research of soft tissue sarcoma and ovarian cancer .
|
-
- 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-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-N15577
-
|
|
Drug Derivative
|
Cancer
|
|
Antiproliferative agent-69 (Compound 1) is a prenylated kaempferol derivative found in the fresh bud’s fur of Platanus acerifolia. Antiproliferative agent-69 shows significant antiproliferative effects against human breast cancer cells (MCF-7) and human hepatocellular carcinoma cells (Hep-G2) with IC50 values of 38.2 μM and 39.5 μM, respectively. Antiproliferative agent-69 is promising for research of breast cancer and liver cancer .
|
-
- HY-N8508
-
|
|
Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
|
Cancer
|
|
Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC50s of 95, 70, 60, and 25 µM, respectively .
|
-
- HY-161740
-
|
|
AUTOTACs
Estrogen Receptor/ERR
Autophagy
|
Cancer
|
|
PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ .
|
-
- 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-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-155203
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
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-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-172621
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-159 (compound 12), a dihydropyrimidine, is a potent EGFR inhibitor with an IC50 value of 29.00 nM. EGFR-IN-159 exhibits dose-dependent inhibition against EGFR and HER2. EGFR-IN-159 shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 has no BBB permeation. EGFR-IN-159 shows appreciable anti-cancer activity .
|
-
- HY-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-119358R
-
|
|
Reference Standards
Reactive Oxygen Species (ROS)
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Traumatic Acid (Standard) is the analytical standard of Traumatic Acid. This product is intended for research and analytical applications. Traumatic Acid is a wound healing agent and a cytokinin (phytohormone). Traumatic Acid enhances the biosynthesis of collagen in cultured human skin fibroblasts. Traumatic Acid inhibits MCF-7 breast cancer cells viability and enhances apoptosis and oxidative stress. Traumatic Acid can be used in studies of cancer, circulatory disorders (including arterial hypertension), and skin diseases associated with oxidative stress and impaired collagen biosynthesis[1][2].
|
-
- HY-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-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-170999
-
|
|
Caspase
Apoptosis
Ferroptosis
|
Cancer
|
|
Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer activity, showing an IC50 of 90 nM against MCF-7 breast cancer cells.
Antitumor agent-196 promotes Apoptosis by regulating the Bax-caspase 3 signaling pathway, and induces Ferroptosis through the modulation of key signaling molecules, including GPX4.
Antitumor agent-196 holds promising potential for further research in the field of cancer therapy .
|
-
- HY-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-175465
-
|
|
Interleukin Related
STAT
|
Cancer
|
|
SMI-10B13 is an Oncostatin M (OSM) inhibitor with a KD of 6.6 μM. SMI-10B13 inhibits OSM-mediated STAT3 phosphorylation in T47D and MCF-7 cell lines (IC50 = 136 and 164 nM, respectively). SMI-10B13 shows anti-tumor effect in human breast cancer mice models .
|
-
- HY-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-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-179398
-
|
|
Keap1-Nrf2
|
Cancer
|
|
Keap1-Nrf2-IN-29 (Compound 1a), a Curcumin (HY-N0005) analog, is a Keap1 protein inhibitor. Keap1-Nrf2-IN-29 exhibits significant inhibitory activity against A549, PC-3 and MCF-7 cells. Keap1-Nrf2-IN-29 can be used for the study of prostate cancer .
|
-
- HY-164533
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-33 (compound 7f) is a potent STAT3 inhibitor with anti-cancer activity. STAT3-IN-33 exhibits antiproliferative activity in HCT116, MCF-7, and MDA-MB-231 cells, with IC50s of 6.44, 3.29, and 4.86 μM, respectively. STAT3-IN-33 can be used for breast and colon cancer research .
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-
- 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-179160
-
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Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin-IN-61 is a tubulin polymerization inhibitor with an IC50 of ≤7.63 μM. Tubulin-IN-61 induces early apoptosis and triggers significant G2/M phase arrest. Tubulin-IN-61 elevates intracellular ROS levels. Tubulin-IN-61 shows high activity against MCF-7 cells with an IC50 of 5.61 μM. Tubulin-IN-61 can be used for the research of breast cancer .
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-
- HY-172748
-
|
|
Drug Derivative
|
Neurological Disease
Cancer
|
|
9β-Hydroxyhexahydrocannabinol is a synthetic cannabinoid derivative. 9β-Hydroxyhexahydrocannabinol exhibits cytotoxicity against various tumor cell lines, such as HCT-116, MCF-7, K562, MIAPaCa-2, PANC-1, A549, PC-3 and SW-620, with IC50 values ranging from 15.23 to 33.74 μM. 9β-Hydroxyhexahydrocannabinol can be used in the study of cancer .
|
-
- HY-175003
-
|
|
Proton Pump
|
Cancer
|
|
HV1-IN-2 (Compound 14c) is a human voltage-gated proton channel (HV1) inhibitor with an IC50 of 2.14 μM. HV1-IN-2 has a potent anticancer activity with significant antiproliferative effects against THP-1 and MCF-7 cells. HV1-IN-2 can be used for cancers research, such as colorectal tumours, leukaemia, and breast cancer .
|
-
- HY-174404
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.
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-
- HY-N12208
-
|
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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-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) .
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-
- HY-117102
-
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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 .
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-
- HY-179045
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
ERα degrader 14 (Compound B7) is a potent ERα degrader. ERα degrader 14 exhibits significantly potent and selective anti-proliferative activity on two ERα-positive breast cancer cell lines (MCF-7 and T47D). ERα degrader 14 induces cell cycle arrest, inhibits cell migration, and induces cell apoptosis. ERα degrader 14 effectively inhibits tumor growth in mouse models. ERα degrader 14 can be used for the study of breast cancer .
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-
- 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-171477
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
|
-
- HY-169408
-
|
|
Cytochrome P450
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC50s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC50s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cell cycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway .
|
-
- HY-178112
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer .
|
-
- 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-170955
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
HA-CD44 interaction inhibitor 3 (compound 5d) is a Hyaluronic acid (HY-B0633A) (HA)-CD44 interaction inhibitor with antiproliferative activities. HA-CD44 interaction inhibitor 3 inhibits MDA-MB-231 (CD44++) cells and MCF-7 cells (CD44--) with EC50s of 4.24 μM and 14.74 μM, respectively. HA-CD44 interaction inhibitor 3 shows the potential for cancer research .
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-
- 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 .
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-
- HY-175174
-
|
|
Glutaminase
|
Cancer
|
|
Antiproliferative agent-73 (Compound 7) is an antiproliferative agent. Antiproliferative agent-73 significantly inhibits proliferation of human cancer cells with excellent cytotoxicity. Antiproliferative agent-73 has potent anticancer activity with IC50s of 15.20, 18.18, 20.20 and 13.23 μM for HepG2, MCF-7, HCT-116 and WI38 cells, respectively. Antiproliferative agent-73 can be used for cancers research, such as breast, colorectal and liver cancer .
|
-
- HY-128600
-
ERD-308
1 Publications Verification
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity. (Pink: Target Protein Ligand (HY-48027); Black: Linker (HY-172643); Blue: VHL Ligand (HY-112078); VHL Ligand+Linker：(HY-172645))
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-
- HY-180537
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 57 is a apoptosis inducer and Thymidylate Synthase (TS) inhibitor. Apoptosis inducer 57 exhibits cytotoxic activity against SW480 and MCF-7 cancer cells with IC50 values of 15.7 and 16.5 µM, and induces dose-dependent apoptosis and S-phase cell cycle arrest. Apoptosis inducer 57 stalely binds the TS active site via interactions with Asp218 and Met311. TS-IN-9 can be used for breast cancer and colorectal cancer research .
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-
- 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-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-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-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-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 .
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-
- HY-112589
-
|
|
Bacterial
|
Infection
Cancer
|
|
BRITE-338733 is an inhibitor of E. coli RecA ATPase activity (IC50: 4.7 μM). BRITE-338733 also inhibits the ATP hydrolysis activity of RSC chromatin remodeling enzyme by binding to its ATP-binding pocket and DNA (IC50: 0.316 μM). BRITE-338733 exhibits cytotoxicity against MCF-7 and MDA-MB-231 breast cancer cells. BRITE-338733 can be used in studies on antibacterial adjuvants and anticancer research .
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-
- HY-114770
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .
|
-
- HY-151158
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM) .
|
-
- HY-118761
-
|
5,6-epoxy atRA; 5,6-epoxy RA
|
RAR/RXR
|
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-146103
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
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-B0543R
-
|
Thiosinamine (Standard); N-Allylthiourea (Standard)
|
Reference Standards
Reactive Oxygen Species (ROS)
|
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-Y0598R
-
|
|
Fatty Acid Synthase (FASN)
Reference Standards
Apoptosis
Fungal
|
Inflammation/Immunology
Cancer
|
|
trans-Chalcone (Standard) is the analytical standard of trans-Chalcone (HY-Y0598). This product is intended for research and analytical applications. 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-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-170508
-
|
|
Cytochrome P450
|
Endocrinology
|
|
Aromatase-IN-4 (Compound 6a) is an aromatase (Aromatase) inhibitor. Aromatase-IN-4 exhibits anticancer activity, with GI50 values of 2.95 μM, 3.35 μM, 2.27 μM, 8.46 nM, and 1.56 μM against the MDAMB-231, MCF-7, A-549, NCI-H23, and A-498 cell lines, respectively . Aromatase-IN-4 effectively blocks aromatase-dependent estrogen production .
|
-
- 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-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-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-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-179149
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PLK4-IN-6 (compound C05) is an PLK4 inhibitor (IC50 < 0.1 nM). PLK4-IN-6 has anti proliferative activity against various tumor cells, such as IMR-32 (IC50 = 0.948 μM), MCF-7 (IC50 = 0.979 μM), H460 (IC50 = 1.679 μM) cells. PLK4-IN-6 can significantly induce cell apoptosis and block the cell cycle. PLK4-IN-6 can be used for research on various types of cancer .
|
-
- HY-155965
-
|
|
VEGFR
PARP
Apoptosis
|
Cancer
|
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
|
-
- HY-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-172097
-
|
|
Drug Derivative
|
Cancer
|
|
HL22 is a harmaline derivative. HL22 significantly inhibits HCT116, MGC803 and MCF7 cancer cell lines, and inhibits MGC803 cell migration and monoclonal formation. The anti-cancer mechanism of HL22 is related to a variety of metabolic pathways and can be used in the study of cancer .
|
-
- HY-178161
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC degrader-2 is a selective HDAC degrader with a DC50 values of 2.55 μM against HDAC1. HDAC degrader-2 effectively induces the degradation of HDAC1 and HDAC2, but has no significant effect on the degradation of HDAC3, 4, 6 and 8. HDAC degrader-2 exerts potent antiproliferative effects against MM.1S and MCF-7 cells. HDAC degrader-2 induces apoptosis in myeloma cells. HDAC degrader-2 can be used for the study of myeloma .
|
-
- HY-178350
-
|
|
CDK
HDAC
Apoptosis
Histamine Receptor
|
Cancer
|
|
MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer .
|
-
- HY-139434
-
|
|
Histone Demethylase
|
Cancer
|
|
JMJD6-IN-1 is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC50 values of 19.2 μM and 25.2 μM. JMJD6-IN-1 inhibits JMJD6 demethylase activity. JMJD6-IN-1 can be used for the research of lung adenocarcinoma, prostate cancer, breast cancer, pancreatic cancer, colon cancer, oral squamous cell carcinoma, and glioblastoma .
|
-
- HY-W131302
-
|
N,N-Ethylenediglycine
|
Endogenous Metabolite
|
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-N13772
-
|
(+)-Dihydroisorhamnetin
|
Apoptosis
|
Cancer
|
|
3'-O-Methyltaxifolin ((+)-Dihydroisorhamnetin) is a dihydroflavanol found in Pulicaria jaubertii. A mixture of these alcohol compounds including 3'-O-Methyltaxifolin found in Pulicaria jaubertii exhibits antitumor activity with IC50 values of 19.1 μg, 20.0 μg, and 24.1 μg against prostate cancer (PC-3), breast cancer (MCF-7), and hepatocellular carcinoma (HepG-2) cell lines, respectively. Furthermore, 3'-O-Methyltaxifolin can induce cell apoptosis, making it a promising candidate for anticancer research. .
|
-
- HY-149636
-
|
|
EGFR
CDK
VEGFR
Apoptosis
|
Cancer
|
|
Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. 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-179062
-
|
|
Apoptosis
|
Cancer
|
Anticancer agent 280 (Compound 65) is an anti-cancer agent targeting triple-negative breast cancer (TNBC). Anticancer agent 280 exhibits IC50 values of Anticancer agent 280 for MDA-MB-231, MDA-MB-231/LM2-4, Jurkat, and MCF-7 of 7.1, 11.65, 6.99, and 21.51 μM respectively. Anticancer agent 280 can cause significant arrest of cells in the S phase and induce cell apoptosis. Anticancer agent 280 can be used for the study of TNBC .
|
-
- HY-W047131
-
|
|
Bacterial
|
Infection
Cancer
|
|
IPrAgCl is an antibacterial agent. IPrAgCl exhibits antiproliferative activity against MCF7 cell line with an IC50 of 30 nM. IPrAgCl has an IC50 of 35 nM against KB cancer cell line. IPrAgCl induces apoptosis in HL60 cell line. IPrAgCl promotes apoptosis-inducing factor translocation from the mitochondrial to the nuclear compartment .
|
-
- HY-172869
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 9 (Compound 5D) is an estrogen receptor antagonist. Estrogen receptor antagonist 9 shows significant cytotoxicity against MCF7 cells with an IC50 value of 8.50 μM. Estrogen receptor antagonist 9 is promising for research of breast cancers .
|
-
- HY-175512
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin-IN-53 is a potent Tubulin inhibitor with an IC50 of 6.06 μM. Tubulin-IN-53 inhibits the polymerization of tubulin by targeting the colchicine binding site of tubulin and destroys the microtubule network. Tubulin-IN-53 induces MCF-7 cell cycle arrest in the G2/M phase and apoptosis, and inhibits cell migration accompanied by the decrease of mitochondrial membrane potential and increase the accumulation of ROS. Tubulin-IN-53 destroys the angiogenesis of human umbilical vein endothelial cells.Tubulin-IN-53 can used for the study of cancers such as breast cancer and lung cancer .
|
-
- HY-170551
-
|
|
Carbonic Anhydrase
VEGFR
|
Cancer
|
|
CA IX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. CA IX/VEGFR-2-IN-3 exhibits anticancer activity, inhibiting the growth of MCF-7 breast cancer cells (with an IC50 of 22.33 μM) and mouse fibroblast cell line 3T3 (where cell viability is less than 40% at a concentration of 100 μM). CA IX/VEGFR-2-IN-3 can be used for research in the field of cancer treatment .
|
-
- HY-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 .
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-
- HY-178961
-
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PROTACs
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-13 is an orally active PROTAC molecule that efficiently and selectively degrades ERα (DC50 = 3.78 nM). PROTAC ERα Degrader-13 has the characteristics of strong anti proliferation (IC50 = 0.6 nM), induction of apoptosis, and overcoming drug resistance in MCF-7 cells. PROTAC ERα Degrader-13 has good safety and no significant organ toxicity. PROTAC ERα Degrader-13 can be used for cancer research .
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-
- HY-161776
-
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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 .
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-
- HY-169216
-
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|
EGFR
VEGFR
CDK
|
Cancer
|
|
Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM .
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-
- HY-155113
-
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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 .
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-
- 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-146169
-
|
|
Reactive Oxygen Species (ROS)
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.
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-
- 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 .
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-
- 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-173222
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 28 (Compound 4h) is an inhibitor targeting P-glycoprotein (P-gp). It can inhibit the proliferation of cancer cells, and its IC50 value for MCF-7/ADR cells is between 15.88 and 21.96 μM. P-gp inhibitor 28 can increase the accumulation of Rho123 in MCF-7/ADR cells and can be used in research related to cancer and overcoming multidrug resistance in tumors .
|
-
- 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-170849
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
PERK
IRE1
|
Cancer
|
|
Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. Nur77 modulator 4 significantly induces Nur77 expression and apoptosis, showing excellent growth inhibition in HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, thereby inducing cell apoptosis. Nur77 modulator 4 can be used in cancer research applications .
|
-
- 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-178911
-
|
|
Thymidylate Synthase
Apoptosis
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
|
Cancer
|
|
TS-IN-8 is a potent thymidylate synthase (TS) inhibitor. TS-IN-8 can induce apoptosis and cause cell cycle arrest at the G2/M in MCF-7 cells. TS-IN-8 can induce nuclear morphological changes. TS-IN-8 can increase intracellular reactive oxygen species (ROS) levels. TS-IN-8 can activate intrinsic apoptosis pathways by regulating apoptosis-related proteins such as the bax/bcl-2 ratio and caspase activation. TS-IN-8 can be used for the study of breast cancer .
|
-
- 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-178496
-
|
|
Hsp-targeting Chimeras
PARP
HSP
|
Cancer
|
|
DDO3602 is a PARP1 HEMTAC degradation agent mediated by HSP90. DDO3602 has good anti-tumor activity and tumor selectivity. DDO3602 induces G2/M phase arrest, DNA damage, and inhibits cell migration by degrading PARP1 in MCF-7 cells (IC50 = 187 nM). DDO3602 can be used for research on cancer such as breast cancer. (Pink: PARP1 Ligand (HY-75706); Blue: HSP90 Ligand (HY-179203); Black: Linker (HY-W015300))
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-
- 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-147081
-
AS 1411
2 Publications Verification
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 .
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-
- HY-154978
-
|
|
Drug Derivative
|
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-N15392
-
|
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Antibiotic
Bacterial
|
Infection
|
|
Lactonamycin Z is an antitumor antibiotic. Lactonamycin Z has weak anti-Gram-positive bacterial activity. Lactonamycin Z can inhibit human tumor cells HMO2, MCF7 and Hep G2 with GI50 (μg/mL) of 1.9, 0.85 and 5.11, respectively .
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-
- HY-186015
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
Arg-TERRα is a mini-PROTAC targeting ERRα. Arg-TERRα induces ERRα degradation via the N-end rule pathway, thereby in inhibiting the proliferation and migration of MCF7 breast cancer cells. Arg-TERRα can be used for breast cancer research .
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-
- 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-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-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) .
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-
- HY-170895
-
|
|
HSP
Na+/K+ ATPase
|
Cancer
|
|
Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a Kd of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC50 of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC50s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively .
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-
- HY-124456
-
|
|
Bacterial
|
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-N12230
-
|
|
Bacterial
Parasite
Fungal
|
Infection
Cancer
|
|
Penicolinate B is a picolinic acid derivative that can be isolated from Penicillium sp. Penicolinate B exhibits antimalarial activity (IC50: 1.40 μg/mL), antitubercular activity (MIC: 25.0 μg/mL), activity against Bacillus cereus (IC50: 25.0 μg/mL), and activity against Candida albicans (IC50: 1.45 μg/mL). Penicolinate B also has certain cytotoxicity against cancer cells such as MCF-7, KB, and NCI-H187. Penicolinate B can be used in research on malaria, tuberculosis, bacterial/fungal infections and tumors .
|
-
- HY-168439
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
HLB-0532259 is a PROTAC degrader for Aurora-A and N-Myc. HLB-0532259 degrades Aurora-Ain a non-MYCN amplified MCF-7 with a DC50 of 20.2 nM, degrades N-Myc in MYCN amplified cells SK-N-BE and Kelly with DC50 of 179 nM and 229 nM. HLB-0532259 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-168440); Black: linker (HY-W007957); Blue: ligand for E3 ligase Cereblon (HY-41547))
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-
- HY-175838
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC50 = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer .
|
-
- HY-W348485
-
|
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mTOR
|
Cancer
|
|
WRX606 is an orally active nonrapalog inhibitor for mTOR complex 1 (mTORC1M). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 (S6K1) (IC50 = 10 nM) and eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50 = 0.27 μM) in MCF-7 cells. WRX606 suppresses tumor growth in mice without promotion of metastasis. WRX606 can be studied in research as an antitumor agent .
|
-
- 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-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-181235
-
|
|
COX
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
COX-2/Aromatase-IN-1 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-1 can simultaneously inhibit COX-2 and aromatase, significantly suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-1 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-1 can be used for the study of inflammation and breast cancer .
|
-
- HY-171755
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-40 (Compound 15b) is a heat shock protein 90 (Hsp90) C-terminal inhibitor. Hsp90-IN-40 exhibits antiproliferative activity against SKBr3 and MCF-7 breast cancer cells (IC50 of 2.57 µM and 2.43 µM, respectively). Hsp90-IN-40 inhibits cancer cell growth by inhibiting the Hsp90 C-terminal function, leading to Hsp90-dependent protein degradation. Hsp90-IN-40 can be used in breast cancer research .
|
-
- HY-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-181459
-
|
|
PARP
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
PARP1-IN-55 is a potent and selective PARP1 inhibitor with an IC50 value of 0.019 μM. PARP1-IN-55 exhibits anti-proliferative selective activity against MCF-7 breast cancer cells (IC50 = 3.6 μM). PARP1-IN-55 inhibits the PARP1-mediated DNA damage repair pathway, induces ROS accumulation, disrupts mitochondrial membrane potential, induced apoptosis and suppresses cancer cell migration, invasion, and colony formation. PARP1-IN-55 can be used for the study of breast cancer .
|
-
- HY-181236
-
|
|
COX
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
COX-2/Aromatase-IN-2 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-2 can simultaneously inhibit COX-2 and aromatase, suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-2 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-2 can be used for the study of inflammation and breast cancer .
|
-
- HY-179070
-
|
|
Apoptosis
|
Cancer
|
Anticancer agent 280 TFA (Compound 65) is an anti-cancer agent targeting triple-negative breast cancer (TNBC). Anticancer agent 280 TFA exhibits IC50 values of Anticancer agent 280 TFA for MDA-MB-231, MDA-MB-231/LM2-4, Jurkat, and MCF-7 of 7.1, 11.65, 6.99, and 21.51 μM respectively. Anticancer agent 280 TFA can cause significant arrest of cells in the S phase and induce cell apoptosis. Anticancer agent 280 TFA can be used for the study of TNBC .
|
-
- 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-147081A
-
|
AGRO-100 sodium
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium 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 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-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-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-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-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
|
Drug Derivative
|
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-178955
-
|
|
EGFR
HSP
PI3K
Caspase
Apoptosis
CDK
ERK
Akt
|
Cancer
|
|
EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .
|
-
- 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-138098
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
|
-
- HY-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-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-179140
-
|
|
EGFR
VEGFR
Apoptosis
|
Cancer
|
|
EGFR/VEGFR2-IN-8 (compound 10k) is a dual EGFR/VEGFR-2 inhibitor (EGFR IC50 = 57 nM, VEGFR-2 IC50 = 21 nM). EGFR/VEGFR2-IN-8 has anti proliferative activity against various tumor cells, such as MCF-7 (IC50 = 20 nM), Panc-1 (IC50 = 22 nM), A-549 (IC50 = 23 nM), HT-29 (IC50 = 23 nM) cells. EGFR/VEGFR2-IN-8 has antioxidant and apoptosis inducing activity. EGFR/VEGFR2-IN-8 can be used for research on various types of cancer .
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-
- 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 .
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-
- 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 .
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-
- 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-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-168714
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 12 (Compound 2k) is an inhibitor for microtubule polymerization with an IC50 of 22.23 μM. Microtubule inhibitor 12 arrests the cell cycle of B16-F10 at G2/M phase, induces apoptosis in B16-F10, and inhibits cell migration. Microtubule inhibitor 12 inhibits the proliferation of cancer cells B16-f10, A549, HepG2 and MCF-7, with IC50s of 0.098, 0.135, 0.109, and 0.259 μM, respectively. Microtubule inhibitor 12 exhibits antitumor efficacy in mouse model .
|
-
- HY-Z12208
-
|
|
Drug Derivative
|
Cancer
|
|
N1-Phenylsuberamide is an organic amide compound, and its structure can be regarded as a simplified analogue of Vorinostat (HY-10221). N1-Phenylsuberamide exhibits moderate anti-proliferative activity against MDA-MB-231 and MCF-7 cells. N1-Phenylsuberamide does not show significant HDAC inhibitory activity and can only weakly induce the expression of the p21 gene. N1-Phenylsuberamide has extremely low relative binding affinity of estrogen receptor. N1-Phenylsuberamide can be used as a control compound .
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-
- HY-N9848
-
|
|
Others
|
Cancer
|
|
2α,3α,24-Trihydroxyursa-12,20(30)-dien-28-oic acid is a triterpenoid with anticancer effects. 2α,3α,24-Trihydroxyursa-12,20(30)-dien-28-oic acid inhibits HepG2, A549, MCF-7, SK-OV-3, and HeLa cells with IC50 values of 19.62 μM, 18.86 μM, 45.94 μM, 62.41 μM, and 28.74 μM, respectively .
|
-
- HY-170603
-
|
|
Fluorescent Dye
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PRMT5-targeted fluorescent ligand-1 (Compound 7) is a PRMT5-targeted fluorescent ligand, that inhibits PRMT5 with an IC50 of 29.39 nM. PRMT5-targeted fluorescent ligand-1 exhibits cell imaging activity, that exhibits good fluorescence signal in MCF-7 with an IC50 of 29 nM. PRMT5-targeted fluorescent ligand-1 induces apoptosis. PRMT5-targeted fluorescent ligand-1 exhibits a maximal excitation wavelength of 438 nm and a maximal emission wavelength of 550 nm .
|
-
- HY-121149B
-
|
(E/Z)-3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
(E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
|
-
- HY-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-178472
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker) .
|
-
- HY-183618
-
|
|
PROTACs
Histone Demethylase
|
Cancer
|
|
DW-229 is a PROTAC degrader derived from Deferiprone (HY-B0568), targeting Fe(II)/α‑ketoglutarate‑dependent histone lysine demethylases (KDMs). DW-229 degrades KDM2A, KDM3A, KDM5B, KDM4A‑C, KDM5C, KDM6B in breast cancer cells. DW-229 shows IC50 < 0.5 μM against MCF‑7 cells and IC50 of 8.87 μM against MDA‑MB‑231 cells, with high cancer cell selectivity. DW-229 can be used for the research of breast cancer, liver cancer, prostate cancer, lung cancer .
|
-
- HY-114803
-
-
- HY-174800
-
|
|
Topoisomerase
|
Cancer
|
|
ARN21929 is a Topoisomerase II inhibitor with an IC50 of 4.5 μM. ARN21929 exhibits excellent kinetic and thermodynamic solubility as well as metabolic stability. However, ARN21929 shows poor antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cells. ARN21929 can be used in the study of cancer .
|
-
- HY-175269
-
|
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Topoisomerase
|
Cancer
|
|
MGB1Y is a noncovalent DNA minor groove binder (MGB). MGB1Y potently inhibits cancer cells proliferation and topoisomerase I activity. MGB1Y downregulates their breast cancer-related genes in MCF7 and MDA-MB-231 cells. MGB1Y has a broad-spectrum anticancer activity, such as breast cancer, colon cancer, and leukemia .
|
-
- HY-P10790
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
|
-
- HY-178441
-
|
|
Pyruvate Kinase
Reactive Oxygen Species (ROS)
Apoptosis
Microtubule/Tubulin
|
Metabolic Disease
Cancer
|
|
PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer .
|
-
- HY-182275
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
|
-
- HY-173492
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-156 (Compound 7f) is an EGFR inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC50 values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC50 values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers .
|
-
- HY-121255
-
|
(R)-Cryptopleurine; NSC 19912
|
TMV
|
Cancer
|
|
(–)-Cryptopleurine is an alkaloid that has been found in Lauraceae and has diverse biological activities. It inhibits the growth of human A375 melanoma, A431 epidermoid carcinoma, A549 lung, MES-SA uterine sarcoma, and MCF-7 breast cancer cells (IC50=3 nM for all).2 (–)-Cryptopleurine inhibits hypoxia-induced gene expression in a hypoxia response element (HRE) reporter assay (IC50=8.7 nM).3 (–)-Cryptopleurine (500 μg/mL) prevents lesion formation in tobacco (N. tabacum) plants infected with tobacco mosaic virus (TMV). It also inhibits protein synthesis by yeast and mammalian ribosomes.
|
-
- HY-141877
-
MS4322
1 Publications Verification
YS43-22
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-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-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-W179181
-
MSNBA
1 Publications Verification
|
GLUT
|
Metabolic Disease
Cancer
|
|
MSNBA is a potent and selective GLUT5 fructose transport inhibitor with an IC50 of 0.10 mM. MSNBA does not affect the transport activity of human GLUT1, GLUT2, GLUT3, GLUT4 or bacterial GlcPSe. MSNBA competitively inhibits GLUT5 fructose uptake with a Ki of 3.2 μM in MCF7 cells. MSNBA can be used for the study of cancer or diabetes .
|
-
- HY-174232
-
|
|
EGFR
Carbonic Anhydrase
Caspase
|
Cancer
|
|
EGFR/CA-IX-IN-1 (Compound 14) is a dual inhibitor against epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX) with IC50 values of 5.92 nM and 63 nM, respectively. EGFR/CA-IX-IN-1 shows strong cytotoxicity against breast cancer cells (MDA-MB-231, MCF-7) with IC50 values of 5.78 μM and 8.05 μM, respectively. EGFR/CA-IX-IN-1 inhibits the catalytic activity of CA-IX, up-regulates BAX/Bcl-2, activates caspases, and arrests the cell cycle at the G1 phase. EGFR/CA-IX-IN-1 is promising for research of breast cancer .
|
-
- 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-173365
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-67 (Compound 6b) is an inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2). Its IC50 values for MDA-231 and MCF-7 cell lines are 5.91 µM and 7.16 µM respectively, and its inhibitory effect on VEGFR-2 is comparable to that of Sorafenib (HY-10201) (IC50 is 53.63 nM). VEGFR-2-IN-67 exerts significant anti-cancer activity through mechanisms such as inducing Apoptosis (the early apoptosis rate reaches 57.20%), arresting the cell cycle at the G1 phase, upregulating pro-apoptotic markers and downregulating Bcl-2. VEGFR-2-IN-67 can be used for research in the field of cancer .
|
-
- HY-169382
-
|
|
Melatonin Receptor
|
Cancer
|
|
Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.
|
-
- HY-178065
-
|
|
PROTACs
Histone Methyltransferase
GLP Receptor
|
Cancer
|
|
PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468)) .
|
-
- HY-178822
-
|
|
Drug Derivative
|
Cancer
|
|
AQ-13 (Compound 7) is a Chloroquine (HY-17589A) analogue with anti-breast cancer property. AQ-13 shows antiproliferative activities against MDA-MB231 and MCF7 with GI50 of 27.81 and 17.85 μM. AQ-13 shows low cytotoxicity against non-cancerous breast epithelial cells MCF10A (GI50 = 65.26 μM). AQ-13 can be used for the research of breast cancer .
|
-
- 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-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-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-181880
-
|
|
PROTACs
NAMPT
|
Cancer
|
|
PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research .
|
-
- HY-175698
-
|
|
ACSL Family
Ferroptosis
Microtubule/Tubulin
COX
Glutathione Peroxidase
|
Cancer
|
|
Ferroptosis inducer-9 is a ferroptosis inducer and colchicine site tubulin polymerization inhibitor. Ferroptosis inducer-9 inhibits MCF-7 cell growth with an IC50 of 14 nM and inhibits [ 3H]colchicine binding. Ferroptosis inducer-9 reduces expression of GPX4 and FTH, increases COX2 and ACSL4, lowers GSH, NADP+, and NADPH levels, increases LPO, MDA, and Fe(II) levels, and decreases SOD concentrations. Ferroptosis inducer-9 demonstrates significant anti-tumor efficacy in HCT116 CRC xenograft model. Ferroptosis inducer-9 can be used for the study of triple negative breast cancer (TNBC) and colorectal cancer (CRC) .
|
-
- HY-172167
-
|
|
PD-1/PD-L1
HDAC
|
Inflammation/Immunology
Cancer
|
|
PD-L1/HDAC-IN-1 (Compound 14) is the inhibitor for PD-L1 and HDAC that inhibits PD-1/PD-L1 interaction, HDAC2 and HDAC3 with IC50 of 88.10, 27.98 and 14.47 nM, respectively. PD-L1/HDAC-IN-1 exhibits slight cytotoxicity in MCF-7 (IC50=19.34 μM). PD-L1/HDAC-IN-1 upregulates the expression of PD-L1 and CXCL10, promoting anti-tumour immune response by recruiting T-cell infiltration into TME .
|
-
- HY-176834
-
|
|
GLUT
|
Cancer
|
|
3-Deoxy-3-fluoro-D-fructose (Compound 12) is a derivative of 2,5-Anhydro-D-mannitol. 3-Deoxy-3-fluoro-D-fructose is a selective probe of Hexose transporter 5 (GLUT5). 3-Deoxy-3-fluoro-D-fructose inhibits the transport of D-fructose labeled with 14C by GLUT5 with IC50s of 1.16 and 2.37 µM in EMT-6 and MCF-7 cells. 3-Deoxy-3-fluoro-D-fructose can be used for positron emission tomography (PET) imaging of cancers .
|
-
- HY-171895
-
|
12-Nitro-9-cis,12-cis-octadecadienoic acid
|
PPAR
Interleukin Related
NF-κB
TNF Receptor
|
Inflammation/Immunology
|
|
12-Nitrolinoleate (12-Nitro-9-cis,12-cis-octadecadienoic acid) is an activator for peroxisome proliferator-activated receptor γ (PPARγ). 12-Nitrolinoleate is a nitrated form of linoleic acid. 12-Nitrolinoleate can be formed upon exposure to acidified nitrate and found in human red blood cells and plasma. 12-Nitrolinoleate can activate PPARγ-dependent gene expression in MCF-7 cells expressing PPARγ with an EC50 = 0.045 μM. 12-Nitrolinoleate is able to inhibit LPS (HY-D1056)-induced NF-κB transcription in RAW 264.7 cells. 12-Nitrolinoleate can inhibit IL-6, TNF-α and CCL2 induced by LPS .
|
-
- HY-181769
-
|
|
MMP
Polo-like Kinase (PLK)
CDK
PAK
Bcl-2 Family
Caspase
Apoptosis
|
Cancer
|
|
Anticancer agent 306 is a spiro tetramic acid derivative and a inhibitor of MMP1, MMP7 and PLK1. Anticancer agent 306 exerts antiproliferative activity against H1299, RKO and MCF-7 cells with IC50 values of 19.25 μM, 3.29 μM and 102.36 μM, respectively. Anticancer agent 306 can up-regulate p21 protein and down-regulate CCND1 and CCNB1 proteins to induce cell cycle arrest, regulate the expression of Bcl-2 and Bax to induce cell apoptosis. Anticancer agent 306 can down-regulate MMP1 and MMP7 proteins to inhibit tumor invasion and metastasis. Anticancer agent 306 can be used for the research of lung cancer, colorectal cancer, breast cancer .
|
-
- HY-175171
-
|
|
Topoisomerase
VEGFR
c-Met/HGFR
EGFR
Estrogen Receptor/ERR
|
Cancer
|
|
Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα .
|
-
- 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-168435
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-63 (Compound 12b) is the inhibitor for VEGFR2 that inhibits 87.2% VEGFR-2 at 10 μM. VEGFR-2-IN-63 exhibits antiproliferative activity in multiple cancer cell, IC50s for HCT116, MCF7 and PaCa2 is 6.5 μM, 2.1 μM and 4.1 μM, respectively .
|
-
- HY-141877B
-
|
YS43-22 (isomer)
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-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-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-N8146
-
|
|
STAT
Bcl-2 Family
Ser/Thr Kinase
Survivin
c-Myc
Apoptosis
Necroptosis
CDK
|
Infection
Cancer
|
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Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
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- HY-15668
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MMP
Bcl-2 Family
Caspase
Apoptosis
Drug Derivative
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Cancer
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ST09 is an efficient and low toxicity Curcumin (HY-N0005) derivative. ST09 significantly inhibits cell migration and downregulates the expression of MMP1, MMP2, and Vimentin. ST09 has strong cytotoxicity to breast cancer cells, such as MDA-MB-231, MCF7 and T47D cells. ST09 induces cell apoptosis by upregulating Bax and cleaved caspase-3/9. ST09 can be used in the research of cancer such as breast cancer .
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-
- HY-178176
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PROTACs
Cannabinoid Receptor
Akt
ERK
Bcl-2 Family
Apoptosis
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Cancer
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PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)) .
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- HY-N12887
-
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Mitochondrial Metabolism
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Others
Cancer
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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 .
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- HY-180961
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PROTACs
Estrogen Receptor/ERR
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Cancer
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His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast cancer .
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- HY-175297
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VEGFR
EGFR
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Cancer
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EGFR T790M/VEGFR-2-IN-1 (Compound 6) is a dual EGFR T790M mutant (IC50=0.26 μM) and VEGFR-2 (IC50=0.95 μM) inhibitor. EGFR T790M/VEGFR-2-IN-1 blocks tumor cell proliferation and angiogenesis signaling pathways. EGFR T790M/VEGFR-2-IN-1 exhibits potent cytotoxicity against multiple cancer cell lines (HCT116, MCF-7, HepG2, A549; IC50=5.35-9.90 μM). EGFR T790M/VEGFR-2-IN-1 is promising for research of non-small cell lung cancer and solid tumors .
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- HY-P10785
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Bacterial
Antibiotic
|
Infection
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Iturin A-2 is a cyclic lipopeptide discovered in B. subtilis and exhibits inhibitory activity against the plant pathogenic fungus P. expansum (MIC = 8 µg/disk). Iturin A-2 is cytotoxic to MCF-7 and BT474 breast cancer cells, as well as HeLa cervical cancer cells, with IC50 values of 66.81, 95.04, and 77.5 µg/mL, respectively. In greenhouse studies, Iturin A-2 at concentrations of 100 and 300 mg/kg Iturin A-2 reduces the lesion area of southern corn leaf blight caused by B. maydis, and in field studies, concentrations of 300 and 500 mg/kg Iturin A-2 reduce the incidence of the disease. Iturin A-2 (12.5 µg/mL) inhibits cell division, but not nuclear division, in isolated fertilized starfish eggs .
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- HY-159122
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Carbonic Anhydrase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
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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 .
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- HY-172767
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PROTACs
STAT
Apoptosis
|
Cancer
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|
STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting Signal Transducer and Activator of Transcription 3 (STAT3). STAT3-D11-PROTAC-VHL exhibits anti-tumor activity with IC50 values of 1335 nM and 1973 nM against HeLa and MCF-7 cells, respectively. STAT3-D11-PROTAC-VHL binds to the DNA-binding domain of STAT3 and recruits the E3 ligase VHL to form a ternary complex, leading to the ubiquitination of STAT3 and subsequent degradation by the proteasome. STAT3-D11-PROTAC-VHL also inhibits tumor cell growth, induces cell cycle arrest and apoptosis, and suppresses tumor immune evasion .
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- HY-123715
-
|
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Apoptosis
|
Cancer
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|
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 .
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-
- HY-10815
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Sigma Receptor
Apoptosis
|
Neurological Disease
Cancer
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|
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 .
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-
- HY-164619
-
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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 IC50s 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 .
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-
- HY-N15636
-
|
(-)-Coccinine
|
Serotonin Transporter
P-glycoprotein
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Neurological Disease
Cancer
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|
Coccinine ((-)-Coccinine) is a weak inhibitor of SERT (IC50: 196.3 μM; Ki: 106.8 μM) and P-gp (IC50: 0.96 mM). Coccinine exhibits significant anti-tumor activity against various cancer cell lines, such as breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Coccinine can be used in the research of tumors and neurological diseases .
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-
- HY-N7012
-
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5-Hydroxy-3',4',7-trimethoxyflavone
|
Lipoxygenase
TNF Receptor
Interleukin Related
COX
Fungal
Parasite
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
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|
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid with multiple biological activities. 7,3',4'-Tri-O-methylluteolin inhibits soybean lipoxygenase (LOX), with an IC50 value of 23.97 µg/mL. 7,3',4'-Tri-O-methylluteolin possesses anti-inflammatory effects in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 macrophages. 7,3',4'-Tri-O-methylluteolin inhibits the binding of MDM2 with p53 and induces apoptosis in MCF-7 breast cancer cells. 7,3',4'-Tri-O-methylluteolin also has antioxidant, antifungal and antitrypanosomal activities sup>[4]sup>[5].
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-
- HY-N16377
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|
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Others
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Cancer
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|
1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione (Compound 2) is an anthraquinone analog. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione can be isolated from soil Actinomycete Streptomyces. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione has potent cytotoxicity against HepG2, A875, BGC-823 and MCF-7 cells with IC50s of 2.29, 4.90, 0.99 and 1.66 μg/mL, respectively. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione has an antitumor activity .
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-
- HY-179485
-
|
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EGFR
VEGFR
COX
Caspase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
EGFR/VEGFR2-IN-10 is a selective EGFR, VEGFR2 and COX2 inhibitor with IC50s of 8.5, 68 and 158 nM, respectively. EGFR/VEGFR2-IN-10 induces G1-phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8, and elevates caspase-9 protein levels, confirming activation of the intrinsic apoptotic pathway. EGFR/VEGFR2-IN-10 demonstrates exceptional therapeutic potential by simultaneously inhibiting tumor proliferation, angiogenesis, and inflammation pathways while maintaining a favorable selectivity profile. EGFR/VEGFR2-IN-10 can be used as a research tool for cervical, liver, colon, and breast cancer studies .
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-
- HY-111640
-
|
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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.
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-
- HY-P11102
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Bacterial
Fungal
HIV
Parasite
|
Infection
Cancer
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|
Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.) .
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- HY-179433
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|
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PROTACs
Androgen Receptor
Estrogen Receptor/ERR
Src
|
Cancer
|
|
PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
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- HY-149633
-
|
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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 .
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-
- HY-169409
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property .
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-
- HY-161687
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|
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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 .
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-
- HY-170336
-
|
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PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-10 (Compound 160a) is an orally active degrader for ERα with DC50 of 0.37-1.1 nM, in cells MCF7, T47D and CAMA-1. PROTAC ERα Degrader-10 exhibits antitumor efficacy in mouse model . (Pink: ligand for target protein (HY-170339); Black: linker (HY-30105); Blue: ligand for E3 ligase Cereblon (HY-168055))
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-
- HY-103455
-
|
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Estrogen Receptor/ERR
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Others
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|
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.
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-
- HY-161995
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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 .
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-
- HY-N0534
-
|
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DNA/RNA Synthesis
Apoptosis
PI3K
Akt
Caspase
SOD
Interleukin Related
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
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|
Vitexin-2"-O-rhamnoside is an orally active flavonoid glycoside. Vitexin-2"-O-rhamnoside inhibits Apoptosis, increases the phosphorylation levels of PI3K/Akt, inhibits caspase-3, SOD activity, and promotes cytokine (IL-2, IL-6, and IL-12) secretion. Vitexin-2"-O-rhamnoside strongly inhibits DNA synthesis in MCF-7 cells with an IC50 of 17.5 μM. Vitexin-2"-O-rhamnoside enhances immune function and improves the absorption of active compounds. Vitexin-2"-O-rhamnoside has antioxidant activity. Vitexin-2"-O-rhamnoside is used in the study of cardiovascular disease and immune-related diseases .
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-
- HY-174403
-
|
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Bcl-2 Family
c-Myc
Apoptosis
Caspase
|
Cancer
|
|
c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
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-
- HY-155180
-
|
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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 .
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-
- HY-138074
-
|
5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
|
Parasite
|
Infection
|
|
Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
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-
- HY-110193
-
SPP-86
2 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.
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-
- HY-144666
-
|
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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 .
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-
- 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-178034
-
|
|
PROTACs
Oxysterol-binding Protein-related Protein (ORP)
|
Cancer
|
|
PROTAC OSBP Degrader-1 (Compound 5) is a Oxysterol-binding protein (OSBP) PROTAC degrader with a DC50 of 322 nM (24 h). PROTAC OSBP Degrader-1 can rapidly penetrate into cells and induce massive recruitment of OSBP at the Trans-Golgi network. PROTAC OSBP Degrader-1 has potent anticancer activity with potent cytotoxicity against U-87 MG, A549, MCF7, HeLa and MDA-MB-231 cells . Pink: OSBP ligand (HY-178035); Blue: CRBN ligase ligand (HY-10984); Black: linker
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-
- HY-172964
-
|
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PI3K
Akt
mTOR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
KIM-161 is a PIK3CA inhibitor. KIM-161 has significant antiproliferative activity with IC50 values of 1.428 and 1.562 µM against PI3KCA mutant breast cancer MCF7 and T47D cells, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway and inducing ROS production. KIM-161 can be used to study breast cancer and its PI3KCA mutant subtypes .
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-
- 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-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-180546
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-53 (compound 9) is a CDK2 inhibitor with anticancer activity. CDK2-IN-53 selectively inhibits the proliferation of HCT-116 and MCF-7cells with IC50 values of 13.89 and 7.65 μM, respectively, while showing lower cytotoxicity toward normal lung fibroblast (WI-38) cells (IC50 = 71.24 μM). CDK2-IN-53 can be used for cancer research, such as colon and breast cancer .
|
-
- 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-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
-
- HY-139090
-
|
28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin
|
Bacterial
HIV
Drug Derivative
|
Cancer
|
|
3-Oxobetulin acetate (28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin) is a derivative of betulin (HY-N0083), a cholesterol biosynthesis inhibitor. 3-Oxobetulin acetate inhibits the growth of P388 murine lymphocytic leukemia cells (EC50=0.12 μg/mL) and human MCF-7 breast cancer, SF-268 CNS cancer, H460 lung cancer, and KM20L2 colon cancer cells (GI50s=8, 10.6, 5.2, and 12.7 μg/mL), but not BxPC-3 pancreatic cancer cells or DU145 prostate cancer cells (GI50s=>10 μg/mL for both). 3-Oxobetulin acetate inhibits the replication of X4-tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50=13.4 μM). 3-Oxobetulin acetate is also effective against Listeria donovani amastigotes.
|
-
- HY-170932
-
|
|
EGFR
COX
Apoptosis
|
Cancer
|
|
EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR WT, EGFR T790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects .
|
-
- 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-W010713
-
|
Fimaporfin free base
|
Photosensitizer
|
Cancer
|
|
Meso-tetraphenylchlorin (TPCS2a) is a photosensitizer with poor water solubility, which limits its use in the blood circulation. However, TPCS2a@NPs nanoparticles can be prepared based on polylactic-co-polyethylene glycol acid (PLGA) polymer core loaded with TPCS2. Such nanoparticles can be coated with mesenchymal stem cell-derived plasma membranes (mMSCs) to form mMSC-TPCS2a@NPs, which prolongs blood circulation time and improves tumor targeting ability. Compared with uncoated TPCS2a@NPs, mMSC-TPCS2a@NPs can reduce macrophage uptake by 54% to 70% under different conditions. Both nanoparticle forms are effectively accumulated in MCF7 and MDA-MB-231 breast cancer cells, while uptake in normal breast epithelial cells MCF10A is significantly lower .
|
-
- HY-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-178353
-
|
|
EGFR
TNF Receptor
Interleukin Related
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
EGFR/Cytokine-IN-1 is an EGFR (IC50 = 0.03 μM) and Cytokine inhibitor (TNF-α, IC50 = 3.1 μM; IL-6, IC50 = 1.6 μM). EGFR/Cytokine-IN-1 shows potent anticancer activity on A549 and MCF7, respectively. EGFR/Cytokine-IN-1 significantly reduces IL-6 and TNF-α levels in A549 cells, and also shows promising ADMET profiles. EGFR/Cytokine-IN-1 can induce apoptosis in a dose-dependent manner. compound 5h can be used for the study of breast cancer and lung cancer .
|
-
- HY-N0534R
-
|
|
Reference Standards
DNA/RNA Synthesis
Apoptosis
PI3K
Akt
Caspase
SOD
Interleukin Related
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Vitexin-2"-O-rhamnoside (Standard) is the analytical standard of Vitexin-2"-O-rhamnoside (HY-N0534). This product is intended for research and analytical applications. Vitexin-2"-O-rhamnoside is an orally active flavonoid glycoside. Vitexin-2"-O-rhamnoside inhibits Apoptosis, increases the phosphorylation levels of PI3K/Akt, inhibits caspase-3, SOD activity, and promotes cytokine (IL-2, IL-6, and IL-12) secretion. Vitexin-2"-O-rhamnoside strongly inhibits DNA synthesis in MCF-7 cells with an IC50 of 17.5 μM. Vitexin-2"-O-rhamnoside enhances immune function and improves the absorption of active compounds. Vitexin-2"-O-rhamnoside has antioxidant activity. Vitexin-2"-O-rhamnoside is used in the study of cardiovascular disease and immune-related diseases .
|
-
- 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-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-176719
-
|
|
Aldose Reductase
STAT
Amino acid Transporter
Apoptosis
|
Cancer
|
|
AKR1B1/STAT3/SLC7A11-regulator-1 (5a) is an AKR1B1/STAT3/SLC7A11 regulator that reverses DOX resistance in MCF-7/ADR cells by enhancing ferroptosis activity. AKR1B1/STAT3/SLC7A11-regulator-1 can be used in breast cancer research .
|
-
- 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-172889
-
|
|
PI3K
HDAC
Apoptosis
mTOR
Akt
|
Cancer
|
|
PI3K/HDAC-IN-4 (Compound 31f) is a PI3K/HDAC dual inhibitor (IC50: 0.2μM). PI3K/HDAC-IN-4 shows high selectivity for HDAC1-3 (IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively). PI3K/HDAC-IN-4 is a potent PIK3 inhibitor with IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. PI3K/HDAC-IN-4 significantly induces tumor cell apoptosis by simultaneously inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. PI3K/HDAC-IN-4 exhibits potent antiproliferative activity in a variety of tumor cell lines (e.g., MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively). PI3K/HDAC-IN-4 can be used in the study of lymphoma and leukemia .
|
-
- HY-178351
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer .
|
-
- HY-N12606
-
|
|
Fungal
|
Infection
|
|
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
|
-
- HY-173044
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM .
|
-
- HY-173132
-
|
|
Aldose Reductase
|
Cancer
|
|
AKR1Cs-IN-1 (Compound 29) is a potent and broad-spectrum inhibitor targeting members of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). By simultaneously occupying the SP2 and SP3 pockets, it effectively inhibits multiple isoforms and disrupts metabolic pathways associated with drug resistance. In enzymatic activity assays, AKR1Cs-IN-1 exhibited significant inhibitory potency, with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM against AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. In the doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, AKR1Cs-IN-1 showed remarkable resensitization effects and significantly enhanced the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on overcoming drug resistance in breast cancer .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-B0812
-
|
SSA dihydrate
|
Biochemical Assay Reagents
|
|
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
-
|
|
Biochemical Assay Reagents
|
|
β-D-Fructose is a monosaccharide. Derivatives synthesized using β-D-Fructose as the sugar backbone exhibit potent and selective antiproliferative activity against breast cancer MCF-7 cells .
|
-
- HY-113319R
-
|
|
Biochemical Assay Reagents
|
|
β-D-Fructose, (Standard) is the analytical standard of β-D-Fructose (HY-113319R). This product is intended for research and analytical applications. β-D-Fructose is a monosaccharide. Derivatives synthesized using β-D-Fructose as the sugar backbone exhibit potent and selective antiproliferative activity against breast cancer MCF-7 cells .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W016887
-
|
H-Gly-Pro-OH; Gly-Pro
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
Cancer
|
|
Glycyl-L-proline (H-Gly-Pro-OH) is a dipeptide. Glycyl-L-proline can induce MCF-7 cells apoptosis. Glycyl-L-proline can enhance the inhibitory effect of the PRODH/POX knockout on collagen and DNA biosynthesis. Glycyl-L-proline can inhibit Gly-Sar and L-proline transport. Glycyl-L-proline can be used for the researches of cancer and metabolic disease, such as breast cancer .
|
-
- 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-P10790
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
|
-
- HY-P10785
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Iturin A-2 is a cyclic lipopeptide discovered in B. subtilis and exhibits inhibitory activity against the plant pathogenic fungus P. expansum (MIC = 8 µg/disk). Iturin A-2 is cytotoxic to MCF-7 and BT474 breast cancer cells, as well as HeLa cervical cancer cells, with IC50 values of 66.81, 95.04, and 77.5 µg/mL, respectively. In greenhouse studies, Iturin A-2 at concentrations of 100 and 300 mg/kg Iturin A-2 reduces the lesion area of southern corn leaf blight caused by B. maydis, and in field studies, concentrations of 300 and 500 mg/kg Iturin A-2 reduce the incidence of the disease. Iturin A-2 (12.5 µg/mL) inhibits cell division, but not nuclear division, in isolated fertilized starfish eggs .
|
-
- HY-P11102
-
|
|
Bacterial
Fungal
HIV
Parasite
|
Infection
Cancer
|
|
Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.) .
|
-
- 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-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-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-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-119358
-
-
-
- HY-W016887
-
-
-
- HY-N1366
-
-
-
- HY-113319
-
-
-
- HY-Y0598
-
-
-
- HY-N2198
-
-
-
- HY-N5052
-
-
-
- HY-N2887
-
-
-
- HY-N0435
-
-
-
- HY-114803
-
-
-
- HY-113062
-
-
-
- HY-N6990
-
-
-
- HY-149132
-
|
DDA
|
Triterpenes
Terpenoids
Endogenous metabolite
Source Classification
|
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-N4010
-
-
-
- HY-N7654
-
-
-
- HY-W587738
-
-
-
- HY-119358R
-
-
-
- HY-N8679
-
-
-
- HY-N10846
-
-
-
- HY-N3316
-
-
-
- HY-N10871
-
-
-
- HY-N11928
-
-
-
- HY-N13772
-
|
(+)-Dihydroisorhamnetin
|
Flavanonols
Flavonoids
Pulicaria jaubertii E.Gamal-Eldin
Asteraceae
Plants
Source Classification
|
Apoptosis
|
|
3'-O-Methyltaxifolin ((+)-Dihydroisorhamnetin) is a dihydroflavanol found in Pulicaria jaubertii. A mixture of these alcohol compounds including 3'-O-Methyltaxifolin found in Pulicaria jaubertii exhibits antitumor activity with IC50 values of 19.1 μg, 20.0 μg, and 24.1 μg against prostate cancer (PC-3), breast cancer (MCF-7), and hepatocellular carcinoma (HepG-2) cell lines, respectively. Furthermore, 3'-O-Methyltaxifolin can induce cell apoptosis, making it a promising candidate for anticancer research. .
|
-
-
- HY-Z12208
-
|
|
Structural Classification
Microorganisms
Terpenoids
Diterpenoids
Source Classification
|
Drug Derivative
|
|
N1-Phenylsuberamide is an organic amide compound, and its structure can be regarded as a simplified analogue of Vorinostat (HY-10221). N1-Phenylsuberamide exhibits moderate anti-proliferative activity against MDA-MB-231 and MCF-7 cells. N1-Phenylsuberamide does not show significant HDAC inhibitory activity and can only weakly induce the expression of the p21 gene. N1-Phenylsuberamide has extremely low relative binding affinity of estrogen receptor. N1-Phenylsuberamide can be used as a control compound .
|
-
-
- HY-N5103
-
-
-
- HY-W747516
-
-
-
- HY-N2298
-
-
-
- HY-N10777
-
-
-
- HY-N1833
-
-
-
- HY-N10023
-
-
-
- HY-N15577
-
|
|
Flavonols
Platanus acerifolia Aiton) Willd.
Flavonoids
Platanaceae
Plants
Source Classification
|
Drug Derivative
|
|
Antiproliferative agent-69 (Compound 1) is a prenylated kaempferol derivative found in the fresh bud’s fur of Platanus acerifolia. Antiproliferative agent-69 shows significant antiproliferative effects against human breast cancer cells (MCF-7) and human hepatocellular carcinoma cells (Hep-G2) with IC50 values of 38.2 μM and 39.5 μM, respectively. Antiproliferative agent-69 is promising for research of breast cancer and liver cancer .
|
-
-
- HY-N11973
-
-
-
- HY-N3042
-
-
-
- HY-N14603
-
-
-
- HY-N4010R
-
-
-
- HY-N10305
-
-
-
- HY-N2863
-
-
-
- HY-N7464
-
-
-
- HY-N9391
-
-
-
- HY-N8859
-
-
-
- HY-N3443
-
-
-
- HY-113796
-
-
-
- HY-N16642
-
-
-
- HY-N11438
-
-
-
- HY-N3261
-
-
-
- HY-N11919
-
-
-
- HY-N4227
-
-
-
- HY-N15584
-
-
-
- HY-N10959
-
-
-
- HY-N10351
-
-
- HY-N1252
-
-
- HY-126803
-
-
- HY-N6885
-
-
- HY-N3615
-
-
- HY-N16645
-
-
- HY-N12299
-
-
- HY-N14378
-
-
- HY-145379
-
-
- HY-117872
-
|
20-O-Acetylsartorypyrone D
|
Microorganisms
Terpenoids
Diterpenoids
Source Classification
|
Fungal
|
|
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-126618
-
-
- HY-N14255
-
-
- HY-N1107
-
|
NSC 119993; NSC 277290; Odorigeni
|
Apocynaceae
Cardiacglycosides
Plants
Steroids
Source Classification
|
Others
|
|
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-N13162
-
|
|
Triterpenes
Terpenoids
Cucurbitaceae
Plants
Hemsleya pengxianensis W. J. Chang
Source Classification
|
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-N1366R
-
|
Methylumbelliferone (Standard)
|
Structural Classification
other families
Coumarins
Phenylpropanoids
Plants
Source Classification
|
Reference Standards
Apoptosis
Bacterial
|
|
Herniarin (Standard) (Methylumbelliferone (Standard)) is the analytical standard of Herniarin (HY-N1366). This product is intended for research and analytical applications. Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer.
|
-
- HY-N3210
-
-
- HY-N2741
-
-
- HY-N12232
-
-
- HY-138210
-
|
|
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-N15652
-
-
- HY-N14280
-
-
- HY-113319R
-
-
- HY-N14056
-
|
|
Natural Products
Microorganisms
Source Classification
|
Bacterial
|
|
Chrolactomycin is found in the strain of Streptomyces sp. 569N-3. The IC50 of Chrolactomycin for ACHN, A431, McF-7 and T24 cells are 1.2 μM, 1.6 μM, 0.69 μM and 0.45 μM, respectively. Chrolactomycin has only anti-Gram-positive bacteria activity with the MIC of 5.2-10.4 μg/mL .
|
-
- HY-N14892
-
-
- HY-119539
-
-
- HY-N8508
-
|
|
Natural Products
Microorganisms
Source Classification
|
Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
|
|
Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC50s of 95, 70, 60, and 25 µM, respectively .
|
-
- HY-N13115A
-
|
(E)-21-Angeloyl-protoaescigenin
|
Aesculus chinensis Bunge
Triterpenes
Terpenoids
Hippocastanaceae
Plants
Source Classification
|
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
Terpenoids
Hippocastanaceae
Plants
Source Classification
|
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 .
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- HY-N12208
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-
- HY-N12209
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-
- HY-N15392
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-
- HY-N12230
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Microorganisms
Ketones, Aldehydes, Acids
Source Classification
|
Bacterial
Parasite
Fungal
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Penicolinate B is a picolinic acid derivative that can be isolated from Penicillium sp. Penicolinate B exhibits antimalarial activity (IC50: 1.40 μg/mL), antitubercular activity (MIC: 25.0 μg/mL), activity against Bacillus cereus (IC50: 25.0 μg/mL), and activity against Candida albicans (IC50: 1.45 μg/mL). Penicolinate B also has certain cytotoxicity against cancer cells such as MCF-7, KB, and NCI-H187. Penicolinate B can be used in research on malaria, tuberculosis, bacterial/fungal infections and tumors .
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-
- HY-129672
-
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25-Dihydrostichorrenoside E
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Other Terpenoids
Animals
Terpenoids
Source Classification
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Drug Derivative
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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 .
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- HY-138098
-
-
- HY-N9174
-
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Flavonoids
Flavones
Plants
Moraceae
Broussonetia papyrifera (Linnaeus) L'Heritier ex Ventenat
Source Classification
|
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-125620
-
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Quinones
Microorganisms
Anthraquinones
Source Classification
|
Antibiotic
Bacterial
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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 .
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- HY-135453
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-
- HY-N10778
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|
Triterpenes
Terpenoids
Cucurbitaceae
Plants
Source Classification
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-N14604
-
-
- HY-N15306
-
|
|
Microorganisms
Ketones, Aldehydes, Acids
Phenols
Source Classification
|
Apoptosis
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Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
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- HY-N16759
-
-
- HY-N3318
-
-
- HY-N7302
-
-
- HY-N14893
-
-
- HY-N10949
-
-
- HY-N13709
-
-
- HY-N15479
-
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|
Microorganisms
Terpenoids
Sesquiterpenes
Source Classification
|
Bacterial
|
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Nanangenine F is a drimane sesquiterpenoid with weak antibacterial and anticancer activities. Nanangenine F inhibits Bacillus subtilis (ATCC 6633) with an IC50 of 78 µg/mL. Nanangenine F inhibits NS-1, DU-145, MCF-7 and human fibroblast NFF cells with IC50s of 49 µg/mL, 95 µg/mL, 49 µg/mL, and 84 µg/mL, respectively .
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-
- HY-N7340
-
-
- HY-Y0598R
-
-
- HY-N10621
-
|
|
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 .
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-
- HY-N9848
-
|
|
Triterpenes
Senegalia pennata (L.) Maslin
Terpenoids
Labiatae
Plants
Source Classification
|
Others
|
|
2α,3α,24-Trihydroxyursa-12,20(30)-dien-28-oic acid is a triterpenoid with anticancer effects. 2α,3α,24-Trihydroxyursa-12,20(30)-dien-28-oic acid inhibits HepG2, A549, MCF-7, SK-OV-3, and HeLa cells with IC50 values of 19.62 μM, 18.86 μM, 45.94 μM, 62.41 μM, and 28.74 μM, respectively .
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-
- HY-N8146
-
-
- HY-N12887
-
|
|
Natural Products
Marine natural products
Sponge
Source Classification
|
Mitochondrial Metabolism
|
|
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-N15636
-
-
- HY-N7012
-
|
5-Hydroxy-3',4',7-trimethoxyflavone
|
Monophenols
Flavonoids
Classification of Application Fields
Flavones
Labiatae
Phenols
Plants
Swartzia polyphylla DC.
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Lipoxygenase
TNF Receptor
Interleukin Related
COX
Fungal
Parasite
Apoptosis
|
|
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid with multiple biological activities. 7,3',4'-Tri-O-methylluteolin inhibits soybean lipoxygenase (LOX), with an IC50 value of 23.97 µg/mL. 7,3',4'-Tri-O-methylluteolin possesses anti-inflammatory effects in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 macrophages. 7,3',4'-Tri-O-methylluteolin inhibits the binding of MDM2 with p53 and induces apoptosis in MCF-7 breast cancer cells. 7,3',4'-Tri-O-methylluteolin also has antioxidant, antifungal and antitrypanosomal activities sup>[4]sup>[5].
|
-
- HY-N16377
-
|
|
Quinones
Microorganisms
Anthraquinones
Source Classification
|
Others
|
|
1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione (Compound 2) is an anthraquinone analog. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione can be isolated from soil Actinomycete Streptomyces. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione has potent cytotoxicity against HepG2, A875, BGC-823 and MCF-7 cells with IC50s of 2.29, 4.90, 0.99 and 1.66 μg/mL, respectively. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione has an antitumor activity .
|
-
- HY-N0534
-
-
- HY-N12135
-
|
|
Senegalia pennata (L.) Maslin
Terpenoids
Labiatae
Diterpenoids
Plants
Source Classification
|
Others
|
|
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-N0534R
-
|
|
Structural Classification
Flavonoids
other families
Flavones
Phenols
Polyphenols
Plants
Source Classification
|
Reference Standards
DNA/RNA Synthesis
Apoptosis
PI3K
Akt
Caspase
SOD
Interleukin Related
|
|
Vitexin-2"-O-rhamnoside (Standard) is the analytical standard of Vitexin-2"-O-rhamnoside (HY-N0534). This product is intended for research and analytical applications. Vitexin-2"-O-rhamnoside is an orally active flavonoid glycoside. Vitexin-2"-O-rhamnoside inhibits Apoptosis, increases the phosphorylation levels of PI3K/Akt, inhibits caspase-3, SOD activity, and promotes cytokine (IL-2, IL-6, and IL-12) secretion. Vitexin-2"-O-rhamnoside strongly inhibits DNA synthesis in MCF-7 cells with an IC50 of 17.5 μM. Vitexin-2"-O-rhamnoside enhances immune function and improves the absorption of active compounds. Vitexin-2"-O-rhamnoside has antioxidant activity. Vitexin-2"-O-rhamnoside is used in the study of cardiovascular disease and immune-related diseases .
|
-
- HY-N12606
-
|
|
Microorganisms
Saccharides
Monosaccharides
Source Classification
|
Fungal
|
|
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 .
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-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13636S
-
|
|
|
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 .
|
-
-
- HY-13636S1
-
|
|
|
Fulvestrant-d5 (ICI 182780-d5) is a isotope of Fulvestrant (HY-13636) . 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-50936S
-
|
|
|
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-N1366S
-
|
|
|
Herniarin-d3 is the deuterium labeled Herniarin (HY-N1366). Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer .
|
-
-
- HY-13762S
-
|
|
|
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 .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-B1029
-
Danazol
4 Publications Verification
|
|
Alkynes
|
|
Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
|
-
- HY-115997
-
|
|
|
PROTAC Synthesis
|
|
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-111640
-
|
|
|
Azide
|
|
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.
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-147081
-
AS 1411
2 Publications Verification
AGRO-100
|
|
Aptamers
|
|
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-147081A
-
|
AGRO-100 sodium
|
|
Aptamers
|
|
AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium 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 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-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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