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 Damnacanthal - Potent, selective inhibitor of p56lck http://www.tocris.com/dispprod.php?ItemId=83511&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 83511
Product: Damnacanthal (Cat No. 1936)
Category: Kinases > Src Family Kinases
Biological Activity: Potent inhibitor of p56lck tyrosine kinase activity (IC50 = 17 nM for inhibition of autophosphorylation). Displays 7- to 20-fold selectivity over p59fyn and p60src tyrosine kinases, > 40-fold selectivity over c-ErbB2, EGF- and insulin-receptor tyrosine kinases, and > 100-fold selectivity over PKA and PKC. Mobilizes intracellular Ca2+ in dermal fibroblasts and inhibits Ras function. ]]> Kinases New Products 25 Apr 2012 7:47 Psilocin - Non-selective serotonin receptor agonist http://www.tocris.com/dispprod.php?ItemId=325470&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 325470
Product: Psilocin (Cat No. 4412)
Category: 5-HT Receptors > Non-selective 5-HT
Biological Activity: Non-selective serotonin receptor agonist. Active metabolite of psilocybin; hallucinogen. ]]> 5-HT Receptors New Products 18 Apr 2012 7:43 SEN 12333 - α7 nAChR agonist; histamine H3 antagonist http://www.tocris.com/dispprod.php?ItemId=330654&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 330654
Product: SEN 12333 (Cat No. 4441)
Category: Acetylcholine (Nicotinic) Receptors > Nicotinic (a7) Receptors
Biological Activity: α7 nicotinic acetylcholine receptor (nAChR) agonist (EC50 = 1.6 μM, Ki = 260 nM at rat α7 nAChRs). Also displays functional antagonism at histamine H3 receptors (IC50 = 103 nM) and weak agonist activity at human ganglionic α3 nAChRs (IC50 = 8.5 μM). Neuroprotective in a rodent model of quisqualic acid-induced cholinergic degeneration. Brain penetrant and orally bioavailable. ]]> Acetylcholine (Nicotinic) Receptors New Products 2 May 2012 7:38 MRS 2957 triethylammonium salt - Potent and selective P2Y6 agonist http://www.tocris.com/dispprod.php?ItemId=295962&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 295962
Product: MRS 2957 triethylammonium salt (Cat No. 4260)
Category: 7-TM Receptors > Purinergic P2Y Receptors
Biological Activity: Potent P2Y6 agonist (EC50 = 12 nM). Displays 14- and 66-fold selectivity against P2Y2 and P2Y4 receptors respectively. ]]> 7-TM Receptors New Products 9 May 2012 7:25 JMV 390-1 - Inhibits multiple neurotensin and neuromedin N degrading enzymes http://www.tocris.com/dispprod.php?ItemId=164496&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 164496
Product: JMV 390-1 (Cat No. 2575)
Category: Proteases > Other Proteases
Biological Activity: Inhibitor of the major neurotensin and neuromedin N degrading enzymes (IC50 values are 31, 40, 52 and 58 for endopeptidase 24.15, endopeptidase 24.11, leucine aminopeptidase and endopeptidase 24.16 respectively). Exhibits analgesic effects in various nociception assays. ]]> Proteases New Products 9 May 2012 7:25 MMF - Activator of Nrf2 pathway; primary metabolite of DMF http://www.tocris.com/dispprod.php?ItemId=343196&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 343196
Product: MMF (Cat No. 4511)
Category: Other Pharmacology > Antioxidants
Biological Activity: Nuclear factor (erythroid-derived-2)-like 2 (Nrf2) pathway activator. Also exhibits agonist activity at GPR109A. Primary metabolite of DMF (Cat. No. 4512). ]]> Other Pharmacology New Products 9 May 2012 7:25 DMF - Nrf2 pathway activator; neuroprotective http://www.tocris.com/dispprod.php?ItemId=343197&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 343197
Product: DMF (Cat No. 4512)
Category: Other Pharmacology > Antioxidants
Biological Activity: Nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator; induces upregulation of antioxidant gene expression. Displays cytoprotective effects in human spinal cord astrocytes, oligodendrocyte precursor cells and hippocampal neurons following hydrogen peroxide challenge. Exerts neuroprotective effects in vivo in experimental autoimmune encephalomyelitis. Primary metabolite (MMF, Cat. No. 4511) available. ]]> Other Pharmacology New Products 9 May 2012 7:25 IOX 2 - Potent, selective HIF1α prolyl hydroxylase-2 (PHD2) inhibitor http://www.tocris.com/dispprod.php?ItemId=331885&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 331885
Product: IOX 2 (Cat No. 4451)
Category: Enzymes > Hydroxylases
Biological Activity: Potent inhibitor of hypoxia inducible factor 1α (HIF1α) prolyl hydroxylase-2 (PHD2). Displays over 100-fold selectivity for PHD2 over factor inhibiting HIF-1 (FIH-1) and histone demethylases KDM4A, KDM4C, KDM4E and KDM6B. Cell permeable. ]]> Enzymes New Products 16 May 2012 7:32 ML 130 - Inhibits NOD1-induced NF-κB activation http://www.tocris.com/dispprod.php?ItemId=320092&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 320092
Product: ML 130 (Cat No. 4354)
Category: Cytokine and NF-kB Signaling > NF-kB/IkB
Biological Activity: Potent and selective inhibitor of NOD1; displays 36-fold selectivity for NOD1 over NOD2 (IC50 values are 0.56 and >20 μM for NOD1 and NOD2 respectively). Inhibits NOD1-induced NF-κB activation in HEK293 cells with no cytotoxicity. Shown to alter subcellular targeting of NOD1; also thought to alter the conformation of NOD1 protein in vitro. ]]> Cytokine and NF-kB Signaling New Products 16 May 2012 7:32 Cytarabine - Nucleoside analog; inhibits DNA replication http://www.tocris.com/dispprod.php?ItemId=344239&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 344239
Product: Cytarabine (Cat No. 4520)
Category: Cell Metabolism > DNA, RNA and Protein Synthesis
Biological Activity: Nucleoside analog of deoxycytidine; inhibits DNA replication by incorporating into DNA (IC50 = 0.04 μM in L1210 and CEM cell lines). Displays no inhibitory effects on RNA synthesis. Causes S phase cell cycle arrest in ML-1 cell lines; cytotoxic in L5817Y leukemia cells. Antineoplastic and antileukemic agent. ]]> Cell Metabolism New Products 16 May 2012 7:32 Flufenamic acid - Cyclooxygenase inhibitor; NSAID. Also activates TRPC6 http://www.tocris.com/dispprod.php?ItemId=344598&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 344598
Product: Flufenamic acid (Cat No. 4522)
Category: Oxygenases/Oxidases > Cyclooxygenase
Biological Activity: Nonsteroidal anti-inflammatory drug (NSAID). Also increases currents through TRPC6 channels and inhibits currents through TRPC3 and TRPC7 channels. ]]> Oxygenases/Oxidases New Products 16 May 2012 7:32 4μ8C - Inhibits IRE1 endoribonuclease activity http://www.tocris.com/dispprod.php?ItemId=336106&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 336106
Product: 4μ8C (Cat No. 4479)
Category: Esterases > Endonucleases
Biological Activity: Selective inhibitor of IRE1 ribonuclease (RNase) activity (IC50 = 60 nM). Blocks substrate access to the active site of IRE1. Inactivates IRE1-mediated mRNA degradation. Displays no effect on the IRE1-related endoribonuclease RNase L. ]]> Esterases New Products 16 May 2012 7:32 PHP 501 trifluoroacetate - Potent GABAA antagonist http://www.tocris.com/dispprod.php?ItemId=334710&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 334710
Product: PHP 501 trifluoroacetate (Cat No. 4466)
Category: GABAA and GABAC Receptors > GABAA Receptors
Biological Activity: Potent GABAA antagonist (Ki = 0.0028 μM at rat GABAA receptors; IC50 = 0.024 μM at human α1β2γ2 GABAA-expressing tsA201 cells). Displays no inhibitory activity at hGAT-1, hGAT-2, hGAT-3 or hBGT-1 GABA transporters. ]]> GABAA and GABAC Receptors New Products 18 Apr 2012 7:43 MK 0343 - Subtype-selective GABAA receptor partial agonist http://www.tocris.com/dispprod.php?ItemId=325566&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 325566
Product: MK 0343 (Cat No. 4415)
Category: GABAA and GABAC Receptors > GABAA Receptors
Biological Activity: Subtype-selective GABAA partial agonist (Ki values are 0.21, 0.22, 0.23 and 0.40 for α3, α1, α5 and α2 respectively); occupies the benzodiazepine site of GABAA receptors. Displays greater agonist efficacy at α3 compared to α1. Exhibits anxiolytic and non-sedating properties in rodent models. Brain penetrant. ]]> GABAA and GABAC Receptors New Products 18 Apr 2012 7:43 VU 0357121 - Positive allosteric modulator of mGlu5 http://www.tocris.com/dispprod.php?ItemId=330281&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 330281
Product: VU 0357121 (Cat No. 4437)
Category: Glutamate (Metabotropic) Receptors > Glutamate (Metabotropic) Group I Receptors
Biological Activity: Positive allosteric modulator of mGlu5 receptors (EC50 = 33 nM). Binds to a site distinct from that bound by MPEP (Cat. No. 1212). ]]> Glutamate (Metabotropic) Receptors New Products 18 Apr 2012 7:43 TC-N 1752 - Selective NaV1.7 blocker http://www.tocris.com/dispprod.php?ItemId=330224&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 330224
Product: TC-N 1752 (Cat No. 4435)
Category: Sodium Channels > Voltage-gated Sodium Channels
Biological Activity: Selective blocker of human NaV1.7 channels (IC50 values are 0.17, 0.3, 0.4 and 1.1 μM at hNaV1.7, hNaV1.3, hNaV1.4 and hNaV1.5 respectively). Also inhibits tetrodotoxin-sensitive sodium channels. Displays analgesic efficacy in the formalin pain model. ]]> Sodium Channels New Products 18 Apr 2012 7:43 SBHA - Histone deacetylase inhibitor http://www.tocris.com/dispprod.php?ItemId=246276&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 246276
Product: SBHA (Cat No. 3810)
Category: Deacetylases > Histone Deacetylase
Biological Activity: Histone deacetylase (HDAC) inhibitor (ID50 values are 0.25 and 0.3 μM for HDAC1 and HDAC3 respectively). Potentiates the cytostatic effects of 5-Fluorouracil (Cat. No. 3257) in colorectal cancer cells. ]]> Deacetylases New Products 18 Apr 2012 7:43 UA 62784 - Inhibits microtubule polymerization http://www.tocris.com/dispprod.php?ItemId=299577&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 299577
Product: UA 62784 (Cat No. 4286)
Category: Cytoskeleton and Motor Proteins > Microtubules
Biological Activity: Inhibitor of microtubule polymerization in vitro. Interacts with tubulin dimers and promotes the accumulation of mammalian cells in apoptosis. Potentiates antiproliferative effects of vinblastine (Cat. No. 1256) in H2B-GFP HeLa cells. Originally thought to inhibit CENP-E ATPase activity. ]]> Cytoskeleton and Motor Proteins New Products 18 Apr 2012 7:43 Psora 4 - Potent KV1.3 channel blocker http://www.tocris.com/dispprod.php?ItemId=321452&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 321452
Product: Psora 4 (Cat No. 4367)
Category: Potassium Channels > Voltage-Gated Potassium Channels
Biological Activity: Potent KV1.3 channel blocker (EC50 = 3 nM). Preferentially binds the C-type inactivated state of the channel, similar to the activity of CP 339818 (Cat. No. 1399). Displays 17- to 70-fold selectivity over closely-related KV1 channels (KV1, KV2, KV4 and KV7); exhibits activity at KV1.5 (IC50 = 7.7 nM). Suppresses proliferation of human and rat myelin-specific effector memory T cells (EC50 values are 25 and 60 nM respectively). ]]> Potassium Channels New Products 2 May 2012 7:38 Fatostatin A - Cell permeable inhibitor of SREBP activation http://www.tocris.com/dispprod.php?ItemId=330668&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 330668
Product: Fatostatin A (Cat No. 4444)
Category: Cell Metabolism > Lipid Metabolism
Biological Activity: Inhibitor of sterol regulatory element binding protein (SREBP); impairs the activation of SREBP-1 and SREBP-2. Exhibits antiproliferative effects in DU 145 cells independently of IGF-1 signaling (IC50 = 0.1 μM); reverses hyperglycemia in diabetic (ob/ob) mice. Cell permeable. ]]> Cell Metabolism New Products 25 Apr 2012 7:47 Flurizan - γ-secretase inhibitor; lowers Aβ42 levels in vitro http://www.tocris.com/dispprod.php?ItemId=340201&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 340201
Product: Flurizan (Cat No. 4495)
Category: Proteases > Secretase
Biological Activity: Nonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity. Selectively lowers Aβ42 levels in human neuroglioma cells; displays no effect on Aβ40 levels at a concentration of 100 μM. ]]> Proteases New Products 25 Apr 2012 7:47 TC-SP 14 - Potent S1P1 receptor agonist http://www.tocris.com/dispprod.php?ItemId=320459&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 320459
Product: TC-SP 14 (Cat No. 4363)
Category: 7-TM Receptors > Sphingosine-1-phosphate Receptors
Biological Activity: Potent and selective S1P1 agonist (EC50 values are 0.042 and 3.47 μM for human S1P1 and S1P3 respectively). Attenuates immune response to antigen challenge and reduces circulating blood lymphocyte counts in a rodent model of delayed-type hypersensitivity. Orally bioavailable. ]]> 7-TM Receptors New Products 2 May 2012 7:38 Y 11 - Potent and selective FAK inhibitor http://www.tocris.com/dispprod.php?ItemId=340336&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 340336
Product: Y 11 (Cat No. 4498)
Category: Kinases > Focal Adhesion Kinase
Biological Activity: Potent inhibitor of focal adhesion kinase (FAK); prevents FAK autophosphorylation at the Y397 site (IC50 ~ 50 nM in an in vitro kinase assay). Displays selectivity for FAK over a panel of other kinases (concentration used in assay = 1 μM). Decreases cell viability in a number of cancer cell lines; blocks colony formation in SW620 and BT474 cell lines. ]]> Kinases New Products 2 May 2012 7:38 Ribavirin - Antiviral guanosine analog; blocks eIF4E activity http://www.tocris.com/dispprod.php?ItemId=341010&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 341010
Product: Ribavirin (Cat No. 4501)
Category: Cell Metabolism > DNA, RNA and Protein Synthesis
Biological Activity: Antiviral guanosine ribonucleoside analog; misincorporated into mRNA by viral-dependent RNA polymerases. Binds to and redistributes mammalian eIF4E from the nucleus to the cytoplasm (Ki ~ 0.3 μM for the active metabolite, ribavirin triphosphate). Represses colony formation of primary AML-M5 progenitor cells (IC50 ~ 1 μM); reduces disease severity in acute myeloid leukemia (AML). Orally available. ]]> Cell Metabolism New Products 2 May 2012 7:38 A 804598 - Potent and selective P2X7 antagonist http://www.tocris.com/dispprod.php?ItemId=335507&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 335507
Product: A 804598 (Cat No. 4473)
Category: Ligand-gated Ion Channels > P2X Receptors
Biological Activity: Potent, competitive P2X7 receptor antagonist (IC50 values are 8.9 nM, 9.9 nM and 10.9 nM for mouse, rat and human P2X7 receptors respectively). Selective for P2X7 receptors (IC50 > 5-10 μM for a wide array of cell surface receptors and ion channels assayed). Binds with high affinity (Ki app = 2.4 nM for rat P2X7 receptors). ]]> Ligand-gated Ion Channels New Products 2 May 2012 7:38 TC-F 2 - Potent, reversible and selective FAAH inhibitor http://www.tocris.com/dispprod.php?ItemId=320093&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 320093
Product: TC-F 2 (Cat No. 4355)
Category: Hydrolases > Fatty Acid Amide Hydrolase (FAAH)
Biological Activity: Potent, reversible inhibitor of fatty acid amide hydrolase (FAAH) (IC50 values are 28 and 100 nM for human and rat FAAH respectively). Noncovalent inhibitor; displays selectivity for FAAH over cannabinoid-related targets (IC50 > 20 μM for CB1, CB2 and TRPV1). Active in vivo. ]]> Hydrolases New Products 2 May 2012 7:38 NDT 9513727 - Potent, selective human C5a receptor antagonist http://www.tocris.com/dispprod.php?ItemId=220443&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 220443
Product: NDT 9513727 (Cat No. 3333)
Category: Signal Transduction > Complement
Biological Activity: Potent C5a receptor (C5aR) competitive antagonist (IC50 = 11.6 nM); selective for human C5aR (IC50 for rat and mouse C5aR > 10 μM). Exhibits inverse agonist pharmacokinetics. Blocks degranulation response in C5a-stimulated U937 cells (IC50 = 7.1 nM). Orally bioavailable. ]]> Signal Transduction New Products 2 May 2012 7:38 DIM - Induces apoptosis; inhibits EGFR activation http://www.tocris.com/dispprod.php?ItemId=341022&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 341022
Product: DIM (Cat No. 4502)
Category: Cell Cycle > Cell Cycle Inhibitors
Biological Activity: Activator of Chk2 that causes G2/M cell cycle arrest in various cancer cell lines. Antiproliferative and inducer of apoptosis; promotes proteasomal degradation of Cdc25C and Cdk1. Inhibits phosphorylation of EGFR and downstream activation of ERK. ]]> Cell Cycle New Products 2 May 2012 7:38 RuBi-Nicotine - Caged nicotine; rapidly excitable by visible light http://www.tocris.com/dispprod.php?ItemId=248665&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 248665
Product: RuBi-Nicotine (Cat No. 3855)
Category: Acetylcholine (Nicotinic) Receptors > Nicotinic Receptors (Non-Selective)
Biological Activity: Ruthenium-bisbipyridine-caged nicotine, excitable by irradiation with visible light. Undergoes rapid photolysis to release nicotine (< 20 ns); exhibits a high quantum yield. Induces action potential propagation in Retzius neurons of leech ganglia with no detectable toxicity at a concentration of 1 mM. ]]> Acetylcholine (Nicotinic) Receptors New Products 2 May 2012 7:38