Date published: 2025-12-10

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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.

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Enzastaurin is a selective protein kinase C beta (PKCβ) inhibitor that functions by binding to the ATP-binding site of the enzyme, thereby preventing its activation and subsequent downstream signaling. This chemical′s mode of action involves inhibiting the phosphorylation of various proteins involved in cell proliferation, survival, and angiogenesis. By targeting PKCβ, Enzastaurin interferes with the PI3K/Akt signaling pathway, leading to the suppression of cell growth and induction of apoptosis in cancer cells. Enzastaurin may inhibit the activity of the mammalian target of rapamycin (mTOR), further contributing to its anti-proliferative and anti-angiogenic effects. This chemical′s functional role may be useful in the molecular mechanisms underlying PKCβ-mediated signaling pathways and exploring its potential use for investigating the role of PKCβ in various cellular processes.


Enzastaurin (CAS 170364-57-5) References

  1. Enzastaurin (LY317615), a protein kinase Cbeta inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines.  |  Rizvi, MA., et al. 2006. Mol Cancer Ther. 5: 1783-9. PMID: 16891464
  2. Enzastaurin, a protein kinase Cbeta- selective inhibitor, and its potential application as an anticancer agent in lung cancer.  |  Herbst, RS., et al. 2007. Clin Cancer Res. 13: s4641-6. PMID: 17671157
  3. Inhibition of protein kinase Cbeta by enzastaurin enhances radiation cytotoxicity in pancreatic cancer.  |  Spalding, AC., et al. 2007. Clin Cancer Res. 13: 6827-33. PMID: 18006785
  4. Enzastaurin, a protein kinase C beta inhibitor, suppresses signaling through the ribosomal S6 kinase and bad pathways and induces apoptosis in human gastric cancer cells.  |  Lee, KW., et al. 2008. Cancer Res. 68: 1916-26. PMID: 18339873
  5. Enzastaurin renders MCF-7 breast cancer cells sensitive to radiation through reversal of radiation-induced activation of protein kinase C.  |  Jasinski, P., et al. 2008. Eur J Cancer. 44: 1315-22. PMID: 18448327
  6. Pharmacological aspects of the enzastaurin-pemetrexed combination in non-small cell lung cancer (NSCLC).  |  Giovannetti, E., et al. 2010. Curr Drug Targets. 11: 12-28. PMID: 19839931
  7. Enzastaurin hydrochloride for lymphoma: reassessing the results of clinical trials in light of recent advances in the biology of B-cell malignancies.  |  Ysebaert, L. and Morschhauser, F. 2011. Expert Opin Investig Drugs. 20: 1167-74. PMID: 21639821
  8. Enzastaurin has anti-tumour effects in lung cancers with overexpressed JAK pathway molecules.  |  Shimokawa, T., et al. 2012. Br J Cancer. 106: 867-75. PMID: 22333600
  9. Novel therapies, including enzastaurin, in the treatment of ovarian cancer.  |  Vergote, I. 2014. Expert Opin Investig Drugs. 23: 579-98. PMID: 24654681
  10. Enzastaurin inhibits ABCB1-mediated drug efflux independently of effects on protein kinase C signalling and the cellular p53 status.  |  Michaelis, M., et al. 2015. Oncotarget. 6: 17605-20. PMID: 25749379
  11. Combination of Enzastaurin and Ibrutinib synergistically induces anti-tumor effects in diffuse large B cell lymphoma.  |  He, Y., et al. 2019. J Exp Clin Cancer Res. 38: 86. PMID: 30777096
  12. Enzastaurin enhances ATRA-induced differentiation of acute myeloid leukemia cells.  |  Li, ZY., et al. 2020. Am J Transl Res. 12: 7836-7854. PMID: 33437364
  13. Therapeutic natural compounds Enzastaurin and Palbociclib inhibit MASTL kinase activity preventing breast cancer cell proliferation.  |  Polisety, A., et al. 2022. Med Oncol. 39: 100. PMID: 35599277

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Enzastaurin, 10 mg

sc-364488
10 mg
$254.00

Enzastaurin, 50 mg

sc-364488A
50 mg
$600.00

Enzastaurin, 200 mg

sc-364488B
200 mg
$1687.00