UK-78282 hydrochloride

Non Antibodies

KV1.3, KV1.4 K+ channels

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

466, 1

A Blocker of KV1.3 and KV1.4 K+ Channels

200 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).

41116134

UK-78282 hydrochloride blocks KV1.3 and KV1.4 in T lymphocytes1.

Yes

UK-78282 hydrochloride is a novel piperidine blocker of the T lymphocyte voltage-gated K+ channel, KV1.3 and KV1.4 with IC50 values of 0.28 and 0.17 μM respectively. UK-78282 suppresses T lymphocyte mitogenesis and leads to membrane depolarization. UK-78282 also blocks KV1.4 expressed in heart and brain. UK-78282 preferentially blocks the C-type inactivated state of the KV1.3 channel. KV1.3 mutants containing hydrophobic residues that might prefer to be buried, transition slowly into the C-type inactivated conformation and are insensitive to block by UK-78282, possibly because of the inability of the drug to bind the channel. UK-78282 hydrochloride serves as an experimental tool to probe the conformational changes in KV1.3 leading to C-type inactivation and to further define the critical physiological role of KV1.3 in T lymphocyte activation1.