1. Epigenetics
    TGF-beta/Smad
    Autophagy
    Apoptosis
  2. PKC
    Autophagy
    Apoptosis
  3. Enzastaurin

Enzastaurin (Synonyms: LY317615)

Cat. No.: HY-10342 Purity: 99.90%
Handling Instructions

Enzastaurin (LY317615) est un inhibiteur de PKCβ qui est puissant et sélectif avec un IC50 de 6 nM, montrant une sélectivité de 6 à 20 fois sur PKCα , PKCγ et PKCε.

Enzastaurin (LY317615) 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.

Enzastaurin Chemical Structure

Enzastaurin Chemical Structure

CAS No. : 170364-57-5

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10 mM * 1  mL in DMSO USD 57 In-stock
Estimated Time of Arrival: December 31
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50 mg USD 140 In-stock
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200 mg USD 380 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

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  • References

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Description

Enzastaurin (LY317615) 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].

IC50 & Target

PKCβ

6 nM (IC50)

PKCα

39 nM (IC50)

PKCγ

83 nM (IC50)

PKCε

110 nM (IC50)

In Vitro

Enzastaurin (LY317615) application results in a marked dose-dependent inhibition of 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 from 0.6-1.6 μM. Enzastaurin direct impacts human tumor cells, inducing apoptosis and suppressing proliferation in cultured tumor cells. Enzastaurin also suppresses the phosphorylation of GSK3βser9, ribosomal protein S6S240/244, and AKTThr308 while having no direct effect on VEGFR phosphorylation[1].
Enzastaurin increases apoptosis in malignant lymphocytes of CTCL. When combined with GSK3 inhibitors, enzastaurin demonstrates an enhancement of cytotoxicity levels. Treatment with a combination of enzastaurin and the GSK3 inhibitor AR-A014418 leads to increased levels of β-catenin total protein and β-catenin-mediated transcription. Blocking of β-catenin-mediated transcription or small hairpin RNA (shRNA) knockdown of β-catenin induces the same cytotoxic effects as that of enzastaurin plus AR-A014418. Additionally, treatment with enzastaurin and AR-A014418 decreases the mRNA levels and surface expression of CD44[2].

In Vivo

Treatment of xenografts with Enzastaurin and radiation produces greater reductions in density of microvessels than either treatment alone. The decrease in microvessel density corresponds to delayed tumor growth[3].

Clinical Trial
Molecular Weight

515.61

Formula

C₃₂H₂₉N₅O₂

CAS No.

170364-57-5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 8.33 mg/mL (16.16 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9395 mL 9.6973 mL 19.3945 mL
5 mM 0.3879 mL 1.9395 mL 3.8789 mL
10 mM 0.1939 mL 0.9697 mL 1.9395 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.83 mg/mL (1.61 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 0.83 mg/mL (1.61 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Cell Assay
[3]

Induction of apoptosis by enzastaurin is measured by nucleosomal fragmentation and terminal deoxynucleotidyl transferase-mediated nick-end labeling (TUNEL) and staining in HCT116 and U87MG cell lines. Briefly, 5×103 cells are plated per well in 96-well plates (1% FBS-supplemented media conditions), incubated with or without Enzastaurin for 48 to 72 hours. The absorbance values are normalized to those from control-treated cells to derive a nucleosomal enrichment factor at all concentrations as per the manufacturer's protocol. The concentrations studied ranges from 0.1 to 10 μM. In situ TUNEL staining is assayed with the In situ Cell Death Detection. Cells (7.5×104) are plated per well in 6-well plates and incubated 72 hours in 1% FBS-supplemented media Enzastaurin.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.90%

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Keywords:

EnzastaurinLY317615LY 317615LY-317615PKCAutophagyApoptosisProtein kinase CInhibitorinhibitorinhibit

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