Activators & Inhibitors

Activity: Mitochondrial ATPase inhibitor . Function/Pharmacology: Inhibits mitochondrial F1F0 ATP synthase1. A useful tool for decreasing cellular ATP levels2. Induces autophagy3. Stimulates lysosome acidification4. Protects against ischemic kidney in male rats5. Chemical Name: From Streptomyces sp.

Activity: IκB inhibitor . Function/Pharmacology: Binds to, and directly inhibits IκB kinase, resulting in the inhibition of the release of various mediators and inhibition of MAP kinase activation. Demonstrates anti-inflammatory, antisecretory, and spasmolytic activities in vivo. Chemical Name: null

Activity: Oxidative- and ER-stress inducer . Function/Pharmacology: A mycotoxin found in contaminated fruits. Increases ROS generation and oxidative stress in cells which is mediated by p53.1 Displays cytotoxic effects on a variety of cell lines.2 Causes damage to several organs including liver and kidney in laboratory animals.3 Triggers NRF2-mediated survival mechanisms in kidney cells.4 Induces apoptosis through a ROS-mediated ER stress pathway.5 Chemical Name: 4-Hydroxy-4H-furo[3,2-c]pyran-2(6H)-one

Activity: High conductance Calcium activated potassium channel inhibitor . Function/Pharmacology: Fungal mycotoxin. Selective, irreversible blocker of the smooth muscle high conductance Ca2+-activated K+ (BK, KCa1.1) channel (100% block at 10 nM).1 Displays brain neurotoxicity in rats along with dose-dependent convulsions and death.2 An important tool for studying the role of BK channels in vascular function which is effective in cellular, tissue and in vivo experiments.3 Inhibits BK channels in inside-out and cell-attached patches, whereas iberiotoxin (considered the gold standard BK channel blocker) does not.3 May be used to partially ablate Purkinje cells in immature rat cerebellum providing a model for neural stem cell transplantation studies.4 CAUTION: Potent Toxin. Take proper precautions to prevent ingestion, inhalation and skin contact. Chemical Name: null

Activity: Translation inhibitor . Function/Pharmacology: Puromycin is an aminonucleoside antibiotic derived from Streptomyces alboniger. It is a protein synthesis inhibitor that disrupts peptide transfer on ribosomes causing premature chain termination.1 It is an inhibitor of dipeptidyl-peptidase II and cytosolic alanyl aminopeptidase.2 Puromycin also inhibits protein transport in mitochondria.3 Chemical Name: (S)-3′-[[2-amino-3-(4-methoxyphenyl)-1-oxopropyl]-amino]-3′-deoxy-N,N-dimethyl-adenosine dihydrochloride

Activity: Nephropathy inducer . Function/Pharmacology: The nucleoside moiety of puromycin which does not inhibit protein synthesis or induce apoptosis1. It acts as a glomerular epithelial cell toxin2 and as such is a useful tool for producing animal models of nephropathy3,4, or puromycin aminonucleoside nephrosis (1-2.5 mg/100g rat body weight)5. Active in vivo. Chemical Name: 3’-Amino-3’-deoxy-N6,N6-dimethyladenosine

Activity: HSP90 inhibitor . Function/Pharmacology: Radicicol inhibits heat shock protein 90 (Hsp90) activity by binding to the ATP-binding pocket.1 In cells Hsp90 client proteins such as Raf kinase2, HIF-1α3 and estrogen receptor4 are destabilized and proteolytically degraded. Inhibits expression of COX-2 without affecting COX-1 expression in LPS-stimulated macrophages (IC50=27 nM).5 Inhibits angiogenesis.6 Chemical Name: (1aR,2Z,4E,14R,15aR)-8-Chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-6H-oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione

Activity: TRPV1 agonist . Function/Pharmacology: Ultrapotent TRPV1 agonist (Ki=43 pM).1 Resiniferatoxin is 100-10,000 fold more potent than capsaicin for most responses yet displays a spectrum of activity distinct from capsaicin.2 A potent sensory neuron excitotoxin.3 Induces a long lasting analgesia in a rodent model of burn pain.4 Chemical Name: null

Activity: SERCA inhibitor . Function/Pharmacology: Potent inhibitor of sarco-endoplasmic reticulum Ca2+ -ATPase1. (IC50= 30 nM) Induces endoplasmic reticulum stress and autophagy in a variety of cell lines2. Warning: highly irritant to skin and mucus membranes. Chemical Name: Isolated from Thapsia garganica