EnzastaurinA potent inhibitor of PKCβ, PKCα, PKCγ and PKCε

Enzastaurin (CAS 170364-57-5)

Enzastaurin | CAS 170364-57-5 is rated 5.0 out of 5 by 1.
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Synonym: LY-317615
Application: A potent inhibitor of PKCβ, PKCα, PKCγ and PKCε
CAS Number: 170364-57-5
Purity: ≥99%
Molecular Weight: 515.60
Molecular Formula: C32H29N5O2
* Refer to Certificate of Analysis for lot specific data (including water content).

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.

Physical State :
Solid
Solubility :
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).
Storage :
Store at -20° C
Boiling Point :
~767.2° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.72 (Predicted)
IC50 :
PKC β: IC50 = 6 nM; PKC α: IC50 = 39 nM; PKC &gamma: IC50 = 83 nM; PKC ε: IC50 = 110 nM; PKC η: IC50 = 0.4 µM (human)
pK Values :
pKa: 7.88 (Predicted), pKb: 7.61 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
176167
MDL Number :
MFCD11040980
SMILES :
CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)C6CCN(CC6)CC7=CC=CC=N7

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Saba et al Saba 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
Date published: 2015-03-11
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