For research use only.

Catalog No.S7223 Synonyms: E-616452, SJN 2511

13 publications

RepSox Chemical Structure

Molecular Weight(MW): 287.32

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.

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Selleck's RepSox has been cited by 13 publications

3 Customer Reviews

  • (C) Generation of pluripotent stem cell from Yamanaka factors-induced OG2-MEFs under treatment of diverse chemical compounds. Images of GFP+ colonies were taken on day 10 post-infection. VPA, 0.5 mmol/L. CHIR99021, 3 μmol/L. Repsox, 1 μmol/L. (D) Quantification of GFP+ colonies in (C). All figures are representative of three independent experiments (n = 3). All data are presented as mean ± SD. *P < 0.05, **P < 0.01 vs. DMSO

    Protein Cell, 2017, 8(4):273-283. RepSox purchased from Selleck.

  • (a) Subcellular localization of Smad2/3 in HEKs grown in 3T3-J2 co-culture treated with dimethyl sulfoxide (DMSO), as a control, or 1 μM RepSox for 2 hrs (top panels). Lower panels represent corresponding nuclear counterstaining with Hoechst 33342. Bar=10 μm. (b) Nuclear-to-cytoplasmic ratios of Smad2/3 in HEKs as determined by fluorescence intensity using NIH ImageJ. Data shown are mean±SEM (n=6). ***P<0.001. (c) Proliferation of CK5+ epidermal cells in 3T3-J2 co-culture at day 5 as determined by a short-pulse labeling with BrdU, followed by quantification by flowcytometric analysis. Data shown are mean±SEM (n=3). **P<0.01.

    Wound Repair Regen, 2017, 25(3):526-531. RepSox purchased from Selleck.

  • Late Alk4/5/7 activity is required for skeletogenesis in S. purpuratus and L. variegatus. DIC (A-G) and polari ed light (A’-G’) images of S. purpuratus embryos: a control embryo (A, A’) and an embryo exposed to 0.5 μM (B, B’) and 5 μM (C, C’) SB431542, 1 μM (D, D’) and 10 μM (E, E’) SB525334, and 0.1 μM (F, F’) and 1 μM (G, G’) RepSox from the mesenchyme blastula stage (24 hpf) to the prism stage (50 hpf). DIC (H-K) and polarized light (H’-K’) images of L. variegatus embryos: a control embryo (H, H’) and an embryo exposed to 10 μM (I, I’) SB431542, 40 μM (J, J’) SB525334, and 1 μM (K, K’) RepSox from the early gastrula stage to the pluteus stage. The white arrow indicates an anterolateral rod. CB = ciliary band, CP = coelomic pouch, G = tri-partite gut, PC = pigment cell.

    Dev Biol, 2017,421(2):149-160. RepSox purchased from Selleck.

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Biological Activity

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.
TGFβR1(ALK5) [1]
(Cell-free assay)
4 nM
In vitro

RepSox inhibits ATP binding to ALK5 and ALK5 autophosphorylation with IC50 of 23 nM and 4 nM, respectively. RepSox inhibits TGF-β induced cellular PAI-1 luciferase activity with IC50 of 18 nM. [1] RepSox is able to successfully replace Sox2 in reprogramming by inhibiting transforming growth factor-β (Tgf-β) signaling, which in turn induces Nanog expression. Effect of RepSox inducing reprogramming does not require chromatin remodeling. RepSox is found to be efficient at generating iPSCs. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
baculovirus/Sf9 cells MYTGeY5kfGmxbjDhd5NigQ>? Mnf5TY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDBZ5RqfmmwIFGgdoVk\XC2b4KgeJlx\SCLST3sbYtmKGurbnHz[UApSUyNNTmg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|L2PmPUBk\WyuczygTWM2OD12IH7N Mmq3NVU{OTd2NkG=
HepG2 cells MV\GeY5kfGmxbjDhd5NigQ>? M{f3fnN1cW23bHH0bY9vKG:oIGTyZY5{\m:{bXnu[{Boem:5dHig[oFkfG:{IHLleIEhemWlZYD0c5IhUSCtaX7hd4UhcW5iSHXwS|Ih[2WubIOsJGlEPTB;MUCgcm0> Mn\JNVU{OTd2NkG=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
α-SMA / Calponin / Histone H3; 

PubMed: 30365043     

CRL-2097 human dermal fibroblasts were cultured in the presence or absence of the indicated concentration of the TGF-βR1 inhibitor RepSox until day 4 and then subjected to Western blot analysis for myofibroblast markers α-SMA and calponin. Histone H3 was 䲧疝Ỵ疞㧀疜膉痘 

Smad2/3 / cytokeratin ; 

PubMed: 28729719     

Subcellular localization of Smad2/3 in newborn mouse primary epidermal keratinocytes grown in CnT-PR media. The cells were stimulated with 1 ng/ml TGF-β2, 0.1% DMSO (as a control) or 1 μM RepSox for 1 hr. CK, pan-cytokeratin; DNA, nuclear counterstaining 䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ

In vivo RepSox is able to be contribute to forming chimeric embryos in vivo when injected into blastocysts. A one-day treatment with RepSox is sufficient to replace transgenic Sox2. [2]


Solubility (25°C)

In vitro DMSO 57 mg/mL (198.38 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 287.32


CAS No. 446859-33-2
Storage powder
in solvent
Synonyms E-616452, SJN 2511
Smiles CC1=CC=CC(=N1)C2=N[NH]C=C2C3=CC=C4N=CC=CC4=N3

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TGF-beta/Smad Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID