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Inhibits binding of 125I-IP-10 and 125I-ITAC to CXCR3 (IC50 values are 8.0 and 8.2 nM respectively). Inhibits CXCR3-mediated cell migration by the chemokines IP-10, ITAC and MiG in vitro (IC50 values are 8, 15 and 36 nM respectively).
Potent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM for c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity for Raf kinases over a panel of 150 other kinases. Also inhibits growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.
IC50 values are 1, 2 and 2.5 nM for PKD1, PKD3 and PKD2 respectively. Exhibits selectivity for PKD against a panel of >90 protein kinases, including PKCα, MEK, ERK, c-Raf and c-Src. Orally bioavailable.
Kd values are 79 and 28 nM for TNKS1 and TNKS2 respectively; IC50 = 33 nM for TNKS2. Devoid of activity at PARP1 and PARP2 (IC50 >19 μM). Inhibits Wnt signaling and stabilizes Axin2 levels.
Accelerates FRAP recovery of BRD4 and CREBBP in cells at a concentration of 1 μM.
IC50 values are 0.69, 13.6, 47.8 and 136 nM for PI 3-Kβ, PI 3-Kδ, PI 3-Kγ and PI 3-Kα, respectively. Selectively inhibits in vivo growth of the PTEN-deficient tumor xenografts HCC70 and PC3. Exhibits antithrombotic activity.
Displays an orange intracellular fluorescence in response to H2O2 signals produced in RAW 264.7 macrophages and A431 cells during immune response and growth factor stimulation, respectively. Cell permeable.
EC50 = 0.5 nM. Shown to inhibit Wnt-dependent processes such as tailfin regeneration and posterior axis formation in zebrafish; also reduces branching morphogenesis in cultured mouse embryonic kidneys.
IC50 = 0.9 nM. Displays no effect at ASIC1b, ASIC2a, ASIC3, heteromeric ASIC channels, ENaC and KV2.1/2.2/4.2/4.3 channels expressed in oocytes, at concentrations up to 100 nM. Displays potent analgesic properties.
IC50 = 0.8 μM in LPA5-RH7777 cells. Inhibits LPA-induced aggregation of isolated human platelets. Exhibits selectivity for LPA5 against 80 other screened targets.
IC50 = 5.84 μM. Irreversibly suppresses protease function. Decreases NF-κB activity induced by MALT1. Inhibits cell proliferation and MALT1-mediated cleavage activity. Suppresses human TMD8 and HBL-1 activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) tumor xenografts in mice and primary human ABC-DLBCLs ex vivo.
EC50 = 72-132 nM. Displays no activity at S1P1, S1P2, S1P4 and S1P5 receptors at concentrations up to 10 μM. Shows no significant activities in a profiling panel of 55 GPCRs, ion channels and transporters.
IC50 values are < 2, 60, 36, and >100 μM for KAT5, p300, pCAF and GCN5, respectively. Inhibits protein acetylation in prostate cancer cell lines and blocks DNA damage response. Decreases proliferation of LNCaP cells; induces apoptosis via caspase activation.
Inhibits LPI-induced Ca2+ signaling (IC50 = 0.21 μM in HEK-GPR55 cells), ERK1/2 phosphorylation and GPR55-mediated transcription factor activation. Decreases LPI-induced GPR55 internalization.
Displays over 100-fold higher potency at ADAM10 compared to ADAM17. Blocks constitutive release of IL-6R, CX3CL1 and CXCL16 in cell-based cleavage experiments. Inhibits calcium ionophore-induced betacellulin shedding in IMPE cells.
IC50 values are 3, 9 and 31 nM for Aurora C, A and B, respectively. Exhibits both in vitro and in vivo activity against human cancer cell lines and tumor xenograft models. Displays additive antiproliferative effects in combination with chemotherapeutics such as carboplatin (Cat. No. 2626), gemcitabine (Cat. No. 3259) and 5-fluorouracil (Cat. No. 3257).
IC50 = 14 nM. Displays selectivity for ASK1 over other kinases including ASK2 (IC50 = 0.51 μM), MEKK1, TAK1, IKKβ, ERK1, JNK1, p38α, GSK-3β, PKCθ and B-raf (IC50 values are > 10 μM). Blocks downstream JNK1/p38 phosphorylation in cells. Orally bioavailable.
IC50 values are 21-69 and 38 nM for CREBBP and EP300 bromodomains respectively. Displays over 40-fold selectivity for CREBBP over BRD4(1). Accelerates FRAP recovery in cells at a concentration of 1 μM.
IC50 values are 52, 57 and 122 nM for human ROCK2, rat ROCK2 and human ROCK1 respectively by ELISA. Inhibits PKAC-α and PRKX (IC50 values are 200 and 325 nM respectively). Exhibits analgesic effects in rat models of inflammatory (AIA) and noninflammatory (MIA) arthritic pain. Orally bioavailable.
IC50 values for the inhibition of human platelet adhesion to type I collagen are 12 and 715 nM for platelets under static conditions and under flow, respectively. Displays selectivity for α2β1 over αvβ3, α5β1, α6β1 and αIIbβ3 at concentrations exceeding 1000 nM. Reduces collagen IV production in mesangial cells. Active in vivo; prevents ferric chloride-induced clot formation in mice.
Displays antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively). Exhibits selectivity for Trk receptors over a range of kinases, with some activity at PDGFR and c-Kit (IC50 values are 0.87 and 0.91 μM respectively). Orally bioavailable.
Non-peptide urotensin-II (UT) receptor antagonist (Ki values are 9.3, 19.1 and 20.7 nM for human, mouse and rat respectively). Displays ≥100-fold selectivity for the human UT receptor over 86 different receptors, ion channels, enzymes, transporters and nuclear hormones.
IC50 = 0.3 μM). Displays no effect on Epac1. Blocks stimulation of the Epac2-FL FRET sensor in HEK293 cells.
Inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and <10 nM respectively). Exhibits no activity at MCT4.
IC50 values are 33 and 34 nM respectively. Suppresses ligand-induced EGFR autophosphorylation and cell proliferation in NCI-H1975 cells containing L858R and T790M mutations. Circumvents mechanisms of resistance to Iressa (Cat. No. 3000) in non-small-cell lung cancer cells.
IC50 = 11 nM in an in vitro kinase assay. Targets the N-terminal kinase domain. Inhibits MSK1, MSK2, PKA, PKB, RSK and p70S6K activity in cells. Blocks IL-10 production in macrophages.
Targets the binding site of the Cdc42 guanine nucleotide exchange factor, intersectin (ITSN). Inhibits Cdc42-mediated cellular effects, including microspike formation in 3T3 fibroblasts and neuronal branching in primary neonatal cortical neurons. Also suppresses cell motility and migration in PC3 cells, without cytotoxic effects.
IC50 < 10 nM. Inhibits both human and mouse FAAH enzymes; also inhibits mouse and human MAGL at higher concentrations (IC50 values are 410 nM and 1.4 μM respectively). Also displays inhibitory activity against FAAH, MAGL and ABHD6 in vivo.
Inhibitor of the mechanosensitive TRP channels; also blocks stretch-activated cation channels in astrocytes, cardiac cells, and smooth and skeletal muscle cells.
Inhibits 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.
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).
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.
IC50 values are 8.9, 1230 and 27354 nM for lysophosphatidic acid 2 (LPA2), LPA3 and LPA1 receptors respectively, in a LPA-elicited calcium mobilization assay.
IC50 = 53 nM for human NaV1.8 channel. Exhibits selectivity for hNaV1.8 over hNaV1.6, hNaV1.7, hNaV1.1, hNaV1.2 and hNaV1.5 (IC50 values are 4.2, 7.0, 11, 16 and 27 μM respectively). Orally bioavailable.
Ki = 1 nM for human CCR1. Exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4. Inhibits MIP-α/CCL3-induced intracellular Ca2+ mobilization. Orally active; effectively reduces disease severity in a rat model of multiple sclerosis. Decreases renal fibrosis in a mouse model of obstructive nephropathy.
IC50 values are 8.9 and 10.1 nM respectively for LRRK2[G2019S] mutant and wild-type LRRK2 respectively. Displays selectivity for LRRK2 against a panel of 460 other kinases. Blocks Ser910 and Ser935 phosphorylation in vitro and in peripheral tissues in vivo. Brain penetrant.
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.
IC50 = 16 nM for human EP2 receptors. Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors; exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 μM. Inhibits PGE2-induced increases in intracellular cAMP; reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM).
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.
Ki = 0.74 nM. IC50 = 1.6 nM. Inhibits substance P-invoked calcium mobilization and outward current (IC50 = 1.3 nM); blocks NK1-mediated nitric oxide-dependent vasodilation in vivo.
IC50 values are 8.5 and 250 nM for IKKβ and IKKα respectively. Selective for IKKα and IKKβ over IKK3, Syk and MAPKKK4 (IC50 values are > 20 μM). Inhibits DNA binding activity of NF-κB. Blocks NF-κB pathway in multiple myeloma cell lines; induces cell growth arrest and apoptosis.
EC50 = 45 nM. Displays no activity at other S1P receptor subtypes (S1P1-3 and S1P5) at concentrations up to 25 μM.
EC50 = 3.3 μM. Does not activate other LPA GPCRs at concentrations up to 10 μM. Antiapoptotic; inhibits activation of caspases 3, 7, 8 and 9, Bax translocation and PARP-1 cleavage. Activates ERK1/2 survival pathway.
IC50 values are 63 and 175 nM for homomeric rat and human ASIC3 channels, and 0.117, 0.9 and 2 μM for heteromeric rat ASIC3/2b, ASIC3/1b and ASIC3/1a channels, respectively. Displays no effect on homomeric ASIC1a, ASIC1b, and ASIC2a channels. Also inhibits NaV1.8 channels (IC50 = 2.6 μM). Analgesic.
KD = 0.06 nM, IC50 = 0.3 nM in a radioactive assay; blocks H3K79 methylation in A431 cells and MCF10A cells (IC50 values are 2.65 and 8.8 nM respectively). Selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro model of leukemia.
EC50 = 4.0 nM. Exhibits 5000-fold selectivity for human S1P1 over S1P3. Displays efficacy in a rat adjuvant-induced arthritis model.
IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay. Exhibits limited off-target effects in kinome profiling of 154 identified lipid and protein kinases and 922 other proteins. Orally effective in a rodent model of inflammatory disease.
Potent kinesin spindle protein (KSP) inhibitor (IC50 = 6 nM); selective for KSP over >250 other receptors and kinases at a concentration of 10 μM. Induces degradation of Mcl-1; exhibits comparable cytotoxic activity to taxol (Cat. No. 1097) in epithelial ovarian cancer cells. Active in vivo.
IC50 values are 11 and 15 nM for Cdk4 and Cdk6 respectively. Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC50 values are > 10 μM). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines. Brain penetrant.
IC50 values are 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N), BRD4 (C), BRD4 (N) and CREBBP respectively. Induces squamous differentiation in NUT midline carcinoma (NMC) cell lines; inhibits tumor growth in NMC xenograft models in vivo. Exhibits reversible contraceptive effects in germ cells from male mice.
IC50 values are 2.3 nM and 1900 nM for OX2 and OX1 respectively. Displays negligible or no inhibition of a panel of 80 receptors. Blocks orexin-B- and orexin-A-invoked calcium mobilization in hOX2-expressing CHO cells (IC50 values are 7.9 nM and 8.8 nM respectively); reverses orexin-B-induced hyperlocomotion in mice. Brain penetrant.
pEC50 values are 7.36 and 7.77 for human and mouse GPR120 respectively. Selective for GPR120 over free fatty acid receptors (pEC50 = 4.19 for FFA1; displays no activity at FFA2 or FFA3). Cell permeable.
IC50 = 2 nM. Also exhibits inhibitory activity against Bruton's tyrosine kinase (BTK) (IC50 = 2 nM). Displays nanomolar potencies in a cell-based IP1 assay and human whole blood assay (IC50 values are 31 and 48 nM respectively).
IC50 = 4.2 μM. Displays little-to-no inhibition of other USP variants or proteases such as caspase, cathepsins and serine proteases; exhibits some activity at USP47. Induces elevated p53 and induces apoptosis in cancer cell lines; displays antiangiogenic activity in vivo.
IC50 = 7 nM. Displays selectivity for mTOR over PI 3-Kα (~100-fold) and PI 3-Kγ (~500-fold). Inhibits phosphorylation of mTORC1 and mTORC2 substrates including S6K, SGK and Akt; blocks VEGF secretion and HIF-1α expression. Exhibits antiproliferative effects in cancer cell lines through G1 cell cycle arrest and selective apoptosis. ATP-competitive.
Ki values are <2, 395, 540 and 852 nM for ERK2, GSK-3, Aurora Kinase A and Cdk2 respectively. Potently blocks proliferation of HT29 cells (IC50 = 48 nM). Orally bioavailable.
IC50 values are 1, 20, and 112 nM for JAK3, JAK2 and JAK1 respectively. Orally active immunosuppressant; exhibits efficacy in rodent rheumatoid arthritis models.
Potent neuropeptide Y (NPY) Y2 receptor antagonist (IC50 = 19 nM).
IC50 values are 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively. Exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5; displays no significant activity at TRPV1, TRPV3, TRPA1 and TRPM8 channels at concentrations up to 22 μM.