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 selectiveHedgehogacyltransferase(Hhat)inhibitor with anIC50of 850 nM. RU-SKI 43 hydrochloride reduces Gli-1 activation through Smoothened-independent non-canonical signaling and decreasesAktandmTORpathway activity. RU-SKI 43 hydrochloride has anti-cancer activity[1]. |
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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 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. |
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体内研究
(In Vivo) | RU-SKI 43 hydrochloride has a t1/2of 17 min in mouse plasma after IV administration[1].
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| 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 | 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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