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IC50 = 56 nM. Induces increased mitotic abnormalities and mitotic delay. Cell permeable and active in vivo.
IC50 = 0.023 μM. Selective for PFKFB3 over PFKFB2 and PFKFB1 isoforms (IC50 values are 0.382 μM and 2.06 μM, respectively). Reduces levels of fructose-1,6-bisphosphate in A549 cells (IC50 = 0.343 μM). Exhibits no significant inhibition of other kinases.
IC50 = 295 nM. Reduces cell number and increases accumulation of binucleated MCF-1 cells. Enhances cell apoptosis in combination with chemotherapeutics. Also inhibits P1 3-Kδ and P1 3-Kγ kinases (IC50 values are 856 and 867 nM, respectively) and mTOR kinase (IC50= 5.56 μM).
IC50 = 38 and 113 nM in Ba/F3 cell lines containing leukemia-associated D163E and R806Q mutations, respectively. Blocks phosphorylation of TNK2 receptors containing solid-tumor type truncation mutations.
IC50 = 3.58 - 60.3 μM. Increases apoptosis in human cancer cell lines. Reduces senescence and increases lifespan in mouse models of ageing (kl/kl). Inhibits L-NAME (Cat.No. 0665) induced systolic blood pressure increases, telomere length reduction and hypertrophy in mice. Renoprotective. Orally bioavailable.
EC50 values are 20 and 18 nM for rat and human, respectively. Selective for hα4β2 over hα3β2, hα3β4 and hα7. Inhibits (α4)2(β2)3, muscle-type and Torpedo nAChRs (IC50 values are 0.5, 0.7 and 0.2 μM, respectively), but not (α4)3(β2)2 receptors. Exhibits ability to photoincorporate into aliphatic and nucleophilic amino acid side chains.
IC50 values are 1.3, 2.4, 85.8, 2,133 and 9,276 nM for ALK2, ALK1, ALK3, ALK4 and ALK5, respectively. Exhibits selectivity for ALK2 over ALK4 and ALK5 in cellular assays. Inhibits heterotopic ossification in a mutant ALK2 mouse model of fibrodysplasia ossificans progressiva. Also exhibits activity against RIPK2, ABL1 and PDGFR-β (IC50 values < 100 nM).
Cell penetrant Proteolysis Targeting Chimera (PROTAC) compound based on (+)-JQ1 (Cat.No. 4499), conjugated to a von Hippel-Lindau (VHL) ligand. Retains high affinity for BRD2, BRD3 and BRD4 bromodomains (Kd = 13-60 nM) but induces preferential degradation of BRD4 over BRD2 and BRD3 in cells at 10-100 nM concentrations. Exhibits potent cytotoxicity and profound antiproliferative effects in AML cell lines. Negative control cis MZ 1 also available.
Kd = 80-90 nM. Blocks interaction between VHL and HIF-α downstream of HIF-α hydroxylation, initiating hypoxic response. Results in time and concentration-dependent accumulation of hydroxylated HIF-α, and upregulates mRNA and protein levels of HIF target genes. Cell permeable. Negative control cis VH 298 also available.
Inhibits NCX activity in canine cardiac sarcolemmal vesicles, rat cardiomyocytes, cultured neurons, astrocytes and microglia (IC50 values are 90, 92, 33, 5 and 8.3 nM, respectively). Reduces infarct volumes and exhibits protective effects against myocardial ischemia in rats.
Kd values are 2, 2 and 3 nM at RARα, RARβ and RARγ, respectively. Does not bind retinoic X receptors.
IC50 = 1.3 nM. Selective for DDHD2 over 40 other serine hydrolases, but does exhibit cross-reactivity with ABHD6. In vivo active. Increases brain triacylglycerol levels in mice.
IC50 = 210 nM. Inhibits the formation of mature IL-1β. Indirectly inhibits NLRP3. Active in vivo and orally bioavailable.
Supplied as NHS ester. Non-fluorescent until activated at 365 nm. Photochemical quantum yield of uncaging = 2.2%, with improved yield upon protein conjugation. Compatible with self-labeling tag systems. Suitable for single molecule tracking and super resolution microscopy in live cells. Can be multiplexed with PA Janelia Fluor™ 646, SE (Cat. No. 6150) to perform two-colour sptPALM in live cells. Cell permeable. Excitation maximum = 551 - 553 nm; emission maximum = 570 - 573 nm.
IC50 = 30 nM. Selective over all other AAA ATPases, HSP90 and kinases tested (IC50 >10 nM). Activates the unfolded protein response (UPR), and modulates autophagosome maturation. Exhibits antiproliferative activity in cancer cells in vitro. Reduces VCP-sensitaisation to trypsin digestion.
Rapidly and efficiently releases glutamate (Cat. No. 0218) when photolysed (350 - 365 nm excitation). Water soluble and stable at neutral pH, and pharmacologically inactive at neuronal glutamate receptors (up to 200 μM). 5.5 times more photosensitive than MNI-caged L-glutamate (Cat. No. 1490). Laser activation of MDNI-glu evokes a rapid increase in intracellular Ca2+ concentration in astrocytes.
IC50 = 4 nM. Selective for PRMT5 over a panel of other PRMTs and lysine methyltransferases. Inhibits proliferation of mantle cell lymphoma (MCL) in vitro.
IC50 = 1 nM. Attenuates oxaliplatin-induced NF-κB activation, increases oxaliplatin cytotoxicity, and potentiates oxaliplatin-induced apoptosis in AIPC cells. Reduces the numbers of infiltrating neutrophils into both in vitro and in vivo tumor models. Orally bioavailable.
Selectively traces exocytosis in dopaminergic neuronal cell culture and brain tissue. Excitation and emission maxima are 352 and 451 nm, respectively.
IC50 = 0.7 nM. Inhibits proliferation of Karpas-422 cells (non-Hodgkin's lymphoma) in vitro, halts tumor growth and reduces intratumoral H3K27Me3 levels in mice.
IC50 = 0.93 nM. Exhibits >3,000-fold selectivity for S1P1 over S1P2, S1P3, S1P4 and S1P5. Induces lymphocyte sequestration in peripheral lymph nodes and upregulates S1P1 receptor expression. Reduces disease severity in mice with EAE. Increases IFN-α production in stimulated dendritic cells in vivo.
IC50 = 15 nM. Exhibits >60-fold selectivity for mTOR over PI 3-kinases and is inactive against a panel of other kinases. Inhibits growth of ER-positive MCF7 breast cancer cells in vitro (EC50 = 8.5 nM). Cell permeable.
IC50 = 1.3 nM; Kd = 2.7 nM. Inhibits proliferation and anchorage-independent growth of a panel of tumor cell lines in vitro. Suppresses growth of human HCT116 and A549 tumor cell xenografts in mice.
EC50 = 60 nM. Reduces plasma glucose levels in an oral glucose tolerance test in ob/ob mice.
Enhances AMPA receptor-mediated excitatory post-synaptic potentials in the CA1 region of hippocampal slices. Decreases intracellular D-serine (a NMDA co-agonist) concentrations in PC-12 cells (IC50 = 0.68 nM). Exerts antidepressant effects in mice.
Kd values are 33 and 340 nM, respectively. Exhibits >30-fold selectivity for BRD9 over other bromodomains except BRD7. Cell permeable and active in vivo
Inhibits c-Raf, wild type B-Raf and mutant B-Raf (V600E). Cytotoxic in certain melanoma cells lines. Effects enhanced by protein kinase D3 inhibition, preventing reactivation of MAPK signaling and increasing caspase activity. Orally bioavailable.
pEC50 values are 7.06-9.50 at hCTa, 8.11 at rCTa, 7.73-10.1 at hAMY1a, 9.74 at rAMY1a, 7.92 at hAMY1b, 7.78-9.9 at hAMY2a, 7.94 at hAMY2b, 8.09-10.8 at hAMY3a, 9.97 at rAMY and 8.19 at hAMY3b receptors. Suppresses insulin-stimulated glucose uptake. Delays gastric emptying and promotes satiety. Active in vivo.
EC50 = 6.4 nM. Binds heme-free sGC. Exhibits antihypertensive effects in vivo.
Enhances iPSC reprogramming four-fold and accelerates the appearance of iPSC colonies in combination with 4F (Oct4, Sox2, c-Myc and Klf4). Also induces cardiomyocyte-like cells from human fibroblasts, as part of the 9C cocktail (CHIR 99021, A83-01, BIX 01294, AS83541, SC1, Y-27632, SU 16f, JNJ10198409 and OAC-2)