代理Thiazovivin/1226056-71-8 卷曲蛋白激酶(ROCK)抑制剂,50mg 现货


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。
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

其他相关的 ROCK 产品

LEE011

LEE011 是一口服有效的,高度特异性CDK4/6抑制剂。

EHop-016

EHop-016 是一种特异性的Rac GTPase抑制剂,作用于Rac1, IC50为1.1 μM,同等有效抑制Rac3。

ZCL278

ZCL278是一个选择性的Cdc42 GTP酶抑制剂,Kd为11.4 μM。

Y-27632 2HCl

Y-27632 2HCl是一种选择性的ROCK1(p160ROCK)抑制剂,Ki为140 nM,比对其他激酶包括PKC,cAMP依赖性蛋白激酶, MLCK和PAK的作用强200多倍。

GSK429286A

GSK429286A是一种选择性的ROCK1和ROCK2抑制剂,IC50分别为14 nM和63 nM。

特征: More selective than Y-27632.

Fasudil (HA-1077) HCl

Fasudil (HA-1077) HCl是一种有效的ROCK-II, PKA, PKG, PKC,和MLCK抑制剂, Ki分别为0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM,和36 μM。

RKI-1447

RKI-1447是一种有效的ROCK1和ROCK2抑制剂,IC50分别为14.5 nM和6.2 nM,有抗侵入和抗肿瘤活性。

Palbociclib (PD-0332991) HCl

Palbociclib (PD-0332991) HCl是一种高度选择性的CDK4/6抑制剂,IC50为11 nM/16 nM,对CDK1/2/5, EGFR, FGFR, PDGFR, InsR等没有抑制活性。Phase 3。

特征: PD-0332991作为有应用前景的工具测定CDK激酶是否具有明显的治疗价值。

Alisertib (MLN8237)

Alisertib (MLN8237)是一种选择性的Aurora A抑制剂,IC50为1.2 nM,作用于Aurora A比作用于Aurora B选择性强200倍以上。Phase 3。

特征: MLN8237 是第一个口服有效的小分子Aurora A激酶选择性抑制剂。

BI 2536

BI 2536是一种有效的Plk1抑制剂,IC50为0.83 nM,比作用于Plk2和Plk3选择性分别高4和11倍。Phase 2。

特征: BI 2536是第一个有效的Plk1选择性抑制剂,抑制 Plk1的标记。

溶解性 (25°C)*

体外 DMSO 15 mg/mL (48 mM)
<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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