Search Result
Results for "
MDA-MB-231
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-156026
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FAK
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Cancer
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FAK-IN-11 (Compound 4l) is a FAK inhibitor. FAK-IN-11 binds to the ATP binding pocket of FAK, and inhibits phosphorylation of FAK protein. FAK-IN-11 shows cytotoxic activity against the MDA-MB-231 cells with an IC50 of 13.73? μM. FAK-IN-11 induces non-apoptotic cell death in MDA-MB-231 cells .
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- HY-146511
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Others
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Cancer
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Anticancer agent 41 is a potent anticancer agent, shows a potent antitumor activity against MDA-MB-231 cell with an IC50 of 3.99 μM[1].
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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-146037
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Apoptosis
Aurora Kinase
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Cancer
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Aurora A inhibitor 2 (Compound 16h) is a potent Aurora A kinase inhibitor with an IC50 of 21.94 nM. Aurora A inhibitor 2 induces caspase-dependent apoptosis in MDA-MB-231 cells .
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- HY-146783
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PAK
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Cancer
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ZINC194100678 is a potent PAK1 inhibitor with an IC50 value of 8.37 μM. ZINC194100678 can inhibit MDA-MB-231 cell proliferation. ZINC194100678 can be used for researching anticancer .
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- HY-153272
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Biochemical Assay Reagents
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Cancer
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Antitumor agent-93 (compound 7D) is an anticancer agent that can effectively inhibit the growth of several tumor cell lines, such as MDA-MB-231 and HCT-116 cell lines .
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- HY-144638
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Apoptosis
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Cancer
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JMX0293 is an O-alkylamino-tethered salicylamide derivative compound. JMX0293 maintains good potency against MDA-MB-231 cell line (IC50 = 3.38 μM) while exhibiting very low toxicity against human non-tumorigenic breast epithelial cell line MCF-10A (IC50> 60 μM). JMX0293 inhibits STAT3 phosphorylation and contribute to apoptosis in TNBC MDA-MB-231 cells. JMX0293 significantly suppresses MDA-MB-231 xenograft tumor growth in vivo without significant toxicity .
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- HY-161096
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ROR
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Cancer
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Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
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- HY-146203
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FAK
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Cancer
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Compound 26F not only optimized the effective inhibitory enzyme (ic50= 28.2 nm), but also showed relatively less cytotoxicity (ic50= 3.32 μ M) And induced MDA-MB-231 cell apoptosis in a dose-dependent manner, effectively blocking MDA-MB-231 cells in g0/g1 phase.
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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-162034
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FAK
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Cancer
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FAK-IN-17 is a focal adhesion kinase (FAK) inhibitor. FAK-IN-17 possesses anticancer activity against A549 and MDA-MB-231 cell lines with IC50 values of 130 nM and 94 nM .
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- HY-145652
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AMP-945
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FAK
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Cancer
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Narmafotinib (AMP-945) is an inhibitor of the enzyme focal adhesion kinase (FAK, KD=0.21 nM). Narmafotinib inhibits autophosphorylation of 397Y-FAK in MDA-MB-231 cells with an IC50=7 nM and exhibits low general cellular toxicity (IC50=2.7 μM, MDA-MB-231 cells) .
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- HY-149033
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Others
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Cancer
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Kobusine derivative-2, a kobusine derivative, has antiproliferative activity against cancer cells. Kobusine derivative-2 can induce the arrest of MDA-MB-231 cells in the sub-G1 phase. Anticancer activity .
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- HY-N1231
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Kushenol F
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Apoptosis
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Cancer
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Sophoraflavanone G (Kushenol F) is iaolated from Sophora flavescens and shows anti-tumor and anti-inflammatory properties. Sophoraflavanone G (Kushenol F) induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways .
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- HY-156097
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Others
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Cancer
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Anticancer agent 158 (compound 7c) is a potent anticancer agent. The IC50s for inhibiting HepG-2, MDA-MB-231, and HCT-116 cell lines are 7.93 μM, 9.28 μM, 13.28 μM, and 181.89 μM, respectively .
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- HY-W369099
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STAT
Apoptosis
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Cancer
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HJC0152 (free base) is an orally active and potent inhibitor of STAT3. HJC0152 (free base) inhibits cell cycle progression and induces apoptosis. HJC0152 (free base) significantly suppresses MDA-MB-231 xenograft tumor growth in mice .
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- HY-143468
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Apoptosis
MEK
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Cancer
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MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells .
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- HY-163369
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HDAC
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Cancer
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HDAC6-IN-35 (compound C4 (ZINC000077541942)) is a potent and BBB-penetrated HDAC6 inhibitor with the IC50 of 4.7 μM. HDAC6-IN-35 shows cell toxicity against MDA-MB-231 with EC50 of 40.6 μM .
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- HY-156273
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Apoptosis
HDAC
Epigenetic Reader Domain
JAK
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Cancer
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HDAC/JAK/BRD4-IN-1(compound 25ap) is a potent HDAC/JAK/BRD4 triple inhibitor. HDAC/JAK/BRD4-IN-1 inhibit cell growth and induces apoptosis in MDA-MB-231 cells, and shows anticancer activity in vivo .
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- HY-157797
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Others
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Cancer
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SN-38-CM2 is a split esterase, and shows >95% conversion to SN-38 within 5 min in vitro. SN-38-CM2 induces protein-protein interactions (PPI)-dependent esterase to mediate cell death in MDA-MB-231 cells .
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- HY-143903
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PIN1
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Cancer
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ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells .
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- HY-155969
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EGFR
Apoptosis
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Cancer
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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 .
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- HY-155146
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Necroptosis
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Cancer
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Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .
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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-139109
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ADS 780WS
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Fluorescent Dye
Apoptosis
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Others
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IR-783 (ADS 780WS) is a near-infrared (NIR) heptamethine cyanine fluorescent probe. IR-783 significantly inhibits tumour growth and induces apoptosis in MDA-MB-231 xenograft model. IR-783 can be used to study breast cancer .
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- HY-N7507
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Others
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Cancer
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Sempervirine is an indole alkaloid isolated from Gelsemium sempervirens with anti-tumor activities. Sempervirine is against sempervirine-sensitive tumor cells with EC50 values of 2.7 μM, 1.77 μM, and 1.96 μM for Raji, MDA-MB-231 and HeLa cells, respectively .
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- HY-15518
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IAP
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Cancer
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LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
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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-162352
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Epigenetic Reader Domain
Apoptosis
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Cancer
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SDU-071 is a potent and orally active inhibitor of BRD4-p53 inhibitor. SDU-071 inhibits MDA-MB-231 cells proliferation with an IC50 of 10.5 μM. SDU-071 induces cell cycle arrest and apoptosis .
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- HY-N12607
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Others
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Cancer
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Garcilatelic acid (Compound 5) is a compound that can be isolated from Garcinia lateriflora. Garcilatelic acid has antiproliferative activity against tumor cell lines (A549, MDA-MB-231, MCF-7, KB and KB-VIN), with IC50 values of 0.5-1.3 μM .
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- HY-155359
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-55 is a potent inhibitor of Tubulin Polymerization. Tubulin polymerization-IN-55 has antiproliferative activity against A549, K562, HepG2, MDA-MB-231 and HFL-1 with IC50 s of 8, 3, 9, 24 and 62 nM, 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-15985
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Akt
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Metabolic Disease
Inflammation/Immunology
Cancer
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CTX-0294885 is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
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- HY-15985A
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Akt
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Metabolic Disease
Inflammation/Immunology
Cancer
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CTX-0294885 hydrochloride is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 hydrochloride is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
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- HY-112842
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MBQ-167
4 Publications Verification
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Ras
CDK
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Cancer
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MBQ-167 is a dual Rac/Cdc42 inhibitor, with IC50s of 103 nM for Rac 1/2/3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively.
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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-110329
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Others
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Cancer
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ML179 (SR-1309) is a inverse LRH1 (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-155127
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Others
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Cancer
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Antiproliferative agent-33 (Compound 2g) is an anti-proliferative, antifungal, and antibacterial agent. Antiproliferative agent-33 inhibits MDA-MB-231 cell proliferation (IC50: 16.38 μM). Antiproliferative agent-33 inhibits gram-negative bacteria growth, and inhibits S. faecalis with an MIC value of 8 μg/mL .
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- HY-16191
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Microtubule/Tubulin
Apoptosis
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Cancer
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ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.
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- HY-108317
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Others
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Cancer
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ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
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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-138210
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Fungal
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Infection
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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 .
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- HY-149714
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ICMT
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Cancer
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J6-3 is an inhibitor of ICMT with an IC50 of 0.6 μM and has anticancer activity. J6-3 inhibits MDA-MB231 cells with an IC50 of 3.4 μM .
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- HY-146324
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PROTACs
CaMK
Apoptosis
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Cancer
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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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- 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-13808
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Histone Methyltransferase
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Cancer
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UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM .
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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-155249
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Microtubule/Tubulin
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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-155039
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Others
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Cancer
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Antitumor agent-105 (Compound 37) is an antitumor agent. Antitumor agent-105 has antitumor activity against A549, H1299, H460, HCT116, MDA-MB-231 cells, with IC50 values of 6.7, 8.3, 4.3, 4.4, 6.7 μM respectively .
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- HY-N2741
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Bcl-2 Family
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Cancer
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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 .
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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-N3057
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Others
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Cancer
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Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
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- HY-139665
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Monocarboxylate Transporter
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Cardiovascular Disease
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VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism .
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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-115903A
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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HIF-1α-IN-2 hydrochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride suppresses HIF-1α expression by blocking transcription and protein translation .
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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-160066
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Others
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Cancer
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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 .
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- HY-129163
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10-Acetylphenoxazine
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Pim
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Cancer
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HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research .
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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-129578
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- HY-146516
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MDM-2/p53
Apoptosis
Reactive Oxygen Species
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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-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-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-115903
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation .
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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-N0448
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Others
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Inflammation/Immunology
Cancer
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10-Gingerol is a major pungent constituent in the ginger oleoresin from fresh rhizome, with anti-inflammatory, antioxidant and anti-proliferative activities. 10-Gingerol inhibits the proliferation of MDA-MB-231 tumor cell line with an IC50 of 12.1 μM .
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- HY-163113
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Others
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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-161372
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PARP
c-Met/HGFR
Apoptosis
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Cancer
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PARP1/c-Met-IN-1 (Compound 16) is a selective dual inhibitor for PARP1 and c-Met, with IC50s of 3.3 and 32.2 nM, respectively. PARP1/c-Met-IN-1 induces cell apoptosis and cell cycle arrest in G2/M phase in MDA-MB-231 cells. PARP1/c-Met-IN-1 exhibits antitumor activity in mice .
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- HY-146786
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PAK
Apoptosis
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Cancer
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ZMF-10 is a highly potent PAK1 inhibitor, with IC50s of 174 nM, 1.038 μM and 1.372 μM for PAK1, PAK2 and PAK3, respectively. ZMF-10 can inhibit PAK1 activity to affect PAK1-regulated apoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer .
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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-146103
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Apoptosis
Reactive Oxygen Species
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Cancer
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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 .
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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-148368
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Bcl-2 Family
Apoptosis
|
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-156378
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Aurora Kinase
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Cancer
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|
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 .
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-
- HY-149715
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ICMT
|
Cancer
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|
R1-11 is an indole ICMT inhibitor with an IC50 of 0.6 μM and has anticancer activity. R1-11 inhibits MDA-MB231 and PC3 cells with IC50s of 2.2 μM and 2.0 μM, respectively .
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-
- HY-149354
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Aurora Kinase
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Cancer
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|
Aurora Kinases-IN-4 (Compound 11c) is a covalent and ATP competitive aurora kinase A inhibitor (IC50: 1.7 nM). Aurora Kinases-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 Kinases-IN-4 can be used for research of triple negative breast cancer (TNBC) .
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-
- HY-110243
-
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Carbonic Anhydrase
|
Cancer
|
|
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth .
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-
- HY-124611
-
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HSP
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Cancer
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|
JG-231 is an analogue of JG-98 with anticancer effects. JG-231 inhibits the interaction of Hsp70-BAG3. JG-231 inhibits MDA-MB-231 heterograft tumor models of triple negative breast cancer (TNBC) .
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-
- HY-146285
-
|
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Histone Demethylase
Histone Methyltransferase
|
Cancer
|
|
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-N10965
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Others
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Cancer
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|
Gambogic acid B is an active compound. Gambogic acid B can be isolated from the resin of Garcinia hanburyi.. Gambogic acid B has cytotoxicity against A549, HCT116 and MDA‑MB‑231 cells with IC50 values of 1.60 μM, 6.88 μM and 0.87 μM, respectively .
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-
- HY-W667666
-
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Others
|
Others
|
|
Anthragallol 1,2-dimethyl ether (compound 11) can be isolated from O. umbellata. Anthragallol 1,2-dimethyl ether has cytotoxicity, with IC50 values of 5.9 and 8.8 μg/ml against A549 cells and MDA-MB-231 cells, respectively .
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-
- HY-149729
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|
|
ICMT
|
Cancer
|
|
ICMT-IN-53 (compound 12) is an ICMT inhibitor (IC50=0.96 μM) with PAMPA permeability and antiproliferative activity. ICMT-IN-53 inhibits the proliferation of MDA-MB-231 and PC3 with IC50s of 5.14 μM and 5.88 μM, respectively .
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-
- HY-114324
-
|
|
PROTACs
PARP
|
Cancer
|
|
PROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
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-
- HY-150597
-
|
|
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-155113
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively .
|
-
- HY-109523
-
|
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cardiovascular Disease
Cancer
|
|
Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
|
-
- 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-161257
-
|
|
Autophagy
|
Cancer
|
|
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 .
|
-
- 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-129458
-
|
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cardiovascular Disease
Cancer
|
|
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect .
|
-
- HY-146751
-
|
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
|
PI3K/Akt/mTOR-IN-2 is a PI3K/AKT/mTOR pathway inhibitor. PI3K/Akt/mTOR-IN-2 possess anti-cancer effects and selectivity against MDA-MB-231 cells with IC50 value of 2.29 μM. PI3K/Akt/mTOR-IN-2 can induce cancer cell cycle arrest and apoptosis .
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-
- HY-155982
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-20 (Compound 40) is a selective STAT3 inhibitor (IC50: 0.65 μM). STAT3-IN-20 binds the SH2 domain to inhibit STAT3 phosphorylation, translocation, and downstream gene transcription. STAT3-IN-20 exhibits antiproliferative activities against STAT3-overactivated DU145 and MDA-MB-231 cancer cells (IC50: 2.97 μM and 3.26 μM respectively). STAT3-IN-20 induces cell cycle arrest and apoptosis .
|
-
- HY-149898
-
|
|
Others
|
Cancer
|
|
Antitumor agent-109 (compound 6) is an inhibitor of hyaluronic acid (HY-B0633A) targeting to CD44, as well as an anti-tumor agent. Hyaluronic acid interacts with differentiation cluster 44 (CD44) and is involved in tumor growth and invasion. Antitumor agent-109 inhibits MDA-MB-231 cells with EC50 value of 0.59 μM .
|
-
- HY-156098
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-19 (Compound 21j) is a c-Met inhibitor (IC50: 1.99 nM). c-Met-IN-19 shows cytotoxicity against A549, HT-29, SGC-7901, MDA-MB-231 cells with IC50s of 0.25, 0.36, 0.98, 0.76 μM .
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-
- HY-155350
-
|
|
Microtubule/Tubulin
|
Others
|
|
Tubulin polymerization-IN-53 (compound 4b) is an inhibitor of β-tubulin polymerization. Tubulin polymerization-IN-53 can arrest the cell cycle at the G2/M stage. Tubulin polymerization-IN-53 has antiproliferative efficacy against the MDA-MB-231 cell line with an IC50 value of 3.24 μM .
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-
- HY-161151
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Frangulin B (Compd 11g), a potent anticancer agent, is a potential pan RecQ helicase inhibitor . Frangulin B (Compd 11g) induces apoptosis in both HCT-116 and MDA-MB-231 cell lines, but also causes an G2/M phase cell cycle arrest in HCT-116 cells .
|
-
- 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-100353
-
|
N-Lauroyl-D-erythro-sphingosine; N-Laurylsphingosine
|
|
|
|
C12-Ceramide (N-Lauroyl-D-erythro-sphingosine), a naturally occurring ceramide, is formed by hydrolysis of C12 sphingomyelin. C12-Ceramide can enhance the Doxorubicin toxicity in MDA-MB-231 cells. C12-Ceramide also can be used to diagnose types A and B Niemann-Pick disease .
|
-
- HY-146239
-
|
|
EGFR
Thymidylate Synthase
|
Cancer
|
|
EGFR/HER2/TS-IN-2 (compound 17) is a potent EGFR/HER2 and TS (Thymidylate synthase) inhibitor, with IC50 values of 0.173, 0.125, and 1.12 μM, respectively. EGFR/HER2/TS-IN-2 shows cytotoxic activity against MDA-MB-231 cancer cell lines, with an IC50 of 1.69 µM .
|
-
- 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-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-13807
-
UNC0646
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM .
|
-
- HY-149635
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-6 (compound 3s) is a HIF-1α inhibitor with IC50 values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA .
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-
- HY-114324A
-
|
|
PROTACs
PARP
|
Cancer
|
|
rel-PROTAC PARP1 degrader is the relative configuration of ROTAC PARP1 degrader (HY-114324). ROTAC PARP1 degrader is a PARP1 degrader based on MDM2 E3 ligand. It induces significant PARP1 cleavage and programmed cell death. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line with an IC50 of 6.12 μM.
|
-
- HY-144306
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-108447
-
|
|
Ser/Thr Protease
SARS-CoV
PAI-1
|
Infection
Cancer
|
|
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 .
|
-
- HY-160050
-
|
|
Others
|
Cancer
|
|
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 .
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-
- HY-160051
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- HY-155956
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
GM-90257 is a microtubule acetylation inhibitor that binds directly to α-tubulin. GM-90257 prevents the recruitment of α-tubulin acetyltransferase 1 (αTAT1) to the K40 residue in α-tubulin. GM-90257 causes the apoptosis of MDA-MB-231 cells with weaker effects on MCF-10A or MCF-7 cells, which have a relatively low level of microtubule acetylation .
|
-
- HY-156077
-
|
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
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 .
|
-
- HY-119257
-
|
|
Farnesyl Transferase
Apoptosis
|
Cancer
|
|
ABT-100 is a potent, highly selective and orally active farnesyltransferase inhibitor. ABT-100 inhibits cell proliferation (IC50s of 2.2 nM, 3.8 nM, 5.9 nM, 6.9 nM, 9.2 nM, 70 nM and 818 nM for EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells, respectively), increases apoptosis and decreases angiogenesis. ABT-100 possesses broad-spectrum antitumor activity .
|
-
- HY-149636
-
|
|
EGFR
CDK
VEGFR
|
Cancer
|
|
Multi-target kinase inhibitor 2 (compound 5K) is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values ranging from 40 to 204 nM. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells.
|
-
- HY-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-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-162046
-
|
|
Necroptosis
Ferroptosis
|
Cancer
|
|
Anticancer agent 178 (compound C2) is a potent anticancer agent. Anticancer agent 178 inhibits MDA-MB 231 cells proliferation and metabolic activity with IC50s of 1.1 and 4.2 μM. Anticancer agent 178 induces ferroptosis and necroptosis in cells .
|
-
- HY-156296
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective CDK9-Cyclin T1 protein-protein interaction (PPI) inhibitor. CDK9-Cyclin T1 PPI-IN-1 inhibits cell proliferation in TNBC MDA-MB-231 cells (IC50: 0.044 μM), and induces apoptosis. CDK9-Cyclin T1 PPI-IN-1 inhibits CDK9 transcription activity, reduces the phosphorylation of RNA Pol II CTD ser2. CDK9-Cyclin T1 PPI-IN-1 inhibits tumor growth in a TNBC 4T1 mouse model .
|
-
- HY-149388
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 139 (Compound 6h) has potent anticancer activity. Anticancer agent 139 displayed a π–cationic interaction with the residue Lys352 of Tublin. Anticancer agent 139 has good anticancer activity against SNB-19, OVCAR-8, and NCI-H40 with PGIs of 86.61, 85.26, and 75.99, respectively. Anticancer agent 139 also has moderate anticancer activity against HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 with PGIs of 67.55, 65.46, 59.09, 59.02, 57.88, 56.88, 56.53, 56.4, and 51.88 respectively .
|
-
- 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-100753
-
|
|
|
|
|
STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis .
|
-
- HY-134008
-
|
|
Others
|
Cancer
|
|
Protoapigenone is an antineoplastic agent isolated from ferns. Protoapigenone has significant inhibitory activity against Hep G2, Hep 3B, MCF-7, A549 and MDAMB-231, with IC50s values of 1.60, 0.23, 0.78, 3.88 and 0.27 μg/mL respectively .
|
-
- HY-P99697
-
|
PRO 140
|
CCR
HIV
|
Infection
Cancer
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
|
-
- HY-149204
-
|
|
Others
|
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-157876
-
|
|
P-glycoprotein
BCRP
|
Cancer
|
|
Anticancer agent 191 (Compound 2) is a derivative of probenecid (HY-B0545). As a cancer cell efflux inhibitor, Anticancer agent 191 is designed to inhibit P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and/or multiple multidrug resistance proteins (MRPs). Anticancer agent 191 increases the accumulation of vinblastine in cancer cells, which is used for cancer research .
|
-
- HY-146728
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-10 is a STAT3 inhibitor with an IC50 value of 5.18 µM. STAT3-IN-10 directly binds to STAT3 SH2 domain, induces cancer cells apoptosis .
|
-
- HY-146146
-
|
KAA
|
Kinesin
|
Cancer
|
|
Kolavenic acid analog (KAA) is an anticancer agent. Kolavenic acid analog shows strong activity against HSET-overproducing yeast cells. Kolavenic acid analog inhibits centrosome clustering in human cancer cells containing high HSET levels and supernumerary centrosomes .
|
-
- HY-147799
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCA XII/II/IX-IN-1 (Compound 3) is a potent human carbonic anhydrase (hCA) inhibitor with IC50 values of 2.6, 0.004, 0.005 and 0.001 μM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA XII/II/IX-IN-1 shows anticancer activity .
|
-
- HY-150775
-
|
|
Cytochrome P450
|
Cancer
|
|
Nonsteroidal aromatase inhibitor 1 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC50=0.09 nM). Nonsteroidal aromatase inhibitor 1 has potential for breast cancer research . Nonsteroidal aromatase inhibitor 1 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-149897
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Antitumor agent-108 (compound 5) is an Hyaluronic acid (HA)-CD44 interaction inhibitor that effectively disrupts the integrity of cancer spheroids. Antitumor agent-108 also exhibits antiproliferative activity against cancer cells .
|
-
- HY-150412
-
|
|
Phospholipase
|
Cancer
|
|
VU0364739 is a selective PLD2 inhibitor (IC50: 22 nM). VU0364739 decreases cancer cell proliferation .
|
-
- HY-N12503
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3 activation .
|
-
- HY-B0621
-
|
CGA89317
|
Parasite
Caspase
Bcl-2 Family
PARP
Pyroptosis
|
Infection
|
|
Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
|
-
- HY-N2117
-
-
- HY-N0364
-
|
|
Apoptosis
Autophagy
PPAR
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Falcarindiol, an orally active polyacetylenic oxylipin, activates PPARγ and increases the expression of the cholesterol transporter ABCA1 in cells. Falcarindiol induces apoptosis and autophagy. Falcarindiol has anti-inflammatory, antifungal, anticancer and antidiabetic properties . Falcarindiol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146200
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-8 (Compound 18b) is a PI3K and mTOR dual inhibitor with IC50 values of 0.46 nM and 12 nM against PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-8 induces HCT-116 cells apoptosis and arrests cell cycle at the G1/S phase .
|
-
- HY-147867
-
|
|
MMP
|
Cancer
|
|
MMP-2/9-IN-1 (Compound 4a) is a potent dual MMP-2 and MMP-9 inhibitor with IC50 values of 56 nM and 38 nM, respectively. MMP-2/9-IN-1 inhibits tumor growth, strongly induces cancer cell apoptosis, inhibits cell migration, and suppresses cell cycle progression leading to DNA fragmentation .
|
-
- HY-100683
-
|
|
Phosphatase
|
Cancer
|
|
A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells .
|
-
- HY-151625
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP-2-IN-3 (Compound 12) is a potent PARP-2 inhibitor with an IC50 of 0.07 μM. PARP-2-IN-3 induces apoptosis and necrosis in cancer cells. PARP-2-IN-3 shows appropriate predicted pharmacokinetic parameters and oral bioavailability .
|
-
- HY-P99813
-
|
HER3-DXd
|
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-155023
-
|
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Apoptosis inducer 13 (Compound Ru4) can induce cancer cell apoptosis, and inhibits cancer cell migration and invasion. Apoptosis inducer 13 converts coenzyme NADH to NAD +, and increases intracellular ROS levels .
|
-
- HY-100914
-
|
Ophobolin A
|
Calmodulin
|
Cancer
|
|
A-7 hydrochloride (Ophobolin A) is a calmodulin antagonist and can be used for the research of cancer .
|
-
- HY-144627
-
|
|
PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 µM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis .
|
-
- HY-144624
-
|
|
PROTACs
TAM Receptor
|
Cancer
|
|
PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 µM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis .
|
-
- HY-100574C
-
-
- HY-139327
-
|
|
CDK
|
Cancer
|
|
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1) .
|
-
- HY-139328
-
|
|
CDK
|
Cancer
|
|
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1) .
|
-
- HY-139329
-
|
|
CDK
|
Cancer
|
|
CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1) .
|
-
- HY-100574D
-
-
- HY-143490
-
|
|
PAK
Apoptosis
|
Cancer
|
|
PAK4-IN-2 is a highly potent PAK4 inhibitor with IC50 value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer .
|
-
- HY-146065
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-4 (Compound 7d) is potential FAK inhibitor with anticancer activities. FAK-IN-4 induces cell apoptosis .
|
-
- HY-147801
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .
|
-
- HY-N10444
-
|
|
Others
|
Cancer
|
|
Alterbrassicene B is an anticancer agent, can be isolated from Alternaria brassicicola .
|
-
- HY-151207
-
|
|
Apoptosis
ADC Cytotoxin
|
Cancer
|
|
Anticancer agent 81 (Compound 37b3) is an anticancer agent and can induce tumor cell cycle arrest and apoptosis. Anticancer agent 81 can be used as a payload to conjugate with Trastuzumab (HY-P9907) to obtain the antibody–agent conjugate (ADC) T-PBA. T-PBA maintained its mode of target and internalization ability of Trastuzumab .
|
-
- HY-148242
-
BAY-069
1 Publications Verification
|
Others
|
Cancer
|
|
BAY-069 is a potent branched-chain amino acid transaminases 1 (BCAT1) and BCAT2 inhibitor with IC50 values of 31 nM and 153 nM, respectively. BAY-069 also can be used as a chemical probe. BAY-069 can be used tor research anticancer .
|
-
- HY-112649
-
|
|
STAT
Apoptosis
|
Cancer
|
|
Pomstafib-2 is a potent and selective STAT5b inhibitor. Pomstafib-2 decreases the expression of pSTAT5b and induces Apoptosis .
|
-
- HY-152536
-
|
|
NO Synthase
|
Cancer
|
|
iNOS inhibitor-10 is an iNOS inhibitor (IC50: 65 nM). iNOS inhibitor-10 has antiproliferative effect against triple negative breast cancer cells .
|
-
- HY-107043
-
-
- HY-P99675
-
|
AK112
|
PD-1/PD-L1
VEGFR
|
Cancer
|
|
Ivonescimab (AK112) is a PD-1/VEGF Bispecific Antibody. Ivonescimab can be used for cancer research .
|
-
- HY-132219
-
|
|
Others
|
Cancer
|
|
N. N-dipropyrldopamine is a potent inhibitor of glutamate release and has anticancer activity. The increase of glutamate secretion leads to cancer-induced bone pain (CIBP). N. N-dipropyrldopamine plays an analgesic role in CIBP .
|
-
- HY-155571
-
|
|
MDM-2/p53
IAP
|
Cancer
|
|
MDM2/XIAP-IN-3 (compound 3e) is a dual MDM2/XIAP inhibitor. MDM2/XIAP-IN-3 reduces MDM2 and XIAP protein levels and increases p53 expression, thereby inhibiting cancer cell growth and causing cell death .
|
-
- HY-149858
-
|
|
Wnt
|
Cancer
|
|
β-catenin-IN-7 (Compound 9) is a β-catenin inhibitor. β-catenin-IN-7 inhibits the interaction between β-catenin and Tcf-4, and inhibits Wnt-dependent target gene expression. β-catenin-IN-7 has anti-cancer activity .
|
-
- HY-155229
-
-
- HY-157290
-
|
|
Epigenetic Reader Domain
Src
|
Cancer
|
|
HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC50 values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity .
|
-
- HY-113534
-
|
|
IAP
Apoptosis
|
Cancer
|
|
MV1 is an antagonist of IAP (inhibitor of apoptosis protein), leads to protein knockdown of HaloTag-fused proteins when combined with HaloTag ligand .
|
-
- HY-126275
-
|
|
ROCK
|
Cancer
|
|
HSD1590 is potent ROCK inhibitor, with IC50s of 1.22 and 0.51 nM for ROCK1 and ROCK2, respectively. HSD1590 exhibits single digit nanomolar binding to ROCK (Kds<2 nM). HSD1590 displays low cytotoxicity .
|
-
- HY-102051
-
|
|
IAP
|
Cancer
|
|
XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo .
|
-
- HY-149000
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor. PI3Kα-IN-7 also inhibits PI3Kβ. PI3Kα-IN-7 decreases cancer cells mitochondrial membrane potential and induces apoptosis .
|
-
- HY-107209
-
|
|
ROCK
|
Cancer
|
|
RKI-1313 is a ROCK inhibitor with IC50s of 34, 8 µM for ROCK 1 and ROCK 2, respectively. RKI-1313 shows little effect on the phosphorylation levels of ROCK substrates, migration, invasion or anchorage-independent growth .
|
-
- HY-147865
-
|
|
Galectin
Apoptosis
|
Cancer
|
|
Apoptosis inducer 8 (Compound 7c) is a galectin-1 (gal-1) mediated apoptosis-inducing agent against global major leading lung cancer burden. Apoptosis inducer 8 significantly reduced the gal-1 protein level. Apoptosis inducer 8 is also a PET imaging agent .
|
-
- HY-150757
-
|
|
Autophagy
Apoptosis
|
Cancer
|
|
Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research .
|
-
- HY-151120
-
|
|
Others
|
Cancer
|
|
Anticancer agent 79 (compound 3d) shows good anti-breast cancer activity. Anticancer agent 79 shows good cytotoxic activity in T47-D cells, with an IC50 of 13.64 ± 0.26 μM .
|
-
- HY-124722
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM .
|
-
- HY-149266
-
|
|
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-N8342
-
|
|
VEGFR
|
Inflammation/Immunology
Cancer
|
|
Rhamnazin is an orally active inhibitor of VEGFR2 signaling with an IC50 of 4.68 μM against VEGFR2 kinase. Rhamnazin shows potent antiangiogenic activity and antitumor efficacy . Rhamnazin shows antioxidant and anti-inflammatory properties .
|
-
- HY-18406
-
|
|
HSP
|
Cancer
|
|
HSP70-IN-4 (Compound YM-01) is an Hsp70 inhibitor with an IC50 of 3.2 μM. HSP70-IN-4 is not BBB permeable .
|
-
- HY-149398
-
|
|
Apoptosis
PARP
CDK
|
Cancer
|
|
PARP-1/2-IN-2-IN-1 (Compound 12e) is a PARP1/2/CDK12 inhibitor (IC50: 34, 30 and 285 nM respectively). PARP-1/2-IN-2 inhibits DNA damage repair, promotes cell cycle arrest and apoptosis. PARP-1/2-IN-2 inhibits the growth of TNBC cells and TNBC xenograft tumor .
|
-
- HY-149487
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-8 (Compound 9) is a FGFR1 inhibitor (IC50s: 0.5 nM). FGFR1 inhibitor-8 binds to the ATP-binding pocket of FGFR1. FGFR1 inhibitor-8 has anticancer activity .
|
-
- HY-149488
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor (IC50s: 0.85 nM). FGFR1 inhibitor-9 binds to the ATP-binding pocket of FGFR1. FGFR1 inhibitor-9 has anticancer activity .
|
-
- HY-149616
-
|
|
PROTACs
ERK
|
Cancer
|
|
PPM-3 is a potent and selective PROTAC ERK5 degrader, with an IC50 of 62.4 nM. PPM-3 did not influence tumor cell growth directly. PPM-3 influences tumor development by affecting the differentiation of macrophages .
|
-
- HY-155339
-
|
|
Others
|
Cancer
|
|
Anticancer agent 168 (compound d16) is a inhibitor of DNA2. Anticancer agent 168 induces apoptosis and cell-cycle arrest mainly at S-phase, and exhibits anticancer activities and overcomes chemotherapy resistance in mutp53-bearing cancers .
|
-
- HY-161353
-
|
|
c-Met/HGFR
P-glycoprotein
|
Cancer
|
|
c-Met-IN-23 (Compound 12g) is a c-Met inhibitor (IC50 = 0.052 μM for c-Met). c-Met-IN-23 also inhibits MDR1 and MRP1/2 pumps in the cancerous HepG2 and BxPC3 cells. c-Met-IN-23 is an anticancer agent .
|
-
- HY-162370
-
|
|
Cytochrome P450
|
Infection
Cancer
|
|
CYP51-IN-16 (compound C6) is a phenylpyrimidine CYP51 inhibitor, and shows antifungal activity in in vitro. CYP51-IN-16 inhibits tumor cell growth .
|
-
- HY-161360
-
|
|
SHP2
Apoptosis
|
Cancer
|
|
LXQ-217 is an oral active SHP2 inhibitor with the IC50 of 2.01 μM. LXQ-217 induces apoptosis and inhibits cell growth in vivo and in vitro .
|
-
- HY-114803
-
-
- HY-16916
-
NS1643
1 Publications Verification
|
Potassium Channel
Autophagy
|
Cancer
|
|
NS1643 is a partial agonist of human ether-a-go-go-related gene (hERG) K + channels with an EC50 of 10.5 μM. NS1643 inhibits the growth of breast cancer tumors in TNBC mouse models. NS1643 inhibits cell migration and invasion of breast cancer cells .
|
-
- HY-15861
-
|
TGP-210
|
MicroRNA
Apoptosis
|
Cancer
|
|
Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM) . Targapremir-210 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-104068
-
|
|
Histone Acetyltransferase
Epigenetic Reader Domain
|
Cancer
|
|
Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 µM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 µM. Naphthol AS-E can be used for cancer research.
|
-
- HY-128769
-
|
|
CDK
|
Cancer
|
|
M2N12 is a potent and highly selective cell division cycle 25C protein phosphatase (Cdc25C) inhibitor with an IC50 value of 0.09 μM. M2N12 also has promising activity against Cdc25A and Cdc25B with IC50 values of 0.53 μM and 1.39 μM, respectively. M2N12 has anti-tumor activity and can be used for cancer research .
|
-
- HY-132135
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity .
|
-
- HY-144449
-
|
|
mTOR
HDAC
Apoptosis
Autophagy
|
Cancer
|
|
mTOR/HDAC6-IN-1 is a potent mTOR and HDAC6 dual inhibitor (IC50s of 133.7 nM and 56 nM for mTOR and HDAC6, respectively). mTOR/HDAC6-IN-1 can induce significant autophagy, apoptosis and suppress migration. mTOR/HDAC6-IN-1 has potential to research Triple-negative breast cancer (TNBC) .
|
-
- HY-146093
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-62 (Compound 47) is a NO-releasing antitumor agent. Antitumor agent-62 shows antiproliferative activity against four cancer cell lines. Antitumor agent-62 activates mitochondrial apoptosis pathway and arrests cell cycle at G2/M phase .
|
-
- HY-147877
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 12 (Compound 8c) is a topoisomerase II (topo II) inhibitor, working as a DNA non-intercalator. Topoisomerase II inhibitor 12 shows antineoplastic activity .
|
-
- HY-147219
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
|
Cancer
|
|
SIAIS164018 is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 exhibits better property than Brigatinib (HY-12857) .
|
-
- HY-N10472
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-14 (Compound 1) is a STAT3 inhibitor and has STAT3 phosphorylation inhibitory activity. STAT3-IN-14 (Compound 1) can directly bind to the hinge region of STAT3 .
|
-
- HY-143270
-
-
- HY-150609
-
|
|
SHP2
Phosphatase
CDK
|
Cancer
|
|
SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-151477
-
|
|
SARS-CoV
|
Infection
Cancer
|
|
SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19 .
|
-
- HY-151478
-
|
|
SARS-CoV
|
Infection
Cancer
|
|
SARS-CoV-2-IN-33 (compound 3m) is a COVID-19 inhibitor. SARS-CoV-2-IN-33 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-33 exhibits comparatively good binding affinity (-8.0 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-33 can be used in studies of cancer and COVID-19 .
|
-
- HY-151904
-
|
|
TAM Receptor
FLT3
PDGFR
|
Cancer
|
|
AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion .
|
-
- HY-115594
-
|
|
STAT
Apoptosis
|
Cancer
|
|
Erasin is a potent Erlotinib (HY-50896)-resistance antagonizing STAT3 inhibitor with IC50s of 9.7 and 24 μM against STAT3 and STAT1, respectively. Erasin induces cancer cells apoptosis .
|
-
- HY-149259
-
|
|
FAK
|
Cancer
|
|
FAK-IN-9 (Compound 8f) is a potent and orally active FAK inhibitor with an IC50 of 27.44 nM. FAK-IN-9 induces triple-negative breast cancer (TNBC) cell apoptosis .
|
-
- HY-147219A
-
|
|
PROTACs
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
|
Cancer
|
|
SIAIS164018 hydrochloride is a PROTAC-based ALK and EGFR degrader, with IC50 value of 2.5 nM and 6.6 nM for ALK and ALK G1202R, respectively. SIAIS164018 hydrochloride strongly inhibits cancer cells migration and invasion, causes G1 cell cycle arrest and induces apoptosis. SIAIS164018 hydrochloride exhibits better property than Brigatinib (HY-12857) .
|
-
- HY-155874
-
|
|
CDK
|
Cancer
|
|
ZNL-05-044 is a CDK11 inhibitor with an IC50s of 0.23 μM and 0.27 μM against CDK11A and CDK11B, respectively (NanoBRET assay). ZNL-05-044 leads to G2/M cell cycle arrest and impairs RNA splicing .
|
-
- HY-155490
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
|
Cancer
|
|
Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KD SPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells .
|
-
- HY-15150G
-
|
R428 (GMP); BGB324 (GMP)
|
TAM Receptor
|
Cancer
|
|
Bemcentinib (R428) GMP is an orally active and selective inhibitor of Axl with an IC50 of 14 nM .
|
-
- HY-161082
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 12 (compound 12), a Camptothecin (HY-16560)-based derivative, is a potent Topoisomerase I inhibitor. Topoisomerase I inhibitor 12 shows anticancer activity .
|
-
- 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-163444
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 15 (Compound 3) induces cell apoptosis and cell cycle arrest at G2/M phase. Apoptosis inducer 15 is cytotoxicitic without causing DNA fragmentation .
|
-
- HY-161358
-
|
|
FAK
Apoptosis
|
Cancer
|
|
FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. It can arrest the cell cycle in the G2/M phase and induce cell apoptosis (apoptosis) by generating ROS .
|
-
- HY-10211
-
|
17-AAG; NSC 330507; CP 127374
|
HSP
Autophagy
Mitophagy
Bacterial
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90 . Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression .
|
-
- HY-B0149
-
|
cyclocapron
|
IGF-1R
AMPK
MMP
Mitophagy
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Tranexamic acid (cyclocapron), a cyclic analog of lysine, is an orally active antifibrinolytic agent. Tranexamic acid attenuates the effects of severe trauma, inhibits urokinase plasminogen activator and ameliorates dry wrinkles. Tranexamic acid can used for the research of hemostasis .
|
-
- HY-13513
-
U-104
5 Publications Verification
SLC-0111
|
Carbonic Anhydrase
|
Cancer
|
|
U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model .
|
-
- HY-19992
-
|
Bromopyruvic acid; Hexokinase II Inhibitor II, 3-BP
|
Hexokinase
Apoptosis
Autophagy
|
Cancer
|
|
3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities .
|
-
- HY-19792
-
|
DM1; Maytansinoid DM1
|
Microtubule/Tubulin
ADC Cytotoxin
|
Cancer
|
|
Mertansine (DM1) is a microtubulin inhibitor and is an antibody-conjugatable maytansinoid that is developed to overcome systemic toxicity associated with maytansine and to enhance tumor-specific delivery. Mertansine can be attached to a monoclonal antibody with a linker to create an antibody-drug conjugate (ADC) .
|
-
- HY-103490
-
|
EDHS-206
|
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
|
-
- HY-131183
-
|
|
PROTACs
PD-1/PD-L1
|
Inflammation/Immunology
|
|
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner .
|
-
- HY-18285
-
|
|
Casein Kinase
ERK
CDK
|
Cancer
|
|
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of 5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively .
|
-
- HY-119039
-
|
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis .
|
-
- HY-122639
-
|
|
Others
|
Cancer
|
|
ZINC05007751 is a potent NIMA-related kinase NEK6 inhibitor with an IC50 of 3.4 μM. ZINC05007751 shows antiproliferative activity against a panel of human cancer cell lines, and displays a synergistic effect with Cisplatin and Paclitaxel in a BRCA2 mutated ovarian cancer cell line. ZINC05007751 is very selective against NEK1 and NEK6 with no significant activity was observed against NEK2, NEK7, and NEK9 .
|
-
- 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-147767
-
|
|
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis .
|
-
- HY-147513
-
|
|
Akt
Apoptosis
|
Cancer
|
|
AKT-IN-12 (compound 3e) is a potent Akt kinase inhibitor with an IC50 value of 0.55 μM. AKT-IN-12 induces G0/G1 cell cycle arrest and apoptosis. AKT-IN-12 also inhibits p-AKT, p-ERK, and activates p-JNK, JNK. AKT-IN-12 can be used for researching leukemia .
|
-
- HY-149032
-
|
|
Others
|
Cancer
|
|
Kobusine derivative-1 is a Kobusine derivative. Kobusine derivative-1 shows antiproliferative activities against cancer cells .
|
-
- HY-151119
-
|
|
Cytochrome P450
|
Cancer
|
|
Anticancer agent 78 is a potent anticancer agent. Anticancer agent 78 shows cytotoxicity. Anticancer agent 78 exhibits anti-aromatase activity with an IC50 value of 0.9 µM. Anticancer agent 78 has the potential for the research of breast cancer .
|
-
- HY-151379
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .
|
-
- HY-132578
-
|
|
Phosphatase
|
Cancer
|
|
M5N36 is a potent and selective Cdc25C inhibitor with IC50 values of 0.15, 0.19, 0.06 µM for Cdc25A, Cdc25B, Cdc25C, respectively. M5N36 shows anti-proliferative activity and increases the expression of p-CDK1 and p-CDK2 .
|
-
- HY-P99734
-
|
ADCT-601
|
TAM Receptor
|
Cancer
|
|
Mipasetamab uzoptirine (ADCT-601) is an AXL-targeted antibody-drug conjugates (ADCs). Mipasetamab uzoptirine consists of a humanized anti-AXL antibody, a cleavable linker and the potent pyrrolobenzodiazepine (PBD) dimer cytotoxin SG3199. Mipasetamab uzoptirine can be used for the research of cancers .
|
-
- HY-118961
-
|
|
Kinesin
|
Cancer
|
|
SR31527 chloride is a potent KIFC1 inhibitor with an IC50 value of 6.6 µM. SR31527 chloride decreases cell viability and colony formation .
|
-
- HY-153691
-
|
|
Others
|
Others
|
|
BTB01303 is a (glutamate release) inhibitor. Cancer cells release high levels of (glutamate), which disrupts normal bone turnover and may lead to cancer-induced bone pain. BTB01303 has the potential to improve cancer-induced bone pain .
|
-
- HY-N7223
-
|
|
YAP
Apoptosis
|
Cancer
|
|
Lappaol F, a lignin, is an anticancer agent. Lappaol F inhibits YAP<、b> mRNA and protein level. Lappaol F inhibits tumor cell growth by inducing cell cycle arrest. Lappaol F induces cancer cell apoptosis, and inhibits tumor growth. Lappaol F can be isolated from Arctium lappa Linne (Asteraceae) .
|
-
- HY-101761A
-
|
|
PAI-1
Apoptosis
|
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-139103
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Thailanstatin C is a pre-mRNA splicing inhibitor (IC50= 6.84 μM) and antiproliferative agent from Burkholderia thailandensis MSMB43 .
|
-
- HY-132301
-
|
MCT4-IN-1
|
Monocarboxylate Transporter
|
Cancer
|
|
MSC-4381 (MCT4-IN-1) is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MSC-4381 targets to the cytosolic domain of MCT4. MSC-4381 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MSC-4381 has the potential for MCT4 transporter inhibition research . MSC-4381 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-146681
-
|
|
PAK
|
Cancer
|
|
PAK1-IN-1 is a potent and selective PAK1 inhibitor with an IC50 of 9.8 nM. PAK1-IN-1 inhibits the migration and invasion of PAK1-related tumour cells in a dose-dependent manner .
|
-
- HY-149008
-
|
|
Amylases
|
Metabolic Disease
Cancer
|
|
α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease .
|
-
- HY-150510
-
|
|
Histone Methyltransferase
|
Neurological Disease
Cancer
|
|
MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
|
-
- HY-107551
-
|
|
Gli
|
Cancer
|
|
GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. GLI antagonist-1 shows anti-proliferative activity. GLI antagonist-1 decreases the GLI1 mRNA expression. GLI antagonist-1 inhibits colony formation in a dose-dependent manner .
|
-
- HY-148070
-
|
|
FLT3
FAK
Cytochrome P450
|
Cancer
|
|
FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers .
|
-
- HY-151471
-
|
|
c-Myc
|
Cancer
|
|
Anticancer agent 84 is an anticancer agent. Anticancer agent 84 represses the transcription of c-MYC by stabilizing the G-quadruplex (G4) structure. Anticancer agent 84 can be used for the research of cancer .
|
-
- HY-115436
-
|
|
Apoptosis
|
Cancer
|
|
LYG-202, a flavonoid, has potent anti-angiogenic and antitumor activity. LYG-202 inhibits VEGF-stimulated HUVEC migration and tube formation. LYG-202 induces cancer cell apoptosis .
|
-
- 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-157387
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis .
|
-
- HY-12003
-
|
|
Aurora Kinase
|
Cancer
|
|
SNS-314 mesylate is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
|
-
- HY-135276
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-P1411
-
|
PcTx1; Psalmopoeus caMBridgei toxin-1
|
Sodium Channel
Apoptosis
|
Neurological Disease
Cancer
|
|
Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 is a potent and slective ASIC1a inhibitor (IC50: 0.9 nM) by increasing the apparent affinity for H + of ASIC1a. Psalmotoxin 1 can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 can be used in the research of cancers, or neurological disease .
|
-
- HY-N1506
-
|
|
Others
|
Cancer
|
|
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 .
|
-
- HY-136406
-
|
|
ATP Synthase
|
Infection
Cancer
|
|
Bongkrekic acid is a mitochondrial toxin secreted by the bacteria Pseudomonas cocovenenans . Bongkrekic acid specific ligand for mitochondrial adenine nucleotide translocase (ANT) rather than the electron transport chain. Bongkrekic acid has to cross the mitochondrial inner membrane to produce its inhibitory effect on ADP/ATP transport .
|
-
- HY-N0171B
-
|
β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)
|
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (purity>75%) is a phytosterol with oral activity. Beta-Sitosterol (purity>75%) interferes with a variety of cell signaling pathways, including the cell cycle, apoptosis and cell proliferation. Beta-Sitosterol (purity>75%) has anti-inflammatory, antioxidant, and antitumor activities .
|
-
- HY-135276A
-
|
|
MicroRNA
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-12352A
-
|
|
STAT
Apoptosis
|
Cancer
|
|
HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study .
|
-
- HY-144876
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
RIDR-PI-103 is a reactive oxygen species (ROS)-induced drug release prodrug with a self-cyclizing moiety linked to a pan-PI3K inhibitor (PI-103).
|
-
- HY-146754
-
|
|
MMP
Apoptosis
|
Cancer
|
|
MMP2-IN-1 is a moderate potenet MMP2 inhibitor with IC50 of 6.8 µM. MMP2-IN-1 exhibits remarkable antiproliferative activity in certain cancer cells by arresting the cell cycle and inducing apoptosis .
|
-
- HY-108344
-
|
|
Aurora Kinase
|
Cancer
|
|
SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively .
|
-
- HY-146889
-
|
|
Others
|
Cancer
|
|
ATX inhibitor 16 is a potent ATX inhibitor with an IC50 of 0.0021 µM. ATX inhibitor 16 shows excellent anti-proliferative activities in breast cancer cells .
|
-
- HY-146890
-
|
|
Others
|
Cancer
|
|
ATX inhibitor 17 is a potent ATX inhibitor with an IC50 of 0.019 µM. ATX inhibitor 17 shows excellent anti-proliferative activities in breast 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-150655
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-15 is an Hsp90 inhibitor with anticancer activity. Hsp90-IN-15 induces cell apoptosis, arrests the cell cycle at S phase and decreases the expression level of Hsp90 in Hela cell .
|
-
- 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-115589
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity .
|
-
- HY-N10558
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research .
|
-
- HY-136699
-
|
|
Others
|
Cancer
|
|
Excisanin A is a potent anticancer agent. Excisanin A inhibits cell proliferation, migration, adhesion and invasion. Excisanin A decreases the expression of MMP-2, MMP-9, p-FAK, p-Src, integrin β1 protein. Excisanin A has the potential for the research of breast cancer .
|
-
- HY-155020
-
|
|
Histone Methyltransferase
GLP Receptor
|
Cancer
|
|
Antitumor agent-101 is a selective covalent inhibitor of lysine methyltransferases G9a/GLP, with IC50s of 8.5 nM and 5.5 nM for G9a and GLP, respectively. Antitumor agent-101 shows antitumor efficacy in the PANC-1 xenograft model .
|
-
- 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-13502
-
|
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-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-13302
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 has antitumor efficacy .
|
-
- 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-123847
-
|
|
PIN1
|
Cancer
|
|
KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer .
|
-
- HY-13302B
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 hydrochloride is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 hydrochloride is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 hydrochloride has antitumor efficacy .
|
-
- 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-13302C
-
|
|
VEGFR
FGFR
|
Cancer
|
|
CP-547632 TFA is an orally active, ATP-competitive and potent VEGFR-2 and FGF kinases inhibitor with IC50s of 11 nM and 9 nM, respectively. CP-547632 TFA is selective for VEGFR2 and bFGF over EGFR, PDGFRβ, and related tyrosine kinases (TKs). CP-547632 TFA has antitumor efficacy .
|
-
- HY-108692
-
|
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
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 .
|
-
- HY-145260
-
|
|
Epigenetic Reader Domain
Casein Kinase
Apoptosis
Autophagy
|
Cancer
|
|
BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)
|
-
- HY-137005
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
CS1 is a potent DNA Topo II α inhibitor. CS1 displays broad-spectrum in vitro antitumor effects, low toxicity in vivo and potential anti-multidrug resistance capabilities. CS1 leads to DNA damage, cell cycle arrest at G2/M phase and apoptosis .
|
-
- HY-12486
-
|
10,11-(Methylenedioxy)-20(S)-camptothecin
|
Survivin
Apoptosis
IAP
|
Cancer
|
|
FL118 (10,11-(Methylenedioxy)-20(S)-camptothecin), a Camptothecin (HY-16560) analogue, is a potent and orally active survivin inhibitor. FL118 binds to oncoprotein DDX5 (p68) to dephosphorylates and degrades DDX5. FL118 can be used for the research of cancer .
|
-
- HY-151263
-
|
|
HDAC
G-quadruplex
|
Cancer
|
|
G4/HDAC-IN-1 (compound a6) is a G4/HDAC dual-targeting compound. G4/HDAC-IN-1 inhibits intracellular HDAC activity with an IC50 value of 1.1 μM, and induces G4 formation. G4/HDAC-IN-1 inhibits TNBC proliferation and tumor growth in TNBC xenograft model. G4/HDAC-IN-1 can be used for the research of cancer .
|
-
- HY-N10591
-
|
|
Others
|
Cancer
|
|
Bruceantarin is a potent antineoplastic agent. Bruceantarin can be used for leukemia and breast cancer research .
|
-
- HY-151799
-
|
|
p62
E1/E2/E3 Enzyme
|
Cancer
|
|
Antitumor agent-81 (compound 5a) is a low cytotoxic P62-RNF168 agonist that promotes the interaction of P62 with RNF168. Antitumor agent-81 induces a decrease in RNF168-mediated H2A ubiquitination and impairs homologous recombination-mediated DNA repair. Antitumor agent-81 also inhibits mice xenograft tumor growth in a dose-dependent manner .
|
-
- HY-148685
-
|
|
Others
|
Cancer
|
|
KM04416, an isothiazolone derivative, is a potent glycerol-3-phosphate dehydrogenase (GPD2) inhibitor. KM04416 significantly inhibits PNT1A cell proliferation .
|
-
- HY-149209
-
|
|
CDK
STAT
Early 2 Factor (E2F)
|
Cancer
|
|
LL-K8-22 is a potent, selective and durable 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 .
|
-
- HY-163381
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-48 (compound PC-A1) shows selective antiproliferative activity against triple-negative breast cancer (TNBC) cells .
|
-
- HY-158108
-
|
|
Autophagy
Ferroptosis
Reactive Oxygen Species
|
Cancer
|
|
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 .
|
-
- HY-10181
-
Dasatinib
Maximum Cited Publications
85 Publications Verification
BMS-354825
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib also induces apoptosis and autophagy.
|
-
- HY-10331
-
|
BAY 73-4506
|
VEGFR
Autophagy
PDGFR
Raf
RET
c-Kit
FGFR
Tie
|
Cancer
|
|
Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity .
|
-
- HY-10331A
-
|
BAY 73-4506 monohydrate
|
VEGFR
Autophagy
PDGFR
Raf
RET
FGFR
c-Kit
Tie
|
Cancer
|
|
Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity .
|
-
- HY-10181A
-
|
BMS-354825 hydrochloride
|
Bcr-Abl
Src
Autophagy
Apoptosis
|
Cancer
|
|
Dasatinib (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively . Dasatinib hydrochloride also induces apoptosis and autophagy.
|
-
- HY-123938
-
|
CYH33
|
PI3K
|
Cancer
|
|
Risovalisib (CYH33) is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. Risovalisib inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. Risovalisib has potent activity against solid tumors .
|
-
- HY-122181
-
|
|
Histone Methyltransferase
|
Cancer
|
|
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 .
|
-
- HY-110368
-
|
|
CDK
|
Cancer
|
|
BS-181 dihydrochloride is a potent and selective CDK7 inhibitor (IC50=21 nM) than Seliciclib (HY-30237). BS-181 is also against CDK2, CDK5 and CDK9 with IC50 values of 880 nM, 3000 nM and 4200 nM, respectively (fails to block CDK1, 4 and 6). BS-181 dihydrochloride inhibits a panel of cancer cells growth (IC50=11.5 μM-37.3 μM) and induces cell apoptosis. BS-181 dihydrochloride has the potential for the research of cancer therapy .
|
-
- HY-123938A
-
|
|
PI3K
|
Cancer
|
|
CYH33 methanesulfonate is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 methanesulfonate inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 methanesulfonate has potent activity against solid tumors .
|
-
- HY-B0509A
-
|
BAY 41-6551
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Amikacin (BAY 41-6551) is a semisynthetic kanamycin analog that is active against most Gram-negative bacteria, including gentamicin- and tobramycin-resistant strains. Significant inhibitory effect. Amikacin is ototoxic and nephrotoxic. Amikacin can be used in bacteriostatic, anti-cancer and analgesic studies .
|
-
- HY-144318
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
CREB-IN-1 TFA is a potent, orally active CREB inhibitor (IC50=0.18 µM). CREB-IN-1 TFA inhibits breast cancer cell growth .
|
-
- HY-143491
-
|
|
VEGFR
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells) .
|
-
- HY-129156
-
|
|
Apoptosis
|
Cancer
|
|
HS-1793 is a Resveratrol (HY-16561) analogue with antitumor activities in a variety of cancer cell lines . HS-1793 induces cell apoptosis .
|
-
- 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 .
|
-
- HY-10331B
-
|
BAY 73-4506 mesylate
|
VEGFR
PDGFR
RET
Raf
c-Kit
FGFR
Autophagy
Tie
|
Cancer
|
|
Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity .
|
-
- HY-120234
-
|
Z-Leu-Leu-Nle-CHO; GSII
|
γ-secretase
Proteasome
Apoptosis
|
Cancer
|
|
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia .
|
-
- HY-149086
-
|
|
RAR/RXR
Apoptosis
PARP
Bcl-2 Family
|
Cancer
|
|
BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis .
|
-
- HY-116107
-
|
|
Necroptosis
|
Cancer
|
|
AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines .
|
-
- HY-138657
-
|
|
Phosphatase
|
Cancer
|
NCGC00378430 is a potent SIX1/EYA2 interaction inhibitor. NCGC00378430 partially reverses transcriptional and metabolic profiles mediated by SIX1 overexpression and reverses SIX1-induced TGF-β signaling and epithelial-mesenchymal transition (EMT). NCGC00378430 inhibits SIX1-mediated breast cancer metastasis in a mouse model .
|
-
- HY-150613
-
|
|
Epigenetic Reader Domain
PARP
Apoptosis
|
Cancer
|
|
PARP1/BRD4-IN-2 is a potent and selective PARP1 and BRD4 inhibitor with IC50 values of 197 nM and 238 nM, respectively. PARP1/BRD4-IN-2 inhibits DNA damage repair, arrests G0/G1 transition and induces apoptosis. PARP1/BRD4-IN-2 has anti-tumor activity in MDA-MB-468 xenograft mouse model. PARP1/BRD4-IN-2 can be used for researching triple-negative breast cancer (TNBC) .
|
-
- HY-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-12352
-
|
|
STAT
Apoptosis
|
Cancer
|
|
HJC0416 is a potent and orally active STAT3 inhibitor. HJC0416 shows antiprolifeative activity and induces apoptosis. HJC0416 decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity .
|
-
- HY-155008
-
|
|
Hexokinase
|
Cancer
|
|
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .
|
-
- HY-135699
-
TD52
1 Publications Verification
|
Apoptosis
Phosphatase
Akt
|
Cancer
|
|
TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-145438
-
|
|
Others
|
Cancer
|
|
Antitumor agent-38 is a potent antitumor agents. Antitumor agent-38 shows antiproliferative activity for cancer cells. Antitumor agent-38 induces cell cycle arrest at the late S and G2/M phase without interfering with microtubule formation or cell morphology[1].
|
-
- HY-135699A
-
|
|
Akt
Phosphatase
Apoptosis
|
Cancer
|
|
TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-151971
-
|
|
Aurora Kinase
Polo-like Kinase (PLK)
|
Cancer
|
|
Aurora Kinases-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10 .
|
-
- HY-122650
-
|
|
Autophagy
|
Cancer
|
|
PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
|
-
- HY-109583
-
|
4-Oxo-4-HPR
|
Apoptosis
Reactive Oxygen Species
Drug Metabolite
|
Cancer
|
|
4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
|
-
- HY-N2460
-
-
- HY-147803
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
TrxR-IN-5 (compound 4f) is a potent TrxR (thioredoxin reductase) inhibitor, with an IC50 of 0.16 μM. TrxR-IN-5 increases the levels of ROS, thus leading to potent antiproliferative effects. TrxR-IN-5 exhibits prominent anticacer and anti-metastasis effects .
|
-
- HY-119995
-
|
|
Apoptosis
Histamine Receptor
|
Cardiovascular Disease
Cancer
|
|
Chloropyramine is competitive reversible H1 receptor antagonist. Chloropyramine also has anti-tumour activity in breast cancer. Chloropyramine can be used for the research of allergic conditions, such as conjunctivitis and bronchial asthma .
|
-
- HY-123611
-
|
RX-5902
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM .
|
-
- HY-118762
-
|
|
Cathepsin
|
Cancer
|
|
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 .
|
-
- HY-147373
-
|
|
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 .
|
-
- HY-N10577
-
|
|
TGF-beta/Smad
|
Cancer
|
|
Chlorfortunone A is a novel sesquiterpenoid dimers, can be isolated from the roots of Chloranthus fortunei. Chlorfortunone A inhibits transforming growth factor (TGF)-β activity .
|
-
- HY-157135
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCAIX-IN-19 is a sulfonamides inhibitor against hCA IX with an inhibition constant (KI ) of 6.2 nM and show good selectivity over hCA I (hCA I/ hCA IX = 117) .
|
-
- HY-132302
-
|
|
Akt
PKA
PKC
ROCK
Ribosomal S6 Kinase (RSK)
SGK
|
Cancer
|
|
Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
|
-
- HY-132302A
-
|
|
Akt
PKA
PKC
ROCK
Ribosomal S6 Kinase (RSK)
SGK
|
Cancer
|
|
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
|
-
- HY-146740
-
|
|
PD-1/PD-L1
|
Cancer
|
|
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 .
|
-
- HY-122182
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
OTS193320, a imidazo[1,2-a]pyridine compound, is a SUV39H2 methyltransferase activity inhibitor. OTS193320 decreases global histone H3 lysine 9 tri-methylation levels in breast cancer cells and triggers apoptotic cell death. Combination of OTS193320 with Doxorubicin (DOX; HY-15142A) results in reduction of γ-H2AX levels as well as cancer cell viability compared to a single agent OTS193320 or DOX .
|
-
- HY-138071
-
|
8αTGH
|
STAT
Pyroptosis
Apoptosis
Reactive Oxygen Species
c-Myc
Bcl-2 Family
TrxR
|
Cancer
|
|
8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo .
|
-
- HY-114657A
-
|
|
Arp2/3 Complex
|
Inflammation/Immunology
Cancer
|
|
Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis .
|
-
- HY-149486
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor 7 (compound 5) is an inhibitor of FGFR1 Tyrosine Kinase with IC50 value of 0.33 nM. FGFR1 inhibitor 7 shows broad-spectrum cytotoxicity agasinst human cancer cell lines, and inhibits MOLT3 cells with IC50 of 2.1 μM .
|
-
- HY-14543
-
-
| Cat. No. |
Product Name |
Type |
-
- HY-15150G
-
|
R428 (GMP); BGB324 (GMP)
|
Fluorescent Dye
|
|
Bemcentinib (R428) GMP is an orally active and selective inhibitor of Axl with an IC50 of 14 nM .
|
| Cat. No. |
Product Name |
Type |
-
- HY-139109
-
|
ADS 780WS
|
Biochemical Assay Reagents
|
|
IR-783 (ADS 780WS) is a near-infrared (NIR) heptamethine cyanine fluorescent probe. IR-783 significantly inhibits tumour growth and induces apoptosis in MDA-MB-231 xenograft model. IR-783 can be used to study breast cancer .
|
-
- HY-15150G
-
|
R428 (GMP); BGB324 (GMP)
|
Biochemical Assay Reagents
|
|
Bemcentinib (R428) GMP is an orally active and selective inhibitor of Axl with an IC50 of 14 nM .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3212
-
|
|
Peptides
|
Cancer
|
|
Allo-aca, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca blocks leptin signaling and action in numerous in vitro and in vivo models .
|
-
- HY-P5831
-
|
|
Peptides
|
Cancer
|
|
Biotin-H10 is a specific anterior gradient homolog 2 (AGR2) inhibitor with a KD of 6.4 nM. Biotin-H10 inhibits cancer cells viability .
|
-
- HY-P1411
-
|
PcTx1; Psalmopoeus caMBridgei toxin-1
|
Sodium Channel
Apoptosis
|
Neurological Disease
Cancer
|
|
Psalmotoxin 1 (PcTx1) is a protein toxin that can bind at subunit-subunit interfaces of acid-sensing ion channel 1a (ASIC1a). Psalmotoxin 1 is a potent and slective ASIC1a inhibitor (IC50: 0.9 nM) by increasing the apparent affinity for H + of ASIC1a. Psalmotoxin 1 can induce cell apoptosis, also inhibits cell migration, proferliration and invasion of cancer cells. Psalmotoxin 1 can be used in the research of cancers, or neurological disease .
|
-
- HY-P3212A
-
|
|
Peptides
|
Cancer
|
|
Allo-aca TFA, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca TFA blocks leptin signaling and action in numerous in vitro and in vivo models .
|
-
- HY-P2588
-
|
|
Peptides
|
Inflammation/Immunology
Cancer
|
|
Osteocalcin (1-49) (human) is a vitamin K-dependent bone specific protein. Osteocalcin (1-49) (human) is chemotactic for several of the cell types frequently found at bone remodeling surfaces .
|
-
- 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 .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99697
-
|
PRO 140
|
CCR
HIV
|
Infection
Cancer
|
|
Leronlimab (PRO 140) is a humanized IgG4 anti-CCR5 monoclonal antibody. Leronlimab inhibits CCR5-mediated HIV-1 viral and lung metastasis in mouse tumor models. Leronlimab can be used for the research of HIV nonalcoholic steatohepatitis (NASH) and cancer .
|
-
- HY-P99813
-
|
HER3-DXd
|
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-P99675
-
|
AK112
|
PD-1/PD-L1
VEGFR
|
Cancer
|
|
Ivonescimab (AK112) is a PD-1/VEGF Bispecific Antibody. Ivonescimab can be used for cancer research .
|
-
- HY-P99734
-
|
ADCT-601
|
TAM Receptor
|
Cancer
|
|
Mipasetamab uzoptirine (ADCT-601) is an AXL-targeted antibody-drug conjugates (ADCs). Mipasetamab uzoptirine consists of a humanized anti-AXL antibody, a cleavable linker and the potent pyrrolobenzodiazepine (PBD) dimer cytotoxin SG3199. Mipasetamab uzoptirine can be used for the research of cancers .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
|
Classification |
-
- HY-15861
-
|
TGP-210
|
|
Azide
|
|
Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM) . Targapremir-210 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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- HY-135699
-
TD52
1 Publications Verification
|
|
Alkynes
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TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity . TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-135699A
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Alkynes
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TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity . TD52 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-157411
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Alkynes
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anti-TNBC agent-5 (compound 10C) is a triple-negative breast cancer (TNBC) inhibitor with good stability and pharmacokinetic properties. anti-TNBC agent-5 exhibits antiproliferative activity against a variety of cancer cells. anti-TNBC agent-5 can also effectively inhibit TNBC lung metastasis activity in the MDA-MB-231 xenograft model. anti-TNBC agent-5 can be used in cancer research .
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