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Displays 68-fold selectivity over ERα (EC50 values are 2 and 155 nM for ERβ and ERα respectively). Displays antianxiolytic and antidepressive effects in vivo.
IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively. Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.
EC50 values are 240 and 110 nM at human and rat receptors respectively. Inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. Brain penetrant.
Ki = 11 nM, EC50 = 2 nM. Displays no activity at ERα and ERβ at concentration up to 10 μM. Inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants (IC50 values are 0.7 and 1.6 nM respectively) in vitro.
IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively. Potentiates the effects of radiation, doxorubicin and etoposide in human tumor cell lines in vitro and etoposide in a human tumor xenograft model in vivo.
Ki values are 1 and > 10000 nM at CB1 and CB2 receptors respectively. Inhibits food intake in vivo following oral administration.
IC50 values are 5, 21.5, ~100, 17600 and 19800 nM for FGFR3, FGFR1, VEGFR2, PDGFR and c-Src respectively. Inhibits VEGF- and FGF-induced angiogenesis in the mouse cornea model of angiogenesis.
D3 > D2 > D4. Causes biphasic spontaneous locomotor activity and contralateral circling in 6-OHDA-lesioned mice. Displays antiParkinsonian activity.
Non-benzodiazepine agent that acts as an agonist at the benzodiazepine site. Displays hypnotic, anxiolytic, myorelaxant and anticonvulsant activity.
Ki = 3.3 nM, IC50 = 5.9 nM. Displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. Reduces food intake and body weight via central Y1 inhibition and is brain penetrant.
Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 20 μM), and induces cell cycle arrest.
Ki = 0.86 nM. Displays > 55-fold selectivity over σ2 receptors and > 6000-fold selectivity over D1, D2, 5-HT1A, 5-HT2 and PCP receptors. Exhibits reversible binding (Kd = 1.2 nM) and displays antipsychotic activity in vivo. Orally active.
Selectively inhibits HIV reverse transcriptase (RNA-dependent DNA polymerase). Prevents cytotoxicity in SIV-infected C-8166 cells in vitro (IC50 = 1.5 μM). Antiviral agent.
IC50 values are 5.4, > 1000, > 10 000 and > 10 000 nM at Y5, Y1, Y2 and Y4 receptors respectively. Significantly inhibits NPY-induced feeding but not through blockade of Y5 receptors.
Ki = 11 nM, IC50 = 14 nM. Displays > 15 000-fold selectivity over DPP-II and a range of proline-cleaving proteases. Exhibits antidiabetic activity in vivo.
IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively. Devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo. Orally active.
IC50 = 10 nM. Displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively. Suppresses DNA synthesis and induces apoptosis in cells that proliferate in response to Raf-1 and A-Raf but not B-Raf.
IC50 = 16.2 nM. Displays no activity at a range of other serine hydrolases. Selectively inhibits FAAH within the central nervous system. Orally active.
Ki values are 22.7 nM and > 10 μM for CB2 and CB1 receptors respectively, EC50 = 5.57 nM. Displays antiallodynic activity in the rat hindpaw incision model of postoperative pain.
Ki values are 0.3, 916, > 5000 and > 5000 nM at EP3, EP4, EP1 and EP2 respectively. Attenuates sulprostone-induced inhibition of EFS-evoked twitch and contractile responses in vivo.
pKi - 9.02 - 8.92. Increases extracellular glutamate and aspartate in the frontal cortex, and exhibits anticonvulsant activity (EC50 = 0.16 μM).
IC50 values are 62 and 103 nM for SGK1 and SGK2 respectively. Displays > 30-fold selectivity over Akt and other related kinases. Inhibits androgen-stimulated growth of LNCaP cells, a human prostate carcinoma cell line (IC50 ~ 1 μM).
EC50 = 0.8 μM. Displays selectivity towards β1 subunit-containing heterotrimers. Inhibits fatty acid synthesis (IC50 = 3.2 μM) and decreases plasma glucose and triglyceride levels in vivo.
Ki = 1.2 - 1.7 nM. Acts at the benzodiazepine site. Displays ~ 10-fold selectivity for α1 subunit-containing receptors. Exhibits sedative, hypnotic, anxiolytic and anticonvulsant activity in vivo and is orally active.
EC50 values are 0.3, 5, 42, 52 and 92.5 nM at M1, M3, M5, M4 and M2 receptors respectively. Exhibits antipsychotic activity, and improves cognitive deficits and behavioural disturbances in Alzheimer's disease and schizophrenia.
IC50 = 0.48 nM. Displays 38-fold and 400-fold selectivity over calcitonin and CGRP receptors respectively. Increases glucagon secretion, accelerates gastric emptying, alters plasma glucose levels and increases food intake in vivo.
IC50 values are 15.8 and > 30 000 nM at GlyT1 and GlyT2 respectively. Induces a dose-dependent elevation in CSF levels of glycine, and enhances acetylcholine and dopamine release in the striatum and prefrontal cortex respectively. Produces profound locomotor and respiratory impairments at higher doses.
IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively. Inhibits embryonic left-right determination and exhibits potent anticancer activity in vitro and in vivo.
Exhibits species-specific activity; acts as a negative allosteric modulator of human P2X7 (pIC50 = 6.9 - 7.2) and a positive allosteric modulator of rat P2X7.
pEC50 = 6.7). Displays no activity at other PAR subtypes. Stimulates cell proliferation, PI hydrolysis and Ca2+ mobilization in vitro (pEC50 values are 6.7, 5.9 and 6.6 respectively) and exhibits pronociceptive activity in vivo.
IC50 = 25 nM in rat cortical neurons. Displays potent anticonvulsant activity. Also significantly blocks the persistent component of Nav1.6 channel activity. Brain penetrant and orally active.
C50 values are 3, 4, 4, 6 and 20 nM for MMP -1, -2, -9, -7 and -3 respectively). Exhibits antiproliferative, anti-invasive and antimetastatic activity in human ovarian carcinoma xenografts in vivo.
Ki = 2.2 nM, IC50 values are 13, 2500, 9300, 16600, >100000 and > 100000 nM at ATM, DNA-PK, mTOR, PI 3-K, PI 4-K and ATR respectively. Decreases viability of MCF-7, A549 and HCT116 cells and decreases p21CIP1 levels in vitro.
IC50 values are 21, 22 and 38 nM for ErbB4, EGFR and ErbB2 respectively). Displays potent growth inhibition of human cancer cell lines overexpressing ErbB2 in vitro (IC50.
IC50 = 5 nM in Ca2+-flux assay; Ki= 16 nM. Displays anxiolytic activity in vivo and is orally active.
IC50 = 0.4 μM). Displays no major inhibition of human cytochrome P450 isoenzymes (IC50 > 30 μM). Exhibits antiangiogenic properties in vitro (IC50 = 1 μM).
Ki = 300 nM. Blocks intestinal fluid secretion induced by cholera toxin and Escherichia coli and suppresses cyst growth in animal models of polycystic kidney disease. Orally active.
IC50 values are 7.7 and 14 nM for CK1ε and CK1δ respectively. Displays > 30 fold selectivity over 42 other common kinases. Attenuates methamphetamine-stimulated locomotion in vivo.
KD values are 1.4 and 19 nM at human and rat P2X7 receptors respectively. Binds in a positive cooperative manner to sites distinct from, but coupled to, the ATP binding site and acts as a negative allosteric modulator.
IC50 values are 0.182, 0.280, 0.227, >10, 15.3, 20.3, 40.5 and >50 μM at PKD1, PKD2, PKD3, PKC, CAK, PLK1, CAMKIIα and Akt respectively. Inhibits prostate cancer cell proliferation, migration and invasion in vitro.
Displays 34-fold selectivity over mGlu5m (IC50 values are 10 and 342 nM respectively). Exhibits analgesic effects; decreases mechanical allodynia in models of neuropathic pain. Also impairs cognitive function.
Displays selectivity over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. Positively influences sensory gating and memory in in vivo models of schizophrenia. Orally active and brain penetrant.
IC50 = 17 nM. Displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. Exhibits equal potency for inhibition of Aβ40 and Aβ42 peptides (IC50 values are 48 and 67 nM respectively in human neuroblastoma cells).
IC50 = 40 nM. Displays > 250 fold selectivity over OX1 and 50 other receptors, ion channels and transporters.
Selectively binds to α1, α2, α3 and α5 subunits (Ki values are 0.79, 0.67, 0.67 and 2.25 nM respectively) but displays no efficacy at α1 (α1-sparing). Exhibits non-sedative anxiolytic, antinociceptive and anti-inflammatory activity in vivo.
IC50 = 190 nM. Displays peripheral selectivity and does not effect serum levels of LH and testosterone. Exhibits potent anticancer activity in vivo.
IC50 = 15nM. Displays no discernible effect on adrenocorticoid hormone synthesis. Reduces plasma estrogen levels and exhibits antitumor activity in vivo. Orally active.
IC50 values are 0.9, 3 and > 25 nM for JAK2, FLT3 and TrkA respectively. Prevents STAT5 phosphorylation (IC50 = 20 - 30 nM). Exhibits antiproliferative activity in vitro and is effective against myeloproliferative disorders in vivo.
IC50 values are 1 and 11 μM for p38α and p38β respectively. Displays no activity at p38γ, p38δ and a range of other kinases. Exhibits cardioprotective and anti-inflammatory activity in vivo. Orally active.
EC50 values are 10 and 20 nM for human and rat receptors respectively. Antipsychotic; reverses amphetamine-induced locomotor activity and amphetamine-induced deficits in prepulse inhibition in rats.
Increases the potency and efficacy of GABA ( > 15-fold and > 149% respectively). Exhibits anxiolytic activity in vivo and is orally active.
Ki = 0.38 nM, EC50 = 60 nM. Enhances the cell killing activity of Gemcitabine (Cat. No. 3259) in breast and prostate cancer cell lines and displays antiproliferative effects in vitro.
IC50 values are 0.02 - 0.13 and > 25 μM for CXCR4 and all other chemokine receptors respectively. Switches inflammatory responses from Th2 to Th1 type and reduces airway hyperresponsiveness in a mouse model of asthma.
IC50 values are 50, > 20000 and > 20000 nM for Pim-1, Pim-2 and MEK1/2 respectively.
IC50 values are 10 and 34 nM respectively. Prevents inititaion of DNA replication and inhibits cell proliferation in a variety of human cell lines (IC50 ~ 0.86 - 5.87 µM).
IC50 = 3 μM. Displays > 30-fold selectivity over P2X2, P2X3 and P22/3 receptors (IC50 > 100 μM).
Ras-Net (Elk-3) pathway inhibitor (IC50 = 10-20 nM). Indirectly inhibits Net phosphorylation upstream of Erk1/2 activation. Inhibits angiogenesis and acts as a microtubule depolymerizing agent in vitro.
IC50 values are 0.4 and 0.12 nM at rat ovary and human placenta cells respectively. Only weakly inhibits the synthesis of other steroid hormones. Reduces plasma estrogen levels into ranges induced by ovariectomy.
IC50 = 93 nM. Suggested to have NR2 subunit selectivity. Exhibits broad anticonvulsant and antiparkinsonian activity in vivo at doses devoid of behavioral toxicity.