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SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII. SD-208 blocka TGF-beta-induced phosphorylation of the receptor-associated Smads, Smad2 and Smad3, and stimulates epithelial-to-mesenchymal transdifferentiation, migration, and invasiveness into Matrigel in vitro.In the murine aortic allograft model, SD-208 effectively reduces the formation of intimal hyperplasia of transplant arteriosclerosis (TA).
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Source | J Neurosci (2016). Figure 5. SD-208 |
| Method | i.p. | |
| Cell Lines | EAN rats | |
| Concentrations | 20 mg/kg/d | |
| Incubation Time | 12 day | |
| Results | In both the SD-208 alone and RvD1 + SD-208 groups, EAN rats showed much more severe neurological scores and significantly prolonged disease duration, not only compared with the RvD1 + vehicle group, but also compared with the vehicle-alone group (Fig. 5B), suggesting that the inhibition of TGF-β signaling not only abolished the exogenous RvD1 effects, but also may suppress endogenous RvD1 functions. |
| Cell Experiment | |
|---|---|
| Cell lines | Murine SMA-560 or human LN-308 glioma cells |
| Preparation method | Proliferation. Glioma cells were cultured in the absence or presence of SD-208 (1 μmol/L) for 48 hours. The cells were pulsed for the last 24 hours with [methyl-3H]thymidine (0.5 μCi) and harvested (Tomtec, Hamden, CT), and incorporated radioactivity was determined in a liquid scintillation counter (Wallac, Turku, Finland). |
| Concentrations | 1 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | SMA-560 cells bearing VM/Dk mice |
| Formulation | deionized water |
| Dosages | 1 mg/mL |
| Administration | p.o. |
| Molecular Weight | 352.75 |
| Formula | C17H10ClFN6 |
| CAS Number | 627536-09-8 |
| Solubility (25°C) | DMSO 8 mg/mL warmed |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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