Cofttek holdings limited

TGF-beta&Smad

RepSox (446859-33-2)

RepSox, also known as SJN 2511, E 616452 and 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)

Not Intended for Therapeutic Use. For research use only.

CAS: 446859-33-2 Category

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:

Product Name RepSox
Synonyms SJN 2511; SJN2511; SJN-2511; ALK5 Inhibitor II; E 616452; E-616452; E616452;TGF-β RI Kinase Inhibitor II
Chemical Name 2-[5-(6-methylpyridin-2-yl)-1~{H}-pyrazol-4-yl]-1,5-naphthyridine
Purity >98%
CAS Number 446859-33-2
Molecular Formula C17H13N5
Molecular Weight 287.326 g/mol
Monoisotopic Mass 287.117 g/mol
MDL number MFCD09037561
InChIKey LBPKYPYHDKKRFS-UHFFFAOYSA-N
InChi Code InChI=1S/C17H13N5/c1-11-4-2-5-16(20-11)17-12(10-19-22-17)13-7-8-14-15(21-13)6-3-9-18-14/h2-10H,1H3,(H,19,22)
SMILES CC1=CC=CC(=N1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4
Form powder
Color Yellow
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

 


=

RIDADR NONH for all modes of transport

References:

  • RepSox improves viability and regulates gene expression in rhesus monkey-pig interspecies cloned embryos. Zhu HY et al. Biotechnol Lett. (2017) Cotreatment with RepSox and LBH589 improves the invitro developmental competence of porcine somatic cell nuclear transfer embryos. Luo ZB et al. Reprod Fertil Dev. (2018)
  • Transforming growth factor β-inhibitor Repsox downregulates collagen expression of scleroderma dermal fibroblasts and prevents bleomycin-induced mice skin fibrosis. Ide M et al. Exp Dermatol. (2017)

1 review for RepSox (446859-33-2)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The RepSox (446859-33-2) is high purity,also customer service is pretty nice !gotta try!!

Add a review

Your email address will not be published. Required fields are marked *