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.
Product Reference: |
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)
|Intended for research use only. Not for use in human, therapeutic, or diagnostic applications.|