RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor.
| 説明 | RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor. |
| ターゲット＆IC50 | TGFβR1(ALK5):4 nM |
| キナーゼ試験 | The kinase domain of ALK5 is cloned by PCR and expressed in a baculovirus/Sf9 cells system. The protein is 6-His tagged in the C terminus and purified by affinity chromatography using a Ni2+column, and the obtained material is used to assess compound activity in an autophosphorylation assay. Purified enzyme (10 nM) is incubated in 50 μL of Tris buffer (Tris 50 mM, pH 7.4; NaCl, 100 mM; MgCl2, 5 mM; MnCl2, 5 mM; and DTT, 10 mM). The enzyme is preincubated with different concentrations of RepSox (0.1% DMSO final concentration in the test) for 10 min at 37°C. The reaction is then initiated by the addition of 3 μM ATP (0.5 μCi γ-33P-ATP). After 15 min at 37°C, phosphorylation is stopped by the addition of SDS?PAGE sample buffer (50 mM Tris-HCl, pH 6.9, 2.5% glycerol, 1% SDS, and 5% β-mercaptoethanol). The samples are boiled for 5 min at 95°C and run on a 12% SDS?PAGE. Dried gels are exposed to a phosphor screen overnight. ALK5 autophosphorylation is quantified using a Storm imaging system[1]. |
| 細胞研究 | RepSox is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 1%) before use[1]. 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]. |
| 別名 | ALK5 Inhibitor II, SJN 2511, E-616452 |
| 分子量 | 287.32 |
| 分子式 | C17H13N5 |
| CAS No. | 446859-33-2 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Ethanol: <1 mg/mL
H2O: <1 mg/mL
DMSO: 53 mg/mL (184.5 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
参考文献引用文献
投与量変換You can also refer to dose conversion for different animals. 詳細
In vivo投与量計算 (透明溶液)計算器bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
RepSox 446859-33-2 Angiogenesis Stem Cells Tyrosine Kinase/Adaptors ALK TGF-beta/Smad TGF-β Receptor E616452 E 616452 ALK5 Inhibitor II Transforming growth factor beta receptors SJN 2511 Inhibitor SJN-2511 E-616452 inhibit SJN2511 inhibitor
