Catalog # Availability Size / Price Qty
RepSox | CAS No. 446859-33-2 | TGF-beta Receptor Inhibitors
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Description: Potent and selective inhibitor of TGF-βRI
Alternative Names: E-616452,SJN 2511,ALK5 Inhibitor II

Chemical Name: 2-(3-(6-Methylpyridine-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine

Purity: ≥99%

Product Details
Citations (9)
Supplemental Products

Biological Activity

RepSox is a potent and selective inhibitor of the TGF-β type I receptor/ALK5 (IC50 values are 4 and 23 nM for TGF-β type I receptor autophosphorylation and binding respectively). RepSox is selective for TGF-β type I receptor over a range of kinases, including p38 MAPK, JNK1 and GSK3 (IC50 > 16 μM). Enhances the efficiency of cellular reprogramming; replaces Sox2 by inducing Nanog expression.

RepSox synthesized to Ancillary Material Grade also available.

For more information about how RepSox may be used, see our protocols: Highly Efficient Generation of CiPSCs from MEFs, Generation of β cells from hPSCs, Reprogramming MEFs into Skeletal Muscle Progenitors.

Technical Data

Soluble to 100 mM in DMSO and to 20 mM in ethanol
Store at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Glycoprotein 2 is a specific cell surface marker of human pancreatic progenitors
    KF Cogger, A Sinha, F Sarangi, EC McGaugh, D Saunders, C Dorrell, S Mejia-Guer, Y Aghazadeh, JL Rourke, RA Screaton, M Grompe, PR Streeter, AC Powers, M Brissova, T Kislinger, MC Nostro
    Nat Commun, 2017;8(1):331.
  2. The metalloprotease ADAM12 regulates the effector function of human Th17 cells.
    Zhou A, El Hed A, Mercer F, Kozhaya L, Unutmaz D
    PLoS ONE, 2013;8(11):e81146.
  3. GARP-TGF-beta complexes negatively regulate regulatory T cell development and maintenance of peripheral CD4+ T cells in vivo.
    Zhou A, Kozhaya L, Fujii H, Unutmaz D
    J Immunol, 2013;190(10):5057-64.
  4. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-γ type I receptor inhibitors.
    Gellibert et al.
    J.Med.Chem., 2004;47:4494
  5. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors.
    Li et al.
    Cell Stem Cell, 2009;4:16
  6. A small-molecule inhibitor of Tgf-β signaling replaces Sox2 in reprogramming by inducing Nanog.
    Ichida et al.
    Cell Stem Cell, 2009;5:491
  7. Stem-Cell-Derived beta-Like Cells with a Functional PTPN2 Knockout Display Increased Immunogenicity
    TM Triolo, JQ Matuschek, R Castro-Gut, AH Shilleh, SPM Williams, MS Hansen, K McDaniel, JM Barra, A Michels, HA Russ
    Cells, 2022;11(23):.

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Citations for RepSox

The citations listed below are publications that use Tocris products. Selected citations for RepSox include:

9 Citations: Showing 1 - 9


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