A selective inhibitor of MEK1 and MEK2 (IC₅₀s = 0.18 and 0.22 μM), the kinases upstream of ERK1/2; rapidly passes the blood-brain barrier and has been used to dissect the effect of RAS/RAF/MEK/ERK signaling pathway inhibition on behavior.

A potent inhibitor of all three human Pim kinases (IC₅₀s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively); induces apoptosis in lymphocytes from patients with CML or ALL; enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant cancer…

A major phase I metabolite of the mycotoxin α-zearalanol (zeranol), a non-steroidal estrogen produced by fungi; an estrogen receptor agonist (EC₅₀ = 0.11 µM).

A cell-permeable inhibitor that binds actin filaments, but not actin monomers, to inhibit polymerization at concentrations as low as 0.2 µM.

A potent, selective inhibitor of Stearoyl-CoA desaturase 1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.

A selective, cell-permeable EZH2 inhibitor (IC₅₀ = 2 nM) that has been shown to inhibit H3K27methylation in MCF10A cells with an IC₅₀ value of 124 nM.

A derivative of glucose used to study carbohydrate metabolism, particularly in the identification, differentiation, and characterization of α-phosphoglucomutase, β-phosphoglucomutase, and α- and β-hexoglucomutases.

BW 245C is a selective agonist for the DP1 receptor. The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM. It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation and an IC50 of 250 nM for the inhibition of…

The Rho family of GTPases regulates diverse signal transduction pathways. One member, the cell division control protein 42 homolog (Cdc42), is involved in filopodia function, cell polarity, cell cycling, and other processes. CASIN is an indole-based small molecule that inhibits activation of the…

An inhibitor of CETP; inhibits plasma CETP with an IC₅₀ value of 9 µM; in rabbits given an atherogenic diet, increases HDL, decreases VLDL, and attenuates induced atherosclerosis; in humans, inhibits CETP activity and increases HDL levels but does not reduce the risk of recurrent…

20-HETE is a major biologically active CYP450 metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation. HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an…

A small molecule inhibitor of JAK2 (IC₅₀ = 6 nM) and the related kinases FLT3 (IC₅₀ = 25 nM) and RET (IC₅₀ = 17 nM) with significantly less potent activity against JAK3 (IC₅₀ = 169 nM); inhibits the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L…

A potent and selective inhibitor of PLD1, both in vitro (IC₅₀ = 46 nM) and in cells (IC₅₀ = 11 nM); also effective as a PLD2 inhibitor at higher concentrations (IC₅₀ = 933 nM in vitro; 1,800 nM in cells); strongly inhibits the invasive migration of several breast…

A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC₅₀ = 5 nM), p59fynT (IC₅₀ = 6 nM), Hck (IC₅₀ = 20 nM).

DAF-2 diacetate is a sensitive fluorescent indicator for the detection and bioimaging of NO. It is a cell-permeable derivative of DAF-2. Upon entry into the cell, DAF-2 diacetate is transformed into the less cell-permeable DAF-2 by cellular esterases thus preventing loss of signal due to diffusion…

A reactive disulfide-containing, fluorescent probe (ex. max 502 nm; em. max 525 nm) designed for fast detection of H2S in biological samples and cells.

The product of nitration of linoleate by NO-derived reactive species; activates PPARγ (Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake; can also be metabolized to produce nitrite derivatives which in turn form NO, leading to increased cGMP production.

9β-hydroxy stereoisomer of PGF2α; much less active than PGF2α in antifertility and bronchoconstrictor activities; exhibits bronchodilating activity in guinea pigs and cats and antagonizes the bronchoconstrictor activity of PGF2α.

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

A water soluble prodrug analog of AEA with similar activity to that of AEA in the growth inhibition of C6 glioma cells; also a structural variant of LPA, however, its effects on the various LPA receptors have not been tested.

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

A selective PAR2 agonist that stimulates cell proliferation, phosphatidylinositol hydrolysis, and calcium mobilization in in vitro functional assays (pEC₅₀s = 6.7, 5.9, and 6.6, respectively); elicits pronociceptive activity in vivo.

A synthetic PGA1 analog with structural features similar to 15-deoxy-Δ12,14-PGJ2, a ligand for PPARγ.

An alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.

The primary metabolite of mycophenolic acid, an inhibitor of inosine monophosphate dehydrogenase that prevents lymphocyte proliferation and activation; typically used as an internal standard for therapeutic drug monitoring analyses of serum or whole blood by HPLC or LC-MS to confirm that patients…

A selective DNA-PK inhibitor (IC₅₀ = 14 nM) that increases the cytotoxicity of ionizing radiation and etoposide in human colon cancer cell lines in vitro and potentiates the effects of etoposide in mice bearing human colon cancer xenograft tumors in vivo.

A cell-permeable triazine compound that inhibits the human E2 ubiquitin-conjugating enzyme Rad6B; selectively docks to the Rad6B catalytic site, inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2/M arrest and apoptosis, and inhibits…

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 enantiomer of C75, which in racemic form is a stable FAS inhibitor that when administered leads to profound weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.

An inverse agonist of LRH-1 (IC₅₀ = 3.7 µM) with maximum efficacy of 64% repression; inactive at the related SF1 transcriptional activator; alters the expression of haptoglobin, SAA1, and SAA4, induces the death of ER negative MDA-MB-231 breast cancer cells, and inhibits the StAR…

PGF2α 1,11-lactone is a lipid-soluble internal ester of PGF2α. Hydrolysis of the lactone by plasma esterases readily produces free PGF2α in rats and monkeys, but not in humans. PGF2α 1,11-lactone is active as an antifertility agent with greatly reduced vasoactivity compared…

A selective inhibitor of 15-hydroxy PGDH (IC₅₀ = ~10 µM).