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

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, selective, and CNS-penetrant 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. : 170364-57-5

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Enzastaurin:

Enzastaurin Related Antibodies

Top Publications Citing Use of Products

    Enzastaurin 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 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 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 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 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.

    View All PKC Isoform Specific Products:

    View All Isoforms
    PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Enzastaurin (LY317615) is a potent, selective, and CNS-penetrant PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε[1][2][3][4].

    IC50 & Target[3]

    PKCβ

    6 nM (IC50)

    PKCα

    39 nM (IC50)

    PKCγ

    83 nM (IC50)

    PKCε

    110 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    PANC-1 IC50
    6.59 μM
    Compound: Enzastaurin
    Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
    Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
    		[PMID: 39151060]
    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].

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

    Enzastaurin Related Antibodies
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    515.61

    Formula

    C32H29N5O2
    CAS No.
    Appearance

    Solid

    Color

    Orange to red

    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 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : 8.33 mg/mL (16.16 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a suspended solution of 0.83 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.80%

    SDS (396 KB)

    COA (260 KB) RP-HPLC (246 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9395 mL 9.6973 mL 19.3945 mL 48.4863 mL
    5 mM 0.3879 mL 1.9395 mL 3.8789 mL 9.6973 mL
    10 mM 0.1939 mL 0.9697 mL 1.9395 mL 4.8486 mL
    15 mM 0.1293 mL 0.6465 mL 1.2930 mL 3.2324 mL
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    Enzastaurin Related Classifications

    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:

    Enzastaurin170364-57-5LY317615LY 317615LY-317615PKCAutophagyApoptosisProtein kinase CInhibitorinhibitorinhibit

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