NSC 109555

NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2, IC50 = 200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50 = 240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro. NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.Formal Name: 2,2'-[carbonylbis(imino-4,1-phenyleneethylidyne)]bis-hydrazinecarboximidamide, dimethanesulfonate. CAS Number: 15427-93-7. Synonyms: DDUG, NCI C04808. Molecular Formula: C19H24N10O . 2CH3SO3H. Formula Weight: 600.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 20 mg/ml, Ethanol: 3 mg/ml, PBS (pH 7.2): 10 mg/ml. lambdamax: 226, 320 nm. SMILES: C/C(C1=CC=C(NC(NC2=CC=C(/C(C)=N/NC(N)=N)C=C2)=O)C=C1)=N\NC(N)=N.O=S(C)(O)=O.O=S(C)(O)=O. InChi Code: InChI=1S/C19H24N10O.2CH4O3S/c1-11(26-28-17(20)21)13-3-7-15(8-4-13)24-19(30)25-16-9-5-14(6-10-16)12(2)27-29-18(22)23,2*1-5(2,3)4/h3-10H,1-2H3,(H4,20,21,28)(H4,22,23,29)(H2,24,25,30),2*1H3,(H,2,3,4)/b26-11+,27-12+,,. InChi Key: HXDBGZUARNKHBV-XMDRLFCYSA-N.