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AdipoGen Life Sciences
LY-333,531 . hydrochloride
90
CHF
CHF 90.00
In stock
AG-CR1-0087-M0011 mgCHF 90.00
AG-CR1-0087-M0055 mgCHF 270.00
| Product Details | |
|---|---|
| Synonyms | Ruboxistaurin |
| Product Type | Chemical |
| Properties | |
| Formula |
C28H28N4O3 . HCl |
| MW | 468.6 . 36.5 |
| Merck Index | 14: 8290 |
| CAS | 169939-93-9 |
| Purity Chemicals | ≥98% (HPLC) |
| Appearance | Red solid. |
| Solubility | Soluble in DMSO. Slightly soluble in 100% ethanol or water. |
| Identity | Determined by 1H-NMR. |
| InChi Key | NYQIEYDJYFVLPO-FERBBOLQSA-N |
| Smiles | Cl.CN(C)C[C@@H]1CCN2C=C(C3=C2C=CC=C3)C2=C(C(=O)NC2=O)C2=CN(CCO1)C1=C2C=CC=C1 |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Handling Advice | Protect from light when in solution. |
| Use/Stability | Stable for at least 1 year after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
Description
- Isozyme selective inhibitor of protein kinase Cβ (PKCβ) [1, 6, 10, 11, 13].
- PKCβI and PKCβII isozyme inhibitor [2-3, 6, 10, 11, 13].
- Amelioriates diabetic retinopathy, diabetic peripheral neuropathy and diabetic nephropathy [1, 3, 5-7, 9-11].
- Anti-cancer and anti-angiogenic compound [4-5, 8].
- Suppresses glucose-induced adhesion of human monocytes to endothelial cells [12].
- Suppresses ERK1/2 and Akt phosphorylation [14].
Product References
- 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)