SB-431542 是 TGF-β 受体激酶抑制剂(TRKI)。SB-431542 对 ALK4、ALK5 和 ALK7 活性有抑制作用，IC50值分别为 1 μM、0.75 μM 和 2 μM。SB-431542 还能抑制 TGF-β 诱导的转录、基因表达、细胞凋亡和生长抑制。SB-431542 可用于癌症及其信号转导途径的研究。
| 生物活性 | SB-431542 is aTGF-β receptorkinase inhibitor (TRKI). SB-431542 has inhibitory activity forALK4,ALK5andALK7withIC50values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression,apoptosis, and growth suppression. SB-431542 can be used for the research ofcancerand signal transduction pathways[1][2][3]. |
| IC50& Target[1] | ALK4 1 μM (IC50) | ALK5 0.75 μM (IC50) | ALK7 2 μM (IC50) |
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体外研究
(In Vitro) | SB-431542 can inhibit the activity for ALK4, ALK5 and ALK7 with IC50values of 1 μM, 0.75 μM and 2 μM, respectively[1].
SB-431542 (0- 10 μM; 24 h) inhibits ALK5 and also the activin type I receptor ALK4 and the nodal type I receptor ALK7, which are very highly related to ALK5 in their kinase domains[1].
SB-431542 (0.1, 0.5, 1, 5, or 10 μM; 30 min) efficiently inhibits Smad phosphorylation induced by TGF-β and activin but not BMP4[1].
SB-431542 (0-10 μM) inhibits TGF-beta-induced transcription, gene expression, apoptosis, and growth suppression[2].
Western Blot Analysis[1] | Cell Line: | NIH 3T3 cells; HaCaT, NIH 3T3, C2C12 cells and T47D cells | | Concentration: | 10 μM; 0.1, 0.5, 1, 5, or 10 μM | | Incubation Time: | 24 h; 30 min | | Result: | Inhibited efficiently phosphorylated Smad2.
Inhibited the TGF-β- and activin-induced phosphorylation of Smad2 but not BMP-induced phosphorylation of Smad1. |
Apoptosis Analysis[2] | Cell Line: | A549 and HT29 cells | | Concentration: | 10 μM | | Incubation Time: | 24 h | | Result: | Inhibited TGF-induced growth suppression and apoptosis. |
Cell Invasion Assay[2] | Cell Line: | A549 cells | | Concentration: | 2, 10 μM | | Incubation Time: | 21 h | | Result: | Blocked TGF- induced tumor cell invasion. |
Cell Migration Assay[2] | Cell Line: | A549 cells | | Concentration: | 2, 10 μM | | Incubation Time: | 5 h , 30 h | | Result: | Blocked TGF- induced tumor cell migration. |
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体内研究
(In Vivo) | SB-431542 (subconjunctival; 0.5 and 2 mM; on days 1, 2, 3, and 7) inhibits scar formation after glaucoma filtration surgery in New Zealand rabbits[3].
| Animal Model: | Rabbits (3 to 5 months, 1.8 - 2.5 kg)[3] | | Dosage: | 0.5 and 2 mM | | Administration: | Subconjunctival injection, on days 1, 2, 3, and 7 | | Result: | Showed wound healing and less severe scar formation. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(650.38 mM;Need ultrasonic) Ethanol : 11.17 mg/mL(29.06 mM;Need ultrasonic and warming) 配制储备液 | 1 mM | 2.6015 mL | 13.0076 mL | 26.0152 mL | | 5 mM | 0.5203 mL | 2.6015 mL | 5.2030 mL | | 10 mM | 0.2602 mL | 1.3008 mL | 2.6015 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。-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 (5.41 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.41 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.41 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 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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