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A peptide inhibitor of DRP1; selectively inhibits DRP1 GTPase activity over OPA1, MFN1, and dynamin 1 at 1 µM; inhibits the MPP+-induced protein-protein interaction between DRP1 and FIS1, as well as stress-induced DRP1 translocation to the mitochondria in SH-SY5Y cells; inhibits MPP+-induced mitochondrial apoptosis and autophagy in SH-SY5Y cells and MPP+-induced mitochondrial fragmentation and cell death in a primary rat dopaminergic neuronal model of Parkinson’s disease
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An inhibitor of SPNS2; inhibits mouse Spns2 by 67% at 2 µM; inhibits S1P export from HeLa cells expressing mouse Spns2 (IC50 = 1.93 µM); decreases blood lymphocyte numbers and plasma S1P levels in mice at 20 mg/kg
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An antimicrobial peptide; active against various Gram-negative and Gram-positive bacteria, including MRSA (MICs = 4-64 UG/ml); synergistic with ampicillin, amoxicillin, and novobiocin against P. aeruginosa; suppresses the development of resistance to kanamycin and ampicillin in E. coli; increases the survival rate of E. tarda-infected O. laptipes
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An endogenous vasodilator; binds to the bradykinin B2 receptor (IC50 = 0.54 nM in COS-7 cells expressing the human receptor) and acts as an agonist but does not bind the bradykinin B1 receptors (Ki = >10,000 nM in HEK293 cells expressing the human receptor); stimulates arachidonic acid release in CHO cells expressing the human bradykinin B2 receptor (EC50 = 0.7 nM); induces relaxation of ACh- or PDBu precontracted isolated porcine coronary arterial rings at 100 nM; induces hyperalgesia in mice at 1 UG/paw; plasma levels are increased in patients during an acute attack of angioedema
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An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM, respectively); activates glycogen synthesis in CHO-IR cells (EC50 = 0.763 μM) and in isolated type 1 diabetic rat skeletal muscle; has been shown to promote self-renewal of embryonic stem cells
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A diterpenoid alkaloid; has antiarrhythmic activity in a rat model of aconitine-induced arrhythmia and antifibrillatory activity in a mouse model of aconitine-induced cardiac fibrillation (ED50s = 8 and 20 mg/kg, respectively)
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A fluorescent nucleotide derivative; inhibits B. pertussis and B. anthracis ACs (Kis = 9.1 and 8.0 µM, respectively); has been used as a probe for binding sites in, as well as ion effects on the enzymatic activity of, B. pertussis and B. anthracis ACs; ex/em = 330/425 nm, respectively
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A vitamin D receptor agonist; induces reporter gene expression in VDR-expressing COS-1 cells at 1 nM; induces differentiation of HL-60 and MG-63 cells (EC50s = 6.2 and 0.18 nM, respectively); reduces the proliferation of MCF-7 cells (EC50 = 4.1 nM); protects primary human keratinocytes against DNA damage induced by UVB irradiation; inhibits acetylcholine- or ATP-induced contractions of aortic rings isolated from spontaneously hypertensive rats at 100 nM; unlike calcitriol, it does not increase serum calcium levels or decrease tibia calcium levels in mice at 80 UG/kg
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A CaMKII inhibitor (IC50 = 0.063 µM); is selective for CaMKII over CaMKIV, MLCK, p38α, Akt1, and PKC (IC500s = >60, 36, 11, 30, and 21 µM, respectively)
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A synthetic peptide derivative that irreversibly and specifically inhibits thrombin-mediated platelet activation by binding with high affinity to the active site of thrombin (Ki = 0.24 nM); used as an anticoagulant (100 μM)
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A C5a receptor antagonist (IC50 = 0.3 µM); inhibits C5a-induced secretion of MPO in isolated human PMNs; inhibits vascular leakage, PMN infiltration, and peritoneal TNF-α and IL-6 production in a rat model of peritoneal Arthus reaction at 10 mg/kg; reduces body weight loss and anorexia and inhibits striatal degeneration in a rat model of 3-NP-induced Huntington’s disease; reduces atherosclerotic lesion size and lipid content in ApoE-/- mice at 3 mg/kg
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An endogenous polyamine; urinary levels are increased in patients with chronic pancreatitis; blood levels are increased in patients with ischemic cardiomyopathy, as well as in patients with Parkinson’s disease
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