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Enzastaurin

Chemical Structure : Enzastaurin

CAS No.: 170364-57-5

Enzastaurin (LY317615;LY-317615;LY 317615)

Catalog No.: PC-42542Not For Human Use, Lab Use Only.

Enzastaurin (LY317615) is a potent, selective, ATP-competitive PKCβ inhibitor with IC50 of 6 nM.

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Biological Activity

Enzastaurin (LY317615) is a potent, selective, ATP-competitive PKCβ inhibitor with IC50 of 6 nM.
Enzastaurin (LY317615) weakly inhibits PKCα, PKCγ, and PKCε with IC50 of 39, 83, and 110 nM, respectively.
Enzastaurin (LY317615) induces apoptosis and suppresses the proliferation of tumor cells, suppresses the phosphorylation of GSK3β Ser9, ribosomal protein S6(S240/244) and AKT(Thr308).
Enzastaurin (LY317615) suppresses tumor growth through multiple mechanism in vivo; orally active.

Physicochemical Properties

M.Wt 515.605
Formula C32H29N5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Pyrrole-2,5-dione, 3-(1-methyl-1H-indol-3-yl)-4-[1-[1-(2-pyridinylmethyl)-4-piperidinyl]-1H-indol-3-yl]-

References

1. Graff JR, et al. Cancer Res. 2005 Aug 15;65(16):7462-9.

2. Faul MM, et al. Bioorg Med Chem Lett. 2003 Jun 2;13(11):1857-9.

3. Querfeld C, et al. J Invest Dermatol. 2006 Jul;126(7):1641-7.

4. Rizvi MA, et al. Mol Cancer Ther. 2006 Jul;5(7):1783-9.

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