Tpl2 Kinase Inhibitor 1 hydrochloride 

Tpl2 Kinase Inhibitor 1 hydrochloride 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 hydrochloride plays an important role in the regulation of the inflammatory response and the progression of some cancers^[1][2].

Tpl2 (Cot/MAP3K8) is a serine/threonine kinase in the MAP3K family that is upstream of MEK in the ERK pathway^[1].
Cancer Osaka thyroid (COT) kinase (Tpl2) is an important regulator of pro-inflammatory cytokines in macrophages^[2].
Tpl2 Kinase Inhibitor 1 (compound 2p) hydrochloride also inhibits MK2 and p38, with IC₅₀s of 110 μM and 180 μM, respectively in A431 cells^[1].
Tpl2 Kinase Inhibitor 1 hydrochloride inhibits lipopolysaccharide-induced TNF-a production from primary human monocytes and human whole-blood, with IC₅₀s of 0.7 μM and 8.5 μM, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

441.29

C₂₁H₁₅Cl₂FN₆

2934185-09-6

FC1=CC=C(NC2=C(C=NC3=C2C=C(NCC4=CN=CC=C4)N=C3)C#N)C=C1Cl.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]