359017-79-1
359017-79-1
Chemical Structure
Enzastaurin hydrochloride
Synonym(s): LY317615 hydrochloride
- CAS No.: 359017-79-1
- Formula:C32H30ClN5O2
- Molecular Weight:552.07
IUPAC Name: 3-(1-methyl-1H-indol-3-yl)-4-(1-(1-(pyridin-2-ylmethyl)piperidin-4-yl)-1H-indol-3-yl)-1H-pyrrole-2,5-dione hydrochloride
InChIKey: UUADYKVKJIMIPA-UHFFFAOYSA-N
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.Cl
Biological Activity: Enzastaurin (LY317615) hydrochloride 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][2][3].
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Enzastaurin hydrochloride | Enzastaurin (LY317615) hydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε. | |||||||||||||||||||||
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References
- [1]. 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), [Content Brief]
- [2]. Rovedo MA, et al. Inhibition of glycogen synthase kinase-3 increases the cytotoxicity of enzastaurin. J Invest Dermatol, 2011, 131(7), 1442-1449. [Content Brief]
- [3]. 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. [Content Brief]
