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Granta-519

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-126256A
    PRMT5-IN-1 hydrochloride

    		Histone Methyltransferase Cancer
    PRMT5 IN-1 hydrochloride (compound 9), a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 hydrochloride can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions .
    PRMT5-IN-1 hydrochloride
  • HY-136250
    BSJ-03-204

    		PROTACs CDK Cancer
    BSJ-03-204 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity .
    BSJ-03-204
  • HY-136250A
    BSJ-03-204 triTFA

    		PROTACs CDK Cancer
    BSJ-03-204 triTFA is a PROTAC connected by ligands for Cereblon and CDK. BSJ-03-204 triTFA is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and has anti-cancer activity .
    BSJ-03-204 triTFA
  • HY-12137
    Volasertib
    20+ Cited Publications

    BI 6727

    		 Polo-like Kinase (PLK) Apoptosis Cancer
    Volasertib (BI 6727) is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib induces mitotic arrest and apoptosis. Volasertib, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
    Volasertib
  • HY-136342
    Antitumor agent-23

    		Others Cancer
    Antitumor agent-23 is a potent anti-cancer agent with GI50s of 38, 48, 5, 27, 80, and 28 nM for lymphoma cell line GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI, respectively. Antitumoral activity .
    Antitumor agent-23
  • HY-168190
    PROTAC TBL1X degrader-1

    		PROTACs Cancer
    PROTAC TBL1X degrader-1 (Compound TD11) is a PROTAC degrader for Transducin β-like protein 1 X-linked (TBL1X), and exhibits cytotoxicity in lymphoma cell Riva, Pfeiffer and Granta-519 with IC50 of 0.795, 0.397 and 0.522 μM, respectively. (Pink: ligand for target protein: TBL1X ligand 1 (HY-168191); Black: linker (HY-168193); Blue: ligand for E3 ligase: Thalidomide 4-fluoride (HY-41547))
    PROTAC TBL1X degrader-1
  • HY-126256
    PRMT5-IN-1

    		Histone Methyltransferase Cancer
    PRMT5 IN-1, a hemiaminal, is a potent, selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions .
    PRMT5-IN-1
  • HY-12137A
    Volasertib trihydrochloride

    BI 6727 trihydrochloride

    		 Polo-like Kinase (PLK) Apoptosis Cancer
    Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models .
    Volasertib trihydrochloride

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