An activator of sGC that binds to a regulatory site, resulting in activation in an NO-independent manner (Kd = 3.2 nM); reduces hypertension, limits cardiomyocyte hypertrophy, protects against ischemia/reperfusion injury, and reduces morbidity and mortality in response to endotoxic shock.

11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…

An analog of 2-OG that has been developed as an inhibitor of HIF-PHs.

A small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…

An internal standard for the quantification of OEA by GC- or LC-MS.

An inhibitor of the HATs p300 and pCAF (IC50 = 7 and 5 μM, respectively) that also inhibits the HAT Gcn5; promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells; induces apoptosis in several types of cancer cells and has anti-inflammatory actions.

An analog of AEA that potentiates the activity of endogenous AEA by blocking its re-uptake into presynaptic neurons; selectively inhibits the carrier-mediated transport of AEA without affecting anandamide hydrolysis; inhibits the transport of AEA with an IC₅₀ value of 1 µM in rat…

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.

CAY10499 is a potent inhibitor of human HSL exhibiting an IC50 of 90 nM for the recombinant enzyme. The in vivo pharmacological efficacy of CAY10499 has not been reported.

A potent LTB4 receptor antagonist that inhibits the specific binding of [3H]-LTB4 to isolated human neutrophils with an IC50 value of 13.2 nM; inhibits the LTB4-induced aggregation of guinea pig and human neutrophils with IC50 values of 74 and 100 nM, respectively.

A GABAA receptor agonist (IC₅₀ = 19 nM) that has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.

A small diffusible signaling molecule produced by wild-type E. carotovora strain SCC 3193 involved in quorum sensing, controlling gene expression, and affecting cellular metabolism.

A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC₅₀ = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC₅₀ = 0.6 µM); shows good in vivo potency and duration of action.

An ER agonist that binds to ERα and ERβ with Ki values of 27.4 and 15.4 nM, respectively; demonstrates higher ER agonist activity at ERα compared to ERβ (EC50 = 66 and 330 nM, respectively).

A selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.

An inhibitor of ethylene biosynthesis that, at 1 µM, blocks the activity of both ACSs and ACOs; reduces ethylene-mediated plant changes in growth and development; inhibits cystathionine γ-lyase (Ki = 10.5 μM) with slow- and tight-binding characteristics.

A selective, irreversible inhibitor of BTK (IC₅₀ = 0.5 nM in vitro in B cell lymphoma cell lines) that targets and covalently binds to BTK at cysteine-481; inhibits osteoclast function and reduces osteoclast-stimulated proliferation of multiple myeloma cells in animal models of…

A cell-permeable inhibitor of sirtuin NAD+-dependent deacetylases, inhibiting the yeast sirtuin Sir2p with an IC50 value of 68 μM and the human sirtuins SIRT1 and SIRT2 with IC50 values of 131 and 38 μM, respectively; does not alter HDAC1 activity.

A homolog of EPEA, characterized by the addition of an (R)-β-methyl group at the terminal ethanolamine carbon.

A more lipid soluble derivative of Tafluprost, a very potent FP receptor agonist (Ki = 0.4 nM).

A β-adrenergic receptor agonist with potent positive inotropic effects in vivo; strongest effects on β1 receptors, with lesser but significant β2 receptor activation and only weak α1 receptor actions; strongly increases cardiac contractility.

A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).

A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC₅₀s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC₅₀s = 0.92 and 1.04 µM for mouse…

A noncompetitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC₅₀ = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC₅₀s range from 1-7 μM).

An analog of scriptaid that lacks scriptaid’s HDAC inhibitory effects; used as a negative control in experiments involving scriptaid.

An orally-available, highly selective inhibitor of B-RafV600E (IC₅₀ = 13 nM); less effective against wild type B-Raf (IC₅₀ = 160 nM) as well as several other kinases; induces cell cycle arrest and apoptosis in cells and xenografts expressing the mutant of B-Raf.

An inhibitor of p300 histone acetyltransferase (KAT3B; IC₅₀ = 1.98 µM in vitro); blocks acetylation of histones and p53 in cells treated with trichostatin A or etoposide, respectively, and reduces STAT3 phosphorylation.

An analytical reference material categorized as a phytocannabinoid; intended for research and forensic applications

Linolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…

A symmetric bis-glycolamide that inhibits the eIF2α phosphorylation-mediated unfolded protein response (IC₅₀ = 5 nM in a cell-reporter assay); passes through the blood-brain barrier and significantly enhances learning and memory in mice and rats.

An analytical reference standard categorized as a phytocannabinoid; intended for research and forensic applications

A bioactive saponin used in traditional Chinese medicine; has diverse protective effects for the cardiovascular, immune, digestive, and nervous systems.