Search Result
Results for "
clonogenicity
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-172262
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VDAC
Bcl-2 Family
Apoptosis
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Cancer
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WEHI-3773 is a VDAC2 ligand and apoptosis modulator. WEHI-3773 directly binds to the β7-β10 region of VDAC2 and disrupts its interaction with BAX and BAK. WEHI-3773 regulates BAX-mediated apoptosis in BAK-deficient cells by modulating conformational activation of BAX, mitochondrial redistribution, and cytochrome c release. WEHI-3773 overcomes Venetoclax (HY-15531) resistance, resensitizes leukemia cells carrying BAX mutations to BH3 mimetics, and enables long-term clonogenic survival of BAK-deficient cells treated with BH3 mimetics. WEHI-3773 is applicable to research related to acute myeloid leukemia .
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- HY-13297
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E1/E2/E3 Enzyme
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Cancer
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PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells .
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- HY-P99899
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PR-1498487
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ADC Antibody
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Cancer
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Samrotamab (PR-1498487) is a humanized IgG1-κ chimeric antibody targeting LRRC15. Samrotamab markedly reduces bladder cancer cells viability and inhibits clonogenic growth, migratory and invasive capabilities. Samrotamab significantly increases LRRC15 mRNA level while suppressing SCG5 mRNA expression. Samrotamab can be used for synthesis of ADC ABBV-085 .
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- HY-122590
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Gli
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Cancer
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Glabrescione B is the first compound that binds the Hedgehog (Hh) modulator Gli1. Glabrescione B impairs its activity by interfering with Gli1-DNA interaction. Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells, the self-renewal ability, and clonogenicity of tumor-derived stem cells .
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- HY-138537
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IKK
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Cancer
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NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells .
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- HY-159147
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PROTACs
ROS Kinase
Apoptosis
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Cancer
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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- HY-123141
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Pim
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Cancer
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K00135 is a potent and selective inhibitor of PIM kinases. K00135 inhibits survival and clonogenic growth of acute leukemia cells. K00135 inhibits the phosphorylation of PIM downstream targets .
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- HY-178164
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Apoptosis
Akt
mTOR
STAT
NF-κB
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Cancer
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HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor (KD = 38.4 nM). HBS-101 significantly reduces cell viability, clonogenic survival, and invasiveness and increases apoptosis. HBS-101 involves suppression of the Akt/mTOR, STAT3, and NF-κB pathways. HBS-101 can be used for the study of Triple-negative breast cancer (TNBC) .
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- HY-P99707
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HH1
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Apoptosis
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Cancer
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Lilotomab (HH1) is a murine anti-CD37 monoclonal antibody. Lilotomab reduces clonogenic survival. Lilotomab shows anti-tumor activity .
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- HY-172824
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Deubiquitinase
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Cancer
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MS7131 is a USP1-recruiting DUBTACs. MS7131 effectively reduces histone H3 lysine 27 trimethylation and significantly suppresses the proliferation and clonogenicity of cancer cells .
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- HY-175243
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Adenosine Deaminase
Apoptosis
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Cancer
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ADAR1-IN-1 is a potent ADAR1 inhibitor. ADAR1-IN-1 significantly suppressed DU-145 cell proliferation (IC50 = 1.11 μM), clonogenicity, migration, and invasion, arrests cell cycle, and induces apoptosis. ADAR1-IN-1 safely and effectively inhibits tumor growth. ADAR1-IN-1 can be used for the study of prostate cancer (PCa) .
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- HY-179095
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Ligands for Target Protein for PROTAC
IRAK
NF-κB
p38 MAPK
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Cancer
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UR241-2 is an IRAK4 inhibitor. UR241-2 suppresses IL-1–induced IRAK1/4 signaling, NF-κβ activation, and phosphorylation of p65 and p38. UR241-2 selectively inhibits leukemia stem cell clonogenicity. UR241-2 can serve as a ligand for target proteins for PROTAC, facilitating the development and design of PROTAC degraders for IRAK4. UR241-2 can be used in the research of acute myeloid leukemia .
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- HY-179228
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CTLA-4
TGF-beta/Smad
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Cancer
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AN02 is a derivative of Curcumin (HY-N0005). AN02 inhibits the proliferation and clonogenicity, migration and invasion of ovarian cancer cells. AN02 dose-dependently upregulates the expression of APC and mediates the degradation of CTLA-4 through SMAD4. In the small xenograft model, AN02 significantly inhibits tumor growth and reverses the tumor immune-suppressive microenvironment. AN02, when combined with Ipilimumab (HY-P9901), can enhance efficacy and inhibit epithelial-mesenchymal transition. AN02 can be used for the study of ovarian cancer .
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- HY-162966
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Cyclic GMP-AMP Synthase
PROTACs
STING
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Cancer
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MS7829 is a deubiquitinase-targeting chimera (DUBTAC) that targets cGAS. MS7829 recruits OTUB1 to cGAS, binds covalently to OTUB1, stabilizes the protein abundance of cGAS, and activates the cGAS-STING-IRF3 innate immune signaling pathway in an OTUB1-dependent manner. MS7829 is applicable to cancer-related research .
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- HY-139211
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3,4-Difluorobenzylidene curcumin
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Reactive Oxygen Species (ROS)
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Cancer
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Difluorinated Curcumin (3,4-Difluorobenzylidene curcumin) is a fluorinated curcumin analog with high bioavailability and anticancer activity. Difluorinated Curcumin inhibits the self-renewal ability of tumor stem/stem-like cells, clonogenicity, invasiveness and angiogenesis of tumor cells. Difluorinated Curcumin also increases cell sensitivity to chemotherapy .
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- HY-175030
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HDAC
Apoptosis
Pyroptosis
Necroptosis
PANoptosis
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Cancer
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TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC50 of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer .
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- HY-155852
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Ferroptosis
Apoptosis
ACSL Family
Glutathione Peroxidase
Reactive Oxygen Species (ROS)
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Inflammation/Immunology
Cancer
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Lepadin H is a ferroptosis inducer and apoptosis inducer with in vitro cytotoxicity and in vivo antitumor efficacy against cancer cells. Lepadin H reduces GPX4 and SLC7A11 levels, increases p53 and ACSL4 expression, drives lipid hydroperoxide production, elevates reactive oxygen species (ROS) levels, reduces cellular glutathione (GSH) levels, induces lipid peroxidation and G2/M phase cell cycle arrest, and suppresses clonogenic growth and migration of cancer cells.Lepadin H can be used for the research of melanoma .
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- HY-W783415
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FAK
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Cancer
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STARD3-IN-1 (Compound VS1) is a STARD3 inhibitor with an IC₅₀ of 35 μM. STARD3 is a protein that is overexpressed in various cancers and is involved in cholesterol transport. STARD3-IN-1 exhibits anti-proliferative activity in breast cancer and colon cancer cells, significantly weakening the clonogenic ability of cancer cells. STARD3-IN-1 increases the protein levels of FAK and pTyr397-FAK. STARD3-IN-1 can be used for research on breast cancer and colon cancer .
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- HY-179388
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PROTACs
Sirtuin
Apoptosis
Akt
mTOR
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Cancer
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PROTAC Sirt2 Degrader-2 is a highly efficient and selective PROTAC degrader targeting SIRT2. PROTAC Sirt2 Degrader-2 demonstrates the most potent anti-proliferative activity both in vitro and in vivo. PROTAC Sirt2 Degrader-2 leads to a marked increase in H4K16Ac levels. PROTAC Sirt2 Degrader-2 significantly suppresses clonogenic formation and migration, induces cell cycle arrest, and promotes apoptosis. PROTAC Sirt2 Degrader-2 inhibits the AKT/mTOR signaling pathway by indirectly degrading SIRT2 and blocking downstream protein phosphorylation, thereby disrupting the signaling cascade and suppressing tumor development. PROTAC Sirt2 Degrader-2 can be used for the study of ovarian cancer .
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- HY-163121
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Glycosyltransferase
TGF-β Receptor
FAK
Galectin
Collagen
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Endocrinology
Cancer
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PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease .
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- HY-N14618
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Src
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Cancer
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Rhodomycin A can suppress lung cancer cell progression via modulating Src-related pathways.?Rhodomycin A significantly suppressed cancer cell proliferation, migration, invasion, and clonogenicity in vitro and tumour growth in vivo .
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- HY-168143
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Histone Methyltransferase
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Cancer
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YD1342 is a prodrug of YD1130, which exhibits potent inhibitory effects on cellular substrate methylation, breast cancer cell clonogenicity, and tumor growth in animal models, exceeding or matching known PRMT4-specific inhibitors. .
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- HY-178325
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin-IN-57 is a Tubulin inhibitor. Tubulin-IN-57 is a potent antiproliferative agent that inhibits clonogenic formation, migration, and invasion of ovarian cancer cells. Tubulin-IN-57 inhibits tubulin polymerization, which in turn induces G2/M arrest and apoptosis in SKOV3 cells. Tubulin-IN-57 demonstrates potent antitumor activity without observable toxicity in an SKOV3 xenograft model. Y60S can be used for the study of ovarian cancer .
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- HY-155781
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COX
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Inflammation/Immunology
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Anti-inflammatory agent 53 (compound 7c) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in S phase and G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
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- HY-155780
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COX
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Inflammation/Immunology
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Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
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- HY-175473
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FLT3
Apoptosis
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Cancer
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HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication
(FLT3-|TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML) .
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- HY-175565
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Microtubule/Tubulin
VEGFR
Reactive Oxygen Species (ROS)
Apoptosis
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Cancer
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Tubulin/VEGFR-2-IN-1 is a dual inhibitor of tubulin and VEGFR-2 (IC50 = 1.52 μM) with anti-angiogenic activity. Tubulin/VEGFR-2-IN-1 exhibits potent cytotoxicity against the cancer cells. Tubulin/VEGFR-2-IN-1 elevates ROS production, induces apoptosis and causes G0/G1 phase arrest in HepG-2 cells. Tubulin/VEGFR-2-IN-1 inhibits the migratory ability and the clonogenic ability in HepG-2 cells. Tubulin/VEGFR-2-IN-1 can be used for the study of cancer .
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- HY-161826
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Wnt
β-catenin
HSP
CDK
c-Myc
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Cancer
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Antitumor agent-174 (Compound 10) directly engages the N-terminal site of Hsp90 and promotes the degradation of β-catenin, thereby suppressing the Wnt/β-catenin signaling. Antitumor agent-174 effectively inhibits proliferation, induce S and G2/M phases arrest and block the clonogenic ability in CRC cells. Antitumor agent-174 down-regulates CDK1, Cyclin D1, c-Myc, Cyclin B1, and Cyclin A2, and upregulaties P21 proteins. Antitumor agent-174 has significant anti-tumor efficacy against colorectal cancer (CRC) with excellent pharmacokinetics and low toxicity .
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- HY-116504
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EGFR
Akt
ERK
Apoptosis
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Cancer
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WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
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- HY-101349
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Dopamine Receptor
Apoptosis
Autophagy
PDGFR
ERK
mTOR
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Neurological Disease
Cancer
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L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma .
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- HY-101349A
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Dopamine Receptor
Apoptosis
Autophagy
PDGFR
ERK
mTOR
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Neurological Disease
Cancer
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L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma .
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- HY-116562
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Drug Derivative
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Cancer
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DK-139 is a polyphenol compound bearing a cinnamaldehyde scaffol. DK-139 inhibits clonogenic growth of Cisplatin (HY-17394)-resistant human ovarian cancer. DK-139 can be used for the research of Cisplatin-resistant ovarian cancer .
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- HY-177995
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Monoisoamyl meso-2,3-dimercaptosuccinic acid
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Reactive Oxygen Species (ROS)
SOD
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Neurological Disease
Cancer
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MiADMSA (Monoisoamyl meso-2,3-dimercaptosuccinic acid) is an orally active thiol chelator that can effectively remove heavy metals such as arsenic and lead from the body of animals. Arsenic binds with two vicinal sulfhydryl groups available in MiADMSA leading to marked reduction in body arsenic burden and also marked reduction in various oxidative stress parameters and antioxidant enzymes like-ROS, nitrite, TBARS, GSH, SOD and catalase. MiADMSA attenuates urinary bladder carcinogenesis, protects against oxidative stress, ameliorates copper-induced histopathology, reverses neurotoxicity, and is safe in animals. MiADMSA can be used in studies of bladder cancer, arsenic, and lead-induced developmental neurotoxicity .
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- HY-183258
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TGF-β Receptor
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Neurological Disease
Cancer
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TGFβ1-IN-5 is a TGF-β1 inhibitor with blood-brain barrier permeability. TGFβ1-IN-5 reduces extracellular TGF-β1 levels in glioblastoma cells. TGFβ1-IN-5 exerts antiproliferative, antimigratory and clonogenic inhibitory effects in glioblastoma cells while maintaining the viability of non-cancerous cells. TGFβ1-IN-5 can be used for the research of glioblastoma .
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- HY-W718262
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(Rac)-CGP 52547
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Antibiotic
Fungal
Bacterial
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Infection
Cancer
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Dihydroaeruginoic acid ((Rac)-CGP 52547), an antifungal antibiotic, is a thiazoline iron chelator. Dihydroaeruginoic acid is the condensation product of salicylate and one cysteine residue. Dihydroaeruginoic acid chelates Fe(III), inhibits DNA replication via ribonucleotide reductase, induces G1/S cell cycle block, reduces leukemia cell clonogenic viability. Dihydroaeruginoic acid inhibits phytopathogenic fungi and bacteria, suppresses Candida albicans development, and inhibits Agrobacterium tumefaciens biofilm formation via extracellular iron sequestration. Dihydroaeruginoic acid can be used for the research of phytopathogenic fungal and bacterial infections, and leukemia .
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- HY-183098
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PROTACs
IKK
Apoptosis
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Cancer
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UNC8209 is a selective PROTAC-based TANK-binding kinase 1 (TBK1) degrader. UNC8209 recruits cereblon (CRBN) to mediate ubiquitin-proteasome pathway-dependent TBK1 degradation and reduces AAK1, GAK, and AURKA abundance. UNC8209 suppresses tumor cell proliferation, impairs in vivo tumor growth, inhibits colony and clonogenic growth and enhances tumor cell sensitivity to TNFα or IFN-γ. UNC8209 modulates cell cycle and induces mild apoptosis. UNC8209 can be used for the research of clear cell renal cell carcinoma, non-small cell lung cancer, pancreatic ductal adenocarcinoma .
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- HY-182285
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5-HT Receptor
DNA/RNA Synthesis
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Cancer
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FOXM1-IN-4 is a selective 5-HT7 receptor inhibitor with a Ki of 92 nM. FOXM1-IN-4 blocks 5-HT7 receptor signaling to reduce FOXM1, p-FOXM1, cyclin B1, and cdc25B levels. FOXM1-IN-4 acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. FOXM1-IN-4 can be used for the research of triple-negative breast cancer .
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- HY-182285A
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5-HT Receptor
DNA/RNA Synthesis
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Cancer
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FOXM1-IN-4 hydrochloride is a selective 5-HT7 receptor inhibitor with a Ki of 92 nM. FOXM1-IN-4 hydrochloride blocks 5-HT7 receptor signaling to reduce FOXM1, p-FOXM1, cyclin B1, and cdc25B levels. FOXM1-IN-4 hydrochloride acts as an antiproliferative, clonogenic inhibitor, and cell cycle inhibitor that induces G2/M arrest, reduces G0/G1 population. FOXM1-IN-4 hydrochloride can be used for the research of triple-negative breast cancer .
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- HY-181080
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Topoisomerase
DNA/RNA Synthesis
Apoptosis
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Cancer
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TOP1/TDP1-IN-1 is a DNA topoisomerase 1B (TOP1) and tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with a TDP1 IC50 of 17.8 μM. TOP1/TDP1-IN-1directly suppresses TOP1 catalytic activity without forming a DNA-TOP1 ternary complex, inhibits TDP1-mediated repair of TOP1-induced DNA damage, and exhibits low acute toxicity. TOP1/TDP1-IN-1 disrupts DNA repair pathways, induces apoptosis, suppresses clonogenic growth, and elicits antiproliferative effects in cancer cells. TOP1/TDP1-IN-1 can be used for the research of non-small cell lung cancer, cervical cancer, colon cancer .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P99899
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PR-1498487
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ADC Antibody
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Cancer
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Samrotamab (PR-1498487) is a humanized IgG1-κ chimeric antibody targeting LRRC15. Samrotamab markedly reduces bladder cancer cells viability and inhibits clonogenic growth, migratory and invasive capabilities. Samrotamab significantly increases LRRC15 mRNA level while suppressing SCG5 mRNA expression. Samrotamab can be used for synthesis of ADC ABBV-085 .
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(5)
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- HY-P99707
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HH1
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Apoptosis
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Cancer
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Lilotomab (HH1) is a murine anti-CD37 monoclonal antibody. Lilotomab reduces clonogenic survival. Lilotomab shows anti-tumor activity .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
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Classification |
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- HY-159147
-
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Azide
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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- HY-178164
-
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Alkynes
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HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor (KD = 38.4 nM). HBS-101 significantly reduces cell viability, clonogenic survival, and invasiveness and increases apoptosis. HBS-101 involves suppression of the Akt/mTOR, STAT3, and NF-κB pathways. HBS-101 can be used for the study of Triple-negative breast cancer (TNBC) .
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