For research use only. Not for therapeutic Use.
SB-505124（Cat No.:I004609）is a selective small molecule inhibitor of the transforming growth factor-beta (TGF-β) type I receptor (ALK5). TGF-β signaling is involved in various biological processes, including cell growth, differentiation, and fibrosis. Dysregulated TGF-β signaling is associated with several diseases, such as cancer, fibrosis, and chronic inflammatory conditions. By inhibiting ALK5, SB-505124 suppresses TGF-β-mediated signaling, which can reduce fibrotic tissue formation and inhibit tumor progression. It is being investigated in preclinical models for potential therapeutic applications in treating fibrotic diseases and certain types of cancer, particularly those with TGF-β pathway overactivation.
| Catalog Number | I004609 |
| CAS Number | 694433-59-5 |
| Synonyms | 2-[4-(1,3-benzodioxol-5-yl)-2-(1,1-dimethylethyl)-1H-imidazol-5-yl]-6-methyl-pyridine |
| Molecular Formula | C20H21N3O2 |
| Purity | ≥95% |
| Target | TGF-β Receptor |
| Solubility | DMSO 67 mg/mL; Water <1 mg/mL; Ethanol 67 mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 47 ± 5 nM (ALK5); 129 ± 11 nM (ALK4) |
| IUPAC Name | 2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine |
| InChI | InChI=1S/C20H21N3O2/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15/h5-10H,11H2,1-4H3,(H,22,23) |
| InChIKey | WGZOTBUYUFBEPZ-UHFFFAOYSA-N |
| SMILES | CC1=NC(=CC=C1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4 |
| Reference | </br>1:Development and validation of an LC-MS/MS method for the determination of SB-505124 in rat plasma: Application to pharmacokinetic study. Jiang J, Zhang Y, Zhang Q, Li Y, Gong T, Zhang Z, Ding R, Sun X.J Pharm Biomed Anal. 2016 Jan 5;117:205-9. doi: 10.1016/j.jpba.2015.09.002. Epub 2015 Sep 3. PMID: 26363490 </br>2:Thermoreversible gel for delivery of activin receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Sutariya V, Miladore N, Geldenhuys W, Bhatia D, Wehrung D, Nakamura H.Pharm Dev Technol. 2013 Jul-Aug;18(4):957-62. doi: 10.3109/10837450.2011.647035. Epub 2011 Dec 30. PMID: 22206499 </br>3:SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. DaCosta Byfield S, Major C, Laping NJ, Roberts AB.Mol Pharmacol. 2004 Mar;65(3):744-52. PMID: 14978253 Free Article |
