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A dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC50s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively); improves glucose homeostasis in diet-induced insulin resistant mice.
A fungal mycotoxin that inhibits the Lys9-specific histone methyltransferases SU(VAR)3-9 (IC50 = 0.8 μM), G9a (IC50 = 2.5 μM), and DIM5 (IC50 = 3 μM).
An aminoglycosidic antibiotic that is commonly used for the selection of genetically engineered cells neo neon toxic prokaryotic genes eukaryotic cells.
CGRP is a 37 amino acid peptide synthesized in the central and peripheral nervous system from a calcitonin/CGRP gene complex. Two isoforms have been described which differ by three amino acids and display similar biological activities: CGRP-α, which is produced by alternative splicing of a...
A synthetic intermediate useful for pharmaceutical synthesis.
11β-PGF2α is the primary plasma metabolite of PGD2 in vivo, the levels of which can increase from 6 pg/ml in a normal healthy volunteer to 490 ng/ml in patients with systemic mastocytosis. The normal human urinary excretion of 11β-PGF2α is about 11 ng/mmol creatinine (~400...
A cell-permeant inhibitor of CK1 (IC50 = 200 nM from S. pombe, 300 nM for CK1δ); only weakly affects the activities of a panel of kinases tested.
A dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 µM; restores the chemosensitivity of taxane-resistant cells to paclitaxel; orally bioavailable, inhibiting FAK and augmenting paclitaxel action against ovarian cancer cell tumors in...
An internal standard for the quantification of DGLA by GC- or LC-MS.
A potent, selective, brain permeable inhibitor of GSK3α and GSK3β (Kis = 6.9 and 31 nM, respectively); shows good bioavailability after oral administration in vivo, inhibiting hippocampal tau phosphorylation and reversing cognitive deficits induced by the NMDA receptor antagonist MK-801.
The racemic version of a minor CYP450 metabolite of arachidonic acid with stereospecific effects on renal function; 16(R)-HETE dose-dependently stimulates vasodilation of the rabbit kidney while 16(S)-HETE potently inhibits proximal tubule ATPase activity.
A BLT1 receptor antagonist with a Ki value of 159 nM on guinea pig lung membranes; does not antagonize the binding of [3H]-LTB4 to the human BLT2 receptor.
PGH1 is a COX metabolite of DGLA and is the precursor to all 1-series PGs and thromboxanes. PGH1 is a suicide inhibitor of platelet thromboxane synthase with a Ki of 28 µM.
A cell-permeable STAT3 activator (EC50 = 2 nM) that is more than 28,000-fold selective for STAT3 over STAT1 and NF-κB; increases the expression of BCL3, a known STAT3-dependent oncogene, and enhances STAT3 activation by the pro-inflammatory cytokine IL-6.
A selective inhibitor of BAZ2A (Kd = 109 nM; IC50 = 130 nM) and BAZ2B (Kd = 170 nM; IC50 = 180 nM) bromodomains.
Aldosterone, a steroid hormone secreted by the adrenal cortex, is the principle mineralocorticoid controlling sodium and potassium balance. Serum aldosterone levels in normal upright adult individuals are generally less than 300 pg/ml. Only a fraction of urinary aldosterone is excreted intact, thus...
A natural fungal metabolite which reversibly interferes with protein trafficking and secretion mediated by the Golgi apparatus and endoplasmic reticulum; directly and reversibly inhibits Sec7 domain-containing GEFs which are necessary for Arf activation associated with vesicular transport (IC50 =...
A second generation histamine H1 receptor antagonist (IC50 = 1.3 nM) and mast cell stabilizer; inhibits the quick phase reaction in a rat antigen-induced immediate airway response model.
Antigen: human hepsin amino acids 241-260 Host: rabbit Cross Reactivity: (+) human hepsin; other species produce bands of unknown identity Application(s): IHC (formalin-fixed paraffin-embedded tissue) and WB Hepsin is a type II membrane-associated protein that has an extracellular proteolytic domain...
An unsaturated fatty acid found in royal jelly produced from the hypopharyngeal and mandibular gland secretions of honeybees; isolated in conjunction with 10-HDA (Item No. 10976) and both demonstrate weak estrogenic activity, inhibiting binding of 17β-estradiol (Item No. ISO60155) to estrogen...
A natural alkaloid with antiviral properties, inhibiting the replication of hepatitis B alone and in combination with lamivudine; prevents fibrosis in a number of organs including liver, at least in part by interfering with TGF-β signaling.
PGD2 is synthesized by H-PGDS in mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. H-PGDS is therefore a key target for development of selective, potent inhibitors for therapeutic use against these diseases. Cayman’s H-PGDS FP-Based Inhibitor Screening...
An internal standard for the quantification of 2-AG by GC- or LC-MS.
A cannabidiol analog with close structural similarity to O-1918, a selective antagonist of abnormal cannabidiol (Abn-CBD) at the non-CB1/CB2 endothelial receptor; O-1918 does not bind to CB1 or CB2 receptors at concentrations up to 30 µM and inhibits the vasorelaxant effects of Abn-CBD in...