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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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.
|Related PKC Products|
Delcasertib (KAI-9803) is a potent and selective δ-protein kinase C (δPKC) inhibitor, it could ameliorate injury associated with ischemia and reperfusion in animal models of acute myocardial infarction (MI).
VTX-27 is a novel potent and selective PKCθ inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.
PKCβ inhibitor is a potent and selective inhibitor of PKCβ isozymes (IC50 = 5 nM and 21 nM for human PKCβII and βI).
Chelerythrine is potent, cell-permeable inhibitor of protein kinase C (IC50 = 660 nM); competitive with respect to the phosphate acceptor and non-competitive with respect to ATP.
1-Naphthyl PP1(1-NA-PP 1) is a selective inhibitor of src family kinases v-Src and c-Fyn as well as the tyrosine kinase c-Abl (IC50 values are 1.0, 0.6, 0.6, 18 and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II respectively).
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