Tpl2 Kinase Inhibitor (hydrochloride)

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 (1,25-dihydroxy vitamin D₃; Item No. 71820) 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

WARNING This product is not for human or veterinary use.

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 relationships. Bioor. 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 cells. J. 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 D₃. Cell Cycle 9(22), 4542-4551 (2010).