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LY333531 hydrochloride

Cat. No. M3629
LY333531 hydrochloride Structure
Synonym:

Ruboxistaurin

Size Price Availability
5mg USD 200 Out of stock
10mg USD 365 Out of stock
50mg USD 800 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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).

Protocol
Cell Experiment
Cell lines HUVECs
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.
Concentrations 5µM
Incubation time 24h
Animal Experiment
Animal models Male Sprague-Dawley rats diabetes models
Formulation dissolved in citrate buffer (0.1 mol/L, pH 4.5)
Dosages 1 mg/kg/day
Administration oral gavage for 4 weeks
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 505.01
Formula C28H28N4O3.HCl
CAS Number 169939-93-9
Purity >99%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Journal of Molecular and Cellular Cardiology (2015). Figure 7.LY333531 (Abmole Company, Shanghai, China)
Method Western blot
Cell Lines HUVECs
Concentrations 5 µM
Incubation Time 24 h
Results We found that PKC-β inhibitor LY333531 significantly suppressed augmented gp91phox expression.
Rating
Product Citations
References

(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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: LY333531 hydrochloride, Ruboxistaurin supplier, PKC, inhibitors

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