LY-333531 . hydrochloride
| Code | Size | Price |
|---|
| AG-CR1-0087-M001 | 1 mg | £70.00 |
Quantity:
| AG-CR1-0087-M005 | 5 mg | £190.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
Ambient
Storage:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
Ruboxistaurin
Appearance:
Red solid.
CAS:
169939-93-9
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Handling Advice:
Protect from light when in solution.
Hazards:
H315, H319, H332
InChi:
InChI=1S/C28H28N4O3.ClH/c1-30(2)15-18-11-12-31-16-21(19-7-3-5-9-23(19)31)25-26(28(34)29-27(25)33)22-17-32(13-14-35-18)24-10-6-4-8-20(22)24;/h3-10,16-18H,11-15H2,1-2H3,(H,29,33,34);1H/t18-;/m0./s1
InChiKey:
NYQIEYDJYFVLPO-FERBBOLQSA-N
Long Description:
Chemical. CAS: 169939-93-9. Formula: C28H28N4O3 . HCl. MW: 468.6 . 36.5. Isozyme selective inhibitor of protein kinase Cbeta (PKCbeta). PKCbetaI and PKCbetaII isozyme inhibitor. Amelioriates diabetic retinopathy, diabetic peripheral neuropathy and diabetic nephropathy. Anti-cancer and anti-angiogenic compound. Suppresses glucose-induced adhesion of human monocytes to endothelial cells. Suppresses ERK1/2 and Akt phosphorylation.
MDL:
MFCD00940226
Molecular Formula:
C28H28N4O3 . HCl
Molecular Weight:
468.6 . 36.5
Package Type:
Vial
Precautions:
P261, P271, P280, P304, P340, P302, P352
Product Description:
Isozyme selective inhibitor of protein kinase Cbeta (PKCbeta) [1, 6, 10, 11, 13]. PKCbetaI and PKCbetaII 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].
Purity:
>98% (HPLC)
Signal word:
Warning
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
Solubility Chemicals:
Soluble in DMSO. Slightly soluble in 100% ethanol or water.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 1 year after receipt when stored at -20°C.
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)