sk2

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.

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

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

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

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

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.

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

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.

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

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

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.

GSK2292767 is a potent and selective inhibitor of PI3Kδ.

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).

GSK2033 is an antagonist of LXR (pIC50s: 7 and 7.4 for LXRα or LXRβ, respectively).

GSK2837808A is a potent and selective inhibitor of lactate dehydrogenase A (LDHA) with IC50 values of 1.9 nM for LDHA and 14 nM for LDHB.

GSK2983559 active metabolite (RIPK2-IN-1) is a potent, selective receptor-interacting protein-2 (RIP2) kinase inhibitor.

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.

GSK2606414 is an oral-available and specific PERK inhibitor (IC50=0.4 nM).

GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor.

GSK269962A (GSK269962A HCl) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.

GSK2795039 inhibits reactive oxygen species (ROS) production and NADPH consumption. GSK2795039 decreases apoptosis. GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) (pIC50: 6 in different cell-free assays).

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

GSK251 is a novel, orally bioavailable inhibitor of PI3Kδ, exhibiting high potency and selectivity, with a unique binding mode.

GSK2838232, a novel human immunodeficiency virus (HIV) maturation inhibitor, inhibits HIV reverse transcriptase activity across a broad panel of HIV-1 isolates.

GSK2256294A (GSK 2256294) is potent, selective inhibitor of recombinant human, rat and mouse sEH with IC50 of 27 pM, 61 pM and 189 pM, respectively.

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380, 000-fold selectivity versus PDE1 2 3 5 6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2.

GSK2578215A is a potent and selective LRRK2 kinase inhibitor.

GSK2801 is an effective, specific and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd: 136 nM) and BAZ2B(Kd: 257 nM) bromodomains.

GSK2200150A is an anti-tuberculosis (TB) agent identified by high-throughput screening (HTS) campaign.

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.

GSK217 is a potent and selective inhibitor of the bromo and extraterminal domain (BET) second bromodomain (BD2) with high solubility, utilized in oncology and immune inflammation research [1].

KSK213 is a potent inhibitor of Chlamydia trachomatis Infectivity (EC50 = 60 nM). KSK213 potently inhibited multiple serovars of C. trachomatis while not affecting the growth of key species from the commensal flora or host cell viability at 25 μM.

GSK268 is a BET inhibitor.

GSK2565363C is a betulin derivative wth antitumor activity.

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

GSK2818713 is a novel inhibitor of the Hepatitis C NS5A replication complex.

GSK256073 is an agonist of G-protein coupled receptor 109A (GPR109A). It acts by reducing serum glucose in subjects with type 2 diabetes mellitus.

GSK2850163 hydrochloride is a novel inositol-requiring enzyme-1α (IRE1α) inhibitor that inhibits the kinase (IC50: 20 nM) and RNA enzyme (IC50: 200 nM) activities of IRE1α.

GSK2646264 (Compound 44) is a highly effective and specific inhibitor of spleen tyrosine kinase (SYK) with a pIC50 of 7.1. It also inhibits multiple kinases, including LCK (pIC50 5.4), LRRK2 (pIC50 5.4), GSK3β (pIC50 5.3), JAK2 (pIC50 5), VEGFR2 (pIC50 4.5), Aurora B (pIC50 <4.6), and Aurora A (pIC50 <4.3). Notably, GSK2646264 demonstrates skin penetrability, reaching both the epidermis and dermis [1].

GSK2018682 is an agonist of sphingosine-1-phosphate receptor (s1p1) and (s1p5) agonist(pEC50s of 7.7 and 7.2,respectively).

GSK2018682 is a novel sphingosine-1-phosphate receptor 1 (s1p1) and 5 (s1p5) agonist.

HSK205 is a dual FLT3 and haspin inhibitor, exhibiting potent antitumor activity [1], with an IC50 of 0.187 nM for FLT3.

GSK2945 hydrochloride is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist (EC50s: 21.5 μM and 20.8 μM). It enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.

GSK2188764 is an inhibitor of T. brucei IPMK, partially inhibits rTbIPMK activity.

RSK2-IN-3 (Compound 26) is a covalent, reversible inhibitor of the RPS6KA3 (RSK2) kinase.

GSK2210875 is a mGluR5 antagonist with oral activity.

Fingolimod (FTY-720A) is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).