1226056-71-8
中文名稱
THIAZOVIVIN
英文名稱
Thiazovivin
CAS
1226056-71-8
分子式
C15H13N5OS
MDL 編號
MFCD16495823
分子量
311.362
MOL 文件
1226056-71-8.mol
更新日期
2025/01/23 13:36:08
1226056-71-8 結構式
基本信息
中文別名
N-芐基-2-(嘧啶-4-基氨基)噻唑-4-羧酰胺N-芐基-2-(嘧啶-4-基氨基)噻唑-4-甲酰胺
英文別名
ThiazovivinThiazovivin, >=98%
N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide
N-(Phenylmethyl)-2-(4-pyrimidinylamino)-4-thiazolecarboxamide
Thiazovivin N-(Phenylmethyl)-2-(4-pyrimidinylamino)-4-thiazolecarboxamide
N-(Phenylmethyl)-2-(4-pyrimidinylamino)-4-thiazolecarboxamide Thiazovivin
所屬類別
生物化工：ROCK 抑制劑物理化學性質
密度1.379
儲存條件-20°C
儲存條件-20°C儲存
溶解度在DMSO中的溶解度為20mg/mL，澄清
酸度系數(pKa)13.87±0.46(Predicted)
形態(tài)粉末
顏色白色到米色到棕色
穩(wěn)定性Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
常見問題列表
生物活性
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。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. Thiazovivin at 1 μM increases the reprogramming efficiency of CB mononuclear cells to induced pluripotent stem cells (iPSCs) by more than 10 times.生物活性
Thiazovivin是一種新型ROCK抑制劑，無細胞試驗中IC50為0.5 μM，在單細胞分離后，促進人胚胎干細胞（hESC）的存活。靶點
| Target | Value |
|
ROCK
(Cell-free assay) | ~0.5 μM |
體外研究
盡管對細胞增殖影響較小，Thiazovivin治療顯著增強人胚胎干細胞(hESCs)的存活，使其被酶解后的存活增強30多倍，同時均勻維持特有集落形態(tài)的多潛能，和典型多潛能標志物，如堿性磷酸酶(ALP) 的表達，和正常核型。解離的hESCs用Thiazovivin處理幾小時內顯著增加其對人工基底膜-或層粘連蛋白涂覆板的粘附，而對明膠涂覆的平板沒有影響。Thiazovivin治療增加細胞-ECM粘附介導的β1整合蛋白活性，其與生長因子協同促進細胞存活。除了活化整合蛋白，Thiazovivin，而不是Tyrintegin (Ptn)，也能夠通過E-鈣黏蛋白介導的細胞-細胞相互作用，保護hESCs在ECM缺乏的懸浮液中免于死亡。Thiazovivin治療有效抑制E-鈣黏蛋白的內吞作用，從而穩(wěn)定細胞表面的E-鈣黏蛋白，并使細胞-細胞相互作用恢復，這對hESC在無ECM環(huán)境下的存活是必須的。Thiazovivin，而不是Tyrintegin (Ptn)，在2 μM濃度下抑制Rho相關的激酶(ROCK)活性，并保護hESCs，與廣泛使用的選擇性ROCK抑制劑Y-27632在10 μM濃度下的作用類似，表明Rho-ROCK信號調節(jié)細胞-ECM和細胞-細胞粘附。1 μM Thiazovivin增加CB單核細胞的重組效能，以誘導10倍以上的多功能干細胞(iPSCs)。