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RU-SKI 43
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
RU-SKI 43图片
CAS NO:1043797-53-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
RU-SKI 43 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 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 具有抗癌活性。
生物活性

RU-SKI 43 is a potent and selectiveHedgehogacyltransferase(Hhat)inhibitor with anIC50of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreasesAktandmTORpathway activity. RU-SKI 43 has anti-cancer activity[1].

IC50& Target

IC50: 850 nM (Hhat)[1]

体外研究
(In Vitro)

RU-SKI 43 (10 μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells[2].
RU-SKI 43 (10 or 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours[1].
RU-SKI 43 (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells[2].
RU-SKI 43 (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[2].
RU-SKI 43 behaves as an uncompetitive inhibitor (Ki=7.4 μM) with respect to Shh, and as a noncompetitive inhibitor (Ki=6.9 μM) with respect to125I-iodo-palmitoylCoA[1].

Cell Proliferation Assay[2]

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[1]

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
(In Vivo)

RU-SKI 43 has a t1/2of 17 min in mouse plasma after IV administration[1].

分子量

386.55

Formula

C22H30N2O2S

CAS 号

1043797-53-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.