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IC50 = 0.11 μM. Selective and non-competitive. Inhibits GTPγ35S binding to mGlu2-containing membranes.
Ki values are 0.29 μM and 1.11 μM for Bcl-2 and Bcl-XL respectively. Inhibits the angiogenic potential of endothelial cells in vitro. Induces S-phase arrest and apoptosis in pancreatic cancer cell lines; also inhibits the activation of Notch-1 and Jagged-1 in vitro and in vivo.
Ki values are 0.33, 57.6, 160.5 and 2109 nM for NOP, μ-, κ- and δ-receptors respectively. Antagonizes the pronociceptive action of nociceptin (Cat. No. 0910) in an acute pain model. Potentiates the action of morphine in morphine-tolerant animals and blocks hyperalgesia in an inflammatory pain model.
Anticonvulsant and antiepileptic; also used to treat neuropathic pain. Binds with high affinity and selectivity to the α2δ subunit of voltage-sensitive Ca2+ channels and modulates their activity. Displays anxiolytic-like activity in ethological and conflict models of anxiety. Analog of GABA (Cat. No. 0344).
Integrin very late antigen-4 (VLA-4; α4β1) antagonist (IC50 = 4.4 nM). Blocks the activation of inflammatory cells.
TRPM8 channel blocker. Inhibits icilin-induced (Cat. No. 1531) TRPM8 channel activation in a rat model (pIC50 = 6.23).
Histamine H3 receptor inverse agonist (EC50 = 1.5 nM) and antagonist (Ki = 0.16 nM). Exhibits nootropic effects in cognitive disorders; reduces locomotor hyperactivity induced by methamphetamine. Brain penetrant.
High affinity CB1 receptor antagonist (Ki = 4.1 nM). Exhibits significantly reduced lipophilicity compared to other CB1 antagonists.
P-glycoprotein (P-gp) modulator; inhibits P-gp-mediated multidrug-resistance (MDR). Reverses resistance to several cytotoxic drugs including mitoxantrone and doxorubicin (resistance factors are 2.0 and 6.5 respectively) in human MDR cancer cell lines. Non-immunosuppressive analogue of cyclosporin A (Cat. No. 1101).
Allosteric agonist of the human calcium-sensing receptor (hCaSR). Exhibits calcimimetic activity. Has the ability to restore function to hCaSR mutants that cause familial hypocalciuric hypercalcemia (FHH) and neonatal severe hyperparathyroidism (NSHPT). Exerts a suppressive effect on parathyroid (PT) hormone secretion; inhibits PT cell proliferation in rats with renal insufficiency.
IC50 = 35 nM. Oral adminstration inhibits cold water stress-induced tau hyperphosphorylation in the mouse brain.
IC50 = 12 nM in vitro. Displays selectivity for ceramide kinase (CerK) over sphingosine kinases (IC50 ≥100 μM) and other lipid kinases.
Displays high affinity (Ki = 4.5 nM) and is >1000-fold selective for H4 over other histamine receptors.
Cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) (Ki = 20 nM; IC50 = 160 nM). Suppresses the S6K1-mediated phosphorylation of S6, Rictor and mTOR in response to IGF1; displays no effect on the activity of RSK and MSK in vivo. Exhibits no significant inhibition of S6K2 or other AGC kinases (e.g. Akt, PKA and ROCK) in vitro.
IC50 = 1 - 10 μM. Attenuates Dnm1- and Drp1-mediated mitochondrial division. Inhibits mitochondrial outer membrane permeabilization (MOMP) and attenuates apoptosis.
IC50 = 0.5 μM. Inhibits cell proliferation of multiple human tumor cell lines in vitro. Also binds Hsc70 and Grp78; selective against Hsp90β.
IC50 = 98.2 nM. Mimics the action of LY 379268 (Cat. No. 2453); attenuates ketamine-evoked histamine release in vivo.
IC50 = 12 nM. Inhibits Aβ40 and Aβ42 formation in vitro (IC50 values are 7.4 and 7.9 nM respectively) and reduces Aβ in the brain, plasma and cerebrospinal fluid in vivo. Exhibits no Notch toxicity. Brain penetrant.
EC50 = 3 nM. Exhibits affinity at benzodiazepine binding site of recombinant human GABAA receptors (Ki values are 0.77 nM, 0.83 nM, 0.85 nM and 1.4 nM for α3-, α1-, α2-, and α5-containing respectively). Increases long-term potentiation (LTP) in mouse hippocampal slices. Exhibits no anxiogenic or proconvulsant activity.
IC50 values are 0.004 and 0.023 μM for ALK5 autophosphorylation and ALK5 binding respectively. Selective for ALK5 over a range of kinases, including p38 MAPK, JNK1 and GSK3 (IC50 > 16 μM). Enhances the efficiency of cellular reprogramming.
In vitro Ki values are 14 and 121 nM for GABAA α2 and GABAA α1 respectively. Exhibits non-sedative anxiolytic activity in vivo.
pEC50 values are < 5.5 and 8.3 respectively. Selective against the D4 receptor in both agonist and antagonist assays. Brain penetrant.
IC50 = 15.7 nM. Displays > 96-fold selectivity over MCH2. Exhibits antidepressant and anxiolytic activity in vivo. Also displays affinity for 5-HT1A and 5-HT2B receptors (IC50 values are 62.9 and 266 nM respectively). Orally active.
IC50 = 104 nM. Exhibits specificity for GSK-3 over cdk2 and cdk5 (IC50 values are > 100 μM) and over 26 other kinases. Inhibits β-amyloid-mediated neurodegeneration in hippocampal slices.
Inhibitor of Wnt signaling. Induces an increase in Axin2 protein levels; promotes β-catenin phosphorylation by stabilizing Axin-scaffolded destruction complexes.
Ki = 0.6 nM in vitro. Enhances the action of selective 5-HT reuptake inhibitors and reverses citalopram-induced inhibition of serotonergic cell firing.
IC50 = 30 nM. Induces neuronal differentiation in pluripotent murine embryonal carcinoma cells and embryonic stem cells (ESCs).
Inhibits acid- and capsaicin-induced activation of rat TRPV1 receptors (IC50 values are 6.0 and 35 nM respectively). Displays analgesic properties in rat models of inflammatory and neuropathic pain. CNS penetrant.
IC50 values are 1 and 17 μM for neuronal NOS and endothelial NOS respectively. Reduces ischemic cell damage after middle cerebral artery (MCA) occlusion in rats. Displays a synergistic neuroprotective effect when combined with either an NMDA or AMPA receptor antagonist.
EC50 = 380 nM. Induces 21-fold shift in ACh potency at M4 receptor. Displays no activity at other mAChR subtypes.
EC50 = 1.35 nM. Activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1. Induces acute lymphopenia in mice. Brain penetrant.
KD values are 3.7 and 17 nM respectively.
Inactivates Porcn, a membrane-bound O-acyltransferase (MBOAT), and selectively inhibits palmitoylation of Wnt. Blocks Wnt-dependent phosphorylation of Lrp6 receptor and Dvl2, and β-catenin accumulation.
pKi values are 8.24 and 8.47 in human and rat H4 receptors respectively. Displays 162-fold, 620-fold, and > 1600-fold selectivity over human H3, H1 and H2 receptors. Blocks zymosan-induced neutrophil reflux and attenuates thermal hypersensitivity in vivo (ED50 = 42 μmol/kg, ip).
Blocks P2X4-mediated currents in Chinese hamster ovary cells (IC50 = 0.50 μM).
IC50 = 64 nM. Displays no effects on other cardiac channels; IC50 values are 3.3, >10, 11.1 and 12.6 μM for INa, ICa, Ito and IKr channels respectively. Prolongs QT and causes unprovoked torsades de pointes (TdP).
Ki = 1.5 nM in vitro. Displays ≥ 3300-fold affinity for Y5 over Y1, Y2 and Y4 receptors. Also binds human 5-HT2B and 5-HT1A receptors (Ki values are 247 and 478 nM respectively). Exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity.
Ki values are 0.2 and 3 nM for OX2 and OX1 receptors respectively. Inhibits ADL-orexin B-mediated locomotion following i.p. administration in vivo. Brain penetrant.
Displays 30-fold selectivity over PI3Kδ and PI3Kβ and 7.5-fold selectivity over PI3Kα. Suppresses the progression of joint inflammation and damage in both lymphocyte-independent and lymphocyte-dependent mouse models of rheumatoid arthritis.
IC50 values are 3.1, >10000, >10000 and >10000 nM for Y5, Y1, Y2 and Y4 receptors respectively. Does not block NPY-induced feeding in vivo. Orally active and brain penetrant.
Ki = 7.1 nM, EC50 = 4.8 nM. Displays 62-fold selectivity over ERα.
IC50 values are 0.27, 2500, 6700 and > 10000 nM for NOP, κ-, μ- and δ-receptors respectively. Inhibits nociceptin-induced stimulation of [35S]-GTPγS binding and Ca2+ mobilization in CHO cells in vitro.
pKi values are 7.15 and 8.12 at human and rat receptors respectively. Blocks inflammation in a peritonitis mouse model and displays efficacy in inflammatory pain and neuropathic pain models.
Ki values are 0.06, 240, 322 and 3540 nM for α4β2, α3β4, α7, α1βγδ receptors respectively. Reduces nicotine-evoked dopamine release in vitro and decreases nicotine self-administration in vivo.
Ki values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFRβ and KIT respectively. Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.
Ki values are 6.3 nM and 1.2 μM for CB2 and CB1 receptors respectively. Displays analgesic activity in the formalin test in mice.
Blocks ADP-induced inhibition of adenylyl cyclase in vitro (PKB =7.6) and inhibits ADP-induced aggregation of washed human platelets (pIC50 = 8.16).
IC50 values are 220, 80 and 14 nM for cdk1/cyclin B, cdk5/p25 and CK1 respectively. Selective over GSK-3 α/β (IC50= 4.1 μM). Also shown to inhibit amyloid-β production in N2A-APP695 cells.
Ki = 20 nM. Displays no affinity for ERα and ERβ at concentrations up to 10 μM. Inhibits agonist-induced calcium mobilization in vitro (EC50 of ~185 nM) and antagonizes the antidepressive effects of estrogen in vivo.
IC50 values are 24 and 100 nM for Pim-1 and Pim-2 respectively. Displays selectivity over a panel of ~50 other kinases tested. Exhibits cytotoxicity in PC3 prostate carcinoma cells in vitro (IC50 = 17 μM).
IC50 ~10 nM for mTORC1 and mTORC2 respectively. Displays no activity at PI 3-K or 76 other kinases tested. Suppresses cell growth and induces G1 cell cycle arrest in vitro.
Interacts with NME2 and inhibits its nuclear translocation. Increases the efficiency of directed differentiation of mouse and human embryonic stem cells (ESCs) in vitro.
Ki values are 3.0, 3.4, 4.4, 59, 154 and 527 nM for MMP-1, MMP-13, MMP-8, MMP-9, MMP-2 and MMP-3 respectively. Inhibits cartilage breakdown in vitro and in vivo and displays antiarthritic activity. Orally active.
EC50 = 142 nM for α4β3δ receptors. Displays no effects on GABA responses mediated by α4β3γ2 and α1β3γ2 receptors.
IC50 values are 18 and 40 nM for rat and human receptors respectively. Displays selectivity over a variety of P2X and P2Y receptors up to a concentration of 100 μM. Reduces nociception in animal models of persistent neuropathic and inflammatory pain.
IC50 = 4 nM. Displays > 2500-fold selectivity over C5aR, LTD4, CCR7, CXCR1 and CXCR2 receptors. Inhibits eotaxin-, eotaxin-2- and MCP-4-induced Ca2+ mobilization.
IC50 values are 0.011 and 0.004 μM for TNKS1 and TNKS2 respectively. Antagonizes wnt signaling via stimulation of β-catenin degradation and stabilization of axin.
RN 1747 is a selective TRPV4 agonist (EC50 values are 0.77, 4.0 and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4 respectively) that also antagonizes TRPM8 at relevant concentrations (IC50 = 4 μM). RN 1734 is a selective TRPV4 antagonist (IC50 values are 2.3, 5.9 and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4 receptors respectively).