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An inhibitor of mitochondrial dysfunction increases intracellular ATP levels in Hep3B cells at a 3 UM rescues LPS-induced apoptosis and decreases in the mitochondrial membrane potential in BV-2 microglial cells at 5 UM protects against BSO-induced decreases in cell viability in fibroblasts isolated from patients with various mitochondrial diseases (EC50s 2.3-5.1 UM) in an electron transport chain-independent manner reduces plasma levels of creatinine and decreases acute renal tubular necrosis in a mouse model of bilateral retroperitoneal renal ischemia-reperfusion injury at 50 mg/kg
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A derivative of sorafenib selectively inhibits proliferation of BEL-7402 MGC803 and T24 bladder cancer cells (IC50s 5 77 5 21 and 3 97 UM respectively) over non-cancerous HCV-29 cells (IC50 23 19 UM) induces apoptosis in T24 cells at 2-6 UM induces ferroptosis in T24 cells at 6 UM when incubated for 10 hours induces autophagy at 6 UM when incubated for 8 hours
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A degrader of cyclin K the levels of cyclin K in patient-derived CRC cells in a concentration-dependent manner inhibits cancer cell proliferation in CRC tissue samples isolated from the colon (IC50s 0.9-20.6 UM) as well as from hepatic lung and rectal metastases (IC50s 0.5-11.8 1 and 1.4-38.4 UM respectively) decreases the levels of ATM and RAD51 in patient-derived CRC tissues at 0.7 and 0.5 UM respectively reduces the number of spheroids formed and induces PARP cleavage in patient-derived CRC spheroid cultures at 3 UM
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An inhibitor of plasma kallikrein (Ki 0 81 M) reduces bradykinin generation induced by kaolin and -carrageenan ex vivo in human plasma prolongs partial thromboplastin and euglobulin clot lysis times reduces hyperplasia pannus formation and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis
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An Hsp27 and microtubule inhibitor inhibits migration and invasion of MDA-MB-231 cells in vitro in an Hsp27-dependent manner inhibits PKC phosphorylation of Hsp27 induces HCT116 cell cycle arrest in the G2/M phase via formation of the Mad2/p55CDC inhibitory complex and Bax activation of apoptosis inhibits microtubule polymerization in HCT116 cells reduces tumor volume in an HCT116 mouse xenograft model (50-100 mg/kg)
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A diterpene alkaloid inhibits Nav1.7 in HEK293 cells expressing the human channel (IC50 25.8 nM) scavenges DPPH radicals by 65.3 at 1 mM increases the mechanical pain threshold in the von Frey test in streptozotocin-induced diabetic but not non-diabetic mice at 10 mg/kg
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ABlactamase inhibitor (Kis 29-110 nM for class A and class C enzymes) selective for bacterialBlactamases over a panel of mammalian serine proteases (IC50s 1000 M) potentiates the activity of biapenem against K pneumonia expressing KPC-2 at 0 02 g/ml potentiates the activity of carbapenem antibiotics against clinical isolates of various bacteria (MICs 0 06-4 and 4-64 g/ml in the presence and absence of compound respectively) reduces the number of CFUs in the lung in a neutropenic mouse lung infection model when used in combination with biapenem or meropenem at 50 mg/kg
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A flavonoid glycoside with diverse biological activities potentiates TRAIL-induced cytotoxicity and apoptosis in U87MG human glioma cells potentiates TRAIL-induced tumor cell apoptosis and reduction of tumor growth in a U87MG mouse xenograft model reduces pulmonary platelet count edema and macrophage polymorphonuclear leukocyte and lymphocyte infiltration as well as inhibits TXNIP/NLRP3 MAPK and NF-KB signaling in a mouse model of LPS-induced acute lung injury from 12 5-50 mg/kg inhibits AChE and induces dyskinesia recovery in a zebrafish model of Alzheimers disease in tank water at 50 g/ml
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Ths mxture contans the prmary COX products produced by most mammalan tssues Contents Prostaglandn D2 Prostaglandn E2 6keto Prostaglandn F1a Prostaglandn F2a and Thromboxane B2 (100 Ug each)
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A partal agonst of PPARY actvates PPARY wth a lower potency (K 15 versus 0 035 UM) but a smlar maxmal effcacy compared to rosgltazone mproves nsuln resstance n normal detnduced glucosentolerant and n dabetc db/db mce yet reduced adpogenc actvty
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mmunogen Synthetc peptde from the Ctermnal regon of human 5OxoETE receptor Host Rabbt Speces Reactvty ( ) Human Cos7 (Afrcan green monkey) mouse porcne and rat Applcatons CC and WB
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