1. Epigenetics
    TGF-beta/Smad
  2. PKC

PKC412 (Synonyms: CGP41231; Midostaurin; CGP 41251)

Cat. No.: HY-10230 Purity: 98.60%
Handling Instructions

PKC412 is an inhibitor of protein kinase C (PKC) and can inhibit other kinases including PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR.

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

PKC412 Chemical Structure

PKC412 Chemical Structure

CAS No. : 120685-11-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 126 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
1 mg USD 60 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
100 mg USD 770 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

    PKC412 purchased from MCE. Usage Cited in: Haematologica. 2018 Jul 5. pii: haematol.2018.191650.

    Induction of tumor suppressor protein p53 in MV4-11 (A) and MOLM-13 cells (B) treated for 24 hours with the indicated amounts of NVP-HDM201 and midostaurin. Relative quantitation of CDKN1A mRNA (C) and MCL-1 mRNA (D) in AML cells treated for 24 hours with PKC412 and NVP-HDM201 alone or in combination.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PKC412 is an inhibitor of protein kinase C (PKC) and can inhibit other kinases including PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR.

    In Vitro

    PKC412 shows a broad antiproliferative activity against various tumor and normal cell lines in vitro, and is able to reverse the Pgp-mediated multidrug resistance of tumor cells in vitro. Exposure of cells to PKC412 results in a dose-dependent increase in the G2/M phase of the cell cycle concomitant with increased polyploidy, apoptosis and enhanced sensitivity to ionizing radiation[1]. Midostaurin with ponatinib induced substantial inhibition of KIT-, Lyn-, and STAT5 activity, but did not suppress Btk in HMC-1 cells and primary neoplastic mast cells[2]. PKC412 inhibits EN fusion tyrosine kinase in hematopoietic Ba/F3 cells. PKC412 significantly inhibits EN phosphorylation in M0-91 and IMS-M2 cells in a dose-dependent manner[3].

    In Vivo

    PKC412 strongly inhibits retinal neovascularization as well as laser-induced choroidal neovascularization in murine models[1]. PKC412 (25 mg/kg, i.p.) protects mouse livers of the K18 Arg90Cys-overexpressing transgenic mice from Fas-induced apoptosis[4].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 1.7524 mL 8.7621 mL 17.5242 mL
    5 mM 0.3505 mL 1.7524 mL 3.5048 mL
    10 mM 0.1752 mL 0.8762 mL 1.7524 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [3]

    PKC412 is dissolved in DMSO.

    Proliferation is determined by trypan blue dye exclusion test. Cells in suspension are seeded in six-well plates at a density of 1×105 cells/mL in the presence of different concentrations of PKC412 for 3 days. In control wells, DMSO instead of PKC412 is added. After the treatment, 10 μL of the cell suspension is mixed with 10 μL of 0.4% trypan blue, and alive cells are counted manually using a hemacytometer. Results are calculated as the percentage of the values measured when cells are grown in the absence of the reagent. All experiments are performed in triplicate. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    PKC412 is dissolved in DMSO.

    K8-deficient, K18-deficient, and human K18 R90C-overexpressing mice with age of 6-8 weeks are used in the assay. Age and sex matched mice are treated with PKC412 (25 mg/kg), daily for 4 d or with an equal volume of DMSO as vehicle (both administered intraperitoneally). On day 5 post-treatment, apoptosis is induced by intraperitoneal injection of Fas ligand (Fas-L) (0.15 μg/g body weight). Mice are fasted overnight before Fas Ab injection, and 18 mice are used per DMSO or PKC412 group for the Fas-treated mice while 6 mice are used per DMSO or PKC412 group for the control non-Fas-treated mice. Mice are sacrificed by CO2 inhalation 6 h after Fas Ab injection. Blood is collected by intracardiac puncture, and livers are harvested for hematoxylin and eosin (HE) staining (after fixation in 10% formalin) or frozen in optimum cutting temperature compound for immunofluorescence staining. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    570.64

    Formula

    C₃₅H₃₀N₄O₄

    CAS No.

    120685-11-2

    SMILES

    O=C(C1=CC=CC=C1)N(C)[[email protected]]2[[email protected]@H](OC)[[email protected]@]3(C)N(C4=C5C=CC=C4)C6=C5C7=C(C(NC7)=O)C8=C6N(C9=CC=CC=C98)[[email protected]@](O3)([H])C2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 21 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 98.60%

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    Inquiry Information

    Product Name:
    PKC412
    Cat. No.:
    HY-10230
    Quantity: