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product name RepSox


Description: RepSox, also known as SJN 2511, E 616452 and ALK5 Inhibitor II,  is a potent, cell permeable, 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 slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. 

References: J Med Chem. 2004 Aug 26;47(18):4494-506; Cell Stem Cell. 2009 Nov 6; 5(5): 491–503.



Molecular Weight (MW)

287.32
Formula

C17H13N5 
CAS No.

446859-33-2
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 57 mg/mL (198.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)

 
Synonyms

E-616452, SJN 2511

other peoduct :

In Vitro

In vitro activity: 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. 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.


Kinase Assay


Cell Assay: RepSox was found to replace the function of Sox2 to induce reprogramming of iPS cells, via the mechanism of inhibiting TGFβR-1. MEF cells were treated with RepSox for 3 days, and then it was removed at the time of transduction with Oct4, Klf4, and cMyc. The result showed the TGFβR-1 -associated expression of L-Myc was increased by 5-fold after RepSox treatment. A partially reprogrammed cell line (OKMS 6) was treated with RepSox and performed global gene expression analysis at 10, 24, and 48 hours following the initiation of treatment. The result showed the Id1, Id2 and Id3 gene, repressed by TGFβR-1 signaling, were released from that repression and the expression level was increased. Additionally, other genes responsive for TGFβR-1 signaling were inhibited. It suggested RepSox was able to inhibit TGFβR-1 and suppress the TGFβR-1 downstream signaling.

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.
Animal model  
Formulation & Dosage  
References J Med Chem. 2004 Aug 26;47(18):4494-506; Cell Stem Cell. 2009 Nov 6; 5(5): 491–503.

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Author: Sodium channel