货号:A160473 同义名: c-Cot Kinase Inhibitor;Tumor Progression Locus 2 Kinase Inhibitor
Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor that plays an important role in the regulation of the inflammatory response and the progression of some cancers[1].
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产品名称 | p38 MAPK ↓ ↑ | p38α ↓ ↑ | p38β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BMS-582949 |
+++
p38 MAPK, IC50: 13 nM |
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SB 203580 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
Pexmetinib | ✔ | Tie-2 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Skepinone-L |
++++
p38α, IC50: 5 nM |
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Doramapimod |
++++
p38α, IC50: 38 nM p38α, Kd: 0.1 nM |
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VX-702 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
Ralimetinib dimesylate |
++++
p38α, IC50: 7 nM |
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SB 202190 |
++
p38α, IC50: 50 nM |
++
p38β, IC50: 100 nM |
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Losmapimod |
++++
p38α, pKi: 8.1 |
+++
p38β, pKi: 7.6 |
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Neflamapimod |
+++
p38α, IC50: 10 nM |
+
p38β, IC50: 220 nM |
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PH-797804 |
++
p38α, IC50: 26 nM |
+
p38β, IC50: 102 nM |
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TAK-715 |
++++
p38α, IC50: 7.1 nM |
+
p38β, IC50: 0.20 μM |
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SB 239063 |
++
p38α, IC50: 44 nM |
++
p38β, IC50: 44 nM |
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Pamapimod |
+++
p38α, IC50: 0.014 μM |
+
p38β, IC50: 0.48 μM |
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | Tpl2 Kinase Inhibitor 1, a 3-pyridylmethylamino analog, selectively inhibits Tpl2 (IC50=50 nM), encompassing COT kinase and MAP3K8. It significantly contributes to controlling inflammation and the advancement of certain cancers[1][2]. |
体外研究 | Tpl2 (Cot/MAP3K8), a serine/threonine kinase within the MAP3K family, functions upstream of MEK in the ERK pathway[1]. Tpl2 Kinase Inhibitor 1 also targets MK2 and p38, exhibiting IC50 values of 110 μM and 180 μM, respectively, in A431 cells[1]. Tpl2 Kinase Inhibitor 1 suppresses TNF-alpha production triggered by lipopolysaccharide in primary human monocytes and whole blood, with IC50 values of 0.7 μM and 8.5 μM, respectively[1]. Cancer Osaka thyroid (COT) kinase (Tpl2) significantly regulates pro-inflammatory cytokine production in macrophages[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.35mL 2.47mL 1.24mL |
24.70mL 4.94mL 2.47mL |
CAS号 | 871307-18-5 |
分子式 | C21H14ClFN6 |
分子量 | 404.827 |
别名 | c-Cot Kinase Inhibitor;Tumor Progression Locus 2 Kinase Inhibitor;TC-S 7006;MAP3K8 Kinase Inhibitor;Tpl2 Kinase Inhibitor |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(259.37 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |