LY333531 hydrochloride competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50 values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). LY333531 exhibits ATP dependent competitive inhibition of PKC beta I and is selective for PKC in comparison to other ATP dependent kinases (protein kinase A, calcium calmodulin, caesin kinase, src tyrosine kinase).
J Mol Cell Cardiol. 2015 Oct;138-47.
Irisin improves endothelial function in type 2 diabetes through reducing oxidative/nitrative stresses.
LY333531 hydrochloride purchased from AbMole
|Source||Journal of Molecular and Cellular Cardiology (2015). Figure 7.LY333531 (Abmole Company, Shanghai, China)|
|Incubation Time||24 h|
|Results||We found that PKC-β inhibitor LY333531 significantly suppressed augmented gp91phox expression.|
|Preparation method||Western blot Aortas and HUVECs were lysed in lysis buffer or membrane and cytosol protein extraction kit and total proteins in the supernatant were extracted to perform Western blot analysis. Equal amounts of proteins were separated through electrophoresis on SDS-PAGE gels and transferred to nitrocellulose membranes (Millipore, MA, USA). After blocked with 5% skim milk, the membranes were incubated with the appropriate primary antibodies respectively against PKC-β (Abcam, CA, USA), and β-actin (Zhong Shan Golden Bridge Biotechnology, Beijing, China) with recommended dilution at 4 °C overnight. The membranes were washed and further incubated with corresponding secondary antibodies [Anti-Rabbit IgG; Anti-mouse IgG (Zhong Shan Golden Bridge Biotechnology, Beijing, China)] with horseradish peroxidase (HRP) conjugation at 37 °C for 60 min. The films were developed using an ECL Plus chemiluminescence reagent kit (Millipore, MA, USA) and visualized using ChemiDocXRS (Bio-Rad Laboratory, CA, USA). Densitometries were analyzed using Quantity One software.|
|Animal models||Male Sprague-Dawley rats diabetes models|
|Formulation||dissolved in citrate buffer (0.1 mol/L, pH 4.5)|
|Administration||oral gavage for 4 weeks|
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta.
Jirousek MR, et al. J Med Chem. 1996 Jul 5;39(14):2664-71. PMID: 8709095.
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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).
|Zoledronic acid monohydrate
Zoledronic acid monohydrate(CGP 42446; ZOL 446) is an activator of protein kinase C with apoptotic effects on multiple myeloma cell lines. It inhibited proliferation of human foetal osteoblastic cell line (hFOB) with an IC50 of 40 uM.
Ingenol Mebutate is a substance found in the sap of the plant Euphorbia peplus and an inducer of cell death.
|Phorbol 12-myristate 13-acetate
Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.
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