An isomer of 17-phenyl trinor PGF2α, characterized by an inverted (β) hydroxyl group at C-15.

An irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain; produces rapid apoptosis in the various cancer cell (IC50s = 40-128 μM).

A potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC₅₀ = 14.36 nM); blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression; effective in vivo, preventing the development of fibrosis in animals.

An amino acid derivative and an intermediate, by-product, or modulator of several metabolic pathways, including the activated methyl cycle and cysteine biosynthesis; also a product of SAM-dependent methylation of biological molecules, including DNA, RNA, and histones, and other proteins.

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 second generation analog of amiloride that inhibits TRPP3-mediated Ca2+-activated (IC₅₀ = 0.14 μM) and ENaC (IC₅₀ = 10 nM); inhibits active sodium transport of human and ovine bronchial epithelial cells (IC₅₀s = 75 and 116 nM, respectively).

A cell-permeable inhibitor of JMJD2E (KDM4DL; IC₅₀ = 920 nM); reduces the expression of immediate early genes of HSV (IC₅₀ = ~10 µM) and hCMV, blocks viral infection, and suppresses the level of viral reactivation in a ganglia explant model of latently infected mice.

Butaprost is a structural analog of PGE2 with good selectivity for the EP2 receptor subtype. Butaprost has frequently been used to pharmacologically define the EP receptor expression profile of various human and animal tissues and cells. Serious confusion as to the structure of Butaprost was…

A thiazide-like diuretic that targets the Na+-Cl- cotransporter responsible for salt reabsorption in the distal convoluted tubule of the kidney (IC₅₀ = 0.3 µM in rat); inhibits human carbonic anhydrase isoforms VII, XII, and XIII (Kis = 2.1, 5.4, and 15 nM, respectively).

The angiotensin II (AII) inhibition cocktail has been developed by Bertin Pharma in order to fix physiological concentration of AII in biological samples, namely blood. Indeed, it has been observed that sample preparation is highly recommended when dosing AII for preventing the formation or…

A natural chalcone that has anti-inflammatory actions, supporting its use as a skin lightening agent, particularly for rosacea and atopic dermatitis; induces apoptosis and suppresses migration and invasion of cancer cells in vitro; has antibacterial and anti-parasitic actions.

A common C-12 saturated far plentiful in coconut and other nut oils.

An antimycotic prodrug that is converted by cytosine deaminase to 5-fluorouracil, a cytotoxic drug that inhibits viral infections and has cytotoxic effects on cancer cells.

A selective inhibitor of PI3Kα that is equipotent against both wild type and several mutant isoforms (IC₅₀s = 4.0-4.8 nM); dose-dependently inhibits the growth of PI3Kα-dependent xenograft tumors in mice, alone or in combination with other kinase inhibitors.

A corticosteroid prodrug that is converted to its active form, des-CIC, a glucocorticoid receptor agonist (Ki = 0.31 nM); used to ameliorate symptoms of airway inflammatory diseases.

15(R)-HEDE is isolated by the chromatographic resolution of (±)15-HEDE. There are no reports of biological activity associated with 15(R)-HEDE in the literature.

A reversible, selective, allosteric antagonist of mGluR7 that blocks agonist-induced calcium mobilization (IC₅₀ = 26 nM).

A broad spectrum tyrosine kinase inhibitor that blocks angiogenesis through its actions on VEGFR isoforms; has low nanomolar efficacy against VEGFR1 (FLT1), VEGFR2, VEGFR3 (FLT4), and KIT, as well as CSF1R, PDGFRA, and PDGFRB; effective in vivo and useful in the management of certain types of cancer.

Oleyloxyethyl phosphorylcholine is an inhibitor of PLA2 with an IC₅₀ value of 6.2 µM for porcine pancreatic PLA2.

A less potent IWP-2 derivative that has been used to determine which structural features of IWP-2 are essential for impairing Wnt/ β-catenin pathway activity.

Endogenous ligand of the APJ receptor, with an EC50 of 0.37 nM; acts primarily in the periphery and CNS, playing important roles in regulating cardiovascular function, fluid homeostasis, hypertension, and insulin sensitivity.

A natural oxidative metabolic product of the mycotoxin aflatoxin B2.

A cell-permeable, fluorescent dye that accumulates in acidic organelles in a pH-dependent manner and is used for autophagy detection and cell cycle determination; emits green fluorescence (ex. max: 502 nm; ,em. max: 525 nm) at neutral pH or when bound to dsDNA and red fluorescence (ex. max: 460 nm;…

An inhibitor of p53-Mdm2 interaction (IC50 = 0.09 µM); induces the expression of p53-regulated genes and exhibits potent antiproliferative activity in cells with functional p53.

A selective NMDA receptor antagonist (Kd = 1.4 μM) that competitively inhibits the glutamate binding site of NMDA receptors; widely used to study the activity of NMDA receptors particularly in regard to researching synaptic plasticity, learning, and memory.

Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2, AKR1C3, and AKR1C4 (Ki = 0.087, 4.2, and 18.2 μM, respectively); potently inhibits the metabolism of progesterone in endothelial cells overexpressing AKR1C1 (IC₅₀ = 460 nM).

A “hybrid” analog which incorporates components of both the AEA-like and dopaminergic neurotransmitter pathways; is nearly inactive as a TRPV1 ligand and fails to elicit hyperalgesic or nocifensive responses in vivo; exhibits an “entourage” effect at concentrations of 0.1-10…

DuP-697 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK-966 (rofecoxib), SC-58125, and celecoxib. DuP-697 is a potent and time-dependent inhibitor of COX-2. When tested on isolated recombinant enzymes, DuP-697 is at least 50 times more potent in the…

A benzimidazole analog that inhibits IKK-ε with an IC50 value of ~15.8 µM.

A potent disruptor of microtubules used as a chemotherapeutic compound; inhibits growth of cervical (HeLa), lung (A549), breast (MCF-7), colon (HT-29), ovarian (OVG-1), and pancreatic (PC-Sh) carcinomas with IC50 values ranging from 2.5-7.5 nM; induces mitotic arrest and initiates apoptosis of…

AFC is a synthetic substrate for the isoprenylated protein methyltransferase (also known as S-adenosylmethionine-dependent methyltransferase). Because it is able to serve as a substrate for the methyltransferase, it effectively functions as an inhibitor of methylation of endogenous isoprenylated proteins.