Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is <100-fold selectivity over TGF-βRII.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
2 mg | In stock | $ 47.00 | |
5 mg | In stock | $ 73.00 | |
10 mg | In stock | $ 103.00 | |
25 mg | In stock | $ 216.00 | |
50 mg | In stock | $ 327.00 | |
100 mg | In stock | $ 511.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 113.00 |
Description | SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII. |
Targets&IC50 | TGF-βRI (ALK5):48 nM |
In vitro | SD-208 (1 mg/mL, p.o.) significantly prolonged the median survival rate of mice loaded with SMA-560 glioma. In syngeneic 129S1 mice, SD-208 (60 mg/kg, p.o.) inhibited the growth of primary R3T tumors and reduced the number and size of lung metastases. Additionally, in a murine aortic allograft model, SD-208 effectively reduced the formation of intimal hyperplasia associated with transplant arteriosclerosis. |
In vivo | In vitro, SD-208 inhibits TGF-β-induced receptor-associated Smads, Smad2/3 phosphorylation, and stimulates differentiation, migration, and invasion from epithelial to mesenchymal cells into the basal membrane. Additionally, SD-208 blocks the protective effects of TGF-β on the migration and proliferation of neointimal smooth muscle-like cells. In both mouse SMA-560 and human SMA-560 glioma cells, SD-208 suppresses cell growth, constitutive and TGF-β-induced migration and infiltration, and enhances immunogenicity. |
Kinase Assay | Kinase assay: Various kinase activities are assayed by measuring the incorporation of radiolabeled ATP into a peptide or protein substrate. The reactions are performed in 96-well plates and included the relevant kinase, substrate, ATP, and appropriate cofactors. The reactions are incubated and then stopped by the addition of phosphoric acid. Substrate is captured onto a phosphocellulose filter, which is washed free of unreacted ATP. The counts incorporated are determined by counting on a microplate scintillation counter. The ability of SD-208 to inhibit the respective kinase is determined by comparing counts incorporated in the presence of compound with those incorporated in the absence of compound. |
Cell Research | Glioma cells are cultured in the absence or presence of SD-208 (1 μM) for 48 hours. The cells are pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested, and incorporated radioactivity is determined in a liquid scintillation counter.(Only for Reference) |
Synonyms | ALK5 Inhibitor V, SD208 |
Molecular Weight | 352.75 |
Formula | C17H10ClFN6 |
CAS No. | 627536-09-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.1 mg/mL (20 mM), with gentle warming
You can also refer to dose conversion for different animals. More
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.
SD-208 627536-09-8 Stem Cells TGF-beta/Smad inhibit Transforming growth factor beta receptors TGF-β Receptor Inhibitor SD 208 ALK5 Inhibitor V SD208 inhibitor