Activators & Inhibitors

Activity: Protease inhibitor . Function/Pharmacology: Dehydropeptidase-1 inhibitor. Inhibits the proteolytic conversion of leukotriene D4 to E4.1 Inhibits the mammalian β-lactamase renal dipeptidase (dehydropeptidase-1, DPEP1) and thus is used as an antibacterial adjunct to extend the half-life of β-lactam antibiotics.2 Cilastatin also inhibits bacterial metallo-β-lactamase and thereby may block resistance to the carbapenem family of antibiotics in certain bacteria.3 Suppresses invasion and metastasis of DPEP1-expressing tumor cells.4 Chemical Name: (2Z)-7-[[(2R)-2-Amino-2-carboxyethyl]thio]-2-[[[(1S)-2,2-dimethylcyclopropyl]-carbonyl]amino]-2-heptenoic acid, sodium salt

Activity: NFκB inhibitor . Function/Pharmacology: Tranilast is an anti-allergy agent (inhibition of mast cell degranulation) that has been shown to have potent immunomodulatory effects (via inhibition of endotoxin induced: PGE2, IC50 = 1-20 µM; TXB2, IC50 = 10-50 µM; TGFβ1, IC50 = 100-200 µM; IL-8, IC50 = 100 µM) .1,2,3 Tranilast also displays anti-angiogenic properties.4,5 Chemical Name: N-(3’,4’-Dimethoxycinnamoyl)anthranilic acid

Activity: Neuroinflammation inhibitor (PDE pan-inhibitor) . Function/Pharmacology: Phosphodiesterase inhibitor with some selectivity for PDE4 and 5. (IC50s= 53, 35, 48,12 and10 μM for PDE 1a, 2, 3, 4 and 5 respectively1). Acts as a cerebral vasodilator by selectively inducing a cGMP-independent relaxation of the intracranial vertebrobasilar artery.2 Attenuates neuroinflammation and enhances retinal ganglion cell viability in glaucoma via PKA signaling.3 A glial cell activation inhibitor.4 Enhances morphine analgesia and attenuates tolerance and withdrawaI.5 Orally active and crosses the blood-brain barrier.5 Chemical Name: 3-Isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine

Activity: K-ATP channel activator . Function/Pharmacology: Activates ATP-dependent K+ channels1 via inducing translocation of PKC-epsilon from the cytosol to the mitochondria2. Hyperglycemic agent. Induces powerful protective effects against cardiac ischemia via multiple mechanisms.3 Stimulates mitochondrial ATP synthase activity conferring cardioprotection in a streptozotocin-induced acute diabetes model.4 Prevents alterations in memory and synaptic plasticity induced by Amyloid-ß.5 Chemical Name: 7-Chloro-3-methyl-2H-1,2,4-benzothiadiazine 1,1-dioxide

Activity: Caspase inhibitor . Function/Pharmacology: Z-Asp-CH2-DCB is a cell permeable broad spectrum caspase inhibitor. Chemical Name: Carbobenzyloxy-L-Asp-α-[2,6-dichlorobenzoyl)oxy]methane

Activity: Enhances apoptosis . Function/Pharmacology: Natural sesquiterpene ketone isolated from Zingiber sp. Potentiates TRAIL-induced apoptosis via upregulation of death receptor DR4 and DR5 expression. Induces apoptosis in T-acute lymphoblastic leukemia cells. Has no cytotoxic effect on normal cells. Cell permeable. Chemical Name: (2E,6E,10E)-2,6,9,9-Tetramethyl-2,6,10-cycloundecatrien-1-one

Activity: PPARg activator; increases adipocyte thermogenesis . Function/Pharmacology: A naturally occurring isoflavone isolated from Astragalus and other plants. Increases adipocyte thermogenesis by modulating PPAR activity.1 Activates AMP-activated protein kinase/-catenin signaling to inhibit adipogenesis.2 Accelerates wound repair by increasing expression of Egr-1 transcription factor.3 Potential cancer chemopreventive and chemotherapeutic.4 Provides neuroprotection against traumatic brain injury by inhibition of neuroinflammation in a rat model.5 Chemical Name: 7-hydroxy-3-(4-methoxyphenyl)-4H-1-benzopyran-4-one

Activity: Angiotensin-converting enzyme inhibitor . Function/Pharmacology: Captopril is an angiotensin-converting enzyme (ACE) inhibitor (IC50 = 0.022 μM).1 Also inhibits the bifunctional Zn2+-containing leukotriene A4 hydrolase/aminopeptidase (LTA4 hydrolase) reversibly and competitively (Ki = 6.0 μM for leukotriene B4 formation and Ki = 60 nM for L-lysine-p-nitroanilide).2 Displays vasodilatory and antihypertensive effects in vivo. Clinically useful antihypertensive agent. Chemical Name: (2S)-1-(3-Mercapto-2-methyl-propionyl)-L-proline

Activity: Inhibits actin polymerization and microfilament organization . Function/Pharmacology: Inhibits actin polymerization and disrupts microfilament organization1. Significantly more potent than cytochalasins in the disruption of microfilamament mediated processes.2 Active in cell culture.3,4 Chemical Name: null