Ruboxistaurin
Product Specifications
UNSPSC Description
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
Target Antigen
PKC
Type
Reference compound
Related Pathways
Epigenetics;TGF-beta/Smad
Applications
Metabolism-sugar/lipid metabolism
Field of Research
Metabolic Disease
Assay Protocol
https://www.medchemexpress.com/ruboxistaurin.html
Purity
99.90
Solubility
DMSO : 25 mg/mL (ultrasonic;warming;heat to 60°C)|THF : < 1 mg/mL (ultrasonic)
Smiles
O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[C@H](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O
Molecular Weight
468.55
References & Citations
[1]Jirousek MR, et al. (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. J Med Chem. 1996;39(14):2664-2671.|[2]Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-199.|[3]Kunt T, et al. The beta-specific protein kinase C inhibitor ruboxistaurin (LY333531) suppresses glucose-induced adhesion of human monocytes to endothelial cells in vitro. J Diabetes Sci Technol. 2007 Nov;1(6):929-35.|[4]Nonaka A, et al. PKC-beta inhibitor (LY333531) attenuates leukocyte entrapment in retinal microcirculation of diabetic rats. Invest Ophthalmol Vis Sci. 2000 Aug;41(9):2702-6.Acta Pharm Sin B. 2022.|bioRxiv. 2024 June 29.|FASEB J. 2024 Mar 31;38(6):e23564.|Trop J Pharm Res. 2022; 21(12): 2508.|ACS Omega. 2020 Oct 12;5(41):26551-26561.|Biosci Rep. 2018 Sep 7;38(5):BSR20171459.|Cell Biosci. 2021 Feb 8;11(1):32.|Diabetes Metab Syndr Obes. 2019 Nov 4;12:2289-2302.|Endocrinology. 2018 May 1;159(5):2253-2263.|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-10195/Ruboxistaurin-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-10195/Ruboxistaurin-SDS-MedChemExpress.pdf
Clinical Information
Phase 3
CAS Number
169939-94-0
Available Sizes
Curated Selection
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