G-5555

G-5555 is an inhibitor of p21-activated kinase 1 (PAK1, Ki = 3.7 nM), a non-receptor serine/threonine kinase involved in tumorigenesis. It is selective for PAK1 over the majority of targets in a panel of 235 kinases but does inhibit PAK2, PAK3, KHS1, LCK, MST3, MST4, SIK2, and YSK1 by greater than 70% with IC50 values ranging from 9 to 52 nM. G-5555 inhibits phosphorylation of MEK, a downstream target of PAK1, in EBC1 cells (IC50 = 69 nM). G-5555 (10, 20, and 30 mg/kg) dose-dependently reduces phosphorylation of MEK in tumors from an H292 non-small cell lung cancer (NSCLC) mouse xenograft model. G-5555 inhibits hERG channels less than 50% at a concentration of 10 µM, indicating the potential for a low risk of QT interval prolongation and potentially fatal arrhythmias.Formal Name: 8-[(trans-5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one. CAS Number: 1648863-90-4. Molecular Formula: C25H25ClN6O3. Formula Weight: 493.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMSO: 25 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.20 mg/ml. lambdamax: 304, 353 nm. SMILES: CNC1=NC=C(C=C(C2=C(Cl)C=C(C3=NC(C)=CC=C3)C=C2)C(N4C[C@@H]5OC[C@@H](N)CO5)=O)C4=N1. InChi Code: InChI=1S/C25H25ClN6O3/c1-14-4-3-5-21(30-14)15-6-7-18(20(26)9-15)19-8-16-10-29-25(28-2)31-23(16)32(24(19)33)11-22-34-12-17(27)13-35-22/h3-10,17,22H,11-13,27H2,1-2H3,(H,28,29,31)/t17-,22-. InChi Key: ZBCMHWUFWQFPLV-VVOJOOEHSA-N.