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Ro 31-8220

Cat. No. M3804
Ro 31-8220 Structure
Synonym:

Bisindolylmaleimide IX

Size Price Availability
5mg USD 99  USD110 Out of stock
10mg USD 148.5  USD165 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Ro 31-8220 inhibits MAPK and ERK2, in rat adipocytes and L6 myotubes. Ro 31-8220 also inhibits voltage-dependent Na+ channels in the micromolar range assessed by several independent criteria. Treatment of HMDMs with structurally distinct pan-PKC inhibitors (calphostin C, Ro-31-8220, Go6976) and a PKC inhibitory peptide all significantly decreased apoE secretion without significantly affecting apoE mRNA or apoE protein levels. RO 31-8220 enhances epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation. Ro 32-0432, which showed a 10-fold selectivity for PKC-alpha and a 4-fold selectivity for PKC-beta I over PKC-epsilon.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 457.55
Formula C25H23N5O2S
CAS Number 125314-64-9
Purity >98%
Solubility DMSO
Storage at -20°C
References

Protein kinase C controls vesicular transport and secretion of apolipoprotein E from primary human macrophages.
Karunakaran D, et al. J Biol Chem. 2013 Feb 15;288(7):5186-97. PMID: 23288845.

PKC inhibitors RO 31-8220 and Gö 6983 enhance epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation.
Kim SY, et al. BMB Rep. 2011 Feb;44(2):140-5. PMID: 21345315.

Specificity and mechanism of action of some commonly used protein kinase inhibitors.
Davies SP, et al. Biochem J. 2000 Oct 1;351(Pt 1):95-105. PMID: 10998351.

Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor.
Lingameneni R, et al. FEBS Lett. 2000 May 12;473(2):265-8. PMID: 10812087.

Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C.
Wilkinson SE, et al. Biochem J. 1993 Sep 1;294 ( Pt 2):335-7. PMID: 8373348.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Ro 31-8220, Bisindolylmaleimide IX supplier, PKC, inhibitors

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