[CAS NO. 446859-33-2] RepSox
PRODUCTS SPECIFICATIONS [446859-33-2]
DESCRIPTION [446859-33-2]
Overview
| MDL | MFCD09037561 |
|---|---|
| Molecular Weight | 287.32 |
| Molecular Formula | C17H13N5 |
| SMILES | CC1=NC(C2=NNC=C2C3=NC4=CC=CN=C4C=C3)=CC=C1 |
11 Publications Citing Use of MCE
- [1]Sci Adv. 2021 Apr 14;7(16):eabb2213.
- [2]Biomaterials. 2018 Dec 6;193:30-46.
- [3]Stem Cell Res Ther. 2020 Apr 16;11(1):157.
- [4]Biomedicines. 2020 Nov 9;8(11):485.
- [5]Biomed Pharmacother. 2023 Jan 11;159:114216.
- [6]J Cell Mol Med. 2021 Apr;25(7):3498-3510.
- [7]ACS Comb Sci. 2019 Dec 9;21(12):805-816.
- [8]Brain Science Advances. 2022 Feb.
- [9]Mil Med Res. 2020 Nov 1;7(1):52.
- [10]Mil Med Res. 2020 Sep 6;7(1):42.
- [11]Oncotarget. 2017 Jun 19;8(36):60159-60172.
Summary
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 IC 50 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
IC50: 4 nM (ALK5 autophosphorylation) [1]
In Vitro
RepSox (compound 19) inhibits ALK5 autophosphorylation with an IC
50
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 116.00 mM ; Need ultrasonic)
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 |
| 10 mM | 0.3480 mL | 1.7402 mL | 3.4804 mL |
-
1.
-
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
-
3.
-
4.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 1.67 mg/mL (5.81 mM); Clear solution
-
5.
Add each solvent one by one: 1% DMSO >> 99% saline
Solubility: ≥ 0.33 mg/mL (1.15 mM); Clear solution
References
- [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. J Med Chem. 2004 Aug 26;47(18):4494-506.
- [2] Wan-Zhi Tu, et al. RepSox, a small molecule inhibitor of the TGFβ receptor, induces brown adipogenesis and browning of white adipocytes. Acta Pharmacol Sin. 2019 Dec;40(12):1523-1531.