Description
| Description | SD-208, a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII. |
| Targets&IC50 | TGF-βRI (ALK5):48 nM |
| 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 | SD208, ALK5 Inhibitor V |
| Molecular Weight |
352.75 |
| Formula | C17H10ClFN6 |
| CAS No. | 627536-09-8 |
Storage
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Solubility Information
DMSO: 7.1 mg/mL (20 mM)),
with gentle warming
( < 1 mg/ml refers to the product slightly soluble or insoluble )
