A selective ERRβ/γ receptor agonist (EC₅₀ = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.

8-iso PGE2 isopropyl ester is a more lipophilic form of the free acid, 8-iso PGE2. Prostaglandin esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid upon in vivo administration, making the esters useful prodrugs. In general, the…

A small molecule inhibitor of KCNJ1 (IC₅₀ = 294 nM) which also causes 70% inhibition of KCNJ13 at 10 µM; has no effect on the related channels KCNJ2 (Kir2.1) and KCNJ10 (Kir4.1) at a concentration of 10 µM.

A tetraline that inhibits monoamine transporters with selectivity for the serotonin transporter (IC₅₀s = 70, 520, and 720 nM for the serotonin, dopamine, and norepinephrine transporters, respectively).

A natural polymethoxylated flavonoid and potent antioxidant with good bioavailability; has anti-inflammatory effects that are relevant to a host of diseases, including cancer, arthritis, and neurodegeneration; inhibits P-glycoprotein and BCRP (IC₅₀ = 11.5 and 4.9 μM, respectively).

A competitive, non-NMDA glutamate receptor antagonist (IC₅₀s = 0.3 and 1.5 μM for AMPA and kainate receptors, respectively, versus IC₅₀ = 25 μM for NMDA receptors).

A glycopeptide antitumor antibiotic that produces single and double-strand DNA breaks in tumor cells to interrupt their cell cycle; has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models…

A potent inhibitor that blocks dopamine uptake (IC₅₀ = 1-51 nM); effectively inhibits dopamine uptake in vivo, leading to consequent stimulation of dopamine receptors.

A competitive inhibitor of nucleotide binding by Ras-related GTPases; binds Rab7 (Ki = 13 nM), preventing BODIPY-linked GTP and GDP binding with EC₅₀ values of 11.2 and 21 nM, respectively.

A cell-permeable selective inhibitor of the PI3K catalytic subunit p110δ (IC50 = 0.5 μM). It less effectively inhibits p110γ and p110β (IC50 = 29 and 75 μM, respectively) and has no significant effect on p110α and several other kinases.

A small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…

Prominent plasma metabolite of PGF2α in the 15-hydroxy PGDH pathway.

A natural anthocyanidin.

Molecular Formula: C₁₃H₉ClFNO₂

An inactive metabolite of artemisinin.

Travoprost is the Alcon trade name for fluprostenol isopropyl ester, an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug. Fluprostenol isopropyl ester is a prodrug which is converted by esterase enzymatic activity in the cornea to yield the corresponding…

A potent, competitive inhibitor of HMG-CoA reductase (Ki = 2.3 nM).

A naturally occurring phospholipid produced by cells upon inflammatory stimulation; less potent than PAF C-16 and PAF C-18 in the induction of neutrophil chemotaxis, but is equipotent to PAF C-16 and PAF C-18 in promoting eosinophil migration.

An agonist of the group mGluR, binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 µM, respectively) but not ionotropic glutamate receptors.

Immediate precursor of 4-HNE formed from ω-6 hydroperoxides such as linoleic acid and arachidonic acid.

A selective, ATP-competitive inhibitor of the serine/threonine kinase, glycogen synthase kinase 3β (Ki = 38 nM; IC₅₀ = 104 nM); demonstrates neuroprotective effects by inhibiting tau phosphorylation (IC₅₀ = 2.7 μM) at a GSK3-specific site (Ser396) in cells stably…

A non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC₅₀ value of 200 nM; potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC₅₀ = 28 nM); also effective in vivo, reducing inflammation…

A fluorogenic substrate for chitinases and chitotriosidases.

A polypharmacological cancer therapeutic; potently inhibits RET (IC₅₀ = 2 nM) and reduces the activity of numerous other kinases by more than 80% when given at 1 μM in Drosophila; interferes with kinases downstream of RET, including Src, Raf, and S6K.

An antibiotic that can inhibit cell wall synthesis in plant-pathogenic oomycetes (MIC = 25 µg/ml for P. medicaginis M2913) and certain fungi as well as some bacterial species (MIC = 400 µg/ml for S. aureus).

A selective nonphosphoinositide inhibitor that specifically disrupts PIP3/Akt PH domain binding (IC50 = 31 μM); suppresses PI3K-PDK1-Akt-dependent phosphorylation, which reduces cell viability and induces apoptosis in PTEN-deficient U87MG glioblastoma cells (IC50 = 37 μM).

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis; inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

A chromogenic substrate for N-acetyl-D-galactosaminidase that generates a yellow solution upon cleavage.

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 cyclic polypeptide-containing anticancer antibiotic that binds to DNA and blocks transcription by interfering with RNA synthesis; ~10 nM promotes cell death in a variety of tumors.

A selective inhibitor of class IIa HDACs, with greater than 170-fold selectivity over class I HDACs, including HDAC1; used in cells (1-10 µM) and in mice to elucidate the roles of class IIa HDACs in cell proliferation and differentiation, apoptosis, myogenesis, adipogenesis, and fibrosis.

A cell-permeable, competitive, and irreversible inhibitor of all caspases, inhibiting cleavage of PARP and preventing apoptosis when used at 10-50 µM; blocks caspase-mediated apoptosis in vivo; effectively prevents caspase action in inflammasomes.