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RU-SKI 43 hydrochloride  ≥98%

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包装规格：2mg 5mg 10mg 50mg in glass bottle
溶解性：溶于DMSO（≥51mg/mL）
产品描述：基本信息 产品编号： R10445  产品名称： RU-SKI 43 hydrochloride CAS: 1782573-67-4   储存条件 粉末 -20℃ 四年     分子式： C22H31ClN2O2S 溶于液体 -80℃ 6个月 分子量 423.01 -20℃ 1个月 化学名：  1-[6,7-dihydro-4-[(3-methylphenoxy)methyl]thieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-methylbutyl)amino]-ethanone, monohydrochloride Solubility (25°C)：   体外:   DMSO ≥ 51 mg/mL (120.56mM) Water 2.5 mg/mL (5.91mM; Need ultrasonic) Ethanol   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3640mL 11.8201mL 23.6401mL 5mM 0.4728mL 2.3640mL 4.7280mL 10mM 0.2364mL 1.1820mL 2.3640mL   生物活性 产品描述 一种有效的选择性刺猬酰基转移酶 (Hhat) 抑制剂，IC50 为 850nM。RU-SKI 43 hydrochloride 通过独立于平滑化的非规范信号传导降低 Gli-1 激活，并抑制 Akt 和 mTOR 通路活性。RU-SKI 43 hydrochloride 具有抗癌活性。 靶点 IC50: 850nM (Hhat) 体外研究 RU-SKI 43 hydrochloride (10μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells . RU-SKI 43 hydrochloride (10 or 20μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours. RU-SKI 43 hydrochloride (10μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells. RU-SKI 43 hydrochloride (10μM; 48 hours) results in decreased phosphorylation (47-67%) of four proteins in the Akt pathway, including Akt (phosphorylation at both Thr307 and Ser473), PRAS40, Bad and GSK-3β. RU-SKI 43 treatment also decreases phosphorylation of mTOR and S6, members of the mTOR signaling pathway. RU-SKI 43 hydrochloride behaves as an uncompetitive inhibitor (Ki=7.4μM) with respect to Shh, and as a noncompetitive inhibitor (Ki=6.9μM) with respect to 125I-iodo-palmitoylCoA . Cell Proliferation Assay Cell Line: AsPC-1 and Panc-1 pancreatic cancer cells Concentration: 10μM Incubation Time: For 6 days (drugs were replenished every 48 hours) Result: Strongly decreased cell proliferation (83% in AsPC-1 cells). Western Blot Analysis Cell Line: COS-1 cells expressing HA-Hhat and Shh Concentration: 10 or 20μM Incubation Time: 5 hours Result: Caused dose-dependent inhibition of Shh palmitoylation following only 5 hours. 体内研究 RU-SKI 43 hydrochloride has a t1/2 of 17 min in mouse plasma after IV administration.
保存条件：-20℃

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