| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T426429-1ml |
1ml |
现货  |
|
| 英文别名 | 6-[5-(4-methyl-2-thiazolyl)-1H-imidazol-4-yl]-Benzothiazole hydrochloride |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | TP0427736 HCl |
| 生化机理 | TP0427736 是 ALK5 激酶活性的强效抑制剂，其 IC50 值为 2.72 nM，是 ALK3 抑制效果的 300 倍（ALK3 的 IC50 = 836 nM）。它还能抑制 TGF-β1 诱导的 A549 细胞 Smad2/3 磷酸化，IC50 值为 8.68 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
TP0427736是一种有效的ALK5 kinase抑制剂，IC50为2.72 nM，对ALK3的IC50为836 nM。在A549细胞中，它还能抑制TGF-β1诱导的Smad2/3磷酸化，IC50为8.68 nM。 Information TP0427736 is a potent inhibitor ofALK5 kinase activitywith anIC50of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. Targets ALK5 (Cell-free assay) 2.72 nM In vitro TP0427736 inhibits Smad2/3 phosphorylation in a concentration-dependent manner, with an IC50 value of 8.68 nM. In a cell-based assay of outer root sheath cells, TP0427736 rescued the inhibited proliferation by TGF-β1 and TGF-β2 in a concentration-dependent manner. In vivo TP0427736 decreases shortening of hair follicle length during the transition from the late anagen phase to the catagen phase. Cell Research(from reference) Cell lines：A549 cells Incubation Time：2 h |
| IC50 | ALK5, IC50: 2.72 nM |
|---|---|
| ALogP | 3.084 |
| HBD Count | 1 |
| Rotatable Bond | 2 |
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
| 分子类型 | 小分子 |
|---|---|
| IIUPAC Name | 6-[5-(4-methyl-1,3-thiazol-2-yl)-1H-imidazol-4-yl]-1,3-benzothiazole |
| INCHI | 1S/C14H10N4S2/c1-8-5-19-14(18-8)13-12(15-6-16-13)9-2-3-10-11(4-9)20-7-17-10/h2-7H,1H3,(H,15,16) |
| InChi Key | LLFCXRYULHMNCG-UHFFFAOYSA-N |
| Smiles | CC1=CSC(=N1)C2=C(N=CN2)C3=CC4=C(C=C3)N=CS4 |
| Isomeric SMILES | CC1=CSC(=N1)C2=C(N=CN2)C3=CC4=C(C=C3)N=CS4 |
| PubChem CID | 136105618 |
| 分子量 | 334.85 |
| DMSO(mg / mL) Max Solubility | 67 |
|---|---|
| DMSO(mM) Max Solubility | 200.089592354786 |
| Water(mg / mL) Max Solubility | ＜1 |
| 分子量 | 298.400 g/mol |
| XLogP3 | 3.300 |
| 氢键供体数Hydrogen Bond Donor Count | 1 |
| 氢键受体数Hydrogen Bond Acceptor Count | 5 |
| 可旋转键计数Rotatable Bond Count | 2 |
| 精确质量Exact Mass | 298.035 Da |
| 单同位素质量Monoisotopic Mass | 298.035 Da |
| 拓扑极表面积Topological Polar Surface Area | 111.000 Ų |
| 重原子数Heavy Atom Count | 20 |
| 形式电荷Formal Charge | 0 |
| 复杂度Complexity | 356.000 |
| 同位素原子数Isotope Atom Count | 0 |
| 定义的原子立体中心计数Defined Atom Stereocenter Count | 0 |
| 未定义的原子立体中心计数Undefined Atom Stereocenter Count | 0 |
| 定义的键立体中心计数Defined Bond Stereocenter Count | 0 |
| 未定义的键立体中心计数Undefined Bond Stereocenter Count | 0 |
| 所有立体化学键的总数The total count of all stereochemical bonds | 0 |
| 共价键合单元计数Covalently-Bonded Unit Count | 1 |
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