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Tpl2 Kinase Inhibitor 1 {[allProObj[0].p_purity_real_show]}

货号:A160473 同义名: c-Cot Kinase Inhibitor;Tumor Progression Locus 2 Kinase Inhibitor Ambeed 开学季,买赠积分,赢豪礼

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].

Tpl2 Kinase Inhibitor 1 化学结构 CAS号:871307-18-5
Tpl2 Kinase Inhibitor 1 化学结构
CAS号:871307-18-5
Tpl2 Kinase Inhibitor 1 3D分子结构
CAS号:871307-18-5
Tpl2 Kinase Inhibitor 1 化学结构 CAS号:871307-18-5
Tpl2 Kinase Inhibitor 1 3D分子结构 CAS号:871307-18-5
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Tpl2 Kinase Inhibitor 1 纯度/质量文件 产品仅供科研

货号:A160473 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

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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

{[allProObj[0].p_purity_real_show]}
Doramapimod ++++

p38α, IC50: 38 nM

p38α, Kd: 0.1 nM

{[allProObj[0].p_purity_real_show]}
VX-702 {[allProObj[0].p_purity_real_show]}
Ralimetinib dimesylate ++++

p38α, IC50: 7 nM

{[allProObj[0].p_purity_real_show]}
SB 202190 ++

p38α, IC50: 50 nM

++

p38β, IC50: 100 nM

{[allProObj[0].p_purity_real_show]}
Losmapimod ++++

p38α, pKi: 8.1

+++

p38β, pKi: 7.6

{[allProObj[0].p_purity_real_show]}
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。

Tpl2 Kinase Inhibitor 1 生物活性

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].

Tpl2 Kinase Inhibitor 1 参考文献

[1]Gavrin LK, et al. Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5288-92.

[2]Glatthar R, et al. Discovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors. J Med Chem. 2016 Aug 25;59(16):7544-60.

Tpl2 Kinase Inhibitor 1 实验方案

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

Tpl2 Kinase Inhibitor 1 技术信息

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
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