RepSox

Catalog No.S7223

RepSox 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.

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RepSox Chemical Structure

RepSox Chemical Structure
Molecular Weight: 287.32

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description RepSox 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)
IC50 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]
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]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Gellibert F, et al. J Med Chem, 2004, 47(18), 4494-4506.

[2] Ichida JK, et al. Cell Stem Cell, 2009, 5(5), 491-503.

Chemical Information

Download RepSox SDF
Molecular Weight (MW) 287.32
Formula

C17H13N5

CAS No. 446859-33-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms E-616452, SJN 2511
Solubility (25°C) * In vitro DMSO 57 mg/mL (198.38 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1,5-Naphthyridine, 2-[3-(6-methyl-2-pyridinyl)-1H-pyrazol-4-yl]-

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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