RepSox (446859-33-2) Description:
RepSox is a potent and selective inhibitor of the TGFβR-1/ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation in cell-free assays, respectively.
ALK5 inhibitor II is a cell permeable, selective inhibitor of the TGF-β type 1 activin like kinase receptor ALK5 (IC50s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively). This inhibitor demonstrated less potent activity (IC50s > 16 μM) when tested against a panel of 9 related kinases, including p38 MAPK and GSK3. At 25 μM, this compound has been used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2 via inhibition of the TGF-β signaling pathway and induction of Nanog transcription.
RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression.
RepSox Inhibits TGF-beta receptor signaling. Retroviral transduction of Sox2, Oct4, and Klf4 genes results in direct reprogramming of somatic cells into induced pluripotent stem cells.
RepSox (446859-33-2) Specifications:
|Synonyms||SJN 2511; SJN2511; SJN-2511; ALK5 Inhibitor II; E 616452; E-616452; E616452;TGF-β RI Kinase Inhibitor II|
|Molecular Weight||287.326 g/mol|
|Monoisotopic Mass||287.117 g/mol|
|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||An ATP-competitive inhibitor of TGF-β RI kinase|