Search Result
Results for "
MDA-MB-231 breast cancer cells
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-114979
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Antibiotic
Fungal
Apoptosis
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Infection
Cancer
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Pyoluteorin is an antibiotic that inhibits Oomycete fungi, including the plant pathogen Pythium ultimum, and suppresses plant diseases caused by this fungus . Pyoluteorin induces human triple-negative breast cancer MDA-MB-231 cells apoptosis in vitro. Pyoluteorin can be used for the research of human triple-negative breast cancer .
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- HY-110329
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Others
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Cancer
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ML179 (SR-1309) is a inverse LRH1/NR5A2 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
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- HY-163112
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Others
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Cancer
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Anticancer agent 179 (Compound 3) is a sambutoxin analogue. Anticancer agent 179 can impede migration of MDA-MB-231 breast cancer cells .
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- HY-175544
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Drug Derivative
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Cancer
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anti-TNBC agent-10 is an anti-TNBC agent. anti-TNBC agent-10 shows potent anti-TNBC activity against BT549 cells (IC50 = 0.018 μM) and maintains activity against MDA-MB-231 cells (IC50 = 4.16 μM). anti-TNBC agent-10 9 demonstrates significant anti-tumor efficacy in mice bearing subcutaneous MDA-MB-231 TNBC xenografts. anti-TNBC agent-10 can be used for the study of triple-negative breast cancer (TNBC) .
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- HY-148368
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Bcl-2 Family
Apoptosis
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Cancer
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CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .
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- HY-175173
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EGFR
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Cancer
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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 .
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- HY-175269
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DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Topoisomerase
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Cancer
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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 .
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- HY-170946
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STAT
Bcl-2 Family
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Cancer
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WR-S-462 is a STAT3 inhibitor. WR-S-462 effectively suppresses STAT3 phosphorylation and biological functions in vitro. WR-S-462 inhibits MDA-MB-231 cells with an IC50 of 0.03 μM. WR-S-462 displays a strong binding affinity towards the STAT3 protein with a Kd of 58 nM. WR-S-462 inhibits the nuclear translocation of p-STAT3, selectively inhibits the expression of p-STAT3 Tyr705 and downstream target genes regulated by STAT3 in MDA-MB-231 cells such as Cyclin D1, Bcl-2, and Bcl-xl. WR-S-462 inhibits TNBC (triple-negative breast cancer) growth and metastasis .
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- HY-119948
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Cyclin G-associated Kinase (GAK)
MDM-2/p53
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Cancer
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AKCI is a type of AURKC-IκBα interaction inhibitor, with an IC50 value of 24.9 μM. In MDA-MB-231 cells, AKCI can induce G2/M cell cycle arrest by regulating the p53/p21/CDC2/cyclin B1 pathway, inhibit cell migration and invasion, and reduce colony formation and tumor growth. AKCI can be used for research on breast cancer .
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- HY-146283
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Histone Demethylase
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Cancer
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LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively .
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- HY-146284
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Histone Demethylase
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Cancer
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LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively .
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- HY-146285
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Histone Demethylase
Histone Methyltransferase
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Cancer
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LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
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- HY-120275
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Bcl-2 Family
Apoptosis
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Cancer
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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 .
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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-170947
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STAT
Quinone Reductase
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Cancer
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Antitumor agent-195 (compound 16c) is a dual targeting agent of STAT3 and NQO1. Antitumor agent-195 significantly inhibits phosphorylation of STAT3 at Tyr705 at a concentration of 1 μM and effectively induce Apoptosis in MDAMB-231 and MDA-MB-468 breast cancer cells. Antitumor agent-195 as a NQO1 substrate strongly increases ROS generation and causes severe DNA damage in a dose-dependent manner. Antitumor agent-195 shows encouraging anti-tumor efficacy in the MDA-MB-231 xenograft model .
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- HY-156402
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Topoisomerase
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Cancer
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AuM1Gly is a topoisomerase I inhibitor. AuM1Gly affects the growth of MDA-MB-231 breast cancer cells, with IC50?values in the low nanomolar range .
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- HY-157151
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Histone Methyltransferase
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Cancer
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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 .
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- HY-101567
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Epigenetic Reader Domain
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Cancer
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BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively .
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- HY-175497
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ROR
Apoptosis
Bcl-2 Family
PARP
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Cancer
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ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM). ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC) .
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- HY-P10853
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Autophagy
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Cancer
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Bacilotetrin C analogue is cytotoxic to triple-negative breast cancer cell line MDA-MB-231 with an IC50 of 0.48 μM. Bacilotetrin C analogue can induce tumor cell autophagy and has anti-tumor activity .
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- HY-N13118
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Others
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Cancer
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Sinopodophylline B (compound 2) is a flavonoid glycoside compound that is cytotoxic to breast cancer cells. For example, the IC50 of Sinopodophylline B is 1.5 μM (T47D) and 44.2 μM (MDA-MB-231), respectively .
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- HY-139376
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FGFR
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Cancer
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FGFR1 inhibitor-2 is a FGFR1 inhibitor (IC50 is 4.55 μM in MDA-MB-231 cells). FGFR1 inhibitor-2 can be used for the research of metastatic triple-negative breast cancer .
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- HY-N0431
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MMP
ERK
JNK
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Cancer
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Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
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- HY-155309
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YAP
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Cancer
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LM-41 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2. LM-41 inhibits migration of human MDA-MB-231 breast cancer cells .
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- HY-162826
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Apoptosis
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Cancer
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Apoptosis inducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer (IC50: 12.8 μM) and can induce early apoptosis in breast cancer cells. Apoptosis inducer 27 can bind to DNA molecules, Bax and Bcl-2 proteins, and induce DNA damage .
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- HY-162012
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YAP
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Cancer
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HC-258 (compound 26) binds with the cysteine in TEAD’s PA pocket. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells .
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- HY-173146
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Apoptosis
EGFR
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Cancer
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EGFR-IN-153 (Compound 5l) is an EGFR inhibitor. EGFR-IN-153 can inhibit the proliferation (IC50: 0.73 μM) and induce apoptosis of MDA-MB-231 cell. EGFR-IN-153 can be used for the research of breast cancer .
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- HY-164064
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ClpP
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Cancer
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Anticancer agent 230 (example 65) is a caseinolytic protease P (ClpP) activator with anticancer activity. Anticancer agent 230 is able to induce the degradation of mitochondrial proteins in SUM159 and MDA-MB-231 triple-negative breast cancer cells in a time-dependent manner .
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- HY-163113
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Endogenous Metabolite
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Cancer
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Anticancer agent 180 (compound 4) is a secondary metabolite present in fungal strains and extracted through physical interaction with Streptomyces sp. Anticancer agent 180 has potential anti-tumor activity and can inhibit the migration of MDA-MB-231 breast cancer cells .
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- HY-156403
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Topoisomerase
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Cancer
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AuM1Phe, an N-Heterocyclic carbene (NHC) metal complexe, blocks the human topoisomerase I activity and actin polymerization reaction. AuM1Phe affects the growth of MDA-MB-231 breast cancer cells, with an IC50 value of 1.2 μM .
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- HY-161257
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Autophagy
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Cancer
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CDC20-IN-1 (Compound E1) is a specific inhibitor of CDC20 and can be used in triple-negative breast cancer research. CDC20-IN-1 can induce autophagy in cancer cells and inhibit MDA-MB-231 cell proliferation, with an IC50 value of 1.43 μM .
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- HY-153910
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Others
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Cancer
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AGPS-IN-1 (Compound 2i) is an effective AGPS binder. AGPS-IN-1 reduces ether lipids levels and cell migration rate. AGPS-IN-1 inhibits epithelial-mesenchymal transition (EMT) in prostate PC-3 and breast MDA-MB-231 cancer cells .
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- HY-116904
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Apoptosis
Akt
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Cancer
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Anticancer agent 253 (Compound 26) has anti-cancer activity against breast cancer cells, with IC50s of 6 μM (MCF-7), 10 μM (MDA-MB-231) and 6.4 μM (4T1 cells). Anticancer agent 253 arrests cell cycle and induces mitochondria-mediated apoptosis in cancer cells. Anticancer agent 253 inhibits Akt phosphorylation in human breast and prostate cancer .
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- HY-163760
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HuR
MMP
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Cancer
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ZM-32 is an inhibitor for human antigen R (HuR), that downregulates the expression of VEGF-A and MMP9, and thus inhibits breast cancer tumor angiogenesis. ZM-32 exhibits broad-spectrum anti-proliferative effects in a variety of cancer cell lines, and exhibits antitumor efficacy against MDA-MB-231 in mouse models .
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- HY-P10511
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Apoptosis
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Infection
Cancer
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Pantinin-3 is an antimicrobial peptide with antitumor activity found in the venom of the emperor scorpion (Pandinus imperator). Pantinin-3 shows selective toxicity against breast cancer cells (MDA-MB-231) and prostate cancer cells (DU-145). Pantinin-3 can induce apoptosis in tumor cells. Pantinin-3 can be used in cancer research .
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- HY-172888
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Endogenous Metabolite
FAK
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Cancer
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SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50: 3.59 μM). SPP-037 exhibits anti-MDA-MB-231 cell migration activity by inhibiting integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used in breast cancer research .
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- HY-162868
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c-Met/HGFR
HDAC
Apoptosis
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Cancer
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c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC50 value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G0/G1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines .
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- HY-N0431R
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Reference Standards
MMP
ERK
JNK
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Cancer
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Astragaloside IV (Standard) is the analytical standard of Astragaloside IV. This product is intended for research and analytical applications. Astragaloside IV, an active component isolated from Astragalus membranaceus, suppresses the activation of ERK1/2 and JNK, and downregulates matrix metalloproteases (MMP)-2, (MMP)-9 in MDA-MB-231 breast cancer cells.
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- HY-174160
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TAM Receptor
Apoptosis
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Cancer
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MerTK-IN-2 (compound 15f) is an orally active MerTK inhibitor with an IC50 of 37.5 nM. MerTK-IN-2 can induce apoptosis. MerTK-IN-2 has antitumor activity with IC50 values of 1.79, 18.32, and 2.18 μM for human ovarian cancer cells A2780, breast cancer cells MDA-MB-231, and colon cancer cells HCT116, respectively .
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- HY-144699
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Estrogen Receptor/ERR
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Cancer
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ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
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- HY-173296
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Lipase
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Cancer
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MAGL-IN-222 (Compound ZQ-7) is a covalent inhibitor targeting monoacylglycerol lipase (MAGL) with an IC50 of 42.31 μM. MAGL-IN-222 can reduce the breakdown of 2-arachidonoylglycerol (2-AG) and increase the intracellular 2-AG level, thereby inhibiting the proliferation and migration of MDA-MB-231 breast cancer cells. MAGL-IN-222 can be used in the research of breast cancer and other related diseases .
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- HY-161855
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VEGFR
Apoptosis
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Cancer
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VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer, with an IC50 value of 0.33 μM. VEGFR-2-IN-50 (Compound 10f) has growth inhibitory activity on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, which is expected to be used in the study of breast cancer diseases .
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- HY-126005
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Sodium Channel
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Cancer
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VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability .
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- HY-146516
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MDM-2/p53
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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Anticancer agent 42 (compound 10d) is an orally active anticancer agent, and shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 0.07 μM. Anticancer agent 42 can exert its anticancer activity by activating apoptotic pathway and p53 expression. Anticancer agent 42 can be used to study metastatic breast cancer .
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- HY-158439
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JAK
STAT
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Cancer
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anti-TNBC agent-7 (Compound 13c) possesses anticancer activity, serving as a molecular probe to recognize and regulate the signal transduction of the USP21/JAK2/STAT3 axis, exhibiting nanomolar-level cytotoxicity against MDA-MB-231 and HCC-1806 cancer cells, effectively combating triple-negative breast cancer (TNBC) .
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- HY-N15636
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(-)-Coccinine
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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-132305
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VEGFR
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Cancer
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VEGFR-3-IN-1 is a potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM. VEGFR-3-IN-1 significantly inhibits proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231, and MDA-MB-436 cells by inactivating the VEGFR3 signaling pathway, and also effectively inhibits breast cancer growth .
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- HY-171477
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-108447
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Ser/Thr Protease
SARS-CoV
PAI-1
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Infection
Cancer
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BC-11 hydrobromide is a selective TMPRSS2 inhibitor (TMPRSS2 is a key host cellular factor for viral entry and SARS-CoV-2 pathogenesis), and a selective urokinase (uPA) inhibitor (IC50=8.2 μM). BC-11 hydrobromide is cytotoxic to triple-negative MDA-MB231 breast cancer cells. BC-11 hydrobromide is used in research on viral infections and cancer .
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- HY-174992
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Apoptosis
Bcl-2 Family
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Cancer
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Apoptosis inducer 39 is an apoptosis inducer with IC50s of 4.53 and 15.42 μM against MDA-MB-231 and A549 cells. Apoptosis inducer 39 exerts in vitro anti-tumor activity by decreasing the expression of the anti-apoptotic protein Bcl-2 while increasing the expression of the pro-apoptotic protein Bax. Apoptosis inducer 39 can be used for the study of breast cancer and non-small lung cancer .
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- HY-156077
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Apoptosis
DNA/RNA Synthesis
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Cancer
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anti-TNBC agent-2 (3j) an anti-Triple negative breast cancer (TNBC) purine derivative. anti-TNBC agent-2 induces MDA-MB-231 cells apoptosis, and inhibits its migration and angiogenesis. anti-TNBC agent-2 inhibits tumor growth and metastasis and reduces the expression of Ki67 and CD31 protein in TNBC xenograft models. anti-TNBC agent-2 can be used for Triple negative breast cancer (TNBC) research .
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- HY-149354
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Aurora Kinase
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Cancer
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Aurora kinase-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora kinase-IN-4 inhibits cell proliferation in SJSA-1, MDA-MB-231, A54, HeLa cells with IC50s of 4.27, 1.54, 3.08, 6.99 μM. Aurora kinase-IN-4 can be used for research of triple negative breast cancer (TNBC) .
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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-176713
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PARP
CDK
Wnt
β-catenin
Apoptosis
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Cancer
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KWZY-11 (Compound 11) is a potent PARP/CDK6 dual inhibitor with IC50 values of 156.8, 197.3, and 13.3 nM for PARP1, PARP2, and CDK6, respectively. KWZY-11 inhibits tumor cell proliferation by regulating the Wnt/β-catenin signaling pathway. KWZY-11 induces excessive DNA damage and apoptosis in MDA-MB-231 breast cancer cells .
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- HY-115507
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AMPK
mTOR
ERK
Oxidative Phosphorylation
Reactive Oxygen Species (ROS)
Ras
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Cancer
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NMac1 is an orally active Nm23/NDPK activator. NMac1 directly binds to Nm23-H1 and activates the NDPK activity of recombinant Nm23-H1 with an EC50 of 10.7 uM. NMac1 induces AMPK activation and inhibits mTOR and ERK, leading to mitochondrial OXPHOS dysregulation and suppressing mitochondrial ROS production, which in turn induces mitochondrial dysfunction in MDA-MB-231 cells. NMac1 inhibits Complex I activity and suppresses changes in morphology and actin cytoskeleton organization following Rac1 activation in MDA-MB-231 cells. NMac1 inhibits tumor invasion, migration and metastasis. NMac1 is useful for studying metastatic tumors, such as breast cancer. NMac1 can be isolated from the ginger cassumunar Roxb .
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- HY-146452
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Apoptosis
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Cancer
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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) .
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- HY-119272
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EF24
2 Publications Verification
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ERK
Caspase
NF-κB
Apoptosis
p38 MAPK
Reactive Oxygen Species (ROS)
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Inflammation/Immunology
Cancer
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EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
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- HY-W072781
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Microtubule/Tubulin
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Cancer
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N-Deacetylthiocolchicine is a tubulin inhibitor with an IC50 value of 2.2 nM in MDR-negative MDA-MB 231 breast cancer cells. N-Deacetylthiocolchicine exerts antiproliferative activity by binding to tubulin to interfere with microtubule assembly, arresting cells in mitosis during the cell cycle. N-Deacetylthiocolchicine is promising for research of malignancies such as breast cancer .
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- HY-168106
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Eukaryotic Initiation Factor (eIF)
Apoptosis
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Cancer
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ZMF-24 is an anti-triple-negative breast cancer (TNBC) agent with IC50 values of 0.22 μM and 0.44 μM against TNBC proliferation in BT-549 cells and MDA-MB-231 cells, respectively. ZMF-24 inhibits Eukaryotic translation initiation factor 3 subunit D (EIF3D) that disrupts the energy supply of TNBC by inhibiting glycolysis and further induces profound TNBC apoptosis by stimulating persistent ER stress .
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- HY-172966
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EGFR
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Cancer
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EG31 is an EGFR inhibitor. EG31 effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells (GI50 values of MDA-MB-231 and Hs578T cells are 498.90 nM and 740.73 nM, respectively) and induces apoptosis by inhibiting the EGFR signaling pathway. EG31 still maintains antiproliferative activity against 5-fluorouracil (5-FU)-resistant TNBC cells (GI50: 519.5 nM). EG31 can be used to study TNBC resistance .
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- HY-150597
-
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HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-46 (compound 12c) is a potent HDAC inhibitor with an IC50 value of 0.21 μM and 0.021 μM for HDAC1 and HDAC6, respectively. HDAC-IN-46 upregulates p-p38, and downregulates Bcl-xL and cyclin D1 in MDA-MB-231 cells. HDAC-IN-46 induces significant G2 phase arrest and apoptosis. HDAC-IN-46 can be used for researching triple-negative breast cancer (TNBC) .
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-
- HY-161778
-
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HDAC
VD/VDR
|
Inflammation/Immunology
Cancer
|
|
ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization .
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-
- HY-172562
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
BTR2004 is a selective BET family (BRD2/3/4) protein PROTAC degrader. BTR2004 forms a ternary complex with BRD proteins and KLHL20, inducing ubiquitination and proteasomal degradation through the UPS pathway. BTR2004 is promising for research of PC3 prostate cancer and MDA-MB-231 breast cancer cell lines. Pink: (+)-JQ1-OH (HY-161125); Blue: BTR2000 (HY-172563); Black: Linker (HY-W015236) .
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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-155965
-
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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-174457
-
|
|
STAT
Carbonic Anhydrase
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
|
Cancer
|
|
STAT3/CAIX-IN-1 is a dual-target inhibitor of STAT3 (Kd: 60.03 μM) and CAIX (IC50: 80.45 nM). STAT3/CAIX-IN-1 induces ferroptosis by increases the levels of reactive oxygen species (ROS) and lipid peroxides. STAT3/CAIX-IN-1 inhibits cell migration, induces apoptosis, and causes cell cycle arrest in MDA-MB-231 cells. STAT3/CAIX-IN-1 can be used for the study of triple-negative breast cancer (TNBC) .
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-
- 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-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-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-175466
-
|
|
PARP
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
BER-IN-1 is a base excision repair (BER) inhibtor, targeting DNA abasic sites. BER-IN-1 cleaves abasic sites via β- and β,δ-elimination mechanisms, disrupts the base excision repair (BER) pathway and leads to DNA double-strand breaks (DSBs). BER-IN-1 can enhance the effectiveness of the PARP inhibitor Olaparib (HY-10162) in homologous recombination (HR)-proficient cancer cells (MDA-MB-231, HeLa, and SKOV3). BER-IN-1 induces an S-phase arrest and apoptosis companied with Olaparib. BER-IN-1 can be used for the research of cancer, such as breast, cervical and ovarian cancer .
|
-
- 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-168996
-
|
|
CDK
Apoptosis
|
Cancer
|
|
LA-CB1 is an Abemaciclib (HY-16297A) derivative that targets CDK4/6 and promotes its degradation via the ubiquitin-proteasome pathway, thereby disrupting the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis. LA-CB1 exhibits antiproliferative activity against MDA-MB-231 cells, with an IC50 of 0.27 µM, and effectively inhibits epithelial-mesenchymal transition (EMT), cell migration, invasion, and angiogenesis. In highly aggressive models such as triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth in a dose-dependent manner. LA-CB1 holds potential for research in the field of breast cancer .
|
-
- HY-168650
-
|
|
ROCK
HDAC
|
Inflammation/Immunology
Cancer
|
|
ROCK/HDAC-IN-1 (Compound 10h) is an orally active ROCK/HDAC inhibitor. ROCK/HDAC-IN-1 inhibits ROCK1/2 (IC50: 254.9 nM, 58.18 nM) and HDAC1/2/3/6/8 (IC50: 9.09, 8.03, 6.26, 0.41, 7.69 nM). ROCK/HDAC-IN-1 stimulates the activation of DAMPs, specifically Calreticulin (CRT) exposure and HMGB1 release, indicating that it is a potential ICD inducer.. ROCK/HDAC-IN-1 has antiproliferative activity against breast cancer cells (IC50: 0.37 μM for MDA-MB-231 cell), and inhibits tumor growth and activates T cells without apparent toxicity .
|
-
- HY-123715
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 255 is a monocarbonylated curcumin-1,2,3-oxazole conjugate with significant anticancer activity. The IC50 values of Anticancer agent 255 in prostate cancer cells PC-3 and DU-145 are 8.8μM and 9.5μM respectively. The IC50 values of Anticancer agent 255 against breast cancer cells MCF-7, MDA-MB-231 and 4T1 are 6μM, 10μM and 6.4μM, showing good anti-cancer activity Effect. Anticancer agent 255 can induce mitochondria-mediated apoptosis in cancer cells and prevent cell cycle progression. Anticancer agent 255 down-regulated the cell proliferation marker PCNA and inhibited the activation of cell survival proteins. Anticancer agent 255 up-regulated the pro-apoptotic protein Bax and down-regulated the anti-apoptotic protein Bcl-2 .
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-
- 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-112338
-
|
CPD188
|
STAT
Apoptosis
|
Cancer
|
|
C188 (CPD188) is a STAT3 inhibitor with anticancer effects. C188 inhibits STAT3 SH2/pY-peptide binding (IC50 of 20 µM against pY-peptide binding) and IL-6-mediated STAT3 phosphorylation. C188 is selective for STAT3 over STAT1. C188 inhibits nuclear-to-cytoplasmic translocation of Stat3. C188 shows highly active induces apoptosis in breast cancer cell lines with constitutive Stat3 activation (EC50s of 0.73 µM, 3.96 µM, and 7.01 µM in MDA-MB-468, MDA-MB-231, and MDA-MB-435 cultures, respectively) .
|
-
- HY-172891
-
|
|
CDK
HDAC
Apoptosis
|
Cancer
|
|
CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC50 s of 0.17 μM, 1.73 μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer .
|
-
- HY-176220
-
|
|
AUTACs
Autophagy
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
|
-
- HY-156096
-
|
|
HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
|
-
- 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-155180
-
|
|
PI3K
|
Cancer
|
|
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth .
|
-
- HY-159569
-
|
|
Transferrin Receptor
Ferroptosis
|
Cancer
|
|
TfR-1-IN-1 (compound C4) is an inhibitor of transferrin receptor 1 (TfR-1) with anticancer activity. TfR-1-IN-1 strongly increases intracellular iron (II) levels as a driving force for the induction of ferroptosis. TfR-1-IN-1 significantly reduces the metabolic activity of ovarian cancer (A2780cis), breast cancer (MDA-MB 231), and leukemia (HL-60) cell lines with IC50 values of 0.51, 0.46, and 0.48 μM, respectively .
|
-
- HY-P99813
-
|
HER3-DXd; U3-1402
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) consisting of a fully human anti-HER3 IgG1 monoclonal antibody Patritumab (HY-P99275) attached to a topoisomerase I inhibitor payload via a tetrapeptide-based cleavable linker. Patritumab deruxtecan shows anticancer activity .
|
-
- HY-149204
-
|
|
SDCBP
|
Cancer
|
|
SYNTi is a PDZ domain inhibitor targeting the syndecan/syntenin protein-protein Interaction. SYNTi exhibits an IC50 value of 400 nM and ligand efficiency (LE) value of 0.24. SYNTi can be used for breast cancer research .
|
-
- HY-159112
-
|
|
HDAC
|
Cancer
|
|
AW01178 is a Class I HDAC inhibitor. AW01178 induces the upregulation of E-cadherin at both mRNA and protein levels and inhibits the EMT of breast cancer cells .
|
-
- HY-149266
-
THK01
1 Publications Verification
|
ROCK
|
Cancer
|
|
THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer .
|
-
- HY-161083
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
PARP/EZH2-IN-2 (compound 12e) is a dual target PARP1 and EZH2 inhibitor, with IC50 values of 6.89 and 27.34 nM, respectively. PARP/EZH2-IN-2 shows anticancer activity, with no toxicity to normal cells. PARP/EZH2-IN-2 achieves synthetic lethality indirectly by inhibiting EZH2 to increase the sensitivity to PARP1, and induces cell death by regulating excessive autophagy .
|
-
- HY-152159
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo .
|
-
- HY-175319
-
|
|
CD73
|
Cancer
|
|
CD73-IN-21 (Compound 12f) is an Ecto-5′-nucleotidase (CD73) inhibitor with Kis of 20 and 302 nM for hCD73 and mCD73, respectively. CD73-IN-21 can be used for cancers like breast cancer research .
|
-
- HY-168704
-
|
|
YAP
TAM Receptor
Survivin
|
Cancer
|
|
YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that inhibits the interaction between YAP/TAZ and TEAD. YAP/TAZ-TEAD-IN-2 suppresses the transcriptional activity of TEAD, with an IC50 of 1.2 nM. YAP/TAZ-TEAD-IN-2 inhibits YAP/TAZ-TEAD target genes expression (Cyr61, CTGF, AXL and Survivin) and breast cancer cell proliferation .
|
-
- HY-175253
-
|
|
STAT
Apoptosis
|
Cancer
|
|
YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high
affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer .
|
-
- HY-144876
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
RIDR-PI-103 is a reactive oxygen species (ROS)-induced agent release proagent with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103). Doxorubicin and RIDR-PI-103 shows a synergistic effect in MDA-MB-361 and MDA-MB-231 cells to inhibit cancer cell proliferation .
|
-
- HY-108999A
-
|
BWA770U
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-108999
-
|
BWA770U mesylate
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (BWA770U) mesylate is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol mesylate shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-108999AR
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (Standard) is the analytical standard of Crisnatol. This product is intended for research and analytical applications. Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-159130
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
AO-022 is a potent TALDO1 allosteric inhibitor. AO-022 decreases the expression of vimentin and snail. AO-022 shows antiproliferative activity and antitumor activity. AO-022 has the potential for the research of breast cancer .
|
-
- HY-146684
-
|
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
HDAC-IN-36 (compound 23 g) is an orally active and potent HDAC (histone deacetylase) inhibitor, with an IC50 of 11.68 nM (HDAC6). HDAC-IN-36 promotes apoptosis, autophagy and suppresses migration. HDAC-IN-36 shows anti-tumor and anti-metastatic activity, and can be used for breast cancer research .
|
-
- HY-124632
-
WJ460
2 Publications Verification
|
Ferroptosis
Autophagy
|
Cancer
|
|
WJ460 is a potent inhibitor of myoferlin (MYOF) that interacts directly with MYOF. WJ460 inhibits the migration and growth, induces cell cycle arrest, mitochondrial autophagy, lipid peroxidation and ferroptosis in tumor cells. WJ460 has anti-tumor activity .
|
-
- HY-122181A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-146010
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 13 (compound 7) is a potent carbonic anhydrase (CA) inhibitor, which features 3-methylthiazolo[3,2-a]benzimidazole moiety (as a tail) connected to the zinc anchoring benzenesulfonamide moiety via ureido linker .
|
-
- HY-162037
-
|
|
CDK
FLT3
|
Cancer
|
|
CDDD11-8 is an orally active, potent and selective inhibitor of CDK9 and FLT3-ITD, with Ki values of 8 and 13 nM, respectively. CDDD11-8 reduces the proliferation of leukemia cell lines and was particularly effective against those harboring FLT3-ITD mutation .
|
-
- HY-149894
-
|
|
c-Myc
Cadherin
|
Cancer
|
|
MC-1-F2 is a FOXC2 inhibitor. MC-1-F2 shows a binding affinity (Kd) of 26 μM for full-length FOXC2. MC-1-F2 reduces epithelial-mesenchymal transition (EMT) markers in breast cancer cells, suppresses cancer stem cell (CSC) properties and reduces invasiveness in castration-resistant prostate cancer (CRPC) cells. MC-1-F2 can be used for the study of CRPC and breast cancer .
|
-
- HY-122181B
-
|
|
Histone Methyltransferase
|
Cancer
|
|
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells .
|
-
- HY-13502
-
Mitoxantrone
Maximum Cited Publications
39 Publications Verification
Mitozantrone; NSC 301739
|
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity . Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-13502AS
-
|
Mitozantrone-d8(dihydrochloride); NSC 301739-d8 dihydrochloride
|
Endogenous Metabolite
PKC
Apoptosis
Topoisomerase
Orthopoxvirus
Isotope-Labeled Compounds
|
Infection
Cancer
|
|
Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-13502AR
-
|
Mitozantrone dihydrochloride (Standard); NSC 301739 dihydrochloride (Standard)
|
Reference Standards
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone (dihydrochloride) (Standard) is the analytical standard of Mitoxantrone (dihydrochloride). This product is intended for research and analytical applications. Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-13502R
-
|
Mitozantrone (Standard); NSC 301739 (Standard)
|
Reference Standards
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone (Standard) is the analytical standard of Mitoxantrone. This product is intended for research and analytical applications. Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity . Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-13502A
-
|
Mitozantrone dihydrochloride; NSC 301739 dihydrochloride
|
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-149209
-
|
|
PROTACs
CDK
STAT
Early 2 Factor (E2F)
|
Cancer
|
|
LL-K8-22 is a potent, selective and durable PROTAC CDK8-cyclin C dual degrader, with DC50 values of 2.52 and 2.64 μM, respectively. LL-K8-22 also suppresses STAT1 Ser 727 phosphorylation. LL-K8-22 inhibits E2F- and MYC-driven carcinogenic transcriptional programs. LL-K8-22 can be used for triplenegative breast cancer (TNBC) research. (Pink: Ligand for target protein (HY-168683); Black: Linker (HY-Y0340); Blue: Ligand for E3 ligase (HY-N2427)) .
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- HY-144318
-
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Epigenetic Reader Domain
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Cancer
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CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth .
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- HY-N1506
-
|
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Epigenetic Reader Domain
p38 MAPK
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Cancer
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Ganodermanontriol, a sterol isolated from Ganoderma lucidum, induces anti-inflammatory activity in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells through the expression of HO-1. Ganodermanontriol exhibits hepatoprotective activity .
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- HY-N1506R
-
-
- HY-135276
-
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MicroRNA
Apoptosis
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Cancer
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Targaprimir-96 is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
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- HY-135276A
-
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MicroRNA
Apoptosis
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Cancer
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Targaprimir-96 TFA is a potent inhibitor of microRNA-96 (miR-96) processing. Targaprimir-96 TFA selectively modulates miR-96 production in cancer cells and triggers apoptosis. Targaprimir-96 TFA binds primary miR-96 (pri-miR-96) with low nanomolar affinity. Targaprimir-96 TFA directly engages pri-miR-96 in breast cancer cells and is ineffective on healthy breast cells .
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-
- HY-122181
-
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Histone Methyltransferase
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Cancer
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OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells .
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-
- HY-155249
-
|
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Microtubule/Tubulin
|
Cancer
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KGP591 is a tubulin polymerization inhibitor (IC50 0.57 µM). KGP591 induces significant G2/M stagnation, inhibits cell migration, disrupts microtubule structure and cell morphology in MDA-MB-231 cells. KGP591 shows antitumor activity in orthotopic model of kidney cancer (RENCA) .
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-
- HY-158108
-
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Autophagy
Ferroptosis
Reactive Oxygen Species (ROS)
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Cancer
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anti-TNBC agent-6 (compound pt-3) is a potent anti-TNBC agent. anti-TNBC agent-6 shows cytotoxic activity. anti-TNBC agent-6 induces autophagy and ferroptosis. anti-TNBC agent-6 enhances intracellular ROS accumulatio. anti-TNBC agent-6 shows anti tumor activity and has the potential for the research of breast cancer .
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-
- HY-108692
-
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Apoptosis
Endogenous Metabolite
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Cancer
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Enterolactone is a bioactive phenolic metabolite known as a mammalian lignan derived from dietary lignans. Enterolactone has estrogenic properties and anti-breast cancer activity . Enterolactone is a radiosensitizer for human breast cancer cell lines through impaired DNA repair and increased apoptosis .
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-
- HY-108692R
-
|
|
Reference Standards
Apoptosis
Endogenous Metabolite
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Cancer
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Enterolactone (Standard) is the analytical standard of Enterolactone. This product is intended for research and analytical applications. Enterolactone is a bioactive phenolic metabolite known as a mammalian lignan derived from dietary lignans. Enterolactone has estrogenic properties and anti-breast cancer activity . Enterolactone is a radiosensitizer for human breast cancer cell lines through impaired DNA repair and increased apoptosis .
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-
- HY-165245
-
|
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Transmembrane Glycoprotein
|
Cancer
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SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
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-
- HY-138071
-
|
8αTGH
|
STAT
Pyroptosis
Apoptosis
Reactive Oxygen Species (ROS)
c-Myc
Bcl-2 Family
TrxR
|
Cancer
|
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8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo .
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- HY-P11018
-
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Peptide-Drug Conjugates (PDCs)
Ephrin Receptor
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Cancer
|
|
(123B9)2-L2-PTX is an EphA2-agonistic peptide-drug conjugate (PDC). (123B9)2-L2-PTX consists of a dimeric 123B9 (HY-P10579) and Paclitaxel (HY-B0015). (123B9)2-L2-PTX significantly reduces circulating tumor cells and inhibits lung tumor metastasis in breast-cancer-Metastasis mice model. (123B9)2-L2-PTX can be used for cancers research, such as melanomas and ovarian and breast cancers .
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-
- HY-N10457
-
|
|
Bacterial
|
Infection
Cancer
|
|
Norstictic acid is a potent and selective allossteric transcriptional regulator. Norstictic acid shows anticancer activity. Norstictic acid shows antioxidant activity and antimicrobial activity .
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-
- HY-120234
-
|
Z-Leu-Leu-Nle-CHO; GSII
|
γ-secretase
Proteasome
Apoptosis
|
Cancer
|
|
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia .
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-
- HY-146740
-
|
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PD-1/PD-L1
|
Cancer
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PD-1/PD-L1-IN-27 is a potent PD-1/PD-L1 inhibitor with an IC50 value of 134 nM. PD-1/PD-L1-IN-27 shows antitumor effects with low T cell cytotoxicity. PD-1/PD-L1-IN-27 has the ability to activate CD8 + T cells and reduces T cell exhaustion .
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-
- HY-147373
-
|
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PROTACs
Ligands for E3 Ligase
|
Cancer
|
|
DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research .
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-
- HY-118762
-
|
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Cathepsin
|
Cancer
|
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KGP94 is a selective inhibitor of cathepsin L with an IC50 of 189 nM . KGP94 inhibits migration and invasion of metastatic carcinoma and shows low cytotoxicity (GI50=26.9 µM) against various human cell lines .
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-
- HY-146324
-
|
|
PROTACs
Apoptosis
CaMK
|
Cancer
|
|
PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting PROTAC small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-120234
-
|
Z-Leu-Leu-Nle-CHO; GSII
|
γ-secretase
Proteasome
Apoptosis
|
Cancer
|
|
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia .
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-
- HY-P10853
-
|
|
Autophagy
|
Cancer
|
|
Bacilotetrin C analogue is cytotoxic to triple-negative breast cancer cell line MDA-MB-231 with an IC50 of 0.48 μM. Bacilotetrin C analogue can induce tumor cell autophagy and has anti-tumor activity .
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-
- HY-P10511
-
|
|
Apoptosis
|
Infection
Cancer
|
|
Pantinin-3 is an antimicrobial peptide with antitumor activity found in the venom of the emperor scorpion (Pandinus imperator). Pantinin-3 shows selective toxicity against breast cancer cells (MDA-MB-231) and prostate cancer cells (DU-145). Pantinin-3 can induce apoptosis in tumor cells. Pantinin-3 can be used in cancer research .
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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 .
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-
- HY-P11018
-
|
|
Peptide-Drug Conjugates (PDCs)
Ephrin Receptor
|
Cancer
|
|
(123B9)2-L2-PTX is an EphA2-agonistic peptide-drug conjugate (PDC). (123B9)2-L2-PTX consists of a dimeric 123B9 (HY-P10579) and Paclitaxel (HY-B0015). (123B9)2-L2-PTX significantly reduces circulating tumor cells and inhibits lung tumor metastasis in breast-cancer-Metastasis mice model. (123B9)2-L2-PTX can be used for cancers research, such as melanomas and ovarian and breast cancers .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99813
-
|
HER3-DXd; U3-1402
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
Patritumab deruxtecan (HER3-DXd) is an antibody-drug conjugate (ADC) consisting of a fully human anti-HER3 IgG1 monoclonal antibody Patritumab (HY-P99275) attached to a topoisomerase I inhibitor payload via a tetrapeptide-based cleavable linker. Patritumab deruxtecan shows anticancer activity .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13502AS
-
|
|
|
Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-157411
-
|
|
|
Alkynes
|
|
anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
|
-
- HY-159112
-
|
|
|
Azide
|
|
AW01178 is a Class I HDAC inhibitor. AW01178 induces the upregulation of E-cadherin at both mRNA and protein levels and inhibits the EMT of breast cancer cells .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-160066
-
|
|
|
Aptamers
|
|
SYL3C aptamer sodium is a DNA aptamer that targets the epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets multiple human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III is 38 nM and 67 nM, respectively. SYL3C aptamer sodium provides stability, high binding affinity, and selectivity for targeted cancer therapy, cancer cell imaging, and circulating tumor cell detection .
|
-
- HY-160050
-
|
|
|
Aptamers
|
|
CD63-1 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 38.71 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
|
-
- HY-160051
-
|
|
|
Aptamers
|
|
CD63-2 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 78.43 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
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