For research use only. Not for therapeutic Use.
Ruboxistaurin, also known as LY-333531, is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt.
| Catalog Number | I009230 |
| CAS Number | 169939-93-9 (HCl) |
| Synonyms | Ruboxistaurin; Ruboxistaurin hydrochloride, LY-333531; LY333531; LY 333531.;(12E,32E,7S)-7-((dimethylamino)methyl)-22,25-dihydro-11H,21H,31H-6-oxa-1,3(3,1)-diindola-2(3,4)-pyrrolacyclononaphane-22,25-dione hydrochloride |
| Molecular Formula | C28H29ClN4O3 |
| Purity | ≥95% |
| Target | PKCbeta inhibitor |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| 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 |
| SMILES | CN(C)CC1CCN2C=C(C3=CC=CC=C32)C4=C(C5=CN(CCO1)C6=CC=CC=C65)C(=O)NC4=O.Cl |
| Reference | </br> 1:Al-Onazi AS, Al-Rasheed NM, Attia HA, Al-Rasheed NM, Ahmed RM, Al-Amin MA, Poizat C. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. J Pharm Pharmacol. 2016 Feb;68(2):219-32. doi: 10.1111/jphp.12504. Epub 2016 Jan 28. PubMed PMID: 26817709.</br> 2: Deissler HL, Lang GE. The Protein Kinase C Inhibitor: Ruboxistaurin. Dev Ophthalmol. 2016;55:295-301. doi: 10.1159/000431204. Epub 2015 Oct 26. Review. PubMed PMID: 26501476.</br> 3: Tuttle KR, McGill JB, Bastyr EJ 3rd, Poi KK, Shahri N, Anderson PW. Effect of ruboxistaurin on albuminuria and estimated GFR in people with diabetic peripheral neuropathy: results from a randomized trial. Am J Kidney Dis. 2015 Apr;65(4):634-6. doi: 10.1053/j.ajkd.2014.11.024. Epub 2015 Jan 22. PubMed PMID: 25618186. |
