Activators & Inhibitors

Activity: Mitochondrial division inhibitor . Function/Pharmacology: Selective inhibitor of Dnm1 GTPase (IC50=1-10 μM). Inhibits mitochondrial outer membrane permeabilization. Inhibits mitochondrial division and apoptosis. Cell permeable. Chemical Name: 3-(2,4-Dichloro-5-methoxyphenyl)-2-sulfanyl-4(3H)-quinazolinone

Activity: Hsp70 inhibitor . Function/Pharmacology: Selectively interacts with HSP70 and disrupts its association with co-chaperones and substrate proteins. Inhibits p53 binding to antiapoptotic proteins Bcl-xL and Bcl-2. Recues primary mouse thymocytes from P53-mediated apoptosis induced by radiation. Cell permeable. Chemical Name: 2-Phenylethynesulfonamide

Activity: Cell permeable ceramide . Function/Pharmacology: Cell permeable ceramide analog. Induces apoptosis in a variety of cell types. Stimulates ceramide-activated protein phosphatases. Activates ceramide-activated protein kinases. Chemical Name: N-Acetyl-D-erythro-sphingosine

Activity: Mitochondrial oxidative phosphorylation inhibitor . Function/Pharmacology: An extremely potent uncoupler of mitochondrial oxidative phosphorylation (IC50 = 20 nM).1 Induces apoptosis in a variety of cell lines.2 Inhibits wild type and mutant beta-amyloid production in embryonic kidney 293 cells expressing either wild-type or “Swedish” mutant APP.3 An important tool for inhibiting mitochondrial membrane potential.2,4 Cell permeable. Chemical Name: Carbonyl cyanide 4-(trifluoromethoxy)phenylhydrazone

Activity: Src family kinase inhibitor . Function/Pharmacology: Potent and selective inhibitor of Src family tyrosine kinases. IC50=5 nM (p65lck), IC50=6 nM(P59fynT), IC50=170 nM (p60src). Cell permeable. Chemical Name: 4-amino-1-tert-butyl-3-(4-methylphenyl)pyrazolo[3,4-d]pyrimidine

Activity: MIF antagonist . Function/Pharmacology: Antagonist of macrophage migration inhibitory factor (MIF, a pro-inflammatory cytokine). Displays anti-inflammatory activity. Increases survival in severe sepsis1. Inhibits airway remodeling in mouse asthma model2. Blocks MIF-induced autophagy3. Active in cellular and mouse models. Chemical Name: (S,R)-3-(4-Hydroxyphenyl)-4,5-dihydro-5-isoxazole acetic acid, methyl ester

Activity: Sulfatase inhibitor . Function/Pharmacology: Inhibits steroid sulfatase (IC50=ca. 60 nM). Enhances learning and spatial memory in rats1. Inhibits proliferation of human MCF-7 breast cancer cells2. Chemical Name: (p-O-sulfamoyl)-N-tetradecanoyl tyramine

Activity: VCP inhibitor / Autophagy inhibitor . Function/Pharmacology: Binds to the N-terminal domain of valosin-containing protein (VCP), an essential protein for autophagosome maturation. Xanthohumol inhibits the function of VCP thereby impairing autophagosome maturation and resulting in accumulation of the microtubule-associated protein 1 light chain 3-II (LC3-II)1. Impairs prostate cancer cell growth and proliferation2. Cell permeable. Chemical Name:

Activity: Primes stem cells for differentiation . Function/Pharmacology: Stauprimide dramatically primes embryonic stem cells for differentiation. Its molecular target is NME2, a c-Myc-activating transcription factor. Stauprimide inhibits nuclear localization of NME2 thereby downregulating c-Myc. Chemical Name: N-Benzoyl-7-oxostaurosporine