RepSox

446859-33-2

287.32

DMSO : >= 52 mg/mL (180.98 mM)

TGF-beta/Smad

RepSox (E-616452) is a potent and selective of the TGFbetaR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC₅₀ of 4 nM. IC50 & Target: IC50: 4 nM (ALK5 autophosphorylation)^[1] In Vitro: RepSox also inhibits ATP binding to ALK5 with IC₅₀ of 23 nM. RepSox shows potent activity in both binding and cellular assays and exhibits selectivity over p38 mitogen-activated protein kinase. with IC₅₀ of >16 uM^[1]. RepSox act s as an inhibitor of the Tgfbeta1 kinase. Treatment with 25 uM RepSox almost completely eliminates Smad3 phosphorylation, indicating that RepSox strongly inhibits Tgfbeta signaling in somatic cells. RepSox is most effective at replacing Sox2 during days 10-11 after transduction and that therefore cultures of Oct4, Klf4, and cMyc-transduced MEFs give rise to intermediates capable of responding to RepSox treatment. These intermediates appear at day 4 post-transduction and peak at days 10-11. Treatment with RepSox decreased the proportion of cells in G₂/M phase of the cell cycle, indicating it does not increase the proliferation rate of these partially reprogrammed cells^[2].