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Ruboxistaurin hydrochloride

CAS No. : 169939-93-9

MCE 站：Ruboxistaurin hydrochloride

产品活性：Ruboxistaurin (LY333531) hydrochloride 是一种选择性的，ATP-竞争性的 PKCβ 抑制剂，对 PKCβI 和 PKCβII 的 IC₅₀ 值分别为 4.7 nM 和 5.9 nM，对 PKCη (IC₅₀，52 nM)，PKCα (IC₅₀，360 nM)，PKCγ (IC₅₀，300 nM) 和 PKCδ (IC₅₀，250 nM) 的抑制作用相对较弱，而对 PKCζ (IC₅₀，>100 μM) 无作用。

研究领域：Epigenetics  |  TGF-beta/Smad

作用靶点：PKC

In Vitro: Ruboxistaurin hydrochloride is a selective and ATP-competitive PKCβ inhibitor, with IC₅₀s of 4.7 and 5.9 nM for PKCβI and PKCβII, shows less potent inhibition on PKCη (IC₅₀, 52 nM), PKCα (IC₅₀, 360 nM), PKCγ (IC₅₀, 300 nM), PKCδ (IC₅₀, 250 nM), and has no effect on PKCζ (IC₅₀, >100 μM). Ruboxistaurin (10 and 400 nM) dramatically inhibits glucose-induced monocyte adherence to levels that are not different from baseline adherence of monocytes to endothelial cells under NG conditions. Ruboxistaurin (10 and 400 nM) dose not alter the endothelial expression of adhesion molecules or modify endothelial cell growth. Ruboxistaurin (LY333531; 10 nM) reduces high-glucose (HG)-induced human renal glomerular endothelial cells (HRGECs) viability, and inhibits the increases in swiprosin-1 in HRGECs incubated with HG.

In Vivo: Ruboxistaurin (LY333531; 1 mg/kg/d for 8 weeks) markedly reduces GEC apoptosis as well as swiprosin-1 upregulation, and ameliorates renal glomerular injury in the diabetic mice. Ruboxistaurin also potently attenuates the expression of PARP, cleaved-caspase9, cleaved-caspase3, and the Bax/Bcl-2 ratio, in diabetic mice. Ruboxistaurin (LY333531; 0.1, 1.0, or 10.0 mg/kg/d, po.o.) dramatically reduces the number of leukocytes trapped in the retinal microcirculation of diabetic rats.

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