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