SB-525334

• CAT Number: I003306
• CAS Number: 356559-20-1
• Molecular Formula: C₂₁H₂₁N₅
• Molecular Weight: 343.42
• Purity: ≥95%
• Target: TGF-βR1(ALK5)
• Solubility: 10 mM in DMSO
• Storage: 3 years -20C powder
• IC50: 14.3 nM
• IUPAC Name: 6-[2-tert-butyl-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl]quinoxaline
• InChI: InChI=1S/C21H21N5/c1-13-6-5-7-16(24-13)19-18(25-20(26-19)21(2,3)4)14-8-9-15-17(12-14)23-11-10-22-15/h5-12H,1-4H3,(H,25,26)
• InChIKey: DKPQHFZUICCZHF-UHFFFAOYSA-N
• SMILES: CC1=CC=CC(=N1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=NC=CN=C4C=C3

SB-525334 (CAT: I003306) is a selective and potent small molecule inhibitor of the transforming growth factor-beta (TGF-β) receptor I (ALK5). It belongs to the class of compounds known as kinase inhibitors. By targeting ALK5, SB-525334 blocks the TGF-β signaling pathway, which plays a crucial role in various cellular processes such as cell growth, differentiation, and immune response. SB-525334 has shown promising results in preclinical studies, demonstrating its potential as a therapeutic agent for fibrotic diseases and certain types of cancers. Further research and clinical trials are needed to fully evaluate its efficacy and safety in human patients.

Reference

1. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther, 2005, 313(3), 943-951.
2. Thomas M, et al. Activin-like kinase 5 (ALK5) mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline. Am J Pathol, 2009, 174(2), 380-389.
3. Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res, 2007, 13(10), 3087-3899.