For research use only.

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

36 publications

RepSox Chemical Structure

CAS No. 446859-33-2

RepSox (E-616452, SJN 2511) 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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10mM (1mL in DMSO) EUR 95 In stock
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Selleck's RepSox has been cited by 36 publications

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Biological Activity

Description RepSox (E-616452, SJN 2511) 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 NUXpdGtsTnWwY4Tpc44h[XO|YYm= Mlj6TY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDBZ5RqfmmwIFGgdoVk\XC2b4KgeJlx\SCLST3sbYtmKGurbnHz[UApSUyNNTmg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|L2PmPUBk\WyuczygTWM2OD12IH7N M2\Je|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{G3OFYyLz5zNUOxO|Q3OTxxYU6=
HepG2 cells NIX1fFNHfW6ldHnvckBie3OjeR?= NG\OVG1UfGmvdXzheIlwdiCxZjDUdoFve2[xcn3pcoch\3Kxd4ToJIZi[3SxcjDi[ZRiKHKnY3XweI9zKElia3nuZZNmKGmwIFjldGczKGOnbHzzMEBKSzVyPUGwJI5O M{PYNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{G3OFYyLz5zNUOxO|Q3OTxxYU6=
Sf9 MkiySpVv[3Srb36gZZN{[Xl? NV;TbFhiUW6qaXLpeIlwdiCxZjDoeY1idiCDTFu1JIV5eHKnc4Pl[EBqdiCVZkmgbY5{\WO2IHPlcIx{KHW|aX7nJINie2WrbjDhd{B{fWK|dILheIUhcW5icILld4Vv[2Vib3[gX4didW2jLUOzVH1CXFBuIFnDOVAhRSByLkG4NUDPxE1w NVHwb4VMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|U3QDVpPkK4NVM2Pjh3PD;hQi=>
Sf9 MoW4SpVv[3Srb36gZZN{[Xl? M1vzRWlvcGmkaYTpc44hd2ZibX;1d4UhSUKOIHX4dJJme3OnZDDpckBU\jliaX7z[YN1KGOnbHzzJJV{cW6pIFfHSWFKYUGDUF\LT{BieyC|dXLzeJJifGViaX6gdJJme2WwY3Wgc4YhY2ejbX3hMVM{WF2DVGCsJGlEPTBiPTCyNUDPxE1w NXK5NWhPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixN|U3QDVpPkK4NVM2Pjh3PD;hQi=>
HeLa M4fDNmZ2dmO2aX;uJIF{e2G7 NGLYWJEyKHWP NHjxcIw{OCCvaX7z NV7QT|NjUW6qaXLpeIlwdiCxZjDBUGs2KGmwIIPldpVuKHO2YYL2[YQhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gWGdHNWKndHGtbY5lfWOnZDDTUWFFOi9|IH71Z4xm[XJidILhcpNi[3Srb36gZZQhOSC3TTDwdoUucW6ldXLheIVlKG[xcjCzNEBucW6|IHLl[o9z\SCWR1[tZoV1[SC|dHnteYxifGmxbjDmc5IhOzBibXnud{BjgSCrbX31co9ndHWxcnXzZ4Vv[2ViYX7hcJl{cXN? NGCzSm09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGzOVY5PSd-MkixN|U3QDV:L3G+

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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=NC(=CC=C1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID