Home TGF-beta/Smad TGF-beta/Smad inhibitor RepSox (E-616452) For research use only.

RepSox (E-616452)

Synonyms: SJN 2511,ALK5 Inhibitor II

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

RepSox (E-616452) Chemical Structure

CAS No. 446859-33-2

Purity & Quality Control

RepSox (E-616452) Related Products

Signaling Pathway

TGF-beta/Smad Signaling Pathways

TGF-beta/Smad Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
baculovirus/Sf9 cells Function assay Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells, IC50=4 nM 15317461
HepG2 cells Function assay Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells, IC50=10 nM 15317461
Sf9 Function assay Inhibition of human ALK5 expressed in Sf9 insect cells using casein as substrate in presence of [gamma-33P]ATP, IC50 = 0.181 μM. 28135685
Sf9 Function assay Inhibition of mouse ABL expressed in Sf9 insect cells using GGEAIYAAPFKK as substrate in presence of [gamma-33P]ATP, IC50 = 21 μM. 28135685
HeLa Function assay 1 uM 30 mins Inhibition of ALK5 in serum starved human HeLa cells assessed as reduction in TGF-beta-induced SMAD2/3 nuclear transaction at 1 uM pre-incubated for 30 mins before TGF-beta stimulation for 30 mins by immunofluorescence analysis 28135685
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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
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]
Kinase Assay ALK5 fluorescence polarization binding assay
Compound binding to ALK5 is tested on purified recombinant GST- ALK5 (residues 198-503). Displacement of rhodamine green fluorescently labeled ATP competitive inhibitor by different concentrations of test compounds is used to calculate a binding pIC50. GST -ALK5 is added to a buffer containing 62.5 mM Hepes, pH 7.5, 1 mM DTT, 12.5 mM MgCl2, 1.25 mM CHAPS, and 1 nM rhodamine green-labeled ligand so that the final ALK5 concentration is 10 nM based on active site titration of the enzyme. Forty microliters of the enzyme/ligand reagent is added to 384 well assay plates containing 1 μL of different concentrations of test compound. The plates are read immediately on a fluorescence reader with excitation, emission, and dichroic filters of 485, 530, and 505 nm, respectively. The fluorescence polarization for each well is calculated by the Acquest and is then imported into curve fitting software for construction of concentration -response curves.
Experimental Result Images Methods Biomarkers Images PMID
Western blot α-SMA / Calponin / Histone H3 30365043
Immunofluorescence Smad2/3 / cytokeratin 28729719
In Vivo
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]
Animal Research Animal Models Male C57BL/6 mice
Dosages 10 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 287.32 Formula

C17H13N5
CAS No. 446859-33-2 SDF Download RepSox (E-616452) SDF
Smiles CC1=NC(=CC=C1)C2=C(C=NN2)C3=NC4=C(C=C3)N=CC=C4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (198.38 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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.

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