Enzastaurin CAS: 170364-57-5
MF: C32H29N5O2
MW: 515.60
A 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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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 :
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 :
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

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Certificate of Analysis

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Enzastaurin (CAS 170364-57-5)  Product Citations

See how others have used Enzastaurin (CAS 170364-57-5). Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 32068016  Biochim Biophys Acta Gen Subj. 129561.

PMID: # 33407472  Respir Res. 8.

Citations 1 to 2 of 2 total
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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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