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SB505124
| Product Name | SB505124 |
| Price: | Inquiry |
| Catalog No.: | CN00199 |
| CAS No.: | 694433-59-5 |
| Molecular Formula: | C20H21N3O2 |
| Molecular Weight: | 335.4 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | Cc1cccc(n1)c1[nH]c(nc1c1ccc2c(c1)OCO2)C(C)(C)C |
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| Description | SB-505124 is a selective inhibitor of TGFβR with IC50 of 129 nM and 47 nM for ALK4, ALK5, respectively, and it does not inhibits ALK1, 2, 3, or 6 but ALK7. |
| Target | IC50: 129 nM (ALK4), 47 nM (ALK5) |
| In Vitro | SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC50 value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells[1]. SB-505124 (10 µM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC[3]. |
| Cell Assay | Cell viability is measured as described previously or by using the modified tetrazolium salt WST-1. Approximately 2000 cells are seeded in 96-well dishes in 100 μL of 0.2% FBS phenol red-free media overnight. The cells are treated with 50 μL of SB-505124 (to achieve the final concentrations indicated) for 30 min before being treated with or without TGF-β1 and TNF-α to a final volume of 200 μL. Cell growth is measured at the indicated time points by incubating each well with 10 μL of WST-1 for 3 h at 37°C. Metabolically active cells cleave WST-1 to water-soluble formazan, which is directly quantitated with an enzyme-linked immunosorbent assay plate reader. Each experiment is done at least twice, and treatment for each cell line is done in triplicate. |
| Density | 1.2±0.1 g/cm3 |
| Boiling Point | 509.7±50.0 °C at 760 mmHg |
| Flash Point | 180.5±20.4 °C |
| Exact Mass | 335.163391 |
| PSA | 60.03000 |
| LogP | 4.77 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Storage condition | 2-8°C |