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A fluoroquinolone antibiotic that displays broad spectrum antibacterial activity by inhibiting the bacterial regulatory enzyme DNA gyrase (IC50 = 0.92 µg/ml) as well as topoisomerase IV (IC50 = 1.62 µg/ml).
Indole-4-carboxaldehyde is a synthetic intermediate useful for pharmaceutical synthesis.
An inhibitor of the HAT p300 (IC50 = 1.6 μM); competitively binds p300 (Ki = 400 nM) and does not inhibit several other acetyltransferases; blocks the growth of human melanoma, leukemia, lung, and prostate cancer cells in vitro.
A natural acyldepsipeptide that is effective against Gram-positive bacteria, including penicillin-resistant S. aureus; is also effective against many strains of anaerobic bacteria.
This nuclear receptor assay system utilizes proprietary human cells engineered to provide constitutive, high-level expression of the human vitamin D receptor (NR1I1), a ligand-dependent transcription factor commonly referred to as VDR. INDIGO’s reporter cells include the luciferase reporter...
Arachidonic acid is the keystone essential fatty acid at the origin of the arachidonic acid cascade. It is converted by cyclooxygenase, lipoxygenase, and epoxygenase enzymes into more than one hundred fifty different potent primary autacoid metabolites in species ranging from fungi to plants to...
A fluorogenic substrate that can be cleaved by caspase-4, -5, and -9.
A non-fluorescent analog of the highly selective calcium ionophore A-23187; used in experiments where fluorescent probes are employed.
Formal Name: 4-[6-methoxy-2-[(1E)-2-(3-nitrophenyl)ethenyl]-4-oxo-3(4H)-quinazolinyl]-benzoic acid CAS Number: 1237744-13-6 Molecular Formula: C24H17N3O6
A selective, brain penetrant EP2 antagonist (KB = 2.4 nM); blocks the induced expression of inflammatory markers in microglial cells treated with butaprost; reduces neurodegeneration in a mouse model of status epilepticus; inhibits proliferation and invasion in cancer cells treated with butaprost.
The male-specific mating pheromone of the fruit fly D. melanogaster; acts selectively through the Or67d odorant receptor to control mating behavior in both male and female fruit flies.
An ATP-competitive inhibitor of JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms.
A third generation, irreversible steroidal aromatase inhibitor (Ki = 10.2 nM; Kinact = 26 nM) that induces aromatase degradation, which leads to a decrease in estrogen levels in plasma.
A methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM); inhibits the ERG1, ERG2, and ERG3 isoforms with KD values of 99, 116, and 193 nM, respectively.
A partial agonist of the α2-adrenergic receptor, minimally inhibiting adenylate cyclase through this Gi protein-coupled receptor although it binds avidly (Ki = 1.0 nM); potentiates platelet aggregation by ADP (EC50 = 1.5 µM) and inhibits epinephrine-induced aggregation...
The mechanism for the movement of cholesterol from intracellular sites to their ultimate cellular destination is an unresolved question of fundamental importance to cell biology and medicine. Thus, defining mechanisms of intracellular cholesterol transport and identifying the cellular factors...
An irreversible inhibitor of IκBα phosphorylation, preventing activation of NF-κB by cytokines and lipopolysaccharide (IC50 = 10 μM); blocks gene expression that is regulated through the classical pathway of NF-κB activation and in this way blocks apoptosis,...
Rubiadin is an anthraquinone that is a minor component of certain Rubia species, as well as other plants. It demonstrates antioxidant activity.
A methyl amide analog of fluprostenol.
A selective β3-adrenergic receptor antagonist.
5-(2-Aminopyridyl)amide oxime is a synthetic intermediate useful for pharmaceutical synthesis.
A weak inhibitor of the menin-MLL fusion protein interaction (IC50 = 193 μM), intended as a negative control compound for tests involving MI-2.
A calcium-dependent activator of BKCa channels that is typically used at a concentration of 30 µM to hyperpolarize the membrane potential of single myocytes during studies of smooth muscle relaxation and vasodilation; cardioprotective against pulmonary hypertension as well as ischemia and...
A homolog of DHEA, characterized by the addition of an (S)-α-methyl group at the methylene carbon adjacent to the amide nitrogen.