1. Epigenetics
    TGF-beta/Smad
  2. PKC

Ro 31-8220 mesylate (Synonyms: Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate)

Cat. No.: HY-13866 Purity: 99.28%
Handling Instructions

Ro 31-8220 mesylate 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 mesylate Chemical Structure

Ro 31-8220 mesylate Chemical Structure

CAS No. : 138489-18-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
Estimated Time of Arrival: December 31
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Other Forms of Ro 31-8220 mesylate:

    Ro 31-8220 mesylate 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 mesylate purchased from MCE. Usage Cited in: FASEB J. 2018 Sep 27:fj201800935RR.

    Bile acids (BAs) cause nuclear translocation of NF-kB p65, an effect that is abolished by SB203580.

    Ro 31-8220 mesylate 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Ro 31-8220 mesylate 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[1][2]

    PKC-α

    5 nM (IC50)

    PKC-βII

    14 nM (IC50)

    PKC-βI

    24 nM (IC50)

    PKC-ε

    24 nM (IC50)

    PKC-γ

    27 nM (IC50)

    Rat Brain PKC

    23 nM (IC50)

    MAPKAP-K1b

    3 nM (IC50)

    MSK1

    8 nM (IC50)

    S6K1

    15 nM (IC50)

    GSK3β

    38 nM (IC50)

    In Vitro

    Ro 31-8220 mesylate 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].

    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].

    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8062 mL 9.0310 mL 18.0620 mL
    5 mM 0.3612 mL 1.8062 mL 3.6124 mL
    10 mM 0.1806 mL 0.9031 mL 1.8062 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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
    Molecular Weight

    553.65

    Formula

    C₂₆H₂₇N₅O₅S₂

    CAS No.

    138489-18-6

    SMILES

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

    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

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    Product Name:
    Ro 31-8220 mesylate
    Cat. No.:
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    Ro 31-8220 mesylate

    Cat. No.: HY-13866