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An analog in the enniatin complex; induces apoptosis in cancer cells (EC50 = 5 µM in H4IIE rat hepatoma cells), decreasing the activation of ERK (p44/p42) and inhibiting TNF-α-induced NF-κB activation.
A thiazolinone compound that directly inhibits 5-LO product formation in intact polymorphonuclear leukocytes and a soluble fraction of a S100 PMNL cell lysate (IC50s = 0.28 and 0.09 μM, respectively).
A diamidine that is cytotoxic to protozoa; affects a variety of enzymes and modulates interactions between nucleic acids and proteins; inhibits diamine oxidase with a Ki value of 13 nM; enhances the enzymatic activity of ACE2.
Antigen: synthetic peptide from human cRBP7 amino acids 125-134 (QVCKQTFQRA) Host: rabbit Cross Reactivity: (+) human, mouse, rat, and African green monkey cRBP7; other species not tested Applications: WB and IHC
Produced from Ins(1,2,3,5,6)P5 via a minor enzymatic phytate degradation pathway by K. terrigena; moderately effective in opening calcium channels relative to Ins(1,4,5)P3.
A potent inhibitor of HDACs (IC50 = 15.7 nM); has been shown to alter the expression of several genes whose products are involved in cell morphology, motility, apoptosis, and cell cycle control, reducing the proliferation of cancer cells.
A resorcylic acid lactone with antiviral and antiprotozoan activity; used as negative control for MAPKKK inhibitor (5Z)-7-oxo zeaenol (Item No. 17459).
Antigen: human ARC amino acids 191-208 Host: rabbit Cross Reactivity: (+) human and mouse ARC Application(s): IP and WB ARC interacts with caspase-2 and -8 and inhibits enzymatic activity of caspase-8. ARC suppresses apoptosis induced by cell death adapters FADD and TRADD and by cell death receptors...
A natural mycotoxin and selective inhibitor of PP2A (IC50 = 170 nM); causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts.
Prostaglandin D2 (PGD2) is biosynthesized in the brain by soluble, glutathione-independent lipocalin-type PGD2 synthase. PGD2 accumulates in the cerebrospinal fluid (CSF), where it induces physiologic sleep in rats and humans. PGD2 is also synthesized in mast cells and leukocytes by a cellular,...
A potent, selective, and cell-permeable inhibitor of Raf-1 (IC50 = 9 nM); blocks phosphorylation of ERK1/2 by 90% in cells stimulated with EGF when given at 5 µM; shows more than 100-fold selectivity for Raf-1 versus several related kinases.
A peptide hormone known best as a vasoconstrictor with central roles in chronic hypertension, heart failure, and stroke.
Peptide contains a lysine at position 20 which is a substrate or acceptor peptide for the lysine methyltransferases KMT5A (SET8) and KMT5B (SUV4-20H1).
trans-BTP Dioxolane is a PAF receptor antagonist. This compound demonstrates competitive antagonism of PAF in a rabbit washed platelet assay (Ki = 0.3 µM).
PGD2-biotin is an affinity probe which allows PGD2 to be detected through an interaction with the biotin ligand. It was designed to allow PGD2 to be detected in complexes with transmembrane receptors and/or nucleic acid or protein binding partners. It is thus a tool to be used in the general...
A relatively non-selective inhibitor of all NOS isoforms with Ki values 0.18, 0.4, and 6 µM for nNOs (rat), eNOS (human), and iNOS (mouse), respectively.
An inverse agonist of LRH-1 (IC50 = 3.7 µM) with maximum efficacy of 64% repression; inactive at the related SF1 transcriptional activator; alters the expression of haptoglobin, SAA1, and SAA4, induces the death of ER negative MDA-MB-231 breast cancer cells, and inhibits the StAR...
A dibenzoxazepine which acts as a selective antagonist of PGE2 at the human EP1 receptor (IC50 = 6.7 µM); at doses between 0.3-300 µM, is a competitive antagonist of PGE2-induced smooth muscle contractions of guinea pig ileum and stomach and trachea.
A natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC50 = 11.5 and 4.9 μM, respectively).
A nitroimidazole with radiosensitizing and antineoplastic properties; metabolites accumulate in hypoxic cells and can themselves be cytotoxic or they can increase the chemosensitivity and radiosensitivity of the target cells; used in the imaging of hypoxic regions in tumors and in the cardiovascular...
5(S)-HETE lactone is a cyclic ester formed by acid-catalyzed nucleophilic addition of the C-5 hydroxyl to the C-1 carboxyl of 5(S)-HETE. The ability of (±)5-HETE lactone to inhibit RBL-1 cell 5-LO (IC50 = 27 µM) may be entirely due to the 5(S) isomer, but the enantiomers have...
A full agonist of 5-HT2C receptors (Ki = 3.3 nM) that is ~6-fold less potent at 5-HT2A receptors (Ki = 18 nM) and 20-fold less potent at 5-HT2B receptors (Ki = 60 nM); produces dose-dependent decreases in food intake in 24-hour fasted normal Sprague-Dawley rats, diet-induced obese mice, and obese...
A natural isothiocyanate that has antioxidant, anti-inflammatory, and anti-carcinogenic effects.
A selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.