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Ro 31-8220

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

Bisindolylmaleimide IX

Size Price Availability
5mg USD 110  USD110 Out of stock
10mg USD 165  USD165 Out of stock
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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.

Chemical Information
Molecular Weight 457.55
Formula C25H23N5O2S
CAS Number 125314-64-9
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Karunakaran D, et al. J Biol Chem. Protein kinase C controls vesicular transport and secretion of apolipoprotein E from primary human macrophages.

[2] Kim SY, et al. BMB Rep. PKC inhibitors RO 31-8220 and Gö 6983 enhance epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation.

[3] Davies SP, et al. Biochem J. Specificity and mechanism of action of some commonly used protein kinase inhibitors.

[4] Lingameneni R, et al. FEBS Lett. Inhibition of voltage-dependent sodium channels by Ro 31-8220, a 'specific' protein kinase C inhibitor.

[5] Wilkinson SE, et al. Biochem J. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C.

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

 
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