KIN001-266 (Tpl2-IN-34) is a potent, selective Tpl2 (cot/MAP3K8) inhibitor with IC50 of 1.6 nM.
Tpl2-IN-34 dispalys 6875-fold selectivity over EGFR. P38, Src, CAMKII, MK2, PKA, and PKC (IC50>10 uM).
Tpl2-IN-34 inhibits LPS-induced TNF-α production in whole blood with IC50 of 0.3 uM.
Tpl2-IN-34 shows good efficacy in inhibiting TNF-alpha production in a LPS-stimulated rat inflammation model; orally active.
