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A 83-01 (ALK5 Inhibitor IV) 是一种 TGF-βI 型受体 ALK5、ALK4 和 ALK7 的抑制剂 (IC50=12/45/7.5 nM)。A 83-01 可促进小鼠成纤维细胞重编程为 iPSCs。A 83-01 可用于类器官培养。
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A 83-01 (ALK5 Inhibitor IV) 是一种 TGF-βI 型受体 ALK5、ALK4 和 ALK7 的抑制剂 (IC50=12/45/7.5 nM)。A 83-01 可促进小鼠成纤维细胞重编程为 iPSCs。A 83-01 可用于类器官培养。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 285 | 现货 | |
5 mg | ¥ 493 | 现货 | |
10 mg | ¥ 786 | 现货 | |
25 mg | ¥ 1,460 | 现货 | |
50 mg | ¥ 2,380 | 现货 | |
100 mg | ¥ 3,730 | 现货 | |
500 mg | ¥ 7,580 | 现货 |
产品描述 | A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12/45/7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures. |
靶点活性 | ALK5:12 nM, ALK7:7.5 nM, ALK4:45 nM |
体外活性 | 方法:野生型水貂肺上皮细胞 Mv1Lu 用 A 83-01 (0.03-10 μM) 和 TGF-β (1 ng/mL) 处理 48 h,使用 Coulter counter 检测细胞增殖。 结果:A 83-01 以剂量依赖的方式阻止 TGF-β 对 Mv1Lu 细胞生长的抑制。[1] 方法:小鼠卵巢癌细胞 HM-1 用 A 83-01 (1-10 μM) 处理 30 min,随后用 TGF-β (1-10 ng/mL) 处理 60 min,使用 Western Blot 方法检测靶点蛋白表达水平。 结果:添加 TGF-β1 增加了 pSmad3 的表达,A 83-01 抑制了 TGF-β 的上调。[2] |
体内活性 | 方法:为检测体内抗肿瘤活性,将 A 83-01 (150 μg/只) 腹腔注射给 HM-1 癌症腹膜扩散的 B6C3F1 小鼠模型,每周三次,持续四周。 结果:A 83-01 治疗组的腹水形成往往较慢,A 83-01 显著提高了小鼠的存活率。[2] 方法:为研究在心肌损伤中的作用,将 A 83-01 (10 mg/kg) 腹腔注射给 Nkx2.5 enh-Cre/mTmG 小鼠,每天一次,持续七天。 结果:A 83-01 治疗在基线和心肌损伤后显著增加了 Nkx2.5+ 心肌成肌细胞的数量,导致新形成的心肌细胞增加。A 83-01 治疗显著改善了心室弹性和卒中功,从而改善了损伤后的收缩能力。[3] |
细胞实验 | HM-1 cells are seeded into a 96-well plate and are incubated for 18 hr. A-83-01 (1 μM) or vehicle are then added for 12 hr followed by the addition of TGF-β1 (1 ng/mL) or vehicle for 60 hr. The number of viable cells in each well is examined using the WST-1 assay following the manufacturer's instructions. |
别名 | ALK5 Inhibitor IV, A8301 |
分子量 | 421.52 |
分子式 | C25H19N5S |
CAS No. | 909910-43-6 |
Smiles | Cc1cccc(n1)-c1nn(cc1-c1ccnc2ccccc12)C(=S)Nc1ccccc1 |
密度 | 1.27g/cm3 |
存储 | store at low temperature | Powder: -20°C for 3 years | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 10 mg/mL (23.72 mM), The compound is unstable in solution. Please use soon. 10% DMSO+90% Saline: 1 mg/mL (2.37 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. | ||||||||||||||||||||||||||||||
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