Enzastaurin

Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε[1].

Product Specifications

CAS Number

[170364-57-5]

Product Name Alternative

LY317615

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Autophagy; PKC

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Epigenetics; TGF-beta/Smad

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Enzastaurin.html

Purity

99.80

Solubility

DMSO : 8.33 mg/mL (ultrasonic)

Smiles

O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3C4=CN(C5CCN(CC6=NC=CC=C6)CC5)C7=C4C=CC=C7)NC3=O

Molecular Formula

C32H29N5O2

Molecular Weight

515.61

Precautions

H302, H315, H319, H335

References & Citations

[1]Rovedo MA, et al. Inhibition of glycogen synthase kinase-3 increases the cytotoxicity of enzastaurin. J Invest Dermatol, 2011, 131 (7), 1442-1449.|[2]Podar K, et al. Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl) . Blood, 2007, 109 (4), 1669-1677.|[3]Graff JR, et al. 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. Cancer Res, 2005, 65 (16)