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Glutathione (GSH) is a low molecular-weight tripeptide thiol that serves as a primary cellular anti-oxidant and plays a fundamental role in the elimination of environmental toxins. During early apoptosis, cells may exclude GSH, causing a decrease in intracellular GSH levels. The intracellular level...
An amphipathic CoQ10 homolog that has a tail consisting of five isoprene units. It has been used as an electron acceptor to study a range of oxidoreductases as isolated enzymes, in subcellular fractions, in intact cells in culture, and in perfused organs.
A second generation antiepileptic compound used to prevent convulsions in a variety of settings; binds the synaptic vesicle protein SV2A (pIC50 = 5.7), presumably altering vesicle exocytosis; alters the metabolism and turnover of GABA.
A DYRK1B inhibitor (IC50 = 17 nM) that demonstrates 5-fold and 110-fold selectivity against the related family members DYRK1A and DYRK2, respectively; used as a probe to elucidate the mechanism of DYRK1B regulation of cell cycle progression.
A potent inhibitor of the STAT3/JAK signaling pathway; suppresses levels of tyrosine phosphorylated STAT3, STAT3 DNA binding and STAT3-mediated gene transcription; suppresses tumor growth in vivo.
A selective, cell-permeable, reversible inhibitor of MKLP-2 (IC50s = 0.83-1.35 μM); treatment with 10-50 μM results in binucleated cells, perturbing relocation of Aurora B kinase and survivin to the central spindle in anaphase cells without affecting microtubule polymerization.
A potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50 = 2, 8, 20, 26 nM for DNA-PK, p110α, mTORC1, and PI3-KC2β, respectively).
A cell-permeable inhibitor of the dimerization of c-Myc and Max at 64 µM, preventing c-Myc-dependent gene expression and cell proliferation; induces cell cycle arrest, apoptosis, and myeloid differentiation at 100 µM in human acute myeloid leukemia cells; inhibits the nuclear Myc...
A skeletal muscle relaxant that depresses excitation-contraction coupling in skeletal muscle by binding to the type 1 ryanodine receptor and decreasing free intracellular calcium concentration; inhibits L-type currents in developing myotubes by shifting the voltage-dependence of skeletal L-type Ca2+...
Pranlukast (ONO-1078) is a potent, selective and orally active CysLT1 receptor antagonist. Sold under the trade name Ultair, it was the first cysteinyl (peptidyl) leukotriene receptor antagonist (LTRA) marketed for the treatment of asthma. Clinical studies in Japan, Europe, and North America all...
Inhibitor of Cdk1/cyclin B and Cdk/p25 (IC50s = 600 and 400 nM, respectively).
L-NMMA is a relatively non-selective inhibitor of all NOS isoforms. It is the archetypal NOS inhibitor to which other inhibitors are most often compared. The Ki values for nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 0.18, 0.4, and 6 µM, respectively.
Peptide Sequence: human LPA1 amino acids 342-359 To be used in conjunction with Cayman’s LPA1 polyclonal antibody (Catalog No. 10005280) to block protein-antibody complex formation during immunochemical analysis of LPA1.
Capsaicin is the primary active component of the heat and pain-eliciting lipid-soluble fraction of the Capsicum pepper. Capsaicin is present in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in...
A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC50 = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a...
A selective PHGDH inhibitor that blocks serine synthesis from 3-phosphoglycerate in cells (IC50 = 3.7 µM); reversibly blocks the production of glucose-derived serine in cells.
A selective IDO1 inhibitor (IC50 = 7.1 nM in HeLa cells); promotes T and natural killer-cell growth, increases IFN-γ production, and reduces conversion to Treg-like cells in a coculture system of human allogeneic lymphocytes with either dendritic cells or tumor cells; inhibits tumor...
An NSAID, non-selective COX inhibitor, being marketed as an analgesic to manage postoperative pain as well as an ophthalmic solution to treat ocular pain and inflammation; inhibits COX-1 and COX-2 (IC50s = 20 nM) in vivo.
A partial agonist of the GABAA receptor that acts at the benzodiazepine binding site, dose-dependently stimulating GABA currents with a threshold of 0.3-1.0 µM; displays a broad spectrum of anticonvulsant activity in diverse seizure and epilepsy models without a tendency toward tolerance or...
Pyrimidine-4-carboxylic acid (sodium salt) is a synthetic intermediate useful for pharmaceutical synthesis.
EPZ020411 is an inhibitor of protein arginine methyltranferase 6 (PRMT6; IC50 = 10 nM) that less potently targets PRMT1 and PRMT8 (IC50s = 119 and 223 nM, respectively). It dose-dependently decreases methylation of the PRMT6 substrate H3R2 in A375 cells transiently expressing...
An IDH1 inhibitor.
Cayman’s MTT Proliferation Assay provides an easy to use tool for studying the induction and inhibition of cell proliferation in any in vitro model. This kit will also allow investigators to screen drug candidates involved in cell cycle regulation. In this assay, MTT is taken up by cells and...
Structurally identical to C-6 NBD ceramide, but contains a saturated bond in the C4-C5 position of the sphingosine backbone.