| 產(chǎn)品描述 |
Thiazovivin是一種新型ROCK抑制劑，IC50為0.5 μM，在單細(xì)胞分離后，促進(jìn)人胚胎干細(xì)胞（hESC）的存活。 |
| 靶點(diǎn) |
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(xué)式（C15H13N5OS） |
Thiazovivin/1226056-71-8 卷曲蛋白激酶(ROCK)抑制劑,50mg化學(xué)屬性
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其他相關(guān)的 ROCK 產(chǎn)品
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EHop-016
EHop-016 是一種特異性的Rac GTPase抑制劑，作用于Rac1， IC50為1.1 μM，同等有效抑制Rac3。
ZCL278
ZCL278是一個(gè)選擇性的Cdc42 GTP酶抑制劑，Kd為11.4 μM。
Y-27632 2HCl
Y-27632 2HCl是一種選擇性的ROCK1(p160ROCK)抑制劑，Ki為140 nM，比對(duì)其他激酶包括PKC，cAMP依賴(lài)性蛋白激酶， MLCK和PAK的作用強(qiáng)200多倍。
GSK429286A
GSK429286A是一種選擇性的ROCK1和ROCK2抑制劑，IC50分別為14 nM和63 nM。
特征: More selective than Y-27632.
Fasudil (HA-1077) HCl
Fasudil (HA-1077) HCl是一種有效的ROCK-II， PKA， PKG， PKC，和MLCK抑制劑， Ki分別為0.33 μM， 1.6 μM， 1.6 μM， 3.3 μM，和36 μM。
RKI-1447
RKI-1447是一種有效的ROCK1和ROCK2抑制劑，IC50分別為14.5 nM和6.2 nM，有抗侵入和抗腫瘤活性。
Palbociclib (PD-0332991) HCl
Palbociclib (PD-0332991) HCl是一種高度選擇性的CDK4/6抑制劑，IC50為11 nM/16 nM，對(duì)CDK1/2/5， EGFR， FGFR， PDGFR， InsR等沒(méi)有抑制活性。Phase 3。
特征: PD-0332991作為有應(yīng)用前景的工具測(cè)定CDK激酶是否具有明顯的治療價(jià)值。
Alisertib (MLN8237)
Alisertib (MLN8237)是一種選擇性的Aurora A抑制劑，IC50為1.2 nM，作用于Aurora A比作用于Aurora B選擇性強(qiáng)200倍以上。Phase 3。
特征: MLN8237 是第一個(gè)口服有效的小分子Aurora A激酶選擇性抑制劑。
BI 2536
BI 2536是一種有效的Plk1抑制劑，IC50為0.83 nM，比作用于Plk2和Plk3選擇性分別高4和11倍。Phase 2。
特征: BI 2536是第一個(gè)有效的Plk1選擇性抑制劑，抑制 Plk1的標(biāo)記。
|
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(cè)是由Selleck技術(shù)部門(mén)檢測(cè)的，可能會(huì)和文獻(xiàn)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 |
