| 货号 | 5960/50 |
| 别名 | (3S)-4-[[4-(2-Butyn-1-yloxy)phenyl] |
| 供应商 | Tocris |
| 生物活性 | Adam 17 (TACE) and MMP inhibitor (IC50 values are 3, 4.7, 6.6, 8.4, 12, 26 and 26 nM for MMP-13, MMP-2, MMP-1, ADAM 17, MMP-9, MMP-7 and MMP-14, respectively). Suppresses TNF-α production in an acute LPS-mouse model. Reduces severity score in an in vivo model of rheumatoid arthritis. Displays selective cytotoxicity to tumor cells and cancer stem cells in vitro. Induces tumor apoptosis in a breast cancer in vivo model. Orally bioavailable. |
| 运输条件 | Ambient |
| 存放说明 | -20℃ |
| 纯度 | >98 % |
| 计算分子量 | 398.49 |
| 分子式 | C17H22N2O5 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO and to 20 mM in ethanol |
| 参考文献 | Mezilet al (2012) Tumor selective cytotoxic action of a thiomorpholin hydroxamate inhibitor (TMI-1) in breast cancer PLoS One 7 e43409. PMID: 23028451. Levin (2006) Heterocyclic inhibitors of tumor necrosis factor-α converting enzyme (TACE) Heterocycles 70691. Zhanget al (2004) Identification and characterization of 4-[[4-(2-butynyloxy)phenyl]sulfonyl]-N-hydroxy-2,2-dimethyl-(3S)thiomorpholinecarboxamide (TMI-1), a novel dual tumor necrosis factor-α-converting enzyme/matrix metalloprotease inhibitor for the treatment of rheumatoid arthritis. J.Pharmacol.Exp.Ther. 309 348. PMID: 14718605. |