2. Cell Cycle/DNA Damage
    Epigenetics
    TGF-beta/Smad
  3. CDK
    PKC
  4. CGP60474

CGP60474 

Cat. No.: HY-11009 Purity: 99.23%
COA Handling Instructions

CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.

For research use only. We do not sell to patients.

CGP60474 Chemical Structure

CGP60474 Chemical Structure

CAS No. : 164658-13-3

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Solution
10 mM * 1 mL in DMSO USD 131 In-stock
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10 mM * 1 mL
ready for reconstitution
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5 mg USD 119 In-stock
10 mg USD 168 In-stock
50 mg USD 600 In-stock
100 mg USD 1020 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CGP60474 purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.  [Abstract]

    MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.

    View All CDK Isoform Specific Products:

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    View All PKC Isoform Specific Products:

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

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor[1][2][3].

    IC50 & Target[1]

    CDK1-Cyclin B

    26 nM (IC50)

    CDK2/cyclinE

    3 nM (IC50)

    cdk2/cyclin A

    4 nM (IC50)

    CDK4/cyclin D

    216 nM (IC50)

    Cdk5/p25

    10 nM (IC50)

    CDK7/cyclin H

    200 nM (IC50)

    CDK9/cycT

    13 nM (IC50)

    PKC

     

    In Vitro

    CGP60474 (Compound A) is a potent VEGFR-2 inhibitor, with an IC50 of 84 nM[1]. CGP60474 is also a PKC inhibitor, with competitive kinetics relative to ATP[2].

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

    CGP-60474 (10 mg/kg; i.p.) inhibits the IL-6 level and increases the survival rate in the LPS endotoxemia model[2].

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

    Animal Model: C57Bl/6 mice (LPS endotoxemia model)[2]
    Dosage: 10 mg/kg
    Administration: I.p.
    Result: Had a higher survival rate.
    Molecular Weight

    355.82

    Appearance

    Solid

    Formula

    C18H18ClN5O
    CAS No.
    SMILES

    ClC1=CC(NC2=NC=CC(C3=CC=NC(NCCCO)=C3)=N2)=CC=C1
    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 : ≥ 50 mg/mL (140.52 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8104 mL 14.0520 mL 28.1041 mL
    5 mM 0.5621 mL 2.8104 mL 5.6208 mL
    10 mM 0.2810 mL 1.4052 mL 2.8104 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: ≥ 2.5 mg/mL (7.03 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
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    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.

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    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

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    CGP60474164658-13-3CGP 60474CGP-60474CDKPKCCyclin dependent kinaseProtein kinase CendotoxemicselectiveATP-competitiveIL-6 levelsurvivalLPSInhibitorinhibitorinhibit

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