A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively
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Product Description
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
