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An inhibitor of MTTP (IC50 = 8 nM in vitro) that has been shown to reduce the production of apolipoprotein B, thereby lowering LDL cholesterol levels, in both preclinical and clinical homozygous familial hypercholesterolemia studies.
EPIT is a selective, competitive inhibitor of nNOS having a Ki of 0.32 µM for the purified human enzyme. EPIT exhibits 115-fold and 29-fold selectivity for nNOS compared to iNOS and eNOS, respectively. It exhibits reduced inhibitory potency in whole-cell assays, possibly due to reduced...
A nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (Ki = 3.7 nM); a partial agonist of PPARγ, activating the receptor to 25-30% of that produced by the full agonist rosiglitazone (EC50 = 4.5 μM); potently...
A selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/neu (IC50 = 0.35 µM).
Immunogen: peptide from the N-terminal region of human NAPE-PLD Host: rabbit Species Reactivity: (+) human, mouse, rat, and bovine NAPE-PLD Application(s): WB NAPE-PLD catalyzes the hydrolysis of NAPE to form N-acylethanolamines (NAEs), which are involved in diverse biological processes such as...
Arachidonic acid-biotin was designed to allow arachidonic acid to be detected in complexes with protein binding partners such as fatty acid binding proteins (FABPs). It is thus a tool to be used in the general elucidation of the signaling and transport of free arachidonic acid.
Microcystins are hepatotoxic cyclic heptapeptide toxins produced by cyanobacteria. They are responsible for periodic poisonings of humans and livestock drinking fresh water where the blue-green algae are endemic. Microcystin-LR is a selective inhibitor of protein phosphatase 2A (PP2A) (IC50= 0.04...
A cell permeable, ATP-competitive inhibitor of the four vertebrate isoforms of RSK, RSK1-4 (IC50s = 31, 24, 18, and 15 nM, respectively); also significantly inhibits PLK1, Aurora B, MELK, and MST2 at 100 nM.
A selective, orally bioavailable, mechanism-based inactivator of LSD1/CoREST activity; enhances H3K4 methylation, increasing the expression of tumor-suppressor genes and preventing growth of AML cell lines (EC50s = 2-240 nM).
An internal standard for the quantification of PGD1 by GC- or LC-MS.
ω-3 Arachidonic acid-d8 contains eight deuterium atoms at the 8, 9, 11, 12, 14, 15, 17, and 18 positions. It is intended for use as an internal standard for the quantification of ω-3 arachidonic acid by GC- or LC-MS.
An NSAID that displays slight preferential inhibition for COX-2 (IC50s = 1.3 and 0.34 μM for COX-1 and COX-2, respectively); also inhibits bradykinin-induced nociceptive responses by blocking the activation of PKC.
9-deoxy-9-methylene PGE2 is a stable, isosteric analog of PGE2. 9-deoxy-9-methylene PGE2 retains the biological profile of PGE2 with fewer side effects. In the rat 9-deoxy-9-methylene PGE2 is equipotent to PGE2 in decreasing blood pressure. It also stimulates the gerbil colon and primate uterus at...
Features Each vial contains a mixture of standards packaged in amber ampules purged with argon >1 ml provided at the concentration specified in the insert Designed for direct snap and inject use in mass spectrometry applications Ideally suited for method development and as a system suitability...
A minor tobacco alkaloid that can also be found in a variety of other plants that are commonly eaten, including maize, rice, and potato; weakly binds to neuronal acetylcholine receptors (Ki = 3.3 µM).
A major adduct formed by the reaction of 4-HNE with GSH; 4-HNE-GSH levels in liver, plasma, or isolated cells can serve as biomarkers for oxidative stress.
A derivative of aminoacridine that functions as an inhibitor of both AChE and butyrylcholinesterase; used clinically in the treatment of Alzheimer’s disease; inhibits the uptake of serotonin and noradrenaline in rat cerebral cortex and decreases depolarization-induced calcium influx through...
An inhibitor of PDKs, resulting in an increase in PDH activity (EC50 = 5.2 nM for PDK2); less potently inhibits PDK1 and PDK3 (IC50s = 87 and 600 nM, respectively).
An NSAID commonly used in animals to combat pain and inflammation, particularly as associated with osteoarthritis; inhibits both COX-1 and COX-2 (IC50s = 22.3 and 3.9 µM, respectively) and also FAAH (IC50 = 74 µM).
A cell permeable inhibitor of α-ketoglutarate-dependent enzymes, including JMJD2A, JMJD2C, and JMJD2E (IC50s = 250, 500, and 24 μM, respectively); inhibits the prolyl hydroxylase domain-containing proteins PHD1 and PHD2 with IC50 values of 2.1 and 5.6 μM,...
2-O-ethyl PAF C-16 is a synthetic PAF analog which contains an ethyl group, attached by an ether linkage, at the sn-2 position. It is a less potent agonist than methylcarbamyl PAF C-16 in the induction of platelet aggregation in both human and rabbit PRP. 2-O-ethyl PAF C-16 causes aggregation of...
A tumor-inhibiting antibiotic that inhibits the glutamine-dependent amidotransferases involved in nucleotide biosynthesis, N-formylglycineamidine ribotide synthetase and glucosamine-6-phosphate isomerase; also inhibits the hexosamine biosynthetic pathway, which has been shown to protect against...
A DHA epoxygenase metabolite detected in rat brain and spinal cord, as well as human serum, that acts as a substrate for sEH (Km = 5.1 µM); demonstrates antihyperalgesic activity in inflammatory and neuropathic pain models and potently inhibits angiogenesis and tumor growth in in vitro assays.