Activators & Inhibitors

Activity: PAF antagonist . Function/Pharmacology: Platelet-activating factor (PAF) receptor antagonist (Ki = 1.3 μM)1. Inhibits neutrophil degranulation and superoxide production in vitro1. Inhibits PAF-induced bronchoconstriction in a guinea pig model2. Displays neuroprotective effects in various models3,4. Protects against focal cerebral ischemia via inhibition of the mitochondrial apoptotic pathway5. Chemical Name: Natural product isolated from Ginko biloba

Activity: Benzodiazepine antagonist . Function/Pharmacology: A benzodiazepine antagonist1, panspecific for 1,, or5-containing GABAA receptors2. Reduces withdrawal sequelae in benzodiazepine dependence.3 Reverses the toxic effects, including coma and respiratory depression of zolpidem intoxication4 and gabapentin-induced coma5. Chemical Name: 8-Fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid, ethyl ester

Activity: Hedgehog signaling inhibitor . Function/Pharmacology: Naturally occurring steroidal alkaloid with teratogenic activity. Blocks sonic hedgehog signaling by binding to smoothened. Antitumor activity. Cell Permeable.

Activity: SIRT1 inhibitor . Function/Pharmacology: Selective SIRT1 inhibitor (IC50=98 nM). Does not inhibit other HDACs or SIRT family members. Increases p53 acetylation following DNA damage. Cell permeable. Chemical Name: 6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-xarboxamide (racemic)

Activity: HSP90 inhibitor . Function/Pharmacology: Inhibits HSP90 by binding to its ATP-binding domain (Kd=1.2 µM) and subsequently inhibits HSP90 client proteins. Induces apoptosis in various cell types. Cell permeable. Chemical Name: 9,13-Dihydroxy-8,14,19-trimethoxy-4,10,12,16-tetramethyl-2-azabicyclo[16.3.1]docosa-4,6,10,18,21-pentaene-3,20,22-trione,9-carbamate

Activity: TRPV1 blocker . Function/Pharmacology: Vanilloid receptor I (TRPV1) antagonist, IC50 = 35 nM for capsaicin-induced and 6 nM for acid-induced TRPV1 activation. Displays analgesic activity in rat models of neuropathic pain. Orally active and cell permeable. Chemical Name: 4-(3-Chloro-2-pyridinyl)-N-[4-(1,1-dimethylethyl)phenyl]-1-piperazinecarboxamide

Activity: PDGFR kinase inhibitor . Function/Pharmacology: Potent inhibitor of PDGF receptor kinase (IC50 = 1 µM), c-kit and FGF kinase. Induces apoptosis in H526, small-cell lung cancer cells. Chemical Name: 6,7-Dimethoxy-3-phenylquinoxaline

Activity: CAR agonist . Function/Pharmacology: TCPOBOP is an activator of the mouse constitutive androstane receptor (mCAR) and human Preganane X receptor.1 Tumor promoter of mouse hepatocarcinogenesis Chemical Name: 1,4-Bis-[2-(3,5-dichloropyridyloxy)]benzene

Activity: Serine protease inhibitor . Function/Pharmacology: Potent and reversible serine protease inhibitor (IC50‘s range from 0.3 – 54.0 μM). Inhibits the demethylase activity of the fat mass and obesity-associated protein (FTO).1 Cell permeable. Intended for cell culture or in vivo laboratory experimentation. This product is not approved for human therapeutic use. Chemical Name: 6-Amidino-2-naphthyl-4-guanidinobenzoate dimesylate