RU-SKI 43 hydrochloride RU-SKI 43（盐酸盐）|cas:1782573-67-4|西域试剂

RU-SKI 43 hydrochloride RU-SKI 43（盐酸盐）,99.55%

产品编号：Bellancom-18366A| CAS NO：1782573-67-4| 分子式：C₂₂H₃₁ClN₂O₂S| 分子量：423.01

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货号	价格	库存与货期
Bellancom-18366A	￥800.00	杭州北京（现货）
Bellancom-18366A	￥1100.00	杭州北京（现货）
Bellancom-18366A	￥1600.00	杭州北京（现货）
Bellancom-18366A	￥6900.00	杭州北京（现货）

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

产品介绍

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。

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.

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 ¹²⁵I-iodo-palmitoylCoA.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(In Vivo)

RU-SKI 43 hydrochloride has a t_1/2 of 17 min in mouse plasma after IV administration.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

RU-SKI 43 hydrochloride has a t_1/2 of 17 min in mouse plasma after IV administration.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

RU-SKI 43 hydrochloride has a t_1/2 of 17 min in mouse plasma after IV administration.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

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