A83-01 (909910-43-6) Description:
A-83-01 is an ALK inhibibitor. It was found that A-83-01 inhibited the transcriptional activity induced by TGF-beta 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 was found to be more potent in the inhibition of ALK5 than a previously described ALK-5 inhibitor, SB-431542, and also to prevent phosphorylation of Smad2/3 and the growth inhibition induced by TGF-beta. A-83-01 inhibited the epithelial-to-mesenchymal transition induced by TGF-beta, suggesting that A-83-01 and related molecules may be useful for preventing the progression of advanced cancers.
A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC50=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.
It has little effect on bone morphogenic type I receptors, p38 mitogen-activated protein kinase, or ERK. A 83-01 has been used to reprogram fibroblasts into alternative lineages, including neural stem cells and cardiomyocytes.
A83-01 (909910-43-6) Specifications:
|Synonyms||A8301; A 8301; A-8301|
|Molecular Weight||421.522 g/mol|
|Monoisotopic Mass||421.136 g/mol|
|Color||white to beige|
|Solubility||Soluble in DMSO (20 mg/ml), and ethanol (20 mg/ml).|
|Storage Temp.||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and light|
|Application||A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor; TGF-β/ALK5 inhibitor|