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 GGTI 297 - Geranylgeranyltransferase I (GGTase I) inhibitor http://www.tocris.com/dispprod.php?ItemId=5281&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 5281
Product: GGTI 297 (Cat No. 2774)
Category: Transferases > Other Transferases
Biological Activity: Geranylgeranyltransferase I (GGTase-I) inhibitor (IC50 values are 135 and 418 nM for GGTase-I and FTase inhibition respectively). Inhibits RhoA prenylation leading to inactivation of RhoA/ROCK and a decrease in basal tone of the internal anal sphincter in vitro. ]]> Transferases New Products 14 May 2013 19:37 EIPA - Inhibits TRPP3-mediated currents; also inhibits the Na+/H+ exchanger (NHE) http://www.tocris.com/dispprod.php?ItemId=220896&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 220896
Product: EIPA (Cat No. 3378)
Category: Transient Receptor Potential Channels > TRPP
Biological Activity: TRPP3 channel inhibitor (IC50 = 10.5 μM). Inhibits the Na+/H+ exchanger (NHE). Derivative of amiloride (Cat. No. 0890). ]]> Transient Receptor Potential Channels New Products 30 Apr 2013 14:25 CMPDA - Positive allosteric modulator of GluA2 receptors http://www.tocris.com/dispprod.php?ItemId=321685&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 321685
Product: CMPDA (Cat No. 4373)
Category: Glutamate (Ionotropic) Receptors > AMPA Receptors
Biological Activity: Positive allosteric modulator of GluR2 receptors (EC50 = 45.4 and 63.4 nM at GluR2i and GluR2o respectively, in a calcium influx screening assay). Binds at the modulator binding pocket located at the interdimer interface and the clamshell hinges. ]]> Glutamate (Ionotropic) Receptors New Products 30 Apr 2013 14:25 Cardionogen 1 - Inhibitor of Wnt/β-catenin signaling http://www.tocris.com/dispprod.php?ItemId=335509&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 335509
Product: Cardionogen 1 (Cat No. 4475)
Category: Wnt Signaling > Beta-catenin
Biological Activity: Wnt signaling modulator. Potently inhibits Wnt/β-catenin-dependent transcription in murine ES cells (EC50 = 23 nM) and zebrafish embryos. Enlarges heart size via cardiomyocyte hyperplasia; induces ES cell cardiac differentiation. ]]> Wnt Signaling New Products 21 May 2013 18:46 DBZ - γ-secretease inhibitor; inhibits Notch pathway http://www.tocris.com/dispprod.php?ItemId=339327&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 339327
Product: DBZ (Cat No. 4489)
Category: Proteases > Gamma-Secretase
Biological Activity: Inhibitor of γ-secretase. Blocks Notch cleavage (IC50< 2 nM) in a cell-based assay; inhibits the Notch pathway. ]]> Proteases New Products 30 Apr 2013 14:25 CYM 50308 - Potent and selective S1P4 agonist http://www.tocris.com/dispprod.php?ItemId=358994&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 358994
Product: CYM 50308 (Cat No. 4678)
Category: 7-TM Receptors > Sphingosine-1-phosphate Receptors
Biological Activity: Potent and selective sphingosine-1-phosphate receptor 4 (S1P4) agonist (EC50 values are 56 nM and 2100 nM for S1P4 and S1P5 receptors, respectively). Displays no activity at S1P1, S1P2 and S1P3 receptors at concentrations up to 25 μM. ]]> 7-TM Receptors New Products 14 May 2013 19:37 PPY A - Potent inhibitor of Abl T315l mutant and wild-type Abl kinases http://www.tocris.com/dispprod.php?ItemId=363341&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 363341
Product: PPY A (Cat No. 4730)
Category: Kinases > Abl Kinase
Biological Activity: Potent inhibitor of T315l mutant and wild-type Abl kinases (IC50 values are 9 and 20 nM, respectively). Inhibits growth of cells transformed with either the Bcr-Abl T315l mutant or wild-type Bcr-Abl gene. ]]> Kinases New Products 21 May 2013 18:46 GS 6201 - Selective A2B antagonist http://www.tocris.com/dispprod.php?ItemId=364301&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 364301
Product: GS 6201 (Cat No. 4727)
Category: Adenosine Receptors > Adenosine A2B Receptors
Biological Activity: Selective antagonist of adenosine A2B receptors (Ki values are 22, 1070, 1940 and 3280 nM for human A2B, A3, A1 and A2A receptors respectively). Attenuates allergen-, NECA- and AMP-induced airway reactivity in an allergic mouse model of asthma. Also shown to attenuate the inflammatory response during acute myocardial infarction in mice; reduces caspase-1 activity in the heart. ]]> Adenosine Receptors New Products 7 May 2013 19:28 MIM1 - Mcl-1 inhibitor; proapoptotic http://www.tocris.com/dispprod.php?ItemId=369083&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 369083
Product: MIM1 (Cat No. 4762)
Category: Apoptosis > Bcl-2 Family
Biological Activity: Inhibitor of Mcl-1; selectively targets the BH3-binding pocket. Induces caspase-3/7 activation and cell death in Mcl-1-dependent leukemia cells. Also blocks Mcl-1-mediated suppression of tBID-induced Bax activation in vitro. ]]> Apoptosis New Products 30 Apr 2013 14:25 VUF 10460 - Selective H4 agonist http://www.tocris.com/dispprod.php?ItemId=369499&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 369499
Product: VUF 10460 (Cat No. 4769)
Category: Histamine Receptors > Histamine H4 Receptors
Biological Activity: Selective histamine H4 receptor agonist; displays 50-fold selectivity for the rat H4 receptor over the H3 subtype (pKi values are 5.75 and 7.46 for rat H3 and H4 receptors respectively). Also exhibits affinity for the human H4 receptor (pKi = 8.22). ]]> Histamine Receptors New Products 7 May 2013 19:28 BMS 536924 - Dual IR/IGF1R inhibitor http://www.tocris.com/dispprod.php?ItemId=369583&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 369583
Product: BMS 536924 (Cat No. 4774)
Category: Receptor Tyrosine Kinases (RTKs) > Insulin and insulin-like
Biological Activity: Dual inhibitor of the insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) (IC50 values are 73 and 100 nM respectively). Inhibits receptor autophosphorylation and downstream MEK1/2 and Akt signaling. Induces G1 arrest and apoptosis in ML-1 cells; also inhibits cell proliferation in multiple tumor types. ]]> Receptor Tyrosine Kinases (RTKs) New Products 7 May 2013 19:28 ADWX 1 - Potent and selective KV1.3 channel blocker http://www.tocris.com/dispprod.php?ItemId=372042&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 372042
Product: ADWX 1 (Cat No. 4812)
Category: Potassium Channels > Voltage-Gated Potassium Channels
Biological Activity: Potent and selective KV1.3 channel blocker (IC50 values are 0.0019 and 0.65 nM for KV1.3 and KV1.1, respectively). Inhibits CD4+ CCR7- T cell activation. Ameliorates rat experimental autoimmune encephalomyelitis, in a model for multiple sclerosis. ]]> Potassium Channels New Products 30 Apr 2013 14:25 Paprotrain - Reversible inhibitor of MKLP-2 http://www.tocris.com/dispprod.php?ItemId=372043&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 372043
Product: Paprotrain (Cat No. 4813)
Category: ATPase > Kinesin
Biological Activity: Reversible, non-ATP competitive inhibitor of mitotic kinesin-like protein 2 (MKLP-2) (Ki = 3.4 μM). Inhibits the basal ATPase activity of MKLP-2 (IC50 = 1.35 μM). Exhibits selectivity for MKLP-2 over 12 other members of the kinesin superfamily, including the closely-related MKLP-1. Cell permeable. ]]> ATPase New Products 30 Apr 2013 14:25 PluriSln 1 - Inhibitor of SCD1; selectively eliminates undifferentiated hPSCs from culture http://www.tocris.com/dispprod.php?ItemId=373429&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 373429
Product: PluriSln 1 (Cat No. 4847)
Category: Stem Cells > Stem Cell Differentiation
Biological Activity: Stearoyl-CoA desaturase 1 (SCD1) inhibitor. Used to selectively eliminate undifferentiated human pluripotent stem cells (hPSCs) from culture; induces ER stress, attenuates protein synthesis and induces apoptosis in hPSCs. Prevents teratoma formation in immunocompromised mice. ]]> Stem Cells New Products 30 Apr 2013 14:25 3-Nitropropionic acid - Irreversible mitochondrial respiratory complex II inhibitor http://www.tocris.com/dispprod.php?ItemId=373566&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 373566
Product: 3-Nitropropionic acid (Cat No. 4849)
Category: Cell Metabolism > Oxidative Phosphorylation
Biological Activity: Irreversible mitochondrial respiratory complex II inhibitor; also inhibits succinate dehydrogenase. Induces autophagy in SH-SY5Y cells. Recapitulates Huntington's disease-like pathology and symptoms in primate and rodent models. ]]> Cell Metabolism New Products 21 May 2013 18:46 WIKI4 - Tankyrase inhibitor; inhibits Wnt signaling http://www.tocris.com/dispprod.php?ItemId=374316&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 374316
Product: WIKI4 (Cat No. 4855)
Category: Polymerases > Poly(ADP-ribose) Polymerase
Biological Activity: Inhibitor of Wnt/β-catenin signaling (EC50 ~ 75 nM). Inhibits auto-ADP-ribosylation of tankyrase 2 (TNKS2) (IC50 ~15 nM); prevents the ubiquitination and degradation of axin. ]]> Polymerases New Products 30 Apr 2013 14:25 NS 6180 - Potent KCa3.1 channel blocker http://www.tocris.com/dispprod.php?ItemId=374917&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 374917
Product: NS 6180 (Cat No. 4864)
Category: Potassium Channels > Ca2+-Activated Potassium Channels
Biological Activity: Potent KCa3.1 channel blocker (IC50 values are 9, 14 and 15 nM for rat, human and mouse erythrocyte KCa3.1 channels respectively). Exhibits ~ 50% inhibition of KCa1.1, KV1.3, and KV11.1 channels, norepinephrine and dopamine transporters, L-type Ca2+ channels and melatonin receptors at a concentration of 10 μM. Potently inhibits IL-2 and IFN-γ production in rat lymphocytes (IC50 ~ 50 nM); reduces DBNS-induced experimental colitis in rats. ]]> Potassium Channels New Products 7 May 2013 19:28 Eact - Activator of Ca2+-activated Cl- channel transmembrane protein 16A (TMEM16A) http://www.tocris.com/dispprod.php?ItemId=375287&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 375287
Product: Eact (Cat No. 4876)
Category: Ion Channels > Chloride Channels
Biological Activity: TMEM16A (ANO1) calcium-activated chloride channel (CaCC) activator (EC50 = 3 μM). Ca2+-independent. Displays no effect on CFTR Cl- or ENaC Na+ conductance. Stimulates submucosal gland secretion in human bronchi. ]]> Ion Channels New Products 14 May 2013 19:37 CaCCinh-A01 - Calcium-activated chloride channel (CaCC) inhibitor http://www.tocris.com/dispprod.php?ItemId=375414&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 375414
Product: CaCCinh-A01 (Cat No. 4877)
Category: Ion Channels > Chloride Channels
Biological Activity: Calcium-activated chloride channel (CaCC) inhibitor (IC50 ~ 10 μM). Inhibits CaCC currents in human bronchial and intestinal cells. Also inhibits TMEM16A channels (IC50 = 2.1 μM, in TMEM16A-expressing FRT cells). ]]> Ion Channels New Products 14 May 2013 19:37 H2L5186303 - Potent and selective LPA2 receptor antagonist http://www.tocris.com/dispprod.php?ItemId=375415&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 375415
Product: H2L5186303 (Cat No. 4878)
Category: 7-TM Receptors > Lysophosphatidic Acid Receptors
Biological Activity: Potent and selective lysophosphatidic acid 2 (LPA2) receptor antagonist (IC50 values are 8.9, 1230 and 27354 nM for LPA2, LPA3 and LPA1 receptors respectively, in a LPA-elicited calcium mobilization assay). ]]> 7-TM Receptors New Products 7 May 2013 19:28 PF 4778574 - Positive allosteric modulator of AMPA http://www.tocris.com/dispprod.php?ItemId=378037&utm_campaign=RSS&utm_source=RSS&utm_medium=RSS 378037
Product: PF 4778574 (Cat No. 4900)
Category: Glutamate (Ionotropic) Receptors > AMPA Receptors
Biological Activity: Positive allosteric modulator of AMPA receptors. Prevents ketamine-induced working memory impairments. Brain penetrant. ]]> Glutamate (Ionotropic) Receptors New Products 21 May 2013 18:46