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Oxidative stress in the cellular environment results in the formation of highly reactive and unstable lipid hydroperoxides. Decomposition of the unstable peroxides derived from polyunsaturated fatty acids results in the formation of malondialdehyde (MDA), which can be quantified colorimetrically...
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.