MKK7-COV-3

Biological Activity

MKK7-COV-3 (MKK7 Covalen inhibitor 3) is a potent, selective, covalent MKK7 inhibitor with in vitro IC50 of 5 nM, displays >1,000-fold selectivity over MKK4 (IC50=7.81 uM), shows EC50 of 1.3 uM for reduction of p-JNK in ICW assays in Beas2B cell line, without effect on p-ERK levels at 10 uM; displays remarkable selectivity against a kinome panel of 76 kinases, with very few kinases inhibited by more than 75% at 1 uM: Aurora kinase B, LRRK2, and MKK4, as well as FLT3; inhibits 60% of the CD86+ response in primary mouse B cells in response to LPS stimulation (10 μM, 2 hr pre-incubation).

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.