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A synthetic glucocorticoid that binds to glucocorticoid receptors (IC50 = 1.5 nM; Kd = 2.8 nM); decreases survival of cultured corneal epithelial cells and inhibits their migration in a scratch assay following 12 hours of treatment (0.01%)
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A tetrasaccharide; increases the α-amylase synthesis rate in B. stearothermophilus three-fold greater than sucrose or glucose when used at at 0.1 mM; inhibits the growth of E. carotovora in a cylinder-agar plate assay at 750 μg/ml; inhibits TNF-α-induced expression of ICAM-1 in MOVAS-1 mouse VSMCs
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A thiazide diuretic; inhibitor of carbonic anhydrase (CA); selective for CAII, VB, VII, IX, XII, and XIV (Kis = 305-235 nM) over CAI, IV, and VI (Kis = 2,840-8,250 nM) and CAIII, VA, and XIII (Kis = >10 µM)
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An organochlorine insecticide; active against a variety of insects including bollworms and tobacco budworms (LD50s = 4.14 and 4.95 mg/g, respectively); binds to GABA receptors (IC50 = 60 nM in rat brain membranes); toxic to rats (LD50 = 240 mg/kg)
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An adenosine receptor agonist; binds selectively to A1 over A2A and A3 receptors (Kis = 0.83, 2,300 and 42 nM, respectively, for the human receptors expressed in CHO cells; decreases heart rate in isolated rat atria (EC50 = 8.2 nM) but does not affect vasodilation in bovine coronary arteries; inhibits isoniazid- and pentylenetetrazole-induced convulsions in mice at 8.3 μmol/kg
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A reactive methionine analog that contains an alkyne moiety that is readily inserted into newly-synthesized proteins; can be labeled or captured through click chemistry
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An α-hydroxy acid; metabolized to α-ketoglutarate by L-2-hydroxyglutarate dehydrogenase; levels are increased in 2-hydroxyglutaric aciduria; competitively inhibits α-ketoglutarate-dependent dioxygenases, including several involved in histone lysine and DNA demethylation
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A nucleoside analog that inhibits ribonucleotide reductase and DNA polymerase-α (IC50s = 65 and 3.9 nM, respectively) and is cytotoxic to K562 myelogenous leukemia cells (IC50 = 5 nM) as well as various other leukemias and solid tumors
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A selective α2-adrenoceptor agonist (Ki = 1.62 nM) that binds to α1-adrenoceptors with much weaker potency (Ki = 415 nM); primarily used as a sedative for horses in large animal veterinary medicine
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A β-glucuronidase chromogenic substrate; upon cleavage by β-glucuronidase, an insoluble salmon precipitate is formed that can be used in histochemical analysis of β-glucuronidase activity
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A fluorogenic substrate for CYPs; HFC is released upon O-deethylation by CYPs and its fluorescence can be used to quantify CYP activity; ex/em = 410/510 nm, respectively
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A prodrug form of acetaminophen; reduces acetic acid-induced writhing in mice and LPS-induced pyresis in rats at 200 and 600 mg/kg, respectively; induces hepatotoxicity, decreases hepatic GSH, SOD, and GPX levels, increases hepatic MDA and nitrotyrosine levels, and increases mortality in mice at 1200 mg/kg
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