Enzastaurin (CAS 170364-57-5)

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Alternate Names: LY-317615

Application: Enzastaurin is a potent inhibitor of PKCβ, PKCα, PKCγ and PKCε

CAS Number: 170364-57-5

Purity: ≥99%

Molecular Weight: 515.60

Molecular Formula: C₃₂H₂₉N₅O₂

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

* Refer to Certificate of Analysis for lot specific data (including water content).

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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 :

n²⁰_D 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 :

pK_a: 7.88 (Predicted), pK_b: 7.61 (Predicted)

For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.

WGK Germany :

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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