1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. Ro 31-8220

Ro 31-8220 (Synonyms: Bisindolylmaleimide IX)

Cat. No.: HY-13866A
Handling Instructions

Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

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

Ro 31-8220 Chemical Structure

Ro 31-8220 Chemical Structure

CAS No. : 125314-64-9

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Top Publications Citing Use of Products

    Ro 31-8220 purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Nov;16(5):5924-5930.

    The PKC inhibitor Ro 31 8220 is used to investigate the implication of PKC mediated signaling pathways.

    Ro 31-8220 purchased from MCE. Usage Cited in: Nat Commun. 2018 Sep 11;9(1):3688.

    Levels of phosphorylated FAK and AKT are reduced by the PKN1 inhibitors. Cells are seeded in six-well plates after transfection with PKN1 inhibitors Lestaurtinib and Ro318220 or DMSO as control.
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    Description

    Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.

    IC50 & Target

    IC50: 5 nM (PKCα), 24 nM (PKCβI), 14 nM (PKCβII), 27 nM (PKCγ), 24 nM (PKCε), 23 nM (Rat brain PKC)[1], 3 nM (MAPKAP-K1b), 8 nM (MSK1), 15 nM (S6K1), 38 nM (GSK3β)[2]

    In Vitro

    Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively[1]. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Moreover, Ro 31-8220 directly suppresses voltage-dependent Na+ channels[2]. Ro 31-8220 (1 μM) is neuroprotective against paraoxon-induced neuronal cell death in cerebellar granule neurons, blocks paraoxon-induced caspase-3 activity, and reduces the paraoxon-induced increase in phospho-PKC pan levels[3].

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

    In Vivo

    Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP−/− mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change[4].

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

    Molecular Weight

    457.55

    Formula

    C₂₅H₂₃N₅O₂S

    CAS No.

    125314-64-9

    SMILES

    NC(SCCCN1C=C(C2=C(C3=CN(C)C4=C3C=CC=C4)C(NC2=O)=O)C5=C1C=CC=C5)=N

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
    Cell Assay
    [1]

    A neurotoxic concentration of paraoxon (200 μM) is added to the granule cell cultures for the indicated time on day in vitro (DIV) 8. The following drugs are added to the granule cell cultures prior to or after paraoxon exposure on DIV 8: Ro-81-3220 (1 μM) is added 15 min prior to or 3 h after the addition of paraoxon. TPA (0.1 μM) is added 15 min prior to the addition of paraoxon[1].

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

    Animal Administration
    [4]

    Mice[4]
    The affects of long-term Ro 31-8220 administration over 4 to 6 weeks in MLP−/− heart failure mice are investigated. All mice are assessed for ventricular performance by echocardiography at the beginning of the study and 6 weeks later. Ro 31-8220 (or vehicle) is injected subcutaneously once per day at a dosage of 6 mg/kg/d[4].

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

    References
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    Keywords:

    Ro 31-8220Bisindolylmaleimide IXPKCProtein kinase CInhibitorinhibitorinhibit

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