Cayman Chemical

A potent inhibitor of CREBBP and EP300 bromodomains (IC₅₀s = 21-69 and 38 nM, respectively).

A pyridine regio-isomer of GSK-J1 which poorly inhibits JMJD3 (IC50 > 100 μM), making it an appropriate negative control for in vitro studies involving GSK-J1.

An isomer of latanoprost (free acid) wherein the double bond between carbons 5 and 6 has been changed from cis (Z) to trans (E); intended primarily as an analytical standard.

A highly reactive 2-oxoaldehyde intermediate of the Maillard reaction produced during oxidative stress in response to excess sugar consumption and in association with diabetes; glycates and crosslinks proteins leading to the formation of advanced glycation endproducts.

An extremely potent cannabinoid receptor antagonist with high selectivity for the central CB1 receptor (Ki = 0.35 pM) compared to the peripheral CB2 receptor (Ki = 21 nM)

A major CYP450 metabolite of arachidonic acid that is released from the kidney in response to angiotensin II; a potent vasodilator of renal preglomerular vessels; blocks 20-HETE-induced vasoconstriction of renal arterioles at 1 µM.

A proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase; inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 µM, respectively.

Cyclooxygenase 2 (COX-2) is a 72 kDa protein that has been cloned from a variety of species including human, mouse, rat, and ovine. This preparation of COX-2 microsomes was prepared by solubilization and dilution of the 100,000 x g pellet from the lysate of cytokine-stimulated mouse macrophage...

A carnitine ester that inhibits carnitine-acylcarnitine translocase (IC₅₀ = 33 μM).

An epimer of AFP 07.

A non-selective antagonist of β-adrenergic receptors that blocks β1-, β2-, and β3-adrenoceptors with IC₅₀ values ranging between 0.1 and 8.9 µM; also blocks outward potassium currents in myocardium, exhibiting Class III antiarrhythmic actions.

A potent, selective, and bioavailable antagonist of the OX2R (KB = 4.5 nM for OX2R versus 1.1 µM for OX1R); decreases the latency to persistent sleep and increases persistent sleep time when applied subcutaneously to rats.

An expected J-ring, urinary PGD2 metabolite that may serve as a useful control in the analysis of PGD2 biosynthesis.

A selective inhibitor of the HER2, inhibiting HER2 phosphorylation with an IC₅₀ value of 6 nM; without effect on EGFR, FGFR, PDGFR, Jak1, Src, and Blk (IC₅₀ > 25 μM); inhibits the proliferation of breast, bladder, kidney, and prostate cancer cells in vitro and in vivo.

The sirtuins represent a distinct class of trichostatin A-insensitive lysyl-deacetylases (class III HDACs) that catalyze a reaction coupling lysine deacetylation to the formation of nicotinamide and O-acetyl-ADP-ribose. Cayman’s Direct Fluorescent Screening Assay Kits provide a convenient...

A potent inhibitor of MEK in (IC50 = 2.3 nM; Kd = 74 nM when activated with ATP) that suppresses phosphorylation of ERK in mouse colon 26 tumors (IC50 = 35 nM).

Source: Recombinant N-terminal GST-tagged protein expressed in E. coli Mr: 37 kDa MeCP2 specifically binds to methylated promoters on CpG islands and mediates gene silencing by recruiting corepressor complexes. In vitro work suggests high affinity binding of MeCP2 is facilitated by DNA fragments...

An AChE inhibitor (Kis = 0.2 - 0.4 µM) that is known to prevent the breakdown of the neurotransmitter acetylcholine by binding specifically to its catalytic site; used as part of a battery of pharmacological tests to confirm a diagnoses of myasthenia gravis.

A natural anthocyanidin with significant antioxidant activity; has vasoprotective effects and can interfere with inflammation, carcinogenesis, obesity, and diabetes.

(±)12-HEPE is produced by non-enzymatic oxidation of EPA. It contains equal amounts of 12(S)-HEPE and 12(R)-HEPE. The biological activity of (±)12-HEPE is likely mediated by one of the individual isomers, most commonly the 12(S) isomer in mammalian systems. 12-HEPE inhibits platelet...

A weak antagonist of α1-adrenoceptors, blocking WB-4101 and clonidine binding in brain membrane preparations with pKi values of 2.63 and 1.61, respectively; also has antioxidant effects.

A reversible, orally bioavailable dual inhibitor of IGF-1R and InsR tyrosine kinases (IC₅₀s = 1.8 and 1.7 nM, respectively); inhibits cell proliferation or induces apoptosis in a variety of cancer cells in vitro; inhibits the growth of tumor xenografts in mice.

A K+-competitive inhibitor of H+/K+-ATPases that is best known for its ability to block acid secretion through its action against the gastric H+/K+-ATPase (IC₅₀ = 1.3 µM); effective against gastric H+/K+-ATPases from a variety of species and can inhibit some colonic H+/K+-ATPases.