MAP3K1-IN-1

MAP3K1-IN-1 (51-106) (5 µM) selectively inhibits MAP3K1 by 78.1% in PANC-1 pancreatic cancer cell lysates, while exerting only extremely weak inhibitory effects on most other kinases in the kinase panel^[1].
MAP3K1-IN-1 (5-20 µM; 30 min) dose-dependently inhibits TNFα-induced IKKβ phosphorylation in MiaPaCa2 pancreatic cancer cells^[1].
MAP3K1-IN-1 (0.02-20 µM; 72 h) inhibits the growth of HCT116 MAP3K1 wild-type colorectal cancer cells with an IC₅₀ of 1.8 µM, while its activity is reduced in MAP3K1 knockout cells (IC₅₀ = 8.9 µM)^[1].
MAP3K1-IN-1 (0.625-10 µM; 2 h) induces a dose-dependent decrease in phosphorylation sites (including multiple NPM1 sites) in PANC-1 pancreatic cancer cells, with no significant change in total protein levels^[1].
MAP3K1-IN-1 (10 µM; 2 h) reduces the phosphorylation level of NPM1 at the T199 site in PANC-1 pancreatic cancer cells^[1].
MAP3K1-IN-1 (5-20 µM; 15 min pretreatment followed by 6 h TNFα stimulation) dose-dependently inhibits TNFα-induced NF-κB transcriptional activity in HeLa cells stably expressing an NF-κB-responsive luciferase reporter gene^[1].

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