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Tocris社 11月新製品

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New products are an essential component of our range. Introductions are made on an ongoing basis, with hundreds of new small molecules, peptides and antibodies being added every year. Our aim is to find the latest, otherwise unobtainable research tools, and bring them to the market as quickly as we can.

 

 

 

 

 

 

 

Cat.No. Product Name  Activity
4390 Thiamet G Potent, selective inhibitor of O-GlcNAcase (Ki = 21 nM for human O-GlcNAcase). Decreases the phosphorylation of tau protein in vivo. Orally bioavailable and blood brain barrier permeable. 
3861 UNC 0224 Potent inhibitor of G9a histone lysine methyltransferase (HMTase) (IC50 = 15 nM). 
4333 PSB 1114 Potent, selective P2Y2 agonist (EC50 = 0.134 μM). Displays >60-fold selectivity versus P2Y4 and P2Y6 receptors. 
4418 Saquinavir mesylate Inhibitor of human immunodeficiency virus (HIV) protease (Ki values are <0.1 and 0.12 nM for HIV-2 and HIV-1 protease respectively). Exhibits high antiviral activity and low cytotoxicity. 
2332 (+)-Igmesine hydrochloride Selective σ1 receptor ligand (KD = 19.1 nM), with little or no activity at σ2 receptors (IC50 > 1000 nM). Inhibits the NMDA-induced increase in cGMP in a concentration-dependent manner (IC50 value is approximately 100 nM). Weak inhibitor of brain 5-HT uptake in vitro. Exhibits neuroprotective and antidepressant effects. 
4341 A 582941 Selective α7 nAChR partial agonist; exhibits high affinity for both rat and human α7 receptors (Ki values are 10.8 and 16.7 nM respectively). Displays ~15-fold selectivity for α7 over 5-HT3 receptors (Ki = 150 nM for 5-HT3). 
4408 DMOG Prolyl 4-hydroxylase (P4H) inhibitor; inhibits hypoxia-inducible factor α (HIF-α) prolyl hydroxylase (HIF-PH). Increases levels of HIF-1α; promotes cell survival under hypoxic conditions. 
4336 TG 003 Potent, ATP-competitive inhibitor of Clk-family kinases (IC50 values are 20, 200 and 15 nM for mClk1, 2 and 4 respectively and >10 for mClk3). Suppresses serine/arginine-rich protein phosphorylation; affects the regulation of alternative splicing by phosphorylation of SR protein both in vivo and in vitro. 
4230 NPEC-caged-D-AP5 D-AP5 (Cat.No. 0106) caged with the photosensitive 1-(2-nitrophenyl)ethoxycarbonyl (NPEC) group. NMDA receptor antagonist. 
4086 PE 154 Potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinerase (BChE) (IC50 values are 280 pM and 16 nM respectively). Targets and labels β-amyloid plaques in histochemical analysis. 
3794 iMAC2 Inhibitor of mitochondrial apoptosis-induced channel (MAC) (IC50 = 28 nM). Reduces STS-induced apoptosis in FL5.12 cells by over 50%. Inhibits release of cytochrome c by Bid-induced Bax activation (IC50 = 0.68 μM). 
4314 SB 268262 Selective non-peptide CGRP1 antagonist. Inhibits [125I]CGRP binding and CGRP-activated adenylyl cyclase stimulation in SK-N-MC cell membranes (IC50 values are 0.24 and 0.83 nM respectively). 
4311 GW 542573X Activator of small-conductance Ca2+-activated K+ channels (SK, KCa2); selective for SK1 (EC50 = 8.2 μM in HEK293 cells expressing hSK1) with the profile hSK1 > hSK2 = hSK3 > hIK. 
3219 CGP 36216 Selective GABAB antagonist. Displays activity at presynaptic receptors; ineffective at GABAB postsynaptic receptors. 
4291 CCT 137690 Potent inhibitor of Aurora kinases (IC50 values are 0.015, 0.019 and 0.025 μM at Aurora A, Aurora C and Aurora B respectively). Displays antiproliferative activity in a range of human tumor cell lines. Orally bioavailable. 
4395 Moclobemide Reversible monoamine oxidase A (MOA-A) inhibitor. 
4374 BIMU 8 Potent 5-HT4 receptor full agonist (KD = 77 nM and EC50 = 18 nM for wild type 5-HT4 receptors). Binds to receptors in a mechanism different to that of the endogenous ligand 5-HT. 
4262 KH CB19 Selective, potent inhibitor of CDC2-like kinase (CLK) 1 and 4 (IC50 value of 20 nM for CLK1). Suppresses serine/arginine-rich protein phosphorylation by CLKs under proinflammatory conditions. Displays selectivity over a panel of 71 protein kinases. 
4297 SMER 28 Positive regulator of autophagy in a mechanism independent from the mTOR pathway. Increases autophagosome synthesis and enhances clearance of model autophagy substrates such as A53T α-synuclein associated with Huntington's disease. 
4285 HBX 41108 Inhibitor of ubiquitin-specific protease (USP) 7 activity (IC50 = 424 nM). Displays uncompetitive inhibition. Also inhibits USP7-mediated p53 deubiquitination (IC50 = 0.8 μM). Stabilizes p53 and inhibits cancer cell growth; induces p53-dependent apoptosis in p53 wild type and null isogenic cancer cell lines. 
4347 Ro 67-4853 Positive allosteric modulator of mGlu group I receptors (pEC50 value is 7.16 for the rat mGlu1a receptor). Exhibits activity at all group I receptors, including human and rat mGlu1 and rat mGlu5. Enhances the effects of (S)-DHPG in CA3 neurons (EC50 = 95 nM). 
4351 JHW 007 hydrochloride Dopamine uptake inhibitor; displays high affinity for the dopamine transporter (DAT) (Ki = 25 nM compared to 1330 and 1730 for NET and SERT respectively). Suppresses the effects of cocaine administration in a dose-dependent manner. 
4346 Ro 67-7476 Positive allosteric modulator of mGlu1 receptors. Potentiates glutamate-induced calcium release (EC50 = 60.1 nM at rat mGluR1a). Displays no activity at human mGlu1 receptors. 
4140 EB 47 Potent inhibitor of PARP-1 (IC50 = 45 nM).
3935 RWJ 52353 Agonist of the α2D adrenergic receptor (Ki values are 1.5, 254, 443 and 621 nM for α2D, α2A, α1 and α2B adrenergic receptors respectively). 
4348 Ro 01-6128 Positive allosteric modulator of mGlu1 receptors. Potentiates glutamate-induced calcium release (EC50 = 104.2 nM at rat mGluR1a). 
4289 RP 001 hydrochloride Potent agonist of S1P1 receptors (EC50 = 9 pM). Induces internalization and polyubiquitination of S1P1 in vitro. Selective for S1P1 over S1P2 - S1P4. 
4281 PF 4800567 hydrochloride Selective casein kinase 1ε inhibitor; displays 22-fold greater potency towards CK1ε than CK1δ (IC50 values are 32 and 711 nM for CK1ε and CK1δ respectively). ATP competitive. Displays minimal effect on the circadian clock. 

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