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> RepSox [446859-33-2]

RepSox [446859-33-2]

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Cat# HY-13012-50mg

Size : 50mg

Brand : MedChemExpress


Description

RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes[1][2].

IC50 & Target

ALK5

4 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
0.01 μM
Compound: 19
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells
Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells
[PMID: 15317461]
K562 IC50
>100 μM
Compound: ALK5 inhibitor II
Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
Cytotoxicity against human K562 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
[PMID: 28135685]
MCF7 IC50
>100 μM
Compound: ALK5 inhibitor II
Cytotoxicity against human MCF7 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
Cytotoxicity against human MCF7 cells assessed as decrease in cell proliferation after 72 hrs by calcein AM staining-based assay
[PMID: 28135685]
Sf9 IC50
0.004 μM
Compound: 19
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells
Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expressed in baculovirus/Sf9 cells
[PMID: 15317461]
In Vitro

RepSox (compound 19) inhibits ALK5 autophosphorylation with an IC50 value of 4 nM[1].
RepSox (0-10?μM; 0-8 days) induces adipogenesis from mouse embryonic fibroblasts (MEFs) in fibroblast culture medium[2].
RepSox (0-10?μM; 0-8 days) promotes the differentiation of the brown fat precursor cells and induce browning of the white fat precursor cells[2].
RepSox(0-10?μM; 0-8 days) induces brown adipogenesis in primary mouse fibroblasts and fat precursor cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RepSox Related Antibodies

Western Blot Analysis[2]

Cell Line: Mouse embryonic fibroblasts (MEFs)
Concentration: 3 μM
Incubation Time: 0-8 days
Result: Showed upregulation of UCP1 protein levels.

Immunofluorescence[2]

Cell Line: MEFs
Concentration: 3 μM
Incubation Time: 0-8 days
Result: Increased the number of mitochondria in MEF-derived adipocytes and significantly increased UCP1 levels.

RT-PCR[2]

Cell Line: MEFs
Concentration: 3 μM
Incubation Time: 0-8 days
Result: Induced the activation of a network of genes controlling adipogenesis, energy expenditure, and the thermogenic program in MEFs.
Molecular Weight

287.32

Formula

C17H13N5
CAS No.
Appearance

Solid

Color

Light brown to yellow

SMILES

CC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (116.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4804 mL 17.4022 mL 34.8044 mL
5 mM 0.6961 mL 3.4804 mL 6.9609 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 7.5 mg/mL (26.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 7.5 mg/mL (26.10 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Purity & Documentation
References

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