SB-505124 (hydrochloride)
Modify Date: 2024-01-19 18:49:10
SB-505124 (hydrochloride) structure
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Common Name | SB-505124 (hydrochloride) | ||
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| CAS Number | 356559-13-2 | Molecular Weight | 371.86100 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C20H22ClN3O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of SB-505124 (hydrochloride)SB-505124 hydrochloride 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. |
| Name | 2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine,hydrochloride |
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| Synonym | More Synonyms |
| Description | SB-505124 hydrochloride 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. |
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| Related Catalog | |
| 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]. |
| Kinase Assay | Briefly, phospho-p38 is immunoprecipitated from 200 μg of cell lysates with an immobilized phosphor-p38 antibody overnight at 4°C. p38 kinase activity is measured using 2 μg of ATF-2 fusion protein as the substrate with addition of 200 μM ATP. After a 30-min incubation at 30°C, the reaction is terminated with LaemmLi sample buffer, and the proteins are boiled and resolved by 10% SDS-polyacrylamide gel electrophoresis, transferred to nitrocellulose membrane, and immunoblotted with phospho-ATF-2 antibody. |
| 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. |
| References |
| Molecular Formula | C20H22ClN3O2 |
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| Molecular Weight | 371.86100 |
| Exact Mass | 371.14000 |
| PSA | 60.03000 |
| LogP | 5.27530 |
| Storage condition | 2-8℃ |
| 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrochloride hydrate |
| 2-(5-benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrochloride |
| 2-(5-Benzo[1,3]dioxol-4-yl-2-tert-butyl-1H-imidazol-4-yl)-6-methylpyridine,HCl |
| SB-505124 (hydrochloride) |