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
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TP0427736 HCl
Dangerous GoodsCAS number:864374-00-5 molecular formula:C14H11ClN4S2
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Specs
| Chinese alias | - | ||
| English alias | 6-[5-(4-methyl-2-thiazolyl)-1H-imidazol-4-yl]-Benzothiazole hydrochloride | ||
| CAS number | 864374-00-5 | molecular formula | C14H11ClN4S2 |
| molecular weight | 334.85 g/mol | Exact mass | 10mM in DMSO |
| PSA | 111.000 Ų | logp | 3.084 |
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Safety information
pictogram:
GHS09 , GHS07
Hazard Statement:
H302: 吞食有害 H410: 对水生生物有剧毒并具有长期持续影响
Statement of Preventive Measures:
P273: 避免释放到环境中。 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P270: 使用本产品时,请勿进食、饮水或吸烟。 P391: 收集溢出物 P330: 漱口 P301+P312: 如误吞咽:如感觉不适,呼叫急救中心/医生。
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