Tocris Bioscience - High Performance Life Science Reagents The latest New Products, News and Events from Tocris Bioscience http://www.tocris.com http://www.tocris.com/img/tocris_logo_200.gif Tocris Bioscience | High Performance Life Science Reagents http://www.tocris.com Tocris Bioscience is a leading supplier of innovative, high performance life science research reagents 200 48 DBeQ - Selective and reversible p97 inhibitor http://www.tocris.com/dispprod.php?ItemId=325923&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 325923
Product: DBeQ (Cat No. 4417)
Category: Signal Transduction > Translocation, Exocytosis & Endocytosis
Biological Activity: Selective and reversible inhibitor of p97 ATPase (IC50 = 1.5 μM). Induces executioner caspases (caspase-3 and caspase-7) rapidly. Blocks the degradation of endoplasmic reticulum-associated degradation (ERAD) reporters; also blocks autophagosome maturation and promotes accumulation of LC3-II. ]]> Signal Transduction New Products 10 Jan 2012 19:09 LB 42708 - Selective farnesyltransferase (FTase) inhibitor http://www.tocris.com/dispprod.php?ItemId=300692&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 300692
Product: LB 42708 (Cat No. 4294)
Category: Transferases > Other Transferases
Biological Activity: Selective inhibitor of farnesyltransferase (FTase). Blocks farnesylation of H-Ras, N-Ras and K-Ras4B (IC50 values are 0.8, 1.2 and 2.0 nM respectively). Displays >50,000-fold selectivity for FTase over geranylgeranyltransferase (GGTase) I. Inhibits VEGF-induced Ras activation; suppresses angiogenesis in vivo and in vitro (IC50 = 75 nM). Orally active. ]]> Transferases New Products 10 Jan 2012 19:09 Talopram hydrochloride - Potent, selective inhibitor of noradrenalin transporters http://www.tocris.com/dispprod.php?ItemId=210200&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 210200
Product: Talopram hydrochloride (Cat No. 3145)
Category: Neurotransmitter Transporters > Adrenergic Transporters
Biological Activity: Potent, selective inhibitor of the noradrenalin transporter (NET) (IC50 = 2.9 nM). Exhibits selectivity for NET against SERT (5-HT transporters) and DAT (dopamine transporters). Displays a similar structure but different pharmacological profile to citalopram (Cat. No. 1427). ]]> Neurotransmitter Transporters New Products 17 Jan 2012 22:45 SB 277011A dihydrochloride - Selective D3 antagonist http://www.tocris.com/dispprod.php?ItemId=288970&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 288970
Product: SB 277011A dihydrochloride (Cat No. 4207)
Category: Dopamine Receptors > D3 Receptors
Biological Activity: Selective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively). Brain penetrant. ]]> Dopamine Receptors New Products 10 Jan 2012 19:09 26RFa - Ligand of GPR103; orexigenic neuropeptide http://www.tocris.com/dispprod.php?ItemId=324542&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 324542
Product: 26RFa (Cat No. 4402)
Category: 7-TM Receptors > Orphan 7-TM Receptors
Biological Activity: Hypothalamic RFamide-related neuropeptide. Acts as a natural ligand of the orphan receptor GPR103. Exhibits orexigenic acitivity in mice upon central administration. ]]> 7-TM Receptors New Products 17 Jan 2012 22:45 VU 0360223 - Potent mGlu5 antagonist http://www.tocris.com/dispprod.php?ItemId=324027&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 324027
Product: VU 0360223 (Cat No. 4394)
Category: Glutamate (Metabotropic) Receptors > Glutamate (Metabotropic) Group I Receptors
Biological Activity: Potent antagonist of mGlu5 (IC50 = 61 nM). ]]> Glutamate (Metabotropic) Receptors New Products 17 Jan 2012 22:45 Pyroxamide - Histone deacetylase inhibitor http://www.tocris.com/dispprod.php?ItemId=324545&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 324545
Product: Pyroxamide (Cat No. 4403)
Category: Deacetylases > Histone Deacetylase
Biological Activity: Inhibitor of histone deacetylase (HDAC); potently inhibits affinity purified HDAC1. Also inhibits the growth of tumor cells in vitro and in vivo. Induces p21/WAF1 expression in tumor cells. ]]> Deacetylases New Products 17 Jan 2012 22:45 Rivastigmine tartrate - Dual AChE and BChE inhibitor http://www.tocris.com/dispprod.php?ItemId=330410&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 330410
Product: Rivastigmine tartrate (Cat No. 4440)
Category: Esterases > Cholinesterases
Biological Activity: Dual cholinesterase inhibitor (ChEI); inhibits both butyrylcholinesterase (BChE) and acetylcholinesterase (AChE). Brain penetrant. ]]> Esterases New Products 24 Jan 2012 17:53 TC-DAPK 6 - Potent and selective inhibitor of DAPK1 http://www.tocris.com/dispprod.php?ItemId=300876&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 300876
Product: TC-DAPK 6 (Cat No. 4301)
Category: Kinases > Other Kinases
Biological Activity: Potent and selective, ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) (IC50 values are 69 and 225 nM for DAPK1 and DAPK3 respectively, when assayed with 10 μM ATP). Displays selectivity for DAPK1 over a range of 48 other kinases, including Abl, AMPK, Chk1, Met and Src (IC50 > 10 μM). ]]> Kinases New Products 24 Jan 2012 17:45 Wiskostatin - N-WASP inhibitor; inhibits Arp2/3 activation http://www.tocris.com/dispprod.php?ItemId=330223&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 330223
Product: Wiskostatin (Cat No. 4434)
Category: Cytoskeleton and Motor Proteins > Actin
Biological Activity: Inhibitor of neural Wiskott-Aldrich syndrome protein (N-WASP) activity. Interacts with the regulatory GTPase-binding domain of N-WASP; inhibits activation of Arp2/3 complex by maintaining N-WASP in an inactive conformation. Also inhibits PIP2-induced actin polymerization (EC50 ~ 4μM). ]]> Cytoskeleton and Motor Proteins New Products 31 Jan 2012 16:57 Diclofenac sodium salt - Cyclooxygenase inhibitor; NSAID http://www.tocris.com/dispprod.php?ItemId=332562&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 332562
Product: Diclofenac sodium salt (Cat No. 4454)
Category: Oxygenases/Oxidases > Cyclooxygenase
Biological Activity: Nonsteroidal, anti-inflammatory drug (NSAID); inhibits COX-1 and COX-2 (IC50 values are 0.075 μM for COX-1 and 0.038 μM for COX-2 in human whole blood assay). ]]> Oxygenases/Oxidases New Products 31 Jan 2012 16:57 Amitriptyline hydrochloride - 5-HT and noradrenalin re-uptake inhibitor http://www.tocris.com/dispprod.php?ItemId=332568&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 332568
Product: Amitriptyline hydrochloride (Cat No. 4456)
Category: Neurotransmitter Transporters > 5-HT Transporters
Biological Activity: Inhibitor of serotonin and noradrenalin uptake; also activates α2A-adrenoceptors and antagonizes 5-HT2 receptors. Displays antinociceptive activity. Tricyclic antidepressant (TCA). ]]> Neurotransmitter Transporters New Products 31 Jan 2012 16:57