Activators & Inhibitors

Activity: DUB PSMD14 inhibitor . Function/Pharmacology: Inhibits the deubiquitinating (DUB) activity of PSMD14 exhibiting potent antitumor activity in neck squamous cell carcinoma in vitro and in vivo1. Inhibits endothelial cell adhesion by perturbing HSP27 interactions with components of the actin and intermediate filament cytoskeleton2. Potently inhibits developmental angiogenesis in zebrafish2. Inhibits adhesion of endothelial cells to vitronectin (IC50=0.83 M) inhibiting tumor cell-induced angiogenesis in vivo3. Cell permeable. Active in vivo. Chemical Name: N-(4,5-Dihydro-4-methyl-5-oxo-1,2-dithiolo[4,3-b]pyrrol-6-yl)acetamide

Activity: Acyl-CoA synthase inhibitor . Function/Pharmacology: Long-chain fatty acyl CoA synthetase inhibitor (IC50=3.6-8.7 μM)1. Inhibits mouse macrophage-derived foam cell formation2 and displays anti-atherosclerotic activity3. Cell permeable. Chemical Name: (3E)-1-Hydroxy-3-((2E,4Z,7E)-undeca-2,4,7-triene-1-ylidene)triaz-1-ene

Activity: HDAC inhibitor . Function/Pharmacology: Trichostatin A (58880-19-6) is a potent and selective histone deacetylase (HDAC) inhibitor (Ki = 3.4 nM). Induces reversion of ras transformed cells to normal morphology. Trichostatin A induces dedifferentiation of primordial germ cells into embryonic germ cells. Cell permeable and active in vivo. Decreased global chromatin condensation increasing gene-editing efficiency 2-4X.4 Part of the CRISPY mix for increasing precise gene editing.5 Chemical Name: (2E,4E,6R)-7-(4-(dimethylamino)phenyl)-N-hydroxy-4,6-dimethyl-7-oxo-2,4-heptadienamide

Activity: ER stress inducer . Function/Pharmacology: Fermentation product from Streptomyces lysosuperificus. Provided as a mixture of tunicamycin A (C14), B (C15), C (C16) and D (C17) homologs varying in the number of carbon atoms in the fatty acid chain. The structure shown above is for tunicamycin B (the C15 homolog) Potent inhibitor of GlcNAc phosphotransferase which thereby inhibits glycoprotein biosynthesis1. Causes endoplasmic reticulum stress-induced autophagy2 and unfolded protein response3. Arrests cell cycle in late G14. Chemical Name: null

Activity: Induces loss of mitochondrial membrane potential . Function/Pharmacology: Valinomycin is a selective K+ ionophore capable of transporting potassium ions through lipid membranes.1 It can induce apoptosis in cells by causing a rapid loss of mitochondrial membrane potential via potassium efflux.2,3 Chemical Name: Cyclo(L-Val-D-HyIva-D-Val-L-Lac-)3

Activity: NFκB and angiogenesis inhibitor . Function/Pharmacology: Displays potent antiangiogenesis activity inhibiting endothelial cell sprouting in vitro (IC50 = 12 nM) and in vivo.1 Potently inhibits NF-κB activation by preventing TNFα-induced activation of IKKβ.2 Covalently binds to the intermediate filament protein, vimentin3 inducing its disassembly and serine 56 phosphorylation4. Inhibits reactive gliosis and blocks TNFα-mediated neuronal apoptosis in in vivo models.5 Chemical Name: (4β, 5β, 6β, 22R)-5,6-Epoxy-4,22,27-trihydroxy-1-oxoergosta-2,24-dien-26-oic acid δ-lactone

Activity: PI3K inhibitor . Function/Pharmacology: Potent and selective inhibitor of PI3-kinase which acts via covalent modification of Lys-8022. Inhibits autophagy in rat hepatocytes3. Inhibits adipocyte differentiation of 3T3-L1 cells4. A useful tool for probing PI3-K-mediated cellular events5. Chemical Name: Fermentation product

Activity: EGFR kinase inhibitor . Function/Pharmacology: Potent and selective inhibitor of the EGFR kinase IC50 = 3 nM. Inhibits proliferation of a variety human cancer cell lines1,2. Reduces pulmonary fibrosis in a rat model3. Cell permeable. Chemical Name: N-(3-Chlorophenyl)-6,7-dimethoxy-4-quinazolinanine, free base

Activity: VEGFR kinase inhibitor . Function/Pharmacology: Potent inhibitor of VEGFR-2, -3, and -1, IC50 = 0.2, 0.1-0.3, and 1.2 nM respectively1 displaying minimal activity against a panel of ~100 protein kinases. Inhibits angiogenesis and vascular permeability.2 Also inhibits BCR-ABL1 (T315I) with high potency, Ki = 149 pM for autophosphorylated ABL1 (T315I).3 Inhibits proliferation of Ba/F3 cells expressing BCR-ABL1 (T315I). Clinically useful anticancer agent.4 Chemical Name: N-Methyl-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide