货号 | 3528/50 |
别名 | 6-Chloro-5-[[(2R,5S)-4-[(4-fluoroph |
供应商 | Tocris |
生物活性 | Selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38αin vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α phosphorylation in multiple myeloma cells in vitroandin vivo; activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 549.46 |
分子式 | C27H30ClFN4O |
可溶性/溶解性 | Soluble to 10 mM in water and to 100 mM in DMSO |
参考文献 | Vanderkerkenet al (2007) Inhibition of p38α mitogen-activated protein kinase prevents the development of osteolytic bone disease, reduces tumor burden, and increases survival in murine models of multiple myeloma. Cancer Res. 67 4572. PMID: 17495322. Giafiset al (2006) Role of the p38 mitogen-activated protein kinase pathway in the generation of arsenic trioxide-dependent cellular responses. Cancer Res. 66 6763. PMID: 16818652. Hideshimaet al (2004) p38 MAPK inhibition enhances PS-341 (bortezomib)-induced cytotoxicity against multiple myeloma cells. Oncogene. 23 8766. PMID: 15480425. |