N-1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂，对 ALK5 介导的 Smad3 磷酸化的IC50为 5.3 nM。IN-1130 抑制酪蛋白的 ALK5 磷酸化 (IC50=36 nM)，抑制 p38α 丝裂原活化的蛋白激酶 (IC50=4.3 μM)。IN-1130 可抑制阻塞性肾病中的肾纤维化，阻止乳腺癌的肺转移。
| 生物活性 | IN-1130 is a highly selectivetransforming growth factor-βtype I receptor kinase (ALK5)inhibitor with anIC50of 5.3 nM for ALK5-mediatedSmad3phosphorylation. IN-1130 inhibitsALK5phosphorylation of casein (IC50=36 nM) and p38αmitogen-activated protein kinase(IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breastcancerlung metastasis[1][2]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | IN-1130 (0.5, 1 μM; for 2 hours) inhibits TGF-β-stimulated Smad2 phosphorylation and subsequent nuclear translocation in HepG2 and 4T1 cells[2].
IN-1130 (1 μM; for 72 hours) restores the TGF-β-mediated decrease in E-cadherin protein expression. IN-1130 (1 μM; for 72 hours) inhibits TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs in MCF10A cells[2].
IN-1130 (1 μM; pretreated for 30 min) inhibits TGF-β-induced MDA-MB-231 cells, NMuMG, and MCF10A cells mobility and invasion[2].
Western Blot Analysis[2] | Cell Line: | HepG2 and 4T1 cells | | Concentration: | 0.5, 1 μM | | Incubation Time: | For 2 hours | | Result: | Inhibited TGF-β-stimulated Smad2 phosphorylation. |
RT-PCR[2] | Cell Line: | MCF10A cells | | Concentration: | 1 μM | | Incubation Time: | For 72 hours | | Result: | Inhibited TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs. |
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体内研究
(In Vivo) | IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) reduces the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats[1].
IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys[1].
IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c mice)[2].
| Animal Model: | Six-week-old male Sprague–Dawley rats weighing 180-200 g[1] | | Dosage: | 10 and 20 mg/kg | | Administration: | IP; daily; for 7 and 14 days | | Result: | Reduced the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg. |
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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 : 100 mg/mL(237.83 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.3783 mL | 11.8915 mL | 23.7829 mL | | 5 mM | 0.4757 mL | 2.3783 mL | 4.7566 mL | | 10 mM | 0.2378 mL | 1.1891 mL | 2.3783 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 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.43 mg/mL (3.40 mM); Clear solution
此方案可获得 ≥ 1.43 mg/mL (3.40 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 14.3 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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