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KI1239E-61645210 mg$234

Chemical Characteristic

Product NameE-616452
SynonymsRepSox
CAS No.446859-33-2
Molecular Weight 287.32
FormulaC17H13N5
Chemical Name2-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]-1,5-naphthyridine
Smilesn1c(ccc2ncccc12)c1c(n[nH]c1)c1cccc(n1)C
Chemical Structure

Biological activities

E-616452 is a transforming growth factor-β receptor 1 (Tgfbr1) inhibitor. E-616452 induces the formation of GFP+ colonies with an efficiency similar to viral Sox2.[1] E-616452 replaces Sox2 in reprogramming by inhibiting transforming growth factor-β (Tgf-β) signaling, which in turn induces Nanog expression. E-616452 generates iPSCs in cells transduced with only two TFs, Oct4 and Klf4.[2] E-616452 also inhibits ALK5 autophosphorylation with an IC50 of 4 nM.[3] E-616452 replaces Sox2 by acting on intermediates formed during the reprogramming process. E-616452 at the dose of 25 µM almost completely eliminates Smad3 phosphorylation. [1]

References

[1] Ichida JK, et al. A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog. Cell Stem Cell. 2009, 5(5):491-503.
[2] Solanki A, et al.A step closer to complete chemical reprogramming for generating iPS cells.Chembiochem. 2010, 11(6):755-777.
[3] Gellibert F, et al.Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem. 2004, 47(18):4494-4506.

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