Zoledronic acid, one of the most potent nitrogen-containing BPs(bisphosphonates), induces antiproliferative and apoptotic effects on multiple myeloma cell lines in vitro, by activating protein kinase C, and increases the extracellular calcium concentration. Zoledronic acid and radiation caused a dosedependent and time-dependent decrease in cell viability (approximate 50% growth inhibition values were 48 μM and 20μM for 24 hours and 72 hours, respectively, for zoledronic acid and 500 cGy for radiation).
|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.
|Solubility||Soluble in NaOH|
|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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