LY-333,531 hydrochloride (Ruboxistaurin)
|Biochemicals||Storage: 4°C/-20°CShipping: Blue Ice|
Isozyme selective inhibitor of protein kinase Cbeta (PKCbeta).
PKCbetaI and PKCbetaII isozyme inhibitor.
Amelioriates diabetic retinopathy, diabetic peripheral neuropathy and diabetic nephropathyAnti-cancer and anti-angiogenic compound.
Suppresses glucose-induced adhesion of human monocytes to endothelial cells.
Suppresses ERK1/2 and Akt phosphorylation.
Storage and Stability:
Short-term Storage: +4°C
Long-term Storage: -20°C
Stable for at least 2 years after receipt when stored at -20°C.
C28H28N4O3 . HCl
Purity: >98% (NMR)
Important Note: This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Amelioration of vascular dysfunctions in diabetic rats by an oral PKC beta inhibitor: H. Ishii, et al.; Science 272, 728 (1996)
(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)-dione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase: M.R. Jirousek, et al.; J. Med. Chem. 39, 2664 (1996)
Vascular endothelial growth factor-induced retinal permeability is mediated by protein kinase C in vivo and suppressed by an orally effective beta-isoform-selective inhibitor: L.P. Aiello, et al.; Diabetes 46, 1473 (1997)
Enzymatic rationale and preclinical support for a potent protein kinase C beta inhibitor in cancer therapy: B.A. Teicher, et al.; Adv. Enzyme Regul. 39, 313 (1999)
Protein kinase C in the treatment of disease: signal transduction pathways, inhibitors, and agents in development: P.G. Goekjian & M.R. Jirousek; Curr. Med. Chem. 6, 877 (1999)
A protein kinase C-beta-selective inhibitor ameliorates neural dysfunction in streptozotocin-induced diabetic rats: J. Nakamura, et al.; Diabetes 48, 2090 (1999)
Amelioration of accelerated diabetic mesangial expansion by treatment with a PKC beta inhibitor in diabetic db/db mice, a rodent model for type 2 diabetes: D. Koya, et al.; FASEB J. 14, 439 (2000)
Protein kinase C inhibitors as novel anticancer drugs: P.G. Goekjian & M.R. Jirousek; Expert Opin. Investig. Drugs 10, 2117 (2001)
Effects of the protein kinase C beta inhibitor LY333531 on neural and vascular function in rats with streptozotocin-induced diabetes: M.A. Cotter, et al.; Clin. Sci. 103, 311 (2002)
Ruboxistaurin, a protein kinase C beta inhibitor, as an emerging treatment for diabetes microvascular complications: S.V. Joy, et al.; Ann. Pharmacother. 39, 1693 (2005)
Ruboxistaurin: C.A. Taulien & S.V. Joy; Drugs Today 42, 577 (2006)
The beta-specific protein kinase C inhibitor ruboxistaurin (LY333531) suppresses glucose-induced adhesion of human monocytes to endothelial cells in vitro: T. Kunt, et al.; J. Diabetes Sci. Technol. 1, 929 (2007)
Protein kinase C isozymes and their selectivity towards ruboxistaurin: S. Tang, et al.; Proteins 72, 447 (2008)
Ruboxistaurin, a PKCbeta inhibitor, inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt: S. Nakamura, et al.; Exp. Eye Res. 90, 137 (2010)