| Name | SD-208 |
| Description | SD-208 (ALK5 Inhibitor V), a selective TGF-βRI (ALK5) inhibitor (IC50: 48 nM), is >100-fold selectivity over TGF-βRII. |
| 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) |
| 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. |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 7.1 mg/mL (20 mM), Heating is recommended.
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| Keywords | inhibit | Transforming growth factor beta receptors | TGF-β Receptor | Inhibitor | SD 208 | SD-208 |
| Inhibitors Related | Monocrotaline | SB-431542 | DMH-1 | RepSox | Chromenone 1 | LY-364947 | BMP signaling agonist sb4 | Pirfenidone | A 83-01 | Galunisertib | Alantolactone | Pentabromophenol |
| Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Tyrosine Kinase Inhibitor Library | Anti-Obesity Compound Library | Inhibitor Library | Bioactive Compounds Library Max | Fluorochemical Library | TGF-beta/Smad Compound Library | Anti-Cancer Active Compound Library |
United States
