AdipoGen CRT0066101 HCl
Chemical. CAS 1781742-22-0. Formula C18H22N6O . 3HCl. MW 338.4 . 109.4. CRT0066101 is an inhibitor of all three PKD isoforms IC50s = 1, 2.5, and 2 nM for PKD1, PKD2 and PKD3, respectively. It exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCalpha, PKBalpha, MEK, ERK, c-Raf, c-Src and c-Abl. PKD family members play an important role in regulating several cellular processes and activities, including chromatin organization, Golgi function, gene expression, cell survival, adhesion, motility, differentiation, DNA synthesis and proliferation. CRT0066101 shows anticancer activity by blocking cell proliferation, inducing apoptosis, G2/M phase arrest, inhibiting migration and invasion and reducing the viability of several cancer cells both in vitro and in vivo.