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Ki = 18 nM. Displays no effect at S1P2, S1P3 or S1P5. Enhances capillary leakage and restores lymphocyte egress in vivo.
Ki = 0.8 nM. Blocks NR2B-mediated calcium influx in Ltk cells (Ki = 9.7 nM). Selective for NR2B subunit over α1-adrenergic receptors and hERG channels (IC50 values are 730 nM and 2900 nM respectively). Displays efficacy in the rat carrageenan-induced mechanical hyperalgesia assay.
IC50 values are 1.28 nM and 1.85 nM for wild-type and G2019S mutant forms of LRRK2 respectively. Attenuates neuronal injury induced by LRRK2-G2019S mutant activity in primary human neurons (EC50 = 1 nM).
IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively. Cell permeable (EC50 = 10 μM for PKD1 inhibition). ATP-competitive.
IC50 = 0.8 nM for α1β1 binding to type IV collagen. Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α1β1, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitumor efficacy in a synergistic mouse model of Lewis lung carcinoma; blocks human melanoma growth in nude mice.
Acts as a probe for visualizing the accumulation and intracellular trafficking of anandamide. Blocks anandamide uptake (IC50 = 0.5 μM in HaCaT cells); prevents interaction with FAAH, CB1 and TRPV1.
EC50 values are 1.4 and 2.2 μM at human and rat receptors respectively. Displays no measurable effect on α4β2 nAChRs. Stimulates α7 nAChR-induced ERK1/2 phosphorylation in PC12 cells.
EC50 = 63 nM; displays no significant activity against a range of 47 other kinases, including other Src family kinases such as Fyn, Lck and Src kinase. Reduces blood glucose levels without affecting in vivo insulin secretion. Orally bioavailable.
Represses expression of known HNF4α target genes. Decreases HNF4α DNA binding. Exhibits cytotoxic activity in a range of tumor cell lines, including human hepatocellular carcinoma.
Blocks recruitment of BET to chromatin. Induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively); reduces BCL2 expression in NOMO1 cells. Improves survival in two rodents models of MLL-fusion leukemia in vivo.
Maintains embryonic stem cell (ESC) self-renewal. Enables propagation of undifferentiated murine ESCs in the absence of leukemia inhibitor factor (LIF).
IC50 = 0.5 μM in HEK293 cells transiently expressing mouse Smo. Inhibits ShhN-induced Gli luciferase reporter activity in Shh-light2 cells (IC50 = 2.5 μM); acts as an inverse agonist during nontranscriptional hedgehog pathway activation (IC50 = 2.5 μM in HEK293 cells).
Blocks demethylation of histone H3K27. Attenuates lipopolysaccharide (LPS)-induced proinflammatory cytokine production in primary human macrophages (IC50 = 9 μM for the inhibition of TNFα release). Cell permeable, ethyl ester derivative of GSK J1 (Cat. No. 4593).
IC50 = 47 nM. Induces activation of Trk, Akt and ERK in mouse hippocampus and striatum. Reverses deficits in motor task learning in mice following traumatic brain injury; restores respiratory function in a rat model of Rett syndrome.
Ki = 1.7 nM. Displays no significant activity at a range of ATP-binding kinases or Na+K+ ATPase. Induces degradation of HER-2 in vitro (EC50 = 38 nM in MCF-7 cells). Inhibits growth and promotes cell death in a variety of human tumor cells. Orally bioavailable.
Displays no activity at PAR2, PAR3, or PAR4 subtypes. Blocks thrombin-induced platelet aggregation and activation of MAPK in HUVECs. Also inhibits angiogenesis in a chick embryo angiogenesis model in vivo.
IC50 values are 6.7 and 10 nM for GSK-3β and GSK-3α respectively. Exhibits >500-fold selectivity for GSK-3 over closely related kinases; also displays >800-fold selectivity against 45 additional enzymes and receptors.
Exhibits inhibitory activity at bromodomain-containing protein (BRD) 2 and BRD4.
Inhibitor of the PARP domain of tankyrase 1 and 2 (TNKS1/2). Activity results in stabilization of Axin2 and increased degradation of β-catenin; inhibits the β-catenin signaling pathway. Also shown to decrease canonical Wnt signaling in SW480 and HCT-15 colon carcinoma cell lines; reduces cell cycle progression and proliferation in SW480 cells in vitro.
IC50 values are 0.03 and 6.4 nM for human and rat CGRP receptors respectively. Displays high affinity for human CGRP receptors (Ki = 14.4 pM); exhibits no significant affinity for 75 other receptors.
EC50 values are 2.7 μM for human M5, and >30 μM for M1, M2, M3 and M4 receptors.
Fluorescent probe for imaging hydrogen peroxide (H2O2) in mitochondria of living cells. Displays enhanced emission at 528 nm in the presence of H2O2. Selective for H2O2 over superoxide, nitric oxide and hydroxyl radical. Detects local increases in H2O2 in an in vitro model of Parkinson's Disease.
Ki = 0.67 nM. Potently inhibits mGlu5 glutamate-mediated calcium mobilization (IC50 = 1.22 nM).
Potently induces differentiation of human mesenchymal stem cells (MSCs) into chondrocytes (EC50 = 100 nM). Reduces disease severity in a mouse model of osteoarthritis; displays protective effects against osteoarthritic stimuli in mature chondrocytes in vitro.
EC50 values are 230 and 510 nM for KCNQ2 and KCNQ4 respectively. Displays >80-fold selectivity against KCNQ1, KCNQ3 and KCNQ5 in a thallium-based fluorescence assay.
Ki = 24.9 nM. Unlike clopidogrel (Cat. No. 2490), does not require bioactivation.
Ki = 0.67 nM. Potently inhibits mGlu5 glutamate-mediated calcium mobilization (IC50 = 1.22 nM).
IC50 = 0.28 μM in enzymatic assay. Reduces eEF-2 phosphorylation with little effect on cancer cell growth.
Inhibits glucose uptake in renal cell carcinoma (RCC) 4 cells. Activity causes necrotic cell death in von Hippel-Lindau (VHL)-deficient RCC cells.
EC50 = 8.6 μM; also inhibits the closely related deubiquitinase (DUB) USP47. Demonstrates downstream inhibition of HDM2 and claspin in vitro. Inhibits USP7-mediated p53 deubiquitination.
EC50 = 12 nM. Displays 14- and 66-fold selectivity against P2Y2 and P2Y4 receptors respectively.
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.
IC50 = 267 nM; inhibits proliferation and induces apoptosis in Bcr-abl-expressing cells. Selective for Bcr-abl over a panel of serine, threonine and tyrosine kinases. Non-ATP-competitive.
Ki = 0.6 nM for GSK-3α and GSK-3β. Displays high selectivity (> 50-fold) for GSK-3 over a panel of other kinases tested, including CDK family members. Decreases phosphorylation of microtubule-associated protein Tau in vitro; protects rat primary cortical neurons against β amyloid and glutamate challenge. Brain penetrant.
Displays over 100-fold selectivity for PHD2 over factor inhibiting HIF-1 (FIH-1) and histone demethylases KDM4A, KDM4C, KDM4E and KDM6B. Cell permeable.
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.
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.
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.
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.
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).
IC50 ~ 10 nM. Exhibits no effect on other kinases including Aurora, ROCK, p38 MAPK and PI3K. Suppresses T-loop phosphorylation and subsequent activation of PDK1 substrates S6K1, SGK and RSK in HEK293, U87 and mouse embryonic fibroblast cell lines.
Potent, ATP-competitive inhibitor of mitogen-activated protein kinase (MAPK)-activated protein kinase-2 (MK-2) (IC50 = 5.2 nM; Ki = 3 nM). Inhibits TNFα production in U937 monocytic cells and PBMCs (IC50 = 160 nM); exhibits oral efficacy in acute and chronic inflammatory models.
Significantly elevates cGMP levels and inhibits collagen-stimulated aggregation of washed rabbit platelets ; induces relaxation in denuded phenylephrine-contracted rabbit aortic rings (EC50 = 1.9 μM). Also induces G1 cell cycle arrest in two HCC cell lines.
IC50 values are < 15 nM and 19 nM for G9a and GLP respectively, and > 10000 nM for a range of other histone lysine methyltransferases. Potently inhibits dimethylation of H3K9 in MCF-7 cells (IC50 = 70 nM). Cell permeable.
Selective inhibitor of EphB4 kinase; exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3. Inhibits EphB4 autophosphorylation in transiently transfected HEK 293 cells. Also inhibits VEGF-induced angiogenesis in vivo.
IC50 values are 0.018 and 0.093 μM for ALK5 binding and for TGF-β cellular assay respectively. Inhibits esopheageal squamous cell carcinoma (ESCC)-induced neoangiogenesis. Orally active.
IC50 = 25 nM for inhibition of TRPV1 activation by 50 nM capsaicin. Displays no activity against a range of receptors, including TRPA1, GABA, opioid, and purinergic receptors.
Selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1, MAP3K5) (IC50 = 3 μM, Ki = 500 nM).
Inhibitor of Krüppel-like factor 5 (KLF5) transcription factor (IC50 = 2.3 μM). Selective for colon cancer cells in a panel of 60 different cancer cell lines.
IC50 = 0.13 nM against purified B-RafV600E. Activity reduces phospho-ERK (pERK) levels (IC50 = 63 nM in the Malme-3M cell line). Inhibits the Raf/MEK/ERK signaling pathway in V600E B-Raf mutant cell lines. Does not activate apoptotic pathways in A375 or Colo205 cell lines. Orally bioavailable.
pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively. Brain penetrant.
Specific inhibitor of a yeast SCF family E3 ubiquitin ligase (SCFMet30) in vitro and in vivo. Induces the expression of MET genes; blocks cell proliferation. Enhancer of Rapamycin (Cat. No. 1292).
ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) (IC50 values are 69 and 225 nM for DAPK1 and DAPK3 respectively, when assayed with 10 μM ATP). Displays selectivity for DAPK1 over a range of 48 other kinases, including Abl, AMPK, Chk1, Met and Src (IC50 > 10 μM).
Potent antagonist of mGlu5 (IC50 = 61 nM). Displays no activity at mGlu1-4 and mGlu7-8.
Inhibitor of neural Wiskott-Aldrich syndrome protein (N-WASP) activity. Interacts with the regulatory GTPase-binding domain of N-WASP; inhibits activation of Arp2/3 complex by maintaining N-WASP in an inactive conformation. Also inhibits PIP2-induced actin polymerization (EC50 ~ 4μM).
Inhibits the second deacetylase domain (DD2). Does not inhibit HDAC6 histone deacetylase activity; reversibly inhibits α-tubulin deacetylation. Increases α-tubulin acetylation levels with no effect on histone acetylation or cell cycle progression.
Positive allosteric modulator of AMPA receptors. Exhibits cognitive enhancing properties in rodent behavioral models. Brain penetrant.
Displays greater affinity for rat V1 than human V1 (Ki = 25 and 8800 nM respectively). Exhibits 1000-fold selectivity for V1 receptors over V2 receptors. Orally active.
EC50 = 0.08 μM. Displays greater potency at P2Y6 than UDP (Cat.No. 3111) (EC50 = 0.14 μM).
Interferes with pleckstrin homology domain binding to PIP3 and facilitates Akt ubiquitination. Exhibits anticancer activity in vitro and in vivo.