(E)-SIS3 是一种有效和选择性的Smad3抑制剂,抑制 Smad3 磷酸化的IC50为 3 μM。(E)-SIS3 通过 TGF-β1 抑制成纤维细胞向肌成纤维细胞分化。
生物活性 | (E)-SIS3 is a potent and selective inhibitor ofSmad3with anIC50of 3 μM forSmad3phosphorylation. (E)-SIS3 inhibits the myofibroblast differentiation of fibroblasts byTGF-β1[1]. |
IC50& Target | IC50: 3 μM (Smad3 phosphorylation)[1] |
体外研究 (In Vitro) | (E)-SIS3 (0.3-10 μM; for 1 hour) attenuates the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4[1]. (E)-SIS3 (0.1 , 10, 50 μM; 30 min) significantly suppresses the expression of FN and α-SMA, but not that of Sphk2 provoked by TGF-β1[2]. (E)-SIS3 (10 μM; 24 hours) significantly reduces both α-SMA and palladin expression that is enhanced by TWEAK in Primary human dermal fibroblasts[3]. (E)-SIS3 significantly inhibits L4 development at five concentrations from as low as 2 μM to 50 μM (5 μM, 10 μM, 20 μM and 50 μM) in a dose-dependent manner[4].
Western Blot Analysis[1] Cell Line: | Human dermal fibroblasts | Concentration: | 0.3, 1, 3, 10 μM | Incubation Time: | For 1 hour | Result: | Attenuated the TGF-beta1-induced phosphorylation of Smad3 and interaction of Smad3 with Smad4. |
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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 : 125 mg/mL(255.11 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液 1 mM | 2.0409 mL | 10.2043 mL | 20.4086 mL | 5 mM | 0.4082 mL | 2.0409 mL | 4.0817 mL | 10 mM | 0.2041 mL | 1.0204 mL | 2.0409 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: ≥ 2.08 mg/mL (4.24 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.24 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 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。 *以上所有助溶剂都可在本网站选购。
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