RU-SKI 43 hydrochloride(Synonyms: RU-SKI 43(盐酸盐))

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 hydrochloride (Synonyms: RU-SKI 43(盐酸盐)) 纯度: 98.54%

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。

RU-SKI 43 hydrochloride(Synonyms: RU-SKI 43(盐酸盐))

RU-SKI 43 hydrochloride Chemical Structure

CAS No. : 1782573-67-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1024 In-stock
2 mg ¥800 In-stock
5 mg ¥1100 In-stock
10 mg ¥1600 In-stock
50 mg ¥6900 In-stock
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200 mg   询价  

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生物活性

RU-SKI 43 hydrochloride is a potent and selective Hedgehog acyltransferase (Hhat) inhibitor with an IC50 of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreases Akt and mTOR pathway activity. RU-SKI 43 hydrochloride has anti-cancer activity[1].

IC50 & Target

IC50: 850 nM (Hhat)[1]

体外研究
(In Vitro)

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[2].
RU-SKI 43 hydrochloride (10 or 20 μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours[1].
RU-SKI 43 hydrochloride (10 μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells[2].
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[2].
RU-SKI 43 hydrochloride 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 hydrochloride 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

423.01

Formula

C22H31ClN2O2S

CAS 号

1782573-67-4

中文名称

RU-SKI 43(盐酸盐)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 51 mg/mL (120.56 mM)

H2O : 2.5 mg/mL (5.91 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3640 mL 11.8201 mL 23.6401 mL
5 mM 0.4728 mL 2.3640 mL 4.7280 mL
10 mM 0.2364 mL 1.1820 mL 2.3640 mL

*

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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.91 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.91 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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