Activators & Inhibitors

Activity: Neuroprotective . Function/Pharmacology: P7C3 exerts proneurogenic activity by protecting newborn neurons from apoptosis. Prolonged administration to aged rats impedes neuronal death and preserves cognitive capacity.1 Delays disease progression in G93A-SOD2 mutant mouse model of amyotrophic lateral sclerosis.2 Blocks MPTP-mediated cell death of dopaminergic neurons in the substantia nigra of adult mice, a model of Parkinson disease.3 Restores hippocampal neurogenesis in a mouse model of Down Syndrome.4 The mechanism of action involves activation of nicotinamide phosphoribosyltransferase (NAMPT) with concomitant increase of intracellular levels of NAD.5 Active in vivo. Chemical Name: 1-(3,6-Dibromo-9H-carbazol-9-yl)-3-(phenylamino)propan-2-ol

Activity: Herg channel blocker . Function/Pharmacology: Dofetilide is a clinically useful class III antiarrhythmic that inhibits the rapid component of the delayed rectifier outward potassium current (IKr) via selective blockage of the Kv11.1 (hERG) channel.1,2 Chemical Name: N-[4-(2-{[2-(4-Methanesulfonamidophenoxy)ethyl](methyl)amino}ethyl)phenyl]methanesulfonamide

Activity: Reverses differentiated cells to multipotent stem cells . Function/Pharmacology: Induces differentiated myogenic-lineage-committed cells to become multipotent mesenchymal progenitor cells.1-2 Acts as a selective human A3 adenosine receptor antagonist (Ki = 0.66 µM).3 Cell permeable. Chemical Name: 2-(4-Morpholinoanilino)-6-cyclohexylaminopurine

Activity: Phospholipase substrate . Function/Pharmacology: Chromogenic substrate for phospholipases such as PLA2. Read absorbance at 425 nm. Chemical Name: 4-Nitro-3-(octanoyloxy)benzoic acid

Activity: Voltage-gated sodium channel blocker . Function/Pharmacology: Voltage-gated Na+ channel blocker.1 Protects murine cultured cortical neurons from injury induced by oxygen-glucose deprivation.2 Acts at the ouabain binding site of guinea pig cardiac Na+/K+ ATPase and inhibits the enzyme (IC50 = 34 μM).3 Chemical Name: N-(4-Chlorophenyl)-2-phenyl-N-(1-propan-2-ylpiperidin-4-yl)acetamide hydrochloride

Activity: Cytochrome P450 inhibitor . Function/Pharmacology: Inhibits cytochrome P450-mediated prostaglandin omega hydroxylation. Inhibits steroid 11β-hydroxylase thereby inhibiting cortisol biosynthesis. Chemical Name: 2-Methyl-1,2-dipyridin-3-yl-propan-1-one

Activity: HDAC inhibitor . Function/Pharmacology: Histone deacetylase (HDAC) inhibitor, IC50=13 µM1. More potent and robust than valproic acid at inducing histone hyperacetylation (600% at 50 µM), HSP70 induction and protection against glutamate excitotoxicity in cultured neurons2. Cell permeable. Chemical Name: 2-(2-Propynyl)octanoic acid (racemic)

Activity: Necroptosis inhibitor . Function/Pharmacology: Necrostatin-1 is an inhibitor of necroptosis (non-apoptotic cell death pathway; EC50 = 494 nM).1 It is an ATP-competitive death domain receptor-associated adaptor kinase (RIP1) inhibitor (EC50 = 182 nM).2 It displays a protective effect in a mouse model of ischemic brain injury1, inhibits myocardial cell death and reduces infarct size in various mouse heart models3 and inhibits glutamate-induced oxytosis in HT-22 cells4. Chemical Name: 5-(1H-Indol-3-ylmethyl)-3-methyl-2-thioxo-4-Imidazolidinone

Activity: TRPC channel blocker . Function/Pharmacology: KB-R7943 is a potent and selective inhibitor of the reversed Na+/Ca2+ exchanger (NCE or NCX; IC50’s = 1.2-2.4 µM in cardiomyocytes, smooth muscle cells, NCX1-transfected fibroblasts1; 0.7µM in cultured rat forebrain2). KB-R7943 has also been shown to inhibit the mitochondrial Ca2+ uniporter (MCU) – Ki = 5.5 µM.3 Recently shown to inhibit complex I in the mitochondrial respiratory chain (IC50 = 11.4 µM) and block NMDA receptors (IC50 = 13.4 µM).4 Chemical Name: 2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothioures mesylate