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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
A 83-01 是一种有效的 TGF-β I 型受体 ALK5,ALK4 和 ALK7 的抑制剂,能够抑制 ALK5,ALK4 和 ALK7 诱导的转录,IC50 值分别为 12 nM,45 nM 和 7.5 nM。
Information
A-83-01 is a potent inhibitor ofTGF-β type I receptor (ALK5-TD)with IC50 of 12 nM. A-83-01 also inhibits the transcription induced byactivin/nodal type I receptor (ALK4-TD)andnodal type I receptor (ALK7-TD)with IC50 of 45 nM and 7.5 nM, respectively.Solut
In vitro
A-83-01 inhibits the transcriptional activity induced by TGF-β type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. A-83-01 is potent in the inhibition of ALK5 and also prevents phosphorylation of Smad2/3 and the growth inhibition induced by TGF-β.
In vivo
A83-01 treatment significantly increases the number of Nkx2.5+ cardiomyoblasts at baseline and after myocardial injury, resulting in an increase in newly formed cardiomyocytes. A83-01 treatment significantly improves ventricular elastance and stroke work, leading to improved contractility after injury.
Cell Data
cell lines:
Concentrations:1 μM
Incubation Time:1 h
Powder Purity:
H302: 吞食有害
H315: 引起皮肤刺激
H319: 引起严重眼睛刺激
H335: 可能引起呼吸道刺激