1438881-19-6

CRT0066854 is an inhibitor of PKCι and PKCζ (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 PKCι 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™ assay and migration of NRK-49F cells in a wound assay.

(2S)-3-Phenyl-N1-[5,6,7,8-tetrahydro-2-(4-pyridinyl)[1]benzothieno[2,3-d]pyrimidin-4-yl]-1,2-propanediamine, is used in the synthesis of synthesis of Alpha protein kinase C (PKC) inhibitor.