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A synthetic hexapeptide with an acetylated amino terminus and an amidated carboxyl terminus that inhibits the binding of CXC chemokines to the chemokine receptor CXCR2; inhibits IL-8 binding to neutrophils (Ki = 2.7-13 µM), prevents neutrophil chemotaxis and β-glucuronidase release, and...
A pan-antagonist of LPA1-3 receptors (IC50 = 10, 5.5, and 3.1 µM, respectively)
Immunogen: peptide from an internal region of ovine COX-1 Host: rabbit Cross reactivity: (-) ovine, human, and mouse COX-2 Species reactivity: (+) ovine seminal vesicle, human, bovine endothelial, and porcine COX-1 Applications: WB, ICC, IHC
An inhibitor of FAAH attenuating the FAAH activity from mouse neuroblastoma cells with an IC50 value of 12 µM; alters both the Km and the Vmax of FAAH, indicating that it is a very tight binding, competitive inhibitor; does not inhibit cPLA2 and is essentially devoid of...
A DNA-intercalating antitumor agent that forms covalent adducts in DNA after being enzymatically activated with CYP3A4, CYP1A1, or CYP1A2 or by peroxidases in target tissues; inhibits the proliferation of human breast adenocarcinoma, leukemia, neuroblastoma, and glioblastoma cells (IC50s...
An inhibitor of γ-secretase, blocking the production of total Aβ in human primary neuronal cultures with an IC50 value of 115 nM and Aβ42 with an IC50 value of 200 nM; reduces brain levels of Aβ in vivo when given orally; indirectly inhibits Notch,...
A selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 µM for rat A1 and A2A receptors, respectively).
2-Aminopyrazine is a synthetic intermediate useful for pharmaceutical synthesis.
A stable, cell-permeable analog that blocks calcium release evoked by cADP-ribose in sea urchin egg homogenates with an IC50 value of 1.7 µM; commonly used to investigate intracellular signaling through cADP-ribose in isolated cells and tissues.
A prenylflavonoid with potent estrogenic activity that inhibits both ERα and ERβ (IC50s = 57 and 68 nM, respectively); effective in vivo, suppressing bone loss and temperature changes in rat models of osteoporosis and postmenopausal hot flashes.
LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms). It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several...
Antigen: human SOAT-2/ACAT-2 amino acids 3-20 Host: rabbit Cross Reactivity: (+) human, mouse, ovine, porcine, and rat SOAT-2/ACAT-2 Application(s): ICC, IHC, and WB SOAT-2/ACAT-2 catalyzes the formation of cholesterol esters from cholesterol and long chain fatty acyl-CoA.
Betamethasone is a synthetic corticosteroid.{64715} In vivo, betamethasone (5 mg/kg) reduces bronchoalveolar lavage fluid (BALF) matrix metalloproteinase-2 (MMP-2) and MMP-9 activities, TNF-a levels, and neutrophil number in a mouse model of LPS-induced lung injury. Prenatal administration of...
An aminoglycoside antibiotic that inhibits protein translation by binding to the small subunit of prokaryotic ribosomes; commonly used for the prevention of bacterial contamination of cell cultures.
A natural metabolite formed by CYP450-mediated hydroxylation followed by catechol-O-methyltransferase (COMT) methylation of estradiol; has anticancer agent activity as an angiogenesis inhibitor via the HIF-1α pathway; levels are significantly lower in women with severe pre-eclampsia.
A fluorescent probe commonly used to measure pH.
An ATP-competitive inhibitor of JNK1, JNK2, and JNK3 (IC50s = 150, 220, and 70 nM, respectively); effective in vivo in gerbils, mice, and rats via oral, intravenous, or intraperitoneal administration.
AL 8810 is an 11β-fluoro analog of PGF2α which acts as a potent and selective antagonist at the FP receptor. AL 8810 has weak intrinsic agonist activity on FP receptor preparations in the 200-300 nM range, yet it fully antagonizes the activity of the potent FP receptor agonist...
An inhibitor of PDGF-BB tyrosine kinase with an IC50 value of 4.2 nM when tested in human coronary artery smooth muscle cells.
Nitration product of oleic acid in vivo mediated by peroxynitrite, acidified nitrite, or myeloperoxidase (in the presence of H2O2 and nitrite).
An ATP-competitive inhibitor of Cdk1, 2, 4, 5, 6, and 9 with IC50 values of 210, 47, 100, 13, 170, and 50s = 40-940 nM in vitro) and human tumor xenograft models, inhibiting cell cycle progression and inducing apoptosis.
Source: recombinant N-terminal hexahistidine-tagged protein expressed in E. coli Mr: 19.3 kDa Protein concentration: 0.5 mg/ml
A long-chain N-acylated HSL that functions as a signaling molecule in the quorum sensing of A. vitis.
A selective PI3K inhibitor with an IC50 value of 1.4 µM.