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)
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
PKCα; PKCβ; PKCγ; PKCε
Available Sizes
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