N-benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide
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產(chǎn)品描述 | Thiazovivin是一種新型ROCK抑制劑,IC50為0.5 μM,在單細胞分離后,促進人胚胎干細胞(hESC)的存活。 | |||||
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靶點 | ROCK | |||||
IC50 | ~0.5 μM?[1] | |||||
體外研究 | 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] | |||||
體內(nèi)研究 | ||||||
分子量(311.36),化學式(C15H13N5OS) |
Thiazovivin/1226056-71-8 卷曲蛋白激酶(ROCK)抑制劑,50mg化學屬性
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溶解性 (25°C)?* |
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體外 | DMSO | 15 mg/mL (48 mM) | |
水 | <1 mg/mL (<1 mM) | ||
乙醇 | <1 mg/mL (<1 mM) | ||
體內(nèi) | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
*?<1 mg/ml 指產(chǎn)品微溶或不溶 *?溶解度檢測是由Selleck技術(shù)部門檢測的,可能會和文獻中提供的溶解度有所差異,這是由于生產(chǎn)工藝和批次不同產(chǎn)生的正?,F(xiàn)象。 |
Chemical Name | N-benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide |
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