| Name | Ruboxistaurin hydrochloride |
| Description | Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src). |
| Cell Research | HUVECs are seeded into 96-well plates in low glucose DMEM with 10% FBS for 12 h. Afterwards, HUVECs are starved for 12 h and incubated with BSA (200 μg/ml), AGEs (200 μg/ml) and LY333531 (200 nM)+AGEs (200 μg/ml) for 48 h. Then, the medium is replaced with 0.5 mg/ml MTT and at 37 ?C in a 95% air/5% CO2 incubator for 4 h. Finally, the medium containing MTT is aspirated and replaced by dimethyl sulphoxide (DMSO). OD is measured with a Microplate spectrophotometer. AGEs:advanced glycation end products.(Only for Reference) |
| In vitro | Ruboxistaurin strikingly decreases the chance of HUVEC survival and the effect of Ruboxistaurin on apoptotic cell death in HUVEC significantly increases compared with the AGEs group. Blockade of PKC-beta up-regulates the expression of Bax and Bad proteins and down-regulates the expression of Bcl-2 protein. Moreover, Ruboxistaurin reduces the ratio of Bcl-2/Bax. Ruboxistaurin can further prompt AGEs-induced endothelial cells apoptosis. The increased expression of Bax, Bad and decreased expression of Bcl-2 and Bcl-2/Bax ratio are associated with the apoptotic process[3]. |
| In vivo | A significant up-regulation of TGF-b1, Smad2 and Smad3 mRNA expression was observed in diabetic rats, which was alleviated by administration of ruboxistaurin. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 55 mg/mL (108.91 mM), Sonication is recommended.
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| Keywords | PKCη | PKCδ | PKCγ | PKCβ2 | PKCβ1 | PKC | LY-333531 Hydrochloride | LY333531 Hydrochloride | LY-333531 | LY333531 | LY 333531 |
| Inhibitors Related | Daphnetin | Darovasertib | Ellagic acid | α-Vitamin E | Ro-3306 | Staurosporine | Methyl-Hesperidin | N-Desmethyltamoxifen hydrochloride | Fasudil hydrochloride | Mitoxantrone dihydrochloride | Myricitrin | R59949 |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | ReFRAME Related Library | Kinase Inhibitor Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Wnt/Hedgehog/Notch Compound Library | Human Metabolite Library | TGF-beta/Smad Compound Library |
United States
