Activators & Inhibitors

Activity: Cellular calcium probe . Function/Pharmacology: Cell-permeable acetoxymethyl (AM) ester derivative of Fluo-8. Approximately twice as bright as Fluo-4. Absorbance 452 nm (26,000); Emission 515 nm (after AM hydrolysis; dissolved in 10 mM EGTA, 100 mM KCl, 10 mM MOPS, pH 7.2) Chemical Name: null

Activity: Geldanamycin with ADC linker . Function/Pharmacology: Geldanamycin analog equipped with linker for coupling to proteins or antibodies for the preparation of immunoconjugates, for example. Chemical Name: 17-(3-(4-Maleimidobutylcarboxamido)propropylamino)-demethoxygeldanamycin

Activity: K-ATP channel blocker . Function/Pharmacology: Second generation oral hypoglycemic agent. Acts via ATP-dependent K+ channel (Kir6, KATP) block1. Inhibits Kir6 currents in the pancreas, causing an increase in intracellular Ca2+ and insulin secretion. Also inhibits recombinant CFTR Cl- channels with an IC50 of 20 μM2. Cell permeable. Chemical Name: 5-Chloro-N-[2-[4-[[[(cyclohexylamino)carbonyl]amino]suphonyl]phenyl]ethyl]-2-methoxybenzamide

Activity: p53/mdm2 inhibitor . Function/Pharmacology: Inhibits the p53-MDM2 interation (20 μM).1 Alkylates one catalytic histidine residue (His-397) participating in the charge-relay system of carboxypeptidase Y.2 Has also been shown to inhibit bovine chymotrypsin A-γ. A potent inhibitor of the severe acute respiratory syndrome coronavirus (SARS-CoV) main protease (Mpro), Ki=306 nM.3 Chemical Name: N-Benzyloxycarbonyl-L-phenylalaninylchloromethyl ketone

Activity: ALK inhibitor . Function/Pharmacology: Potent and selective ALK4, 5 and 7 inhibitor1,2. IC50=45, 12 and 7.5 nM respectively. Prevents phosphorylation of Smad2/3 and growth inhibition induced by TGFβ2. Inhibits differentiation of rat induced pluripotent stem cells and increases clonal expansion efficiency3. Together with AMI-5, A83-01 enabled Oct4-induced reprogramming of mouse embryonic fibroblasts4. Cell permeable. Active in vivo. Chemical Name: 3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide

Activity: Wnt/β-cantenin inhibitor . Function/Pharmacology: Suppresses Wnt/β-catenin signaling. It antagonizes PPARγ and PPARδ ligand-dependent activation which is mediated by inhibition of recruitment of the coactivators β-catenin and GRIP1 but not the corepressors NCoR and SMRT1. Inhibits the migration and growth of breast cancer cell lines2 as well as colon, lung and liver cell lines1. Useful tool for probing the involvement of Wnt signaling pathway3,4. Chemical Name: 2,5-Dichloro-N-(2-methyl-4-nitrophenyl)benzenesulfonamide

Activity: PKR inhibitor . Function/Pharmacology: Inhibits RNA-dependent protein kinase (PKR, IC50 = 210 nM)1. Inhibits ER stress-induced neuronal damage2. Reduces brain PKR activation in vivo3. Prevents apoptosis and IL-1β production in an acute excitotoxic and neuroinflammatory rat model4. Prevents β-amyloid peptide-induced inflammation in primary murine mixed co-cultures5. Cell permeable. Chemical Name: 6,8-Dihydro-8-(1H-imidazol-5-ylmethylene)-7H-pyrrolo[2,3-g]benzothiazol-7-one

Activity: LXR agonist . Function/Pharmacology: Cholesterol metabolite. Endogenous agonist for nuclear receptor LXR1. Controls cellular cholesterol homeostasis2. Promotes neural development in zebra fish as well as dopaminergic differentiation of embryonic stem cells3. Cell permeable. Chemical Name: null

Activity: p34/cdc2 inhibitor . Function/Pharmacology: Potent and selective inhibitor of cyclin-dependent kinases displaying higher potency and selectivity compared to olomoucine. p34 cdc2 IC50 = 0.2 µM. Also inhibits p33cdk2 and p33cdk51. Anti-angiogenic2. Prevents PPARγ S273 phosphorylation, promoting browning of white adipose tissue3. Enhances peripheral nerve regrowth4. Chemical Name: (R)-2-((6-(Benzylamino)-9-isopropyl-9H-purin-2-yl)amino)butan-1-ol