| 货号 | 16281-1mg |
| 描述 | SB-525334 is a potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC50 = 14.36 nM).1 It is ~4-fold less effective against ALK4 and inactive against ALK2, ALK3, and ALK6.1 SB-525334 blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression.1 It is effective in vivo, preventing puromycin aminonucleoside-induced renal fibrosis and bleomycin-induced pulmonary fibrosis.1,2,3 SB-525334 also modulates carcinogenesis and suppresses the development of pulmonary arterial hypertension in animals.3,4,5 |
| 别名 | TGF-β RI Kinase Inhibitor VIII; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Grygielko, E.T.,Martin, W.M.,Tweed, C., et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-β type I receptor kinase in puromycin-induced nephritis. Journal of Pharmacology and Experimental Therapeutics 313(3), 943-951 (2005). 2.Higashiyama, H.,Yoshimoto, D.,Kaise, T., et al. Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis. Exp.Mol.Pathol. 83, 39-46 (2007). 3.Jarman, E.R.,Khambata, V.S.,Yun Ye, L., et al. A translational preclinical model of interstitial pulmonary fibrosis and pulmonary hypertension: Mechanistic pathways driving disease pathophysiology. Physiol.Rep. 2(9), 1-19 (2014). 4.Laping, N.J.,Everitt, J.I.,Frazier, K.S., et al. Tumor-specific efficacy of transforming growth factor-βRI inhibition in Eker rats. Clinical Cancer Research 13(10), 3087-3099 (2007). 5.Thomas, M.,Docx, C.,Holmes, A.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. American Journal of Pathology 174(2), 380-389 (2009). | |
| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 343.4 |
| 分子式 | C21H21N5 |
| CAS号 | 356559-20-1 |
| 稳定性 | ≥ 2 years |
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