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Isoprostanes are a family of prostanoid molecules of non-cyclooxygenase origin. 8-iso PGE1 is an isoprostane which is found in human semen at levels of 7 µg/ml. It is a pulmonary vasoconstrictor in anesthetized dogs with a potency similar to PGF2α.
A benzopyrene derivative that is activated by hepatic cytosol into electrophilic sulfuric acid esters, which are capable of forming covalent DNA adducts and inducing mutations.
An internal standard for the quantification of (2R)-octyl-α-hydroxyglutarate by GC- or LC-MS.
An intermediate in purine metabolism, the product of the rate limiting step in the generation of guanosine monophosphate, which is important for DNA, RNA, and glycoprotein synthesis.
An analog of PGE1.
A benzoquinone ansamycin antibiotic which binds Hsp90 and its paralog GRP94; indirectly affects diverse cellular processes, including gene expression, cell proliferation, apoptosis, and angiogenesis; inhibits c-jun expression in HT29 cells (IC50 = 75 nM); shows promise in cancer therapy.
A VCP inhibitor (IC50 = 24 nM) that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases, Hsp90, and 53 additional analyzed kinases (IC50s >10 μM). It has been shown to inhibit the proliferation of HCT116 cancer cells with an...
A novel apelin receptor agonist (EC50 = 3.7 μM) that is >21-fold selective over the closely related angiotensin I receptor (EC50 = >79 μM).
A potent, selective inhibitor of Cdk9 in vitro (IC50 = 0.35 µM); a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 µM, respectively.
A selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.
Single stereoisomer of FTY720-phosphate formed in vivo; exhibits Ki values of 2.1, 5.9, 23, and 2.2 nM for S1P1,3,4,5, respectively, which are 5-130-fold lower than those observed for the FTY720 (R)-phosphate
A synthetic intermediate useful for pharmaceutical synthesis.
An inactive metabolite of PGE2 formed by 15-hydroxy PGDH PGs inactive.
A selective inhibitor of VEGFR2 (aka FLK1; IC50 = 700 nM), having negligible activity at several other serine/threonine and tyrosine kinases; effectively blocks signaling through VEGFR2 both in vitro and in vivo.
A PARP inhibitor and insulin sensitizer; blocks self-ADP-ribosylation of nuclear PARP (Ki = 57 µM) and mono-ADP-ribosylation of GRP78; acts as a co-inducer of Hsp72, augmenting expression induced by Hsf1 in adipocytes and skeletal muscles and improving insulin sensitivity.
Causes concentration-dependent changes in cell shape and actin organization; sequesters G-actin and prevents F-actin assembly; binds monomeric actin with 1:1 stoichiometry and can be used to block actin polymerization both in vitro and in cells (Kd = 60 nM).
An immediate precursor to cholesterol in the Bloch pathway of cholesterol biosynthesis; reported to activate liver X receptor-target genes in both the liver of cholesterol-free mice and in cholesterol-starved macrophage foam cells in atherosclerotic lesions.
Reacts with aldehydes, ketones, and carbonyls, including stress compounds such as glyoxal and methylglyoxal, to produce highly fluorescent benzimidazole derivatives.
The inactive isomer of omeprazole, a gastric proton-pump inhibitor; its hydroxylation is mediated stereoselectively by CYP2C19.
The EP4 receptor is one of four GPCRs that mediate the actions of prostaglandin E2 (PGE2). The diverse effects of PGE2 acting via EP4 receptors point to the need to identify novel agonists and antagonists, both to further elucidate the function of this receptor subtype and for use as therapeutics...
The main component (>80%) of the anthelmintic, ivermectin; binds to glutamate-gated chloride channels, inducing irreversible channel opening (EC50 = 104 nM).
A potent inhibitor of iNOS (IC50 = 0.20 μM), with over 1,000-fold selectivity compared to eNOS (IC50 = 350 μM).
Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM. Iloprost...
HDAC1 and HDAC3 inhibitor (ID50 = 0.01 and 0.07 μM, respectively, in vitro); induces apoptosis in nine different neuroblastoma cell lines in culture (0.5-4.0 μM) and completely suppresses neuroblastoma tumor growth in SCID mice at 200 mg/kg.