RU-SKI 43 HCL;HHAT INHIBITOR
- CAS号:1782573-67-4
- 英文名:2-(2-methylbutylamino)-1-[4-[(3-methylphenoxy)methyl]-6,7-dihydro-4H-thieno[3,2-c]pyridin-5-yl]ethanone:hydrochloride
- 中文名:RU-SKI 43 HCL;HHAT INHIBITOR
- CBNumber:CB13831060
- 分子式:C22H31ClN2O2S
- 分子量:423.01
- MOL File:1782573-67-4.mol
- 储存条件 :Store at -20°C
- 溶解度 :DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
- 形态 :A crystalline solid
- 颜色 :White to off-white
RU-SKI 43 HCL;HHAT INHIBITOR性质、用途与生产工艺
- 生物活性 RU-SKI 43 hydrochloride 是一种有效的选择性刺猬酰基转移酶 (Hhat) 抑制剂，IC50 为 850 nM。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。
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靶点
IC50: 850 nM (Hhat)
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体外研究
RU-SKI 43 hydrochloride (10 μM; 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 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours.
RU-SKI 43 hydrochloride (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells.
RU-SKI 43 hydrochloride (10 μM; 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 (K i =7.4 μM) with respect to Shh, and as a noncompetitive inhibitor (K i =6.9 μM) with respect to 125 I-iodo-palmitoylCoA.
Cell Proliferation Assay
Cell Line: AsPC-1 and Panc-1 pancreatic cancer cells Concentration: 10 μM 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 20 μM 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 t 1/2 of 17 min in mouse plasma after IV administration.
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