Chk2 Inhibitor

Chk2 inhibitor is an inhibitor of checkpoint kinase 2 (Chk2, IC50 = 13.5 nM). It is selective for Chk2 over Chk1 (IC50 = 220.4 nM). It inhibits Chk2 autophosphorylation at the serine in position 516 in non-cancerous 184B5 cells that contain wild-type p53 and in MDA-MB-231 cells that contain mutated p53 when used at concentrations ranging from 0.1 to 30 µM. Chk2 inhibitor enhances survival of 184B5, but not MDA-MB-231, cells following ionizing radiation and inhibits cell cycle arrest at the G2 stage induced by ionizing radiation in 184B5 cells. It also inhibits the production of IL-2 in Jurkat cells stimulated by phorbol 12-myristate 13-acetate (PMA, Cay-10008014) and the production of TNF-alpha in LPS-stimulated THP-1 cells (IC50s = 3.5 and 8.2 µM, respectively). Chk2 inhibitor also inhibits the growth of CEM leukemia T cells (GI50 = 1.73 µM).Formal Name: (5Z)-5-(2-amino-1,5-dihydro-5-oxo-4H-imidazol-4-ylidene)-3,4,5,10-tetrahydro-azepino[3,4-b]indol-1(2H)-one. CAS Number: 724708-21-8. Synonyms: SC-203885. Molecular Formula: C15H13N5O2. Formula Weight: 295.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: Soluble. lambdamax: 236, 297, 355 nm. SMILES: O=C(NCC/1)C2=C(C(C=CC=C3)=C3N2)C1=C4NC(N)=NC/4=O. InChi Code: InChI=1S/C15H13N5O2/c16-15-19-11(14(22)20-15)8-5-6-17-13(21)12-10(8)7-3-1-2-4-9(7)18-12/h1-4,18H,5-6H2,(H,17,21)(H3,16,19,20,22)/b11-8-. InChi Key: SMPPSGXPGZSJCP-FLIBITNWSA-N.