RepSox

• CAT Number: I003580
• CAS Number: 446859-33-2
• Molecular Formula: C17H13N5
• Molecular Weight: 287.3
• Purity: ≥95%
• Target: SMAD
• Solubility: DMSO: ≥ 52 mg/mL
• Storage: 2-8°C
• IC50: 23 nM
• IUPAC Name: 2-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]-1,5-naphthyridine
• InChI: 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)
• InChIKey: LBPKYPYHDKKRFS-UHFFFAOYSA-N
• SMILES: CC1=NC(=CC=C1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4

RepSox (Cat No.:I003580)also known as E-616452, SJN 2511, ALK5 Inhibitor II, is a highly potent and selective inhibitor of TGFβ receptor-1 (ALK5). It specifically targets the ATP binding site of ALK5 and inhibits its autophosphorylation. In cell-free assays, RepSox demonstrates an IC50 of 23 nM for ATP binding to ALK5 and 4 nM for ALK5 autophosphorylation. By blocking ALK5 signaling, RepSox effectively modulates TGFβ pathway activity, which plays a critical role in various cellular processes.

Reference

1:Transforming growth factor β inhibitor Repsox down-regulates collagen expression of scleroderma dermal fibroblasts and prevents bleomycin-induced mice skin fibrosis. Ide M, Jinnin M, Tomizawa Y, Wang Z, Kajihara I, Fukushima S, Hashizume Y, Asano Y, Ihn H.Exp Dermatol. 2017 Apr 18. doi: 10.1111/exd.13366. [Epub ahead of print] PMID: 28418584 2:RepSox improves viability and regulates gene expression in rhesus monkey-pig interspecies cloned embryos. Zhu HY, Jin L, Guo Q, Luo ZB, Li XC, Zhang YC, Xing XX, Xuan MF, Zhang GL, Luo QR, Wang JX, Cui CD, Li WX, Cui ZY, Yin XJ, Kang JD.Biotechnol Lett. 2017 May;39(5):775-783. doi: 10.1007/s10529-017-2308-3. Epub 2017 Feb 28. PMID: 28247195 3:RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. Jajosky AN, Coad JE, Vos JA, Martin KH, Senft JR, Wenger SL, Gibson LF.Stem Cells Transl Med. 2014 Jul;3(7):836-48. doi: 10.5966/sctm.2013-0193. Epub 2014 May 22. PMID: 24855276 Free PMC Article