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- PKC (Protein kinase C)
- Tpl2 Kinase Inhibitor (hydrochloride)
Tpl2 Kinase Inhibitor (hydrochloride)
A Tpl2 inhibitor
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包装价格促销价数量
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1mg￥937.00750.00- +
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5mg￥3687.002950.00- +
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10mg￥5087.004070.00- +
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25mg￥11562.009250.00- +
- 货号: ajcx25278
- CAS: N/A
- 别名: c-Cot Kinase Inhibitor, MAP3K8 Kinase Inhibitor, Tumor Progression Locus 2 Kinase Inhibitor
- 分子式: C21H14ClFN6·XHCl
- 分子量: 404.8
- 纯度: ＞98%
- 溶解度: DMF: slightly soluble,DMSO: slightly soluble
- 储存: -20°C
- 库存: 现货
Background
Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50 = 0.05 µM).1 It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 µM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 µM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 µM.2 Tpl2 kinase inhibitor (5 µM) inhibits the proliferation of KG-1a leukemia cells.3
1.Garvin, L.K., Green, N., Hu, Y., et al.Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: Synthesis and structure-activity relationshipsBioor. Med. Chem. Lett.15(23)5288-5292(2005) 2.Wang, X., and Studzinski, G.P.Expression of MAP3 kinase COT1 is up-regulated by 1,25-dihydroxyvitamin D3 in parallel with activated c-jun during differentiation of human myeloid leukemia cellsJ. Steroid. Biochem. Mol. Biol.121(1-2)395-398(2010) 3.Wang, X., Gocek, E., Novik, V., et al.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 D3Cell Cycle9(22)4542-4551(2010)
