SB 218078

SB 218078 is an inhibitor of checkpoint kinase 1 (Chk1) that blocks phosphorylation of cdc25 with an IC50 value of 15 nM. It less potently inhibits cdc2 and PKC (IC50s = 250 and 1,000 nM, respectively) and causes 85% inhibition of PKD1 at 1 µM. SB 218078 releases G2 cell cycle arrest induced by gamma-irradiation or the topoisomerase I inhibitor topotecan (Cay-14129). In this way, SB 218078 enhances the cytotoxicity of DNA-damaging compounds.Formal Name: 9,10,11,12-tetrahydro-9,12-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-1,3(2H)-dione. CAS Number: 135897-06-2. Molecular Formula: C24H15N3O3. Formula Weight: 393.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS(pH7.2) (1:2): 0.3 mg/ml, DMSO: 5 mg/ml. lambdamax: 237, 278, 287, 318, 414 nm. SMILES: O=C(NC1=O)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5C7OC(CC7)N4C8=C3C=CC=C8. InChi Code: InChI=1S/C24H15N3O3/c28-23-19-17-11-5-1-3-7-13(11)26-15-9-10-16(30-15)27-14-8-4-2-6-12(14)18(22(27)21(17)26)20(19)24(29)25-23/h1-8,15-16H,9-10H2,(H,25,28,29). InChi Key: OTPNDVKVEAIXTI-UHFFFAOYSA-N.