170364-57-5
170364-57-5
Chemical Structure
Enzastaurin
Synonym(s): LY317615
- CAS 番号: 170364-57-5
- Formula:C32H29N5O2
- Molecular Weight:515.61
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
InChIKey: AXRCEOKUDYDWLF-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
Biological Activity: Enzastaurin (LY317615) is a potent, selective, and CNS-penetrant PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε[1][2][3][4].
| 製品番号 | 製品名 | 純度 | 製品説明 | Pricing | |||||||||||||||||||
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Enzastaurin | 99.80% | Enzastaurin (LY317615) is a potent, selective, and CNS-penetrant PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε. | ||||||||||||||||||||
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Enzastaurin (Standard) | ≥98% | Enzastaurin (Standard) is the analytical standard of Enzastaurin. This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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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]
- [4]. Grønberg BH, et al. A placebo-controlled, randomized phase II study of maintenance enzastaurin following whole brain radiation therapy in the treatment of brain metastases from lung cancer. Lung Cancer. 2012 Oct;78(1):63-9. [Content Brief]
