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An inhibitor of microtubule assembly (ID50 = 2 µM) with anticancer properties; inhibits proliferation of hepatocellular carcinoma (IC50s = 9.2-728.2 nM) and other carcinoma cell lines (IC50s = 12.2-2,247 nM); inhibits tumor growth in a hepatocellular carcinoma mouse xenograft model when administered at doses of 2 or 4 mg/kg for 4 weeks; decreases functional vascular volume within hours in a well-vascularized murine colon adenocarcinoma model
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A muscle relaxant that inhibits the release of calcium from skeletal muscle sarcoplasmic reticulum; inhibits a component of store-operated calcium entry (SOCE) that is coupled to the skeletal muscle ryanodine receptor, with 20 µM azumolene causing a 70% reduction in SOCE in myotubes
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A biologically active form of folic acid that functions, in conjunction with vitamin B12, as a methyl-group donor involved in the conversion of homocysteine to methionine
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A natural sapogenin that acts as a bioavailable, potent, and high-affinity agonist of the nuclear receptor RORα (EC50 = 110 nM); up-regulates the expression of several RORα-inducible genes in the livers of mice, when given at 3 mg/kg/d orally for seven days
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A natural sesquiterpene lactone that reduces growth (EC50 = 3-35 μM) and induces apoptosis in assorted cancer cell lines; inhibits the activation of Akt (15 μM) in endometriotic epithelial cells and STAT3 activation in THP-1 cells (EC50 = 10 μM); inhibits telomerase activity in NALM-6 cells
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An agonist of FP receptors (EC50 = 4.12 µM), an active metabolite of unoprostone isopropyl ester. and a derivative of PGF2α; increases inositol phosphate production in HEK293 cells expressing the human receptor; prevents constant light-induced degradation of photoreceptors in rats at 1.2, 3.6, or 6 UG/µl
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A prodrug form of 5-ASA; cleaved by bacterial azoreductases in the intestinal lumen to release 5-ASA; decreases IL-2 levels and increases IL-6 levels in the serum and colonic mucosa membrane, as well as decreases micro- and macroscopic colonic damage, in a rat model of DNCB-induced colitis at 600 mg/kg per day
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A cell-permeable benzoxazolo-sulfonamide compound that blocks human FBPase-1 enzymatic activity by competing at the AMP allosteric binding site (IC50 = 3.4 µM; Ki = 1.1 µM); blocks glucose production in starved rat hepatoma cells (IC50 = 6.6 µM)
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A β1-selective adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity; often used to examine the activity of the drug-transporting MDR1 gene product P-glycoprotein
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A β-adrenergic receptor agonist with potent positive inotropic effects in vivo; strongest effects on β1 receptors, with lesser but significant β2 receptor activation and only weak α1 receptor actions; strongly increases cardiac contractility
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A GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)); acts as an antagonist at ρ1 GABAC receptors (IC50 = 25 µM).
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A serine proteases inhibitor that is capable of inhibiting trypsin (a digestive system protease; Ki = 15 nM), tryptase (a mast cell protease; Ki = 95.3 pM), and additional proteases in the coagulation cascade including thrombin (Ki = 0.84 μM); 300 mg/kg decreases the total number of eosinophils and lymphocytes in bronchoalveolar lavage fluid in a mouse model of allergic asthma
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A potent, selective, and competitive inhibitor of ATGL (IC50 = 0.7 μM); does not inhibit hormone-sensitive lipase, monoglyceride lipase, pancreatic lipase, lipoprotein lipase, or other lysophospholipases; blocks lipolysis by ATGL in vitro, in white adipose tissue organ cultures, and in vivo
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An ATP-competitive inhibitor of Cdk1, 2, 4, 5, 6, and 9 with IC50 values of 210, 47, 100, 13, 170, and 50s = 40-940 nM in vitro) and human tumor xenograft models, inhibiting cell cycle progression and inducing apoptosis
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