RU-SKI 43

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RU-SKI 43 

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。

RU-SKI 43

RU-SKI 43 Chemical Structure

CAS No. : 1043797-53-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

RU-SKI 43 的其他形式现货产品:

RU-SKI 43 hydrochloride

生物活性

RU-SKI 43 is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway 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 to 125I-iodo-palmitoylCoA[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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 t1/2 of 17 min in mouse plasma after IV administration[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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.
参考文献

  • [1]. Petrova E, et al. Inhibitors of Hedgehog acyltransferase block Sonic Hedgehog signaling.Nat Chem Biol. 2013 Apr;9(4):247-9.

    [2]. Petrova E, et al. Hedgehog acyltransferase as a target in pancreatic ductal adenocarcinoma. Oncogene. 2014 Jan 27. doi: 10.1038/onc.2013.575.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务