Enzastaurin (LY317615) is a potent PKC beta inhibitor for PKCβ, PKCα, PKCγ and PKCε with IC50 of 6 nM, 39 nM, 83 nM and 110 nM, respectively. Enzastaurin inhibits growth in all MM cell lines investigated, including MM.1S, MM.1R, RPMI 8226 (RPMI), RPMI-Dox40 (Dox40), NCI-H929, KMS-11, OPM-2, and U266, with IC50 values ranging from 0.6 to 1.6 μM. Enzastaurin induces apoptosis and suppresses proliferation in cultured tumor cells, including malignant lymphocytes of CTCL. Enzastaurin also suppresses the phosphorylation of GSK3βser9, ribosomal protein S6S240/244, and AKTThr308. Enzastaurin is an inhibitor of Akt and GSK-3 beta.
Soluble in DMSO (30 mg/ml at 25° C), water (< 1 mg/ml at 25° C), ethanol (< 1 mg/ml at 25° C), DMF (~16.6 mg/ml), and 1:3 solution of DMF:PBS(pH 7.2) (~0.25 mg/ml).
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Saba et alSaba et al. (PubMed ID 26298175) found that enzastaurin induced growth inhibition in B-cell acute lymphoblastic leukemia cell lines by preventing GSK3 phosphorylation and inducing -catenin accumulation. -SCBT Publication Review
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