Activators & Inhibitors

Activity: BCR-ABL inhibitor . Function/Pharmacology: Imatinib is a tyrosine kinase inhibitor specific for abl (IC50 = 0.038 µM)1, PDGF-R (IC50 = 0.3 µM)1 and c-kit (IC50 = 0.1 µM)2. It is a clinically useful anti-cancer drug approved for the treatment of chronic myelogenous leukemia, gastrointestinal stromal tumors as well as several other cancers. Chemical Name: 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide methanesulfonate

Activity: PLC inhibitor . Function/Pharmacology: Inhibits receptor-coupled phospholipase C-dependent processes in platelets and neutrophils via interfering with G protein-PLC interaction1. A useful tool for probing the involvement of PI-PLC in receptor mediated cellular physiology and processes2-4. Cell permeable. Chemical Name: 1-[6-[[(17β)-3-Methoxyestra-1,3,5(10)-trien-17-yl]amino]hexyl]-1H-pyrrole-2,5-dione

Activity: FKBP12 inhibitor . Function/Pharmacology: FKBP12 inhibitor (IC50=4.4 µM) with neuroregenerative properties. Does not inhibit protein synthesis (as does cycloheximide).1 Mimics a helical peptide in target proteins for binding to the immunophillin Mip homolog, BpML1 (Burkholderia pseudomallei Mip-like protein 1).2 Chemical Name: Ethyl 2-(4-(®-2-((1S, 3S, 5S)-3,5-dimethyl-2-oxocyclohexyl)-2-hydroxyethyl)-2,6-dioxopiperidin-1-yl)acetate

Activity: SIRT1 activator . Function/Pharmacology: A structurally novel activator of SIRT1 (EC50=1 µM). Displays selectivity over SIRT2 and 3 (EC50=25 and 50 µM respectively). Cell permeable. Chemical Name: N-Benzyl-3,5-dicarbethoxy-4-phenyl-1,4-dihydropyridine

Activity: Herg channel blocker . Function/Pharmacology: Antagonist at the histamine H1 receptor. Chemical Name: 1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine

Activity: TRPA1 blocker . Function/Pharmacology: Inhibits TRPA1 channel Chemical Name: Theophylline-7-(N-4-isopropylphenyl)acetamide

Activity: NaV1.8 blocker . Function/Pharmacology: Potent, selective inhibitor of the TTX-resistant voltage-gated sodium channel Nav1.8. Nav1.8 is preferentially expressed in sensory neurons, and inhibition attenuates both inflammatory and neuropathic pain in a variety of animal models. IC50's for rat and human Nav1.8 are 140 nM and 8.0 nM respectively. Chemical Name: 5-(4-Chlorophenyl)-N-(3,5-dimethoxyphenyl)furan-2-carboxamide

Activity: HDAC inhibitor . Function/Pharmacology: Potent and selective histone deacetylase inhibitor. Induces apoptosis in a variety of tumor cell lines. Synergizes with kinase inhibitors to kill CNS tumor cells. Cell permeable. Chemical Name: Suberoylanilide-hydroxamic acid

Activity: TRPC channel blocker . Function/Pharmacology: SKF-96365 (130495-35-1) was originally described as a selective blocker of receptor-mediated calcium entry (RMCE), IC50s= 8.5 and 11.7 µM for ADP- and thrombin-stimulated platelets respectively.1 TRPC channels have been shown to mediate RMCE2 and are believed to be the major target of SKF3. In rat vascular smooth muscle Ca entry was reduced by 10 µM SKF which was attributed to TRPC3.4 It has also been shown to inhibit L-type Ca channels.1 More recently it has been demonstrated to be a potent blocker of LVA hCaV3.1 T-type Ca channels, IC50=563 nM (state independent).5 Thus caution should be exercised when using SKF as a sole agent and appropriate controls are recommended. Chemical Name: 1-[2-(4-Methoxyphenyl)-2-[3-(4-methoxyphenyl)propoxy]ethyl]imidazole hydrochloride