Activators & Inhibitors

Activity: JAK3 inhibitor . Function/Pharmacology: JAK3 inhibitor. Inhibits human glioblastoma cell adhesion and invasion.1 Increases survival in a mouse ALS model.2 Delays or prevents autoimmune type 1 diabetes in NOD mice.3 Exhibits potent anti-inflammatory activity in mouse models of peritonitis, colitis, cellulitis and systemic inflammatory response syndrome.4 Displays protective effects against myocardial ischemia and reperfusion injury in mouse models.5 Chemical Name: 4-[(4’-hydroxyphenyl)amino]-6,7-dimehtoxyquinazoline

Activity: Induces stem cell generation . Function/Pharmacology: Dramatically improves (200-fold) the efficiency of induced pluripotent stem cell generation from human fibroblasts1. Induces direct conversion of porcine embryonic fibroblasts into adipocytes2. Cell permeable. Chemical Name: N-Benzyl-[2-(pyrimidin-4-yl)amino]thiazole-4-carboxamide

Activity: PH domain antagonist . Function/Pharmacology: PH domain antagonist. Specifically blocks the binding of PIP3 to the Akt pleckstrin homology domain (IC50 = 31 μM). Suppresses PI3K-PDK1-Akt-dependent phosphorylation. Induces apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM)1. Inhibiting the binding of PIP3 to effector PH domains is new point of intervention in the PI3K signaling network2. Chemical Name: N-[[(3-Chloro-2-hydroxy-5-nitrophenyl)amino]thioxomethyl]benzamide

Activity: Cdc42 inhibitor . Function/Pharmacology: MLS-573151 is a potent and specific inhibitor of Cdc42 a small GTPase of the Rho-subfamily (IC50=2 μM).1 A useful agent for probing the involvement of Cdc42 in cellular signaling and physiology.2 Chemical Name: 4-[3,5-Diphenyl-4,5-dihydropyrazol-1-yl]benzenesulfonamide

Activity: Endogenous agonist at GPR110 . Function/Pharmacology: Anandamide-like lipid mediator produced from DHA in the brain. Stimulates neurite growth, synaptogenesis and glutamatergic synaptic activity in developing hippocampal neurons at 10-100 nM.1 Potently induces neuronal differentiation of neural stem cells.2 Promotes growth of cortical axons vial modulation of hedgehog signaling.3 Binds to and activates orphan receptor GPR110, stimulating cAMP production at low nM concentrations.4 Reduces LPS-induced TNFα production in cultured microglia cells and ameliorates LPS-induced neuroinflammation in a mouse model.5 Chemical Name: N-Docosahexaenoylethanolamide

Activity: GSK-3 inhibitor . Function/Pharmacology: Selective glycogen synthase kinase 3 (GSK-3) inhibitor, IC50 = 104 nM. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices. Anti-inflammatory activity. Cell permeable. Active in rodent models. Chemical Name: N-[(4-Methoxyphenyl)methyl]-N’-(5-nitro-2-thiazolyl)urea

Activity: p97 inhibitor . Function/Pharmacology: A potent, selective and reversible inhibitor of the AAA-ATPase p97 (ATPase associated with diverse cellular activities). Ki=3.2 M. It blocks ubiquitin-dependent protein clearance pathways. Cell permeable. Chemical Name: N,N’-Dibenzylquinazoline-2,4-diamine

Activity: USP14 inhibitor . Function/Pharmacology: Selective inhibitor of Usp14 (IC50<4 μM). Enhances proteasome activity and substrate proteolysis.1,2 Inhibits Dengue virus replication.3 In prion-infected CAD5 cells activation of the ubiquitin proteasome system by IU1 is sufficient to induce clearance of polyubiquitinated substrates and reduce misfolded prion protein load.4 Attenuates ischemia/reperfusion-induced neuronal injury in a mouse model.5 Cell permeable. Chemical Name: 1-[1-(4-Fluorophenyl)-2,5-dimethyl-1H-pyrrol-3-yl]-2-(1-pyrrolidinyl)ethanone

Activity: TRPV4 channel blocker . Function/Pharmacology: A novel and potent TRPV4 channel agonist. GSK1016790A induced Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300-fold more potent than 4α-PDD and is a valuable tool for investigating the role of TRPV4 in physiological processes. Chemical Name: (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide