Cayman Chemical

An organophosphorus compound that dually inhibits MAGL and FAAH with IC50 values of 0.8 and 3 nM, respectively; at 10 mg/kg, it elevates brain levels of 2-AG and AEA more than 10-fold and decreases levels of arachidonic acid by a similar magnitude.

A potent, selective inhibitor of nNOS with Ki values for inhibition of nNOS, eNOS and iNOS of 100 nM, 12 µM and 60 µM, respectively.

A GABA analogue that acts as an anticonvulsant with proven analgesic effects in various neuropathic pain syndromes.

A PAF analog.

A Gcn5 and pCAF HAT inhibitor.

A synthetic analog of natural PIP3 with C6:0 fatty acids at the sn-1 and sn-2 positions; features the same inositol and diacylglycerol stereochemistry as the natural compound; the short fatty acid chains give it higher solubility in aqueous media, as compared to naturally-occurring PIP3.

An irreversible, mechanism-based inhibitor of LSD1 (IC₅₀ = 16 nM); induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC₅₀s<5 nm).<>

A signaling molecule as well as a cofactor or substrate for many enzymes.

A tremorgenic mycotoxin that selectively inhibits the activation of Maxi-K potassium channels by charybdotoxin with a K1/2 value of 170 nM.

A GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)); acts as an antagonist at...

A trichothecene mycotoxin that can infect grain crops causing alimentary toxic aleukia in humans and animals; inhibits protein synthesis, disrupts membrane phospholipid metabolism, increases lipid peroxides in the liver, and is highly cytotoxic to macrophages (IC50 = 19.47 nM), altering the...

A dual inhibitor of adenosine deaminase (IC₅₀ = 1.2 μM in human red blood cells) and PDE2 (IC₅₀s = 0.8 and 2 μM from human and pig myocardium, respectively, 3.5 μM in rat hepatocyte, and 5.5 μM in human platelet).

A fatty acid amide derived from ricinoleic acid and methyl benzylamine that demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), kidney (786-0), non-small cell lung (NCI-H460), and prostate (PC-3) cancer cells with a mean GI50 value of 6.9...

A potent, selective inhibitor of LRRK2 that inhibits both wild-type and G2019S mutant LRRK2 (IC₅₀s = 13 and 6 nM, respectively); stimulates macroautophagy in H4 neuroglioma cells.

An endogenous component of cell membranes where it serves as a substrate for steroid synthesis, influences lipid metabolism, stabilizes cell membranes, regulates the activity of functional proteins, and plays a role in keratinocyte differentiation and development of the epidermal barrier.

A potent, selective CysLT2 receptor antagonist that inhibits radioligand binding of LTD4 to CysLT2 and CysLT1 receptor cell lines with IC50 values of 35 and >10,000 nM, respectively.

A chiral enantiomer of 13,14-epoxy fluprostenol isopropyl ester whose pharmacology has not been studied extensively to date.

A derivative of 2-DG that is produced in mammalian cells by the action of hexokinase; accumulation of 2-DG6P in cells can inhibit glycolysis, leading to cell death.

A bpV compound that selectively inhibits PTEN (IC₅₀ = 14 nM); also inhibits the vascular endothelial PTP, PTP-β (IC₅₀ = 4.9 μM), and PTP-1βB (IC₅₀ = 25.3 μM) with reduced potency.

The diphosphate of uridine; a specific agonist of the P2Y purinoceptor P2Y6 (EC₅₀ = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction; an antagonist of P2Y14.

A reversible, cell-permeable inhibitor of JARID1 family demethylases (IC₅₀s = 6, 3, 4.9, and 28 µM for JARID1A, JARID1B, JARID1C, and JARID1D, respectively); increases trimethylation of H3K4 in HeLa cells and blocks the proliferation of tumor cells expressing high levels of JARID1B.

A competitive AT1 receptor antagonist (IC50s 1.4 – 3.9 nM and an elimination half-life of 5 to 7 hours) that blocks angiotensin II receptors on both sympathetic nerve terminals and blood vessels.

A potent inhibitor of the Wnt response, blocking a cell-based Wnt/β-catenin pathway reporter response (IC₅₀ = 180 nM); inhibits Wnt-induced accumulation of β-catenin, leading to proteasomal degradation of this protein.

Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 140 nM) versus AKR1C2 and AKR1C3 (Ki = 1.97 and 21 µM, respectively); does not inhibit AKR1C4 at 100 µM.