Home
Products
RepSox
| Product Name | RepSox |
| Price: | Inquiry |
| Catalog No.: | CN00222 |
| CAS No.: | 446859-33-2 |
| Molecular Formula: | C17H13N5 |
| Molecular Weight: | 287.32 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | Cc1cccc(n1)c1n[nH]cc1c1ccc2c(n1)cccn2 |
| Contact us | |
|---|---|
| First Name: | |
| Last Name: | |
| E-mail: | |
| Question: | |
| Description | RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM. |
| Target | IC50: 4 nM (ALK5 autophosphorylation)[1] |
| In Vitro | RepSox also inhibits ATP binding to ALK5 with IC50 of 23 nM. RepSox shows potent activity in both binding and cellular assays and exhibits selectivity over p38 mitogen-activated protein kinase. with IC50 of >16 μM[1]. RepSox act s as an inhibitor of the Tgfβ1 kinase. Treatment with 25 μM RepSox almost completely eliminates Smad3 phosphorylation, indicating that RepSox strongly inhibits Tgfβ signaling in somatic cells. RepSox is most effective at replacing Sox2 during days 10-11 after transduction and that therefore cultures of Oct4, Klf4, and cMyc-transduced MEFs give rise to intermediates capable of responding to RepSox treatment. These intermediates appear at day 4 post-transduction and peak at days 10-11. Treatment with RepSox decreased the proportion of cells in G2/M phase of the cell cycle, indicating it does not increase the proliferation rate of these partially reprogrammed cells[2]. |
| Cell Assay | To test anti-TGF-β activity of compounds, HepG2 cells are seeded in 96 well microplates at a concentration of 35000 cells per well in 200 μL of serum-containing medium. The microplates are then placed for 24 h in a cell incubator at 37°C, 5% CO2 atm. RepSox dissolved in DMSO are then added at concentrations of 50 nM to 10 μM (final concentration of DMSO 1%) for 30 min prior to the addition of recombinant TGF-β (1 ng/mL). After an overnight incubation, the cells are washed with PBS and lysed by addition of 10 μL of passive lysis buffer. Inhibition of luciferase activity relative to control groups is used as a measure of compound activity. A concentration−response curve is constructed from which an IC50 value is determined graphically[1]. |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 501.9±50.0 °C at 760 mmHg |
| Flash Point | 230.5±23.1 °C |
| Exact Mass | 287.117096 |
| PSA | 67.35000 |
| LogP | 1.28 |
| Vapour Pressure | 0.0±1.2 mmHg at 25°C |
| Storage condition | Store at +4°C |