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An orally bioavailable RARγ agonist; increases RARE activity and decreases IL-1β-induced NF-κB activity in primary mouse stromal cells at 60 nM; inhibits activin A-induced chondrogenic and osteogenic differentiation of mouse FAPs expressing ACVR1R206H at 10 nM; inhibits heterotopic ossification and preserves limb movement and growth in a ACVR1R206H FOP mouse model; decreases heterotopic ossification by 50 to 60% in a rat model of traumatic blast injury at 1 mg/kg per day for 14 days
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An ansa macrolide; inhibits polymerization and induces depolymerization of bovine brain tubulin (EC50s = 12 and 43 µM, respectively); inhibits sea urchin egg mitosis at 10 µM and decreases proliferation of KB nasopharyngeal cancer cells (EC50 = 0.19 UG/ml)
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A Notch inhibitor; induces cell cycle arrest at the G0/G1 phase and decreases MYC and CCNA1 expression in Caki human renal cancer cells; reduces tumor growth and increases survival in a 769-P mouse xenograft model at 8 mg/kg per day
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A CRF1 antagonist (IC50 = 6.1 nM); selective for CRF1 (mean IC50 = 10.6 nM) over CFR2β (IC50 = >1,000 nM) in radioligand binding assays and does not bind to the human CRF binding protein (IC50 = >1,000 nM); inhibits CFR-induced ACTH release in primary rat pituitary cells (IC50 = 129 nM); increases the time spent in the open arms of the EPM in rats at 10-30 mg/kg
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A tropic hormone and agonist of GNRHR (Ki = 13 nM in CHO cells expressing the human receptor); stimulates LH and FSH release from rat anterior pituitary cultures (0.1 μg); stimulates LH release from bovine anterior pituitary cultures (1 μM); induces ovulation in rats pretreated with fluphenazine (ED50 = 610.3 ng/kg)
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A long-chain acylcarnitine; levels are increased in the eyes of mice fed a diet high in n-3/n-6 PUFAs, but not in mice fed normal diet, in a mouse model of myopia induced by out-of-focus lenses
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An antagonist of cell surface glycosaminoglycans; binds to heparin, dermatan sulfate, heparan sulfate, and chondroitin sulfate and prevents heparin-induced inhibition of Factor Xa in cell-free assays; inhibits FGF2 binding to CHO cells (IC50 = 5 µM) and FGF2-induced tube formation by primary mouse endothelial cells; inhibits neural differentiation and increases pluripotency in mESCs at 5 µM
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A coumestan with diverse biological activities; reduces CCL4- and GaIN-induced cytotoxicity in rat hepatocytes in a dose-dependent manner; inhibits lethal and hemorrhagic activities of C. rhodostoma venom; inhibits anchorage-independent cell growth of MDA-MB-231 breast cancer cells; decreases the number of lung metastases in an MDA-MB-231 xenograft model in nude mice
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An endocannabinoid that contains linoleate in place of the arachidonate moiety of AEA; has been detected in porcine brain and murine peritoneal macrophages and has weak affinity for the CB1 and CB2 receptors (Kis =10 µM and 25 µM, respectively); 4-fold less potent than AEA at causing catalepsy in mice (ED50 = 26.5 mg/kg); increases ERK phosphorylation and AP-1-dependent transcription approximately 1.5 fold at 15 µM in a CB-receptor-independent manner; inhibits human FAAH-dependent hydrolysis of AEA (Ki = 9.0 µM), but is also effectively hydrolyzed by the enzyme
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A CDK inhibitor that most potently inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p35, and Cdc2/cyclin B (IC50s = 6, 9, 6, and 6 nM, respectively); inhibits the growth of parasites, including Plasmodium, at micromolar doses
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A semisynthetic echinocandin antifungal; inhibits 1,3-β-D glucan synthase from several C. albicans clinical isolates (IC50s = 0.89-7.96 ng/ml for the wild-type enzyme); active against C. albicans, C. parapsilosis, C. tropicalis, and C. guiillermondi (MICs = ≤0.03-4 UG/ml) and A. fumigatus (MIC90 = ≤0.03 UG/ml); increases survival and decreases the severity of pulmonary lesions in A. fumigatus-infected neutropenic rabbits at 10 mg/kg
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