Activators & Inhibitors

Activity: Mre11-Rad50-Nbs1 inhibitor . Function/Pharmacology: Mirin is an inhibitor of the Mre11-Rad50-Nbs1(MRN) complex (IC50 = 12 µM for inhibition of ATM activity), part of the MRN-ATM(ataxia-telangiectasia mutated) pathway, an essential pathway for sensing and signaling from DNA double-strand breaks. Mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells. Chemical Name: 5-(4-Hydroxybenzylidene)-2-imino-1,3-thiazolidin-4-one

Activity: GPR109B agonist . Function/Pharmacology: Highly selective agonist for the human orphan G-protein-coupled receptor GPR109b (EC50 = 400 nM). No activity was reported at the highly homologous high-affinity niacin receptor GPR109a. Chemical Name: 1-(1-Methylethyl)-1H-benzotriazole-5-carboxylic acid

Activity: Intracellular transport inhibitor . Function/Pharmacology: Specific inhibitor of protein translocation from endoplasmic reticulum to Golgi. Induces apoptosis. Activates sphingomyelin metabolism. Cell permeable.

Activity: Nox inhibitor . Function/Pharmacology: NAD(P)H oxidase (Nox) inhibitor. Abolishes PDGF-mediated Nox activation and ROS production (100% at 10 M). Inhibits PMA-induced oxidative burst in HL-60 cells (IC50=2 µM). Enhances TGF-ß-induced apoptosis in liver tumor cells. Chemical Name: 3-Benyl-7-(2-benzoxazolyl)yhio-1,2,3-triazolo(4,5-d)pyrimidine

Activity: BCRP inhibitor . Function/Pharmacology: A potent and selective inhibitor of the breast cancer resistance protein multidrug transporter (BCRP/ABCG2)1. Reverses resistance of MTX and topotecan at 25 nM in human and mouse cell lines.1 Also inhibits ABCB1 and ABCC1 at concentrations >1 μM.2 Restores the sensitivity of triple negative breast cancer cells to photodynamic therapy.3 Prevents the export of the FAAH inhibitor URB937 from the CNS.4 Forces prostate stem cells to undergo and AR-modulated differentiation to an androgen deprivation therapy-sensitive luminal phenotype.5 Active in vivo. Chemical Name: (3S,6S,12aS)-1,2,3,4,6,7,12,12a-Octahydro-9-methoxy-6-(2-methylpropyl)-1,4-dioxopyrazino[1',2':1,6]pyrido [3,4-b]indole-3-propanoic acid 1,1-dimethylethyl ester

Activity: Cholesterol transport inhibitor . Function/Pharmacology: U18666A is an oxidosqualene reductase inhibitor.1 Inhibits the egress of cholesterol from late endosomes and lysosomes.2 Also used to study Niemann-Pick disease and for assessing the importance of molecular trafficking through the lysosomal pathway in other conditions.3 Chemical Name: 3-[2-(Diethylamino)ethoxy]androst-5-en-17-one hydrochloride

Activity: TRPC3 Channel blocker . Function/Pharmacology: Selective antagonist of the TRP cannonical 3 channel (TRPC3)1 which can function as a receptor-operated channel2. A useful tool for dissecting GPCR-downstream signaling mechanisms3. May be effective in reducing cardiac hypertrophy2. Chemical Name: 1-[4-[(2,3,3-Trichloro-1-oxo-2-propen-1-yl)amino]phenyl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid

Activity: VEGFR, PDGFR kinase inhibitor . Function/Pharmacology: A potent inhibitor of multiple receptor tyrosine kinases including VEGFR, PDGFRβ and Kit (Ki = 2-17 nM)1. Also inhibits cFMS (IC50=7 nM)2 and FLT33. Potent inhibitor of angiogenesis4. Clinically useful anticancer agent. Cell permeable. Chemical Name: N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimehyl-1H-pyrrole-3-carboxamide malate

Activity: PDE4 inhibitor . Function/Pharmacology: Selective inhibitor of cAMP-specific phosphodiesterase (PDE4), IC50 = 1 µM. Displays beneficial effects in neurodegenerative diseases. Displays anti-inflammatory activity and synergizes with forskolin. Cell permeable. Chemical Name: 4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone (racemic)