RepSox (E-616452)

Catalog No.S7223 Synonyms: SJN 2511,ALK5 Inhibitor II

For research use only.

RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) 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.

RepSox (E-616452) Chemical Structure

CAS No. 446859-33-2

Selleck's RepSox (E-616452) has been cited by 45 publications

Purity & Quality Control

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Biological Activity

Description RepSox (E-616452, SJN 2511, ALK5 Inhibitor II) 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.
Targets
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 NEexfFJHfW6ldHnvckBie3OjeR?= M1nkemlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgRYN1cX[rbjDBJJJm[2WydH;yJJR6eGViSVmtcIls\SCtaX7hd4UhMEGOS{WpJIV5eHKnc4Pl[EBqdiCkYXP1cI93cXK3cz;T[lkh[2WubIOsJGlEPTB;NDDuUS=> M1fBO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF3M{G3OFYyLz5zNUOxO|Q3OTxxYU6=
HepG2 cells Ml\5SpVv[3Srb36gZZN{[Xl? MV;TeIlufWyjdHnvckBw\iCWcnHud4Zwem2rbneg[5Jwf3SqIH\hZ5RweiCkZYThJJJm[2WydH;yJGkhc2mwYYPlJIlvKEincFeyJINmdGy|LDDJR|UxRTFyIH7N NWi3dm1uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUWzNVc1PjFpPkG1N|E4PDZzPD;hQi=>
Sf9 NFGwUYxHfW6ldHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJGFNUzViZYjwdoV{e2WmIHnuJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiY3Hz[YlvKGG|IIP1ZpN1emG2ZTDpckBxemW|ZX7j[UBw\iCdZ3HtcYEuOzOSXVHUVEwhUUN3MDC9JFAvOThzIN88UU4> M17hc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUO1Olg2Lz5{OEGzOVY5PTxxYU6=
Sf9 NVzIZnBNTnWwY4Tpc44h[XO|YYm= MoG1TY5pcWKrdHnvckBw\iCvb4Xz[UBCSkxiZYjwdoV{e2WmIHnuJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiR1fFRWl[SUGSRlvLJIF{KHO3YoP0doF1\SCrbjDwdoV{\W6lZTDv[kBc\2GvbXGtN|NRZUGWUDygTWM2OCB;IEKxJO69VS5? NGT3U249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGzOVY5PSd-MkixN|U3QDV:L3G+
HeLa MkTlSpVv[3Srb36gZZN{[Xl? M{\h[FEhfU1? NV7jWpZnOzBibXnudy=> NYXETHUxUW6qaXLpeIlwdiCxZjDBUGs2KGmwIIPldpVuKHO2YYL2[YQhcHWvYX6gTIVN[SClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gWGdHNWKndHGtbY5lfWOnZDDTUWFFOi9|IH71Z4xm[XJidILhcpNi[3Srb36gZZQhOSC3TTDwdoUucW6ldXLheIVlKG[xcjCzNEBucW6|IHLl[o9z\SCWR1[tZoV1[SC|dHnteYxifGmxbjDmc5IhOzBibXnud{BjgSCrbX31co9ndHWxcnXzZ4Vv[2ViYX7hcJl{cXN? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF|NU[4OUc,OjhzM{W2PFU9N2F-
Assay
Methods Test Index PMID
Western blot α-SMA / Calponin / Histone H3 30365043
Immunofluorescence Smad2/3 / cytokeratin 28729719
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]

Protocol (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 287.32
Formula

C17H13N5

CAS No. 446859-33-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NC(=CC=C1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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