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Ro 31-8220 Mesylate

CAS No. 138489-18-6

Ro 31-8220 Mesylate( RO31-8220 | RO318220 | RO-318220 )

Catalog No. M17271 CAS No. 138489-18-6

Ro 31-8220 is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Ro 31-8220 Mesylate
  • Note
    Research use only, not for human use.
  • Brief Description
    Ro 31-8220 is a pan-PKC inhibitor for PKC-α/βI/βII/γ/ε (IC50: 5/24/14/27/24 nM), and also shows potent inhibition against MSK1, MAPKAP-K1b, S6K1, and GSK3β.
  • Description
    Ro 31-8220 is a PKC-inhibitor, which inhibits stimulated fluid pinocytosis of human PMNs induced by the PKC-activators phorbol myristate acetate (PMA, IC50 = 1.35 x 10(-6) M) or diacylglycerols (OAG, diC8) by 95%. Ro-31-8220 showed the apoptotic effect on HL-60 cells, which was mediated by a well-characterized transduction process of apoptotic signals: i.e., mitochondrial cytochrome c efflux and the activation of caspase-3 in the cytosol. Moreover, the ability of Ro-31-8220 to induce apoptotic activation was completely inhibited by the over-expression of the apoptotic suppressor gene, Bcl-2, in the cells.
  • 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. 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. 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.
  • 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.
  • Synonyms
    RO31-8220 | RO318220 | RO-318220
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    PKCα| PKCβ1| PKCβ2| PKCγ| PKCε
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    138489-18-6
  • Formula Weight
    553.65
  • Molecular Formula
    C25H23N5O2S·CH4O3S
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 50 mg/mL. 90.31 mM; H2O : < 0.1 mg/mL
  • SMILES
    Cn1cc(c2ccccc12)C1=C(C(=O)NC1=O)c1cn(c2ccccc12)CCCSC(=N)N.CS(=O)(=O)O
  • Chemical Name
    3-(3-(4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl)-1H-indol-1-yl)propyl carbamimidothioate methanesulfonate

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Wilkinson SE, et al. Biochem J. 1993, 294 ( Pt 2), 335-337.
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