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.
|Related PKC Products|
(-) -IndolacTAM V is an activator of PKC, and the Ki values of η -CrD2 (PKCγ -substituted peptide) and γ -CrD2 (PKCγ -substituted peptide) are 3.36 nM and 1.03 μM, respectively. The Kd values for C1A and C1B domains of PKC were 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), respectively. At 137 nM (β-C1B), 138 nM (γ-C1A) and 213 nM (γ-C1B), it has antitumor activity.
Daphnoretin (Dephnoretin) is extracted from Wikstroemia indica and has antiviral activity. Daphnoretin acts similarly to PMA in that it can directly activate protein kinase C, thereby activating NADPH oxidase.
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).
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