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) with IC50s of 22 nM (cPKC-α), 30 nM (cPKC-β1), 31 nM (cPKC-β2), 24 nM (cPKC-γ), 330 nM (nPKC-δ), 160 nM (nPKC-η), 1.25 μM (nPKC-ε), 465 μM (aPKC-ζ), and also inhibits 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
Estimated Time of Arrival: December 31
1 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 770 In-stock
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.

    PKC412 purchased from MCE. Usage Cited in: Cell. 2018 Aug 20. pii: S0092-8674(18)30973-5.

    WB analysis of MV4-11 cells treated for 6.5 hr with Lenalidomide, BTX161, A51, or A86 at the indicated concentrations or DMSO.

    PKC412 purchased from MCE. Usage Cited in: Cell. 2018 Aug 20. pii: S0092-8674(18)30973-5.

    WB analysis of MV4-11 cells treated with BTX161 (6 hr), iCDK9 (4 hr), or THZ1 (4 hr) at the indicated concentrations in different combinations as indicated. PP2Ac is a loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PKC412 is an inhibitor of protein kinase C (PKC) with IC50s of 22 nM (cPKC-α), 30 nM (cPKC-β1), 31 nM (cPKC-β2), 24 nM (cPKC-γ), 330 nM (nPKC-δ), 160 nM (nPKC-η), 1.25 μM (nPKC-ε), 465 μM (aPKC-ζ), and also inhibits PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR.

    IC50 & Target[5]

    nPKC-η

    16 nM (IC50)

    cPKC-α

    22 nM (IC50)

    cPKC-γ

    24 nM (IC50)

    cPKC-β1

    30 nM (IC50)

    cPKC-β2

    31 nM (IC50)

    nPKC-δ

    33 nM (IC50)

    nPKC-ε

    1250 nM (IC50)

    aPKC-ζ

    465000 nM (IC50)

    PPK

    38 nM (IC50)

    KDR

    86 nM (IC50)

    c-Syk

    95 nM (IC50)

    cdk1/cycB

    570 nM (IC50)

    Protein kinase A

    570 nM (IC50)

    c-Fgr

    790 nM (IC50)

    c-Src

    800 nM (IC50)

    Flt-1

    912 nM (IC50)

    EGF-R

    1100 nM (IC50)

    Myosin-light chain kinase

    1900 nM (IC50)

    Flk-1

    3900 nM (IC50)

    c-Lyn

    4300 nM (IC50)

    P70S6 kinase

    5000 nM (IC50)

    CSK

    8000 nM (IC50)

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 250 mg/mL (438.10 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.08 mg/mL (3.65 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (3.65 mM); Clear solution

    References
    Cell Assay
    [3]

    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[3].

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

    Animal Administration
    [4]

    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[4].

    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

    Purity: 98.60%

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

    Cat. No.: HY-10230