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G0/G1+arrest

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-163985
    PROTAC FGFR2 degrader 1

    		PROTACs FGFR Apoptosis Cancer
    PROTAC FGFR2 degrader 1 (compound N5) is a PROTAC that effectively targets FGFR2 with DC50 of 6.46 nM, the FGFR2 IC50 is 0.08 nM. PROTAC FGFR2 degrader 1 has anti-proliferative activity and highly selective, induces G0/G1 arrest of KATOIII and SNU16 cell cycle and inhibits apoptosis by reducing the activation of p-ERK and p-PLCγ, the downstream proteins of FGFR2. PROTAC FGFR2 degrader 1 inhibits gastric cancer cells remained above 50% at a concentration of 0.17 nM. PROTAC FGFR2 degrader 1 potently inhibits the growth of SNU16 xenograft tumors in mouse model (Structure Note: Pink, FGFR2 activator: HY-18708; Blue, E3 ligase ligand: HY--10984; Black, linker: HY-163989; E3 ligase ligand + linker：HY-163986) [1].
    PROTAC FGFR2 degrader 1
  • HY-120458
    LCAHA
    1 Publications Verification

    LCA hydroxyamide

    		 Deubiquitinase Cancer
    LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a [1].
    LCAHA
  • HY-179143
    EGFR-IN-185

    		EGFR Akt Apoptosis Cancer
    EGFR-IN-185 is a EGFR inhibitor. EGFR-IN-185 exhibits potent activity against non-small cell lung cancer (NSCLC) cells harboring EGFR mutations. EGFR-IN-185 inhibits colony formation and migration, induces G0/G1 arrest, and promots apoptosis, which are associated with the suppression of EGFR and AKT phosphorylation. EGFR-IN-185 can be used for the research of  NSCLC [1].
    EGFR-IN-185
  • HY-157148
    1D228

    		c-Met/HGFR Trk Receptor Cancer
    1D228 is a c-Met/TRK inhibitor with antitumor activity. 1D228 inhibits cyclin D1 to induce G0/G1 arrest and inhibit cancer cell proliferation and migration. 1D228 can be used in the study of gastric, liver and vascular tumors [1].
    1D228
  • HY-163090
    HR488B

    		HDAC Reactive Oxygen Species (ROS) Apoptosis Cancer
    HR488B is an efficient HDAC1 inhibitor. HR488B specifically suppressed the growth of CRC cells by inducing cell cycle G0/G1 arrest and apoptosis. HR488B causes mitochondrial dysfunction, reactive oxygen species (ROS) generation, and DNA damage accumulation [1].
    HR488B
  • HY-163160
    BET-IN-23

    		Apoptosis Epigenetic Reader Domain Cancer
    Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro [1].
    BET-IN-23
  • HY-150609
    SHP2/CDK4-IN-1

    		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 [1].
    SHP2/CDK4-IN-1

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