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A natural amino alcohol that serves as an intermediate in the biosynthesis of the amino acid L-histidine in bacteria, archaebacteria, fungi, and plants.
A selective, cell permeable inhibitor of MLCK (IC50 = 50 nM).
An inhibitor of the HAT PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid; dose dependently inhibits histone H4 acetylation in HepG2 cells in vitro at 30-60 μM.
A small molecule inhibitor of NF-κB-dependent expression of TNF-α, IL-1β, and IL-6 (IC50 50 = 2.3 µM).
An aminoquinoline antimalarial compound that is widely used as an autophagy inhibitor, preventing autophagosome fusion with lysosomes and inhibiting lysosomal acidification.
A potent inhibitor of MELK (IC50 = 0.41 nM); blocks the phosphorylation of MELK-specific substrates and reduces the ability of MCF-7 breast cancer cells to invade and form spheroids in Matrigel; suppresses the growth of xenograft tumors in mice.
A purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively); demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.
A small molecule inhibitor of Sir2p HDAC activity, displaying higher activity in vivo (minimal inhibitory concentration = 0.49 µM) than in vitro (IC50 = 60 µM); has diverse effects on mammalian cells.
An analog of L-carnitine that, in the range of 0.25-1 mM, inhibits the uptake of L-carnitine by cells.
A metabolite of 8-iso PGF2α in humans and rats; present in normal human urine at concentrations of 200-300 pg/ml.
A pyrazinone whose biological activity has not been reported, though similar diketopiperazines are known to inhibit calpain and/or regulate S. aureus virulence factor expression.
An N-benzoylindazole derivative that selectively targets the binding domain of neutrophil elastase (IC50 = 7 nM).
An internal standard for the quantification of PtdIns-(3,4,5)-P3 (1,2-dipalmitoyl) by GC- or LC-MS.
A mixture of oligomycins A, B, and C
A natural sesquiterpene quinone that reversibly induces vesiculation of Golgi membranes, blocking the secretory pathway; inhibits SAH hydrolase (IC50 = 40 µM), DNA polymerase β (IC50 = 45.2 µM,) and Cdc25B (IC50 = 92 µM); at 10 µM,...
A mixture of closely related metabolites produced by A. teichomyceticus that are effective against Gram-positive bacteria; prevents bacterial cell-wall synthesis by binding and sequestering a cell-wall precursor with a D-alanine-containing peptide.
A selective antagonist of the dopamine D3 receptor (pKi = 8.0); has high oral bioavailability and enters the central nervous system of the rat.
A potent and selective inhibitor of G9a activity in vitro (IC50 = 4 nM) and G9a/GLP-mediated dimethylation of histone 3 on lysine 9 in MDA-MB-231 cells (IC50 = 25 nM).
A highly selective inhibitor of PLD1 (IC50 = 3.7 nM) versus PLD2 (IC50 = 6.4 μM).
GW 0742 is a selective PPAR.delta. agonist (EC50 = 1.1 nM) that exhibits 1,000-fold selectivity over the other human PPAR subtypes. GW 0742 exhibits time-dependent neuroprotection in low KCl-induced apoptosis in cerebellar granule neuronal cultures. Despite the neuroprotective properties observed,...
Source: Recombinant protein expressed in E. coli RbBP5 is a ubiquitously expressed nuclear protein that contains WD40 repeat-like domains. RbBP5 binds directly to tumor suppressor retinoblastoma protein (RB) and regulates cell proliferation. RbBP5 is also an important component of the multi-subunit...
A selective TRPM8 antagonist (IC50s = 8.3 and 5.8 nM in human and rat, respectively); attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg); reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.
A phospholipid emulsifier used in combination with cationic phospholipids to facilitate DNA-liposome complex transport across membranes; may increase efficiency during DNA transfection studies.
cGMP, synthesized from GTP by both membrane-bound and soluble guanlyate cyclase enzymes, is a key intracellular second messenger molecule that transduces cellular signaling events in response to a variety of hormones, autacoids and drugs. The relative abundance of cGMP within a given cell can serve...