| Bioactivity | Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers[1][2]. | |||||||||
| Invitro | Tpl2 (Cot/MAP3K8) 是 MAP3K 家族中的丝氨酸/苏氨酸激酶，位于 ERK 通路中 MEK 的上游[1]。Tpl2 激酶抑制剂 1 (化合物 2p) 也能抑制 MK2 和 p38，在 A431 细胞中的 IC50 分别为 110 μM 和 180 μM[1]。Tpl2 激酶抑制剂 1 抑制脂多糖诱导的人原代单核细胞和人全血中的 TNF-a 的产生，IC50 分别为 0.7 μM 和 8.5 μM[1]。癌大阪甲状腺 (COT) 激酶 (Tpl2) 是巨噬细胞中促炎细胞因子的重要调节因子[2]。 | |||||||||
| Name | Tpl2 Kinase Inhibitor 1 | |||||||||
| CAS | 871307-18-5 | |||||||||
| Formula | C21H14ClFN6 | |||||||||
| Molar Mass | 404.83 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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
CAS: 871307-18-5 F: C21H14ClFN6 W: 404.83
Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists
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