MEK kinases are central components of diverse intracellular signaling pathways. MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation. AZD 6244 is a potent, highly selective inhibitor of...

Mdivi 1 is a mitochondrial division inhibitor. It inhibits the GTPase activity of yeast, but not human, dynamin-1 (Dnm1, IC50 = ~1-10 µM for the recombinant yeast enzyme) and human dynamin-related protein 1 (DRP1) in A549 lung cancer cells when used at a concentration of 50 µM. Mdivi 1 (50 µM) inhibits mitochondrial...

SNC 80 is a selective nonpeptide agonist of the delta-opioid receptor (Ki = 0.18 nM, IC50 = 2.73 nM) that is over 2,000-fold less effective at the µ-opioid receptor. It effectively activates µ/delta receptor heteromers (EC50 = 52.8 nM) but not kappa/delta or µ/kappa heteromers. SNC 80 has antinociceptive as well as...

Etifoxine is a positive allosteric modulator of alpha1beta2gamma2 and alpha1beta3gamma2 subunit-containing GABAA receptors. It selectively increases GABA-induced currents in X. laevis oocytes expressing alpha1beta2gamma2 or alpha1beta3gamma2 over alpha1beta1gamma2 subunit-containing receptors at 20 µM. Etifoxine...