N-benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide
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产品描述 | Thiazovivin是一种新型ROCK抑制剂,IC50为0.5 μM,在单细胞分离后,促进人胚胎干细胞(hESC)的存活。 | |||||
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靶点 | ROCK | |||||
IC50 | ~0.5 μM [1] | |||||
体外研究 | Although displaying little impact on cell proliferation, Thiazovivin treatment significantly enhances the survival of human embryonic stem cells (hESCs) after enzymatic dissociation more than 30-fold, while homogenously maintaining pluripotency with the characteristic colony morphology, expression of typical pluripotency markers such as alkaline phosphatase (ALP), and normal karyotype. Dissociated hESCs treated with Thiazovivin display dramatically increased adhesion to matrigel- or laminin-coated plates but not to gelatin-coated plates within a few hours. Thiazovivin treatment increases cell-ECM adhesion-mediated β1 integrin activity, which synergizes with growth factors to promote cell survival. In addition to activating integrin, Thiazovivin but not Tyrintegin (Ptn) protects hESCs from death in the absence of ECM in suspension through E-cadherin-mediated cell-cell interaction. Thiazovivin treatment potently inhibits endocytosis of E-cadherin, consequently stabilizing E-cadherin on the cell surface and leading to reestablishment of cell-cell interaction, which is essential for hESC survival in ECM-free conditions. Thiazovivin but not Tyrintegin (Ptn) at 2 μM inhibits Rho-associated kinase (ROCK) activity and protects hESCs at a similar level as the widely used selective ROCK inhibitor Y-27632 at 10 μM, suggesting that Rho-ROCK signaling regulates cell-ECM and cell-cell adhesion. [1] Thiazovivin at 1 μM increases the reprogramming efficiency of CB mononuclear cells to induced pluripotent stem cells (iPSCs) by more than 10 times. [2] | |||||
体内研究 | ||||||
分子量(311.36),化学式(C15H13N5OS) |
Thiazovivin/1226056-71-8 卷曲蛋白激酶(ROCK)抑制剂,50mg化学属性
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溶解性 (25°C) * |
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体外 | DMSO | 15 mg/mL (48 mM) | |
水 | <1 mg/mL (<1 mM) | ||
乙醇 | <1 mg/mL (<1 mM) | ||
体内 | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
* <1 mg/ml 指产品微溶或不溶 * 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。 |
Chemical Name | N-benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide |
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