Ruboxistaurin

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].

Product Specifications

CAS Number

[169939-94-0]

Product Name Alternative

LY333531

UNSPSC

12352005

Target

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

99.48

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 Formula

C28H28N4O3

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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 3

Isoform

PKCα; PKCβ; PKCγ; PKCδ; PKCε; PKCη

Citation 01

Acta Pharm Sin B. 2023 Mar;13 (3) :1053-1070.|bioRxiv. 2024 June 29.|FASEB J. 2024 Mar 31;38 (6) :e23564.|In Vitro Cell Dev Biol Anim. 2025 Jun;61 (6) :635-643.|Rheumatology (Oxford) . 2025 Aug 13:keaf437.|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.