KCC009

An inhibitor of TG2 (Ki = 0.068 mM), reduces radiation-induced increases in TGM2 expression in wild-type H1299 and H1299/M175H-p53 cells at 3.91 µM, sensitizes wild-type H1299 and H1299/M175H-p53 cells to radiation and induces cell cycle arrest at the G0/G1 and G2/M phases, respectively, inhibits fibronectin remodeling in U87MG glioblastoma cells at 1 mM, sensitizes tumors to N,N'-bis(2-chloroethyl)-N-nitrosourea and increases survival in an orthotopic mouse model of DBT-FG glioblastoma when administered in combination with N,N'-bis(2-chloroethyl)-N-nitrosourea at 50 mg/kg, reverses warfarin-induced arterial calcification in rats, prevents relapse in a rat model of EAE. Formulation: A solid. InChI: InChI=1S/C21H22BrN3O5/c22-19-11-17(30-25-19)12-23-20(27)18(10-14-6-8-16(26)9-7-14)24-21(28)29-13-15-4-2-1-3-5-15/h1-9,17-18,26H,10-13H2,(H,23,27)(H,24,28)/t17?,18-/m0/s1. InChIKey: MRULUIQNANUWTK-ZVAWYAOSSA-N. SMILES: O=C(N[C@@H](CC1=CC=C(O)C=C1)C(NCC2ON=C(Br)C2)=O)OCC3=CC=CC=C3