RepSox---TGF-β Type I Receptor ALK5 Inhibitor


Catalog No. size PriceQuantity
M60151-2S 2 mg solid $79
M60151-10S 10mg solid $312

Description

Product Information
Molecular Weight: 287.32
Formula: C17H13N5
Purity: ≥98%
CAS#: 446859-33-2
Solubility: DMSO up to 100 mM
Chemical Name: 2-(5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

 

RepSox (E-616452 or SJN 2511) is a highly potent, selective inhibitor of the TGF-β type I receptor ALK5 with IC50 of 23 nM and 4 nM for ATP binding to ALK5 and ALK5 autophosphorylation, respectively. It has good selectivity for ALK5 over a range of kinases, including p38 MAPK, JNK1 and GSK3 (IC50 > 16 μM). 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.

 


How to Use:

 

 

  • In vitro: RepSox was used at 1-25 µM final concentration in vitro and in stem cell reprogramming.
  • 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.

 

 

Reference:

  1. Gellibert F, et al. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. (2004) J Med Chem. 47(18):4494-506.
  2. Ichida JK, et al. A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog. (2009) Cell Stem Cell. 5(5):491-503.
  3. Li W, et al. Generation of rat and human induced pluripotent stem cells by combining genetic reprogramming and chemical inhibitors. (2009) Cell Stem Cell. 4(1):16-9.
  4. Liu X, et al. Sequential introduction of reprogramming factors reveals a time-sensitive requirement for individual factors and a sequential EMT-MET mechanism for optimal reprogramming. (2013) Nat Cell Biol. 15(7):829-38.
  5. Hou P, et al. Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. (2013) Science. 341(6146):651-4.


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