Description
Enzastaurin (170364-57-5) is a potent and selective PKCβ inhibitor. IC50 = 6, 39, 83 and 110 nM, for PKCβ, PKCα, PKCγ and PKCε respectively.1 Induces apoptosis in multiple myeloma cell lines via inhibition of the AKT signaling pathway.2 Induces mitotic missegregation and preferential cytotoxicity in colorectal cancer cells with chromosomal instability.3 Attenuates amphetamine-stimulated dopamine efflux.4 Inhibits blood-brain barrier leakiness in a mouse model.5
References
[1] JEREMY R GRAFF. The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts.[J]. Cancer research, 2005, 65 16: 7462-7469. DOI:
10.1158/0008-5472.can-05-0071[2] MUJAHID A RIZVI. Enzastaurin (LY317615), a protein kinase Cbeta inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines.[J]. Molecular Cancer Therapeutics, 2006, 5 7: 1783-1789. DOI:
10.1158/1535-7163.mct-05-0465[3] DJAMILA OUARET Annette K L. Protein kinase C β inhibition by enzastaurin leads to mitotic missegregation and preferential cytotoxicity toward colorectal cancer cells with chromosomal instability (CIN).[J]. Cell Cycle, 2014, 13 17: 2697-2706. DOI:
10.4161/15384101.2015.945383[4] ALEXANDER G. ZESTOS. PKCβ Inhibitors Attenuate Amphetamine-Stimulated Dopamine Efflux[J]. ACS Chemical Neuroscience, 2016, 7 6: 757-766. DOI:
10.1021/acschemneuro.6b00028[5] ALEXIS M STRANAHAN. Blood-brain barrier breakdown promotes macrophage infiltration and cognitive impairment in leptin receptor-deficient mice.[J]. Journal of Applied Physics, 2016, 64 1: 2108-2121. DOI:
10.1177/0271678x16642233
