Enzastaurin dihydrochloride (Synonyms: LY317615 dihydrochloride)

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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

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Other In-stock Forms of Enzastaurin dihydrochloride:

Enzastaurin

Other Forms of Enzastaurin dihydrochloride:

Enzastaurin In-stock

11 Publications Citing Use of MCE Enzastaurin dihydrochloride

Cell Proliferation/Viability Assay

RT-PCR

: 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.

: 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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Description

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^[1].

Clinical Trial

Molecular Weight

588.53

Formula

C₃₂H₃₁Cl₂N₅O₂

CAS No.

365253-37-8

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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]

Enzastaurin dihydrochloride Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Enzastaurin365253-37-8LY317615LY 317615LY-317615PKCAutophagyApoptosisProtein kinase CInhibitorinhibitorinhibit

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