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TP0427736 hydrochloride

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Chemical Structure| 2459963-17-6 同义名 : -
CAS号 : 2459963-17-6
货号 : A544247
分子式 : C14H11ClN4S2
纯度 : 99%+
分子量 : 334.847
MDL号 : MFCD32633583
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 2 mg/mL(5.97 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 3 mg/mL(8.96 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 The transforming growth factor-β (TGF-β) type I receptor kinase ALK5 (activin receptor-like kinase 5) is an attractive target for intervention in TGFβ signaling due to its druggability as well as its centrality and specificity in the pathway[1]. TP0427736 potently inhibited ALK5 activity, with an IC50 value of 2.72 nM. Its ability to inhibit ALK3 was quite low compared with ALK5, with an IC50 value of 836 nM.[2]. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 in a concentration-dependent manner, with an IC50 value of 8.68 nM. TP0427736 rescues proliferation of outer root sheath cells suppressed by TGF-β[2]. The topical application of TP0427736 significantly decreased Smad2 phosphorylation in mouse skin, and its repeated application suppressed the shortening of average hair follicle length during the transition from the late anagen phase to the catagen phase[2]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.99mL

0.60mL

0.30mL

14.93mL

2.99mL

1.49mL

29.86mL

5.97mL

2.99mL
参考文献

[1]Ling LE, Lee WC. Tgf-beta type I receptor (Alk5) kinase inhibitors in oncology. Curr Pharm Biotechnol. 2011 Dec;12(12):2190-202. doi: 10.2174/138920111798808257. PMID: 21619541.

[2]Naruse T, Aoki M, Fujimoto N, Arase S, Oura H, Ueda Y, Ikeda A. Novel ALK5 inhibitor TP0427736 reduces TGF-β　induced growth inhibition in human outer root sheath cells and elongates anagen phase in mouse hair follicles. Pharmacol Rep. 2017 Jun;69(3):485-491. doi: 10.1016/j.pharep.2017.01.024. Epub 2017 Jan 25. PMID: 28324846.