A natural isoflavone which promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.

A full antagonist of RXR that demonstrates potent, nanomolar binding affinity; does not affect the corepressor interaction capacity of the RARα subunit in the RAR-RXR heterodimer configuration.

A potent inhibitor of DNA topoisomerase I that induces cytoxicity and DNA damage in human HT-29 colon adenocarcinoma cells (IC₅₀s = 33 nM and 0.28 μM, respectively; demonstrates a broad spectrum of antitumor activity against a variety of other tumors including ovarian cancer, cervical…

A colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

PGD2 is one of the five primary enzymatic prostaglandins derived directly from PGH2. PGD2 is produced abundantly in the CSF by the lipocalin-type PGD synthase, and in the periphery by myeloid cells including mast cells and basophils by a second, hematopoietic-type PGD synthase. PGD2 is chemically…

A selective inhibitor of CBP and EP300 which directly binds their bromodomains (Kds = 0.142 and 0.625 μM); shows only weak cross reactivity with the bromodomains of BET proteins and shows no interaction with other bromodomains.

A stimulator of sGC, increasing the activity of recombinant sGC dose-dependently, from 0.1 nM to 100 μM, up to 92-fold; in vitro, relaxes vessels and inhibits platelet aggregation at nM concentrations; in vivo, decreases blood pressure dose-dependently, prolongs bleeding time, and reduces thrombosis.

FR122047 is a selective inhibitor of COX-1. The IC50 values for inhibition of human COX-1 and COX-2 are 0.028 and 65 µM, respectively. In human platelet-rich plasma, FR122047 inhibits arachidonic acid, collagen, and ADP-induced platelet aggregation with an IC50 of 180-200 nM, which is nearly…

Contains the 16:0 fatty acid, palmitate, at the sn-1 position; at 25 μM inhibits the transcellular migration of MM1 cells across mesothelial cell monolayers without affecting proliferation; at 0.1-25 μM significantly inhibits autotaxin.

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.

Ebselen acts as a glutathione peroxidase mimic and is an excellent scavenger of peroxynitrite with a rate constant of 2 x 106 M−1s−1. The glutathione peroxidase-like activity of ebselen inhibits cyclooxygenase and lipoxygenases at micromolar concentrations.

A phenylalkylamine calcimimetic that facilitates the activation of CaSR, a GPCR that triggers PI-intracellular Ca2+ signaling; stimulates PI hydrolysis and proliferation through human CaSR (pEC₅₀ values are 6.9 and 7.4, respectively) in the presence of calcium.

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction.

A small molecule inhibitor of the TGF-β receptor type 1 kinase (IC₅₀ = 56 nM) that has been used to study the role of TGF-β signaling in triple negative breast cancer cells and hepatocellular carcinoma cells.

8-iso PGF1β is a potential autoxidation product of DGLA. There are no published reports on its isolation from any biological source or on its biological activity.

A selective BRD9 bromodomain inhibitor (pIC₅₀ = 7.3; pKd = 8.7); used to identify genes regulated by BRD9 in Kasumi-1 cells involved in cancer and immune response signaling.

A potent, selective inhibitor of p110δ.

A selective IGF-1R inhibitor (IC₅₀ = 0.17 µM); inhibits tumor proliferation both in vitro and in a mouse model of multiple myeloma.

IDO-IN-1 is a potent indoleamine 2,3-dioxygenase (IDO) inhibitor that demonstrates IC₅₀ values of 59 and 12 nM for human IDO enzymatic activity and HeLa cell assays, respectively. It is inactive against tryptophan 2,3-dioxygenase (TOD; IC₅₀ > 10 µM).

A synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1; phosphorylated by Cdk5 with a Km value of 5 µM.

A metabolite of the nucleoside reverse transcriptase inhibitor, zidovudine, formed by direct conjugation by UGT2B7.

A dual inhibitor of c-Src and Abl (IC50 = 2.7 and 30 nM, respectively); less effectively inhibits other kinases; blocks cell motility, migration, adhesion, invasion, proliferation, differentiation, and survival; reduces osteoclast bone resorption.

A bifunctional photoreactive agent for crosslinking nucleic acids; intercalates into double-stranded regions in DNA or RNA and, upon UV irradiation, forms covalent adducts with pyrimidine bases; used to study different types of RNA from diverse organisms, including viruses.

A macrolide antibiotic with antifungal activity; also cytotoxic against trypanosomes (IC₅₀ = 120-540 ng/ml) while being more than 25,000 times less effective against mammalian cells; inhibits bacterial and mitochondrial ATP synthases.

Hydroxy linoleins are a mixture of 132 possible isomers of mono-, di-, and tri-hydroxy compounds produced by the autoxidation of trilinolein and subsequent reduction of the hydroperoxides. Autoxidation of linoleic acid containing triglycerides (i.e., trilinolein) in vivo could result in the…

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

TXA2 receptor agonist; causes platelet shape change (EC₅₀ ~6 nM) and aggregation (EC₅₀ ~97 nM).

Ro 3-1314 is an inhibitor of both COX and lipoxygenase. Ro 3-1314 inhibits ram seminal vesicle COX with a Ki of 0.6 µM. It is a more effective inhibitor of COX-1 than of 15-LO, inhibiting 95% and 68%, respectively, of these enzymatic activities when used at a concentration of 48 µM.

A form of biotin with a terminal azide group; is used to add biotin to other molecules that bear either an alkyne group, through click chemistry, or a phosphine group, using Staudinger ligation.

A potent and selective inhibitor of reticulocyte 15-LO-1.

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.

Iloprost is a second generation structural analog of prostacyclin (PGI) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the human recombinant IP and EP1 receptors with a Ki of 11 nM. Iloprost…