sk2

NS13001 (N-(4-Chlorophenyl)-2-(3,5-dimethyl-1H-pyrazol-1-yl)-9-methyl-9H-purin-6-amine) is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

CyPPA, a subtype-selective positive modulator of SK channels, decreased spontaneous firing rate, increased the duration of the apamin-sensitive afterhyperpolarization.

GW 542573X is a potent and selective small molecule Ca2+-activated K+ 2 (SK2) channel activator.GW 542573X induces a leftward shift in the Ca2+ response curve of hSK1 from an EC50 (Ca2+) value of 410 nM to 240 nM, which can be used to study neurological disorders.

GSK2593074A (GSK'074) is a programmed necrosis inhibitor that displays inhibitory effects on RIP1 and RIP3.

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α), effectively inhibiting both its RNase activity and IRE1α kinase activity (IC50s: 200 and 20 nM).

GSK2983559 free acid is an effective and selective inhibitor of receptor-interacting protein 2 (RIP2). GSK2983559 free acid shows excellent activity in blocking many proinflammatory cytokine responses in human inflammatory bowel disease explant samples an

GSK2008607 is a potent B-RafV600E inhibitor with anticancer activity and can be used to study breast, colorectal, melanoma, thyroid, and ovarian cancers.

GSK2324 is a potent FXR agonist for the treatment of NAFLD by controlling hepatic lipids through reduced uptake and selective reduction of fatty acid synthesis.

GSK270822A is a selective ROCK1 inhibitor. GSK270822A exhibits IC50 of 9nM, 1100nM, 1550nM for ROCK1, RSK1, p70S6K, respectively.

GSK299115A (GSK-299115A) is a selective ROCK1 Inhibitor. GSK299115A exhibits IC50 of 8nM, 620nM, 560nM for ROCK1, RSK1, p70S6K, respectively.

GSK233705 (Darotropium bromide) is a muscarinic receptor antagonist used in conjunction with the prevention and treatment of chronic obstructive pulmonary disease (COPD) and asthma in humans.

GSK299423 (GSK-299423) is a novel DNA rotamase inhibitor with antimicrobial activity for the study of lung infections.

GSK2292767 is a potent and selective inhibitor of PI3Kδ.

GSK2292767 FA is a potent and selective inhibitor of PI3Kδ (pIC50 : 10.1).GSK2292767 FA is more than 500-fold more selective than other PI3K isoforms.GSK2292767 FA can be used in the study of respiratory diseases.

GSK2556286 (GSK286) is an orally active inhibitor of Mycobacterium tuberculosis (M. tuberculosis), effective against multidrug-resistant (MDR), extensively drug-resistant (XDR), and drug-sensitive (DS) strains. It inhibits the growth of human macrophages with an IC50 value of 0.07 μM.

GSK2850163 (S enantiomer) is the inactive enantiomer of GSK2850163. GSK2850163 is an novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1a).

GSK2656157 is a highly specific and ATP-competitive PERK inhibitor (IC50: 0.9 nM) in a cell-free assay. The selectivty is 500-fold higher against a panel of 300 kinases.

GSK2981278 (ROR gama modulator 1) is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).

GSK2879552 is an orally available, irreversible inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

GSK205 is a selective TRPV4 antagonist that blocks Ca(2+) signaling and may be used to reduce inflammation and pain.

GSK2239633A is an allosteric antagonist of CC-chemokine receptor 4 (CCR4) with a pIC50 of 7.96 for the binding of [125I]-TARC to human CCR4.

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

GSK 256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor (IC50: 3.2 pM for PDE4B). It can be used for the treatment of chronic obstructive pulmonary disease.

GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC 50 of 160 nM for USP20 Ub-Rho. GSK2643943A has anti-tumor efficacy.