CRT0066854

CRT0066854 is an inhibitor of PKCiota and PKCzeta (IC50s = 132 and 639 nM, respectively). It also inhibits the Rho-associated kinase II (ROCK2) kinase domain (IC50 = 620 nM). It is selective for these atypical PKCs and ROCK2 over typical PKCs and 98 other kinases in a panel at 1 µM. CRT0066854 decreases phosphorylation of the atypical PKC substrate lethal giant larvae 2 (LLGL2) in HEK293 cells expressing PKCiota and LLGL2. It decreases viability of A549 lung carcinoma cells (IC50 = 3.47 µM) and decreases colony formation in HeLa cells by 65% when used at a concentration of 1 µM. CRT0066854 impairs lumen formation in MDCK cells in a Matrigel(TM) assay and migration of NRK-49F cells in a wound assay.Formal Name: (2S)-3-phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propanediamine. CAS Number: 1438881-19-6. Molecular Formula: C24H25N5S. Formula Weight: 415.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 30 mg/ml. lambdamax: 227, 254, 288, 350 nm. SMILES: N[C@@H](CC1=CC=CC=C1)CNC2=C3C(SC4=C3CCCC4)=NC(C5=CC=NC=C5)=N2. InChi Code: InChI=1S/C24H25N5S/c25-18(14-16-6-2-1-3-7-16)15-27-23-21-19-8-4-5-9-20(19)30-24(21)29-22(28-23)17-10-12-26-13-11-17/h1-3,6-7,10-13,18H,4-5,8-9,14-15,25H2,(H,27,28,29)/t18-/m0/s1. InChi Key: NRHASZRDWOUMFD-SFHVURJKSA-N.