| 货号 | 5240/50 |
| 别名 | 4-[(3-Chloro-4-fluorophenyl)amino]- |
| 供应商 | Tocris |
| 生物活性 | Potent and selective Tpl2 (Cot; MAP3K8) inhibitor (IC50 = 50 nM). Selective for Tpl2 over MEK, p38, Src, MK2, PKC and EGFR. Inhibits LPS-induced TNF-α secretion from monocytes and attenuates acute myeloid leukemia (AML) cell proliferation in vitro. Also reduces cytolytic activity of human CD8+ cytotoxic T lymphocytes. Cell permeable. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 纯度 | >99 % |
| 计算分子量 | 404.83 |
| 分子式 | C21H14ClFN6 |
| 可溶性/溶解性 | Soluble to 100 mM in DMSO |
| 参考文献 | Chowdhuryet al (2014) Pharmacological inhibition of TPL2/MAP3K8 blocks human cytotoxic T lymphocyte effector functions. PLoS ONE 9 e92187. PMID: 24642963. Wanget al (2010) Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D3. Cell Cycle 9 4542. PMID: 21084834. Gavrinet al (2005) Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg.Med.Chem.Lett. 15 5288. PMID: 16165349. |