α4-α6

BRD9876 is a selective inhibitor of MM1S growth.

CL 218872 is a benzodiazepine agonist displaying selectivity for α1 subunit-containing GABAA receptors (Ki values are 130, 1820, 1530, > 10000, 490 and > 10000 nM for α1, α2, α3, α4, α5 and α6-subunit containing receptors respectively). Orally active anxi

MK0343 is an orally bioavailable GABAA receptor subtype-selective partial agonist and is a non-sedating anxiolytic.

Eg5-IN-3 (5) is an Eg5 inhibitor targeting a novel allosteric site (α4/α6/L11). It disrupts tubulin assembly, leading to abnormal and irregular formations, which subsequently causes typical mitotic arrest, akin to the effects of Monastrol.

PVZB1194, a biphenyl-type inhibitor of Kinesin spindle protein Eg5 (KIF11), exhibits anticancer potential by inducing cell cycle arrest and apoptosis through inhibiting Eg5 ATPase activity. It binds to the α4/α6 allosteric pocket and demonstrates ATP-competitive activity [1].

CVN417 is an orally active antagonist of nAChR containing the α6 subunit, modulating phasic dopaminergic neurotransmission in an impulse-dependent fashion. It inhibits Ca(2+) efflux through nAChR subunits, displaying IC50 values of 0.086 μM (α6), 2.56 μM (α3), and 0.657 μM (α4). CVN417 has shown efficacy in reducing resting tremor in rodent models, suggesting a potential to ameliorate movement disorders in conditions like Parkinson's disease [1].

α-Conotoxin BuIA is a paralytic peptide neurotoxin that acts as a competitive antagonist of nicotinic acetylcholine receptors (nAChR), with inhibitory concentration 50 (IC50) values of 0.258 nM for α6/α3β2, 1.54 nM for α6/α3β4, and 5.72 nM for α3β2. It serves to differentiate between nAChRs containing the β2- and β4-subunits and selectively inhibits αxβ2 nAChRs, exhibiting a potency hierarchy of α6>α3>α2>α4 [1].