Cayman Chemical

A synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki = 2.3 nM).

A highly selective EP3 receptor antagonist with Ki values of 0.3, 916, >5,000, and >5,000 nM at EP3, EP4, EP1, and EP2, respectively; blocks the EP3 agonist activity of sulprostone on guinea pig vas deferens and trachea.

An inhibitor of HMG-CoA reductase.

A competitive antagonist of TRPV1 which blocks the capsaicin-induced uptake of Ca2+ in neonatal rat dorsal root ganglia (IC50 = 0.42 µM) and Chinese hamster ovary cells (IC50 = 17 nM); does not block acid- or heat-induced activation of TRPV1 and may block receptors other than TRPV1.

A number of 17-aryl trinor and 16-aryloxy tetranor PGF2α derivatives have been approved for the treatment of glaucoma. These “ring” prostaglandin analogs have improved efficacy over the prostaglandins with an n-alkyl lower side chain. Of these, the ones wherein the 13,14-double...

A non-reducing inhibitor of 5-LO that shows selectivity for 5-LO over 12-LO or COX; inhibits topoisomerase II activity and arrests cell cycling or induces apoptosis in cancer cells.

A FAHFA in which stearic acid occurs at the 9-position of hydroxy stearic acid.

A more stable form of (±)14(15)-EET used for long-term storage that can be readily hydrolyzed to the free acid as needed.

A second messenger that is biosynthesized from GTP by guanylate cyclases; activates protein kinase G (PKG) and modulates ion channel conductance, with signaling affecting diverse processes including smooth muscle relaxation and proliferation, phototransduction, and energy homeostasis.

A β3-adrenoceptor agonist (EC₅₀ = 3 nM) that is >10,000-fold selective over β1 and β2; causes a rapid decrease in blood glucose level in mice and has been used to study the induction of brown adipocytes and to increase thermogenesis in a mouse model of dietary obesity.

Selectively inhibits human NHE-1 with an IC₅₀ value of 14 nM; reduces infarct size in a rabbit myocardial ischemia-reperfusion model without adversely affecting hemodynamics or cardiac function.

A naphthoquinone derivative that potently and reversibly inhibits indoleamine 2,3-dioxygenase (IC₅₀ = 55 nM); a more potent inhibitor of IDO than annulin B or 1-methyl-d-tryptophan (1MT).

7-Bromoisoquinoline is a synthetic intermediate useful for pharmaceutical synthesis.

Contains a collection of metabolites of vasoactive eicosanoids, including the characteristic metabolites of both PGI2 and TXA2, as well as of several oxylipins postulated to regulate vasoconstriction; designed for direct use in LC-MS applications.

A natural diterpene which elevates serum cholesterol and triglycerides in humans, an effect which does not seem to occur in monkeys, hamsters, rats or gerbils; increase total cholesterol and triglycerides in ApoE3Leiden mice, an effect which is associated with selective activation of FXR and PXR.

A stable analog of PGE2 2-glyceryl ester.

Antigen: synthetic peptide corresponding to amino acids 194-209 of human HDAC4 Host: rabbit Cross Reactivity:(+) human and mouse HDAC4 Application(s): WB, IP, and ChIP HDAC4 is a class II HDAC that can shuttle between the nucleus and cytoplasm, suggesting potential extranuclear functions by...

An HDAC inhibitor that preferentially inhibits HDAC2 (IC₅₀ = 30 nM) and HDAC3 (IC₅₀ = 16 nM) over HDAC1, 4, 6, 7, and 8 (IC₅₀s = 4.8, 5, >10, 4.1, and >10 μM, respectively). At 0.1-0.4 μM, it induces differentiation and promotes apoptosis of acute myeloid...

TRIM is an inhibitor of nNOS and iNOS. It exhibits IC₅₀ values of 28.2 µM, 27.0 µM, and 1.06 mM for the inhibition of nNOS (mouse), iNOS (rat), and eNOS (bovine), respectively. TRIM inhibits mouse nNOS with Ki values of 47.3 and 462 µM in the absence and presence of BH4,...

An orally available inhibitor of native Bcr-Abl tyrosine kinase (IC50 = 0.37 nM) as well as various clinically important mutant forms including Bcr-AblT315I (IC50 = 2 nM); inhibits tumor growth in a Ba/F3 Bcr- AblT315I xenograft model of chronic myeloid leukemia in mice upon oral dosing at 10-30...

An irreversible FAAH inhibitor of the carbamate class with an IC50 value of 14 nM for the human recombinant enzyme when tested using radiolabeled oleamide as the substrate.

A broad spectrum tyrosine kinase inhibitor that blocks angiogenesis through its actions on VEGFR isoforms; has low nanomolar efficacy against VEGFR1 (FLT1), VEGFR2, VEGFR3 (FLT4), and KIT, as well as CSF1R, PDGFRA, and PDGFRB; effective in vivo and useful in the management of certain types of...

An anti-cancer natural product that acts on a variety of cellular pathways; activates caspases, inhibits anti-apoptotic proteins, alters expression of Bcl-2 and Bax; acts as a potent, slow inhibitor of Kir2.1 channels; inhibits the chymotrypsin activity of the 20S proteasome; has effects on AMPK,...

Molecular Formula C₂₀H₂₈N₄O₂ Formula Weight 356.5