Enzastaurin dihydrochloride
Based on 12 publication(s) in Google Scholar
Enzastaurin (LY317615) dihydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
For research use only. We do not sell to patients.
- CAS No.: 365253-37-8
- Formula: C32H31Cl2N5O2
- Molecular Weight:588.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Publications Citing Use of MedChemExpress (MCE) Enzastaurin dihydrochloride
More- Cell. 2023 Jun 22;186(13):2929-2949.e20. [Abstract]
- Autophagy. 2024 Nov;20(11):2460-2477. [Abstract]
- Nat Commun. 2020 Apr 14;11(1):1792. [Abstract]
- Mol Cell. 2026 Jun 18;86(12):2294-2308.e7. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Oncogene. 2022 Mar;41(11):1536-1549. [Abstract]
- NPJ Breast Cancer. 2020 Jan 6:6:1. [Abstract]
- Biochem Pharmacol. 2023 Mar:209:115443. [Abstract]
- Rheumatology (Oxford). 2025 Aug 13:keaf437. [Abstract]
- Microbiol Spectr. 2022 Oct 26;10(5):e0105622. [Abstract]
- bioRxiv. 2025 Sep 21.
- Patent. US20210299273A1.
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Biological Activity
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 365253-37-8
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Molecular Weight 588.53
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Formula C32H31Cl2N5O2
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SMILES
O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3C4=CN(C5CCN(CC6=NC=CC=C6)CC5)C7=C4C=CC=C7)NC3=O.[H]Cl.[H]Cl
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Synonyms
LY317615 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (12)
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Journal Impact Factor
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Most Recent
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Cell
Distinct longevity mechanisms across and within species and their association with aging. [Abstract]2023 Jun 22;186(13):2929-2949.e20. PMID: 37269831 -
Autophagy
(-)-Epigallocatechin 3-gallate protects pancreatic β-cell against excessive autophagy-induced injury through promoting FTO degradation. [Abstract]2024 Nov;20(11):2460-2477. PMID: 38910554 -
Nat Commun
Selective inhibition of cancer cell self-renewal through a Quisinostat-histone H1.0 axis. [Abstract]2020 Apr 14;11(1):1792. PMID: 32286289 -
Mol Cell
2026 Jun 18;86(12):2294-2308.e7. PMID: 42314650 -
Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
Oncogene
Targeting a splicing-mediated drug resistance mechanism in prostate cancer by inhibiting transcriptional regulation by PKCβ1. [Abstract]2022 Mar;41(11):1536-1549. PMID: 35087237
Enzastaurin dihydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2022 Mar;41(11):1536-1549. [Abstract]
Enzastaurin (10 μM). VCaP cells cultured in RPMI1640 supplemented with 5% CSS for 48 h were treated as indicated for 72 h and then immunoblotted for AR and AR-V7.
Enzastaurin dihydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2022 Mar;41(11):1536-1549. [Abstract]
22RV1 cells express AR-V7 protein and contain LBD mutation H875Y. 22RV1 (2000 cells/well) cells were cultured in RPMI1640 supplemented with 5% CSS for 48 h in 96 well plates. In the presence of 0.1 nM DHT, cells were treated with a nine-point threefold dilution series of MDV (beginning at 30 μM) in the presence or absence of a constant concentration of Enzastaurin for five days.
Enzastaurin dihydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2022 Mar;41(11):1536-1549. [Abstract]
Enzastaurin (10 μM). VCaP cells were cultured in RPMI 1640 medium supplemented with 5% CSS for 48 h, pretreated with DHT for 24 h, then washed off the medium, and treated again as shown for 24 h. Finally, AR mRNA transcription levels were analyzed by RT-qPCR.
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NPJ Breast Cancer
LncRNA RP11-19E11 is an E2F1 target required for proliferation and survival of basal breast cancer. [Abstract]2020 Jan 6:6:1. PMID: 31934613 -
Biochem Pharmacol
Enzastaurin cardiotoxicity: QT interval prolongation, negative inotropic responses and negative chronotropic action. [Abstract]2023 Mar:209:115443. PMID: 36720353 -
Rheumatology (Oxford)
Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]2025 Aug 13:keaf437. PMID: 40802538 -
Microbiol Spectr
2022 Oct 26;10(5):e0105622. PMID: 36000889
Enzastaurin dihydrochloride purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Oct 26;10(5):e0105622. [Abstract]
IC50 and CC50 values of Enzastaurin in BHK-21 cells.
Enzastaurin dihydrochloride purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Oct 26;10(5):e0105622. [Abstract]
A549-ACE2 cells were treated with DMSO, Go 6983, Bisindolylmaleimide I, or Enzastaurin for 1 h, followed by virus infection. At 24 h p.i., cells or supernatants were harvested for an immunofluorescence assay.
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Purity & Documentation
References
[1]. Graff JR, et al. The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Res, 2005, 65(16), [Content Brief]
[2]. Rovedo MA, et al. Inhibition of glycogen synthase kinase-3 increases the cytotoxicity of enzastaurin. J Invest Dermatol, 2011, 131(7), 1442-1449. [Content Brief]
[3]. Podar K, et al. Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl). Blood, 2007, 109(4), 1669-1677. [Content Brief]
Calculators
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