An irreversible inhibitor of ornithine decarboxylase that suppresses polyamine biosynthesis; displays antiangiogenic, cytostatic, and antiparasitic effects.

A non-protein amino acid that chelates iron and copper; inhibits certain enzymes that contain iron or copper, including arginase (IC₅₀ = 3.7 µM).

A prodrug for A-771726 that regulates T lymphocyte progression through the cell cycle by selectively inhibiting de novo pyrimidine synthesis; used to slow the disease progression of rheumatoid arthritis and as an immunosuppressive agent to prevent rejection of transplant allografts and xenografts.

A naturally occurring agonist for the nuclear receptor Nur77 (IC₅₀ = 0.278 nM); induces apoptosis in cancer cells and retards xenograft tumor growth; induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat/high cholesterol diet.

A-77-01 is a potent inhibitor of the TGF-β1 receptor ALK5 (IC₅₀ = 25 nM). It has no effects on BMP-regulated transcriptional activity or MAPK pathways. A-77-01 efficiently prevents the growth inhibitory effects of TGF-β on lung epithelial Mv1Lu cells. It completely blocks…

An inhibitor of Wnt production that impairs Wnt pathway activity (IC₅₀ = 27 nM in vitro) by inactivating Porcupine, a membrane-bound O-acyltransferase responsible for palmitoylating Wnt proteins; used to suppress embryonic stem cell self-renewal and to decrease cancer cell proliferation,…

A DR5 agonist (Kd= 1.2 µM; IC₅₀ = 2 µM) that induces DR5 clustering, which leads to the initiation of FADD/caspase-8-dependent apoptosis in various cancer cells.

A nuclesoside analog that disrupts DNA synthesis in blood cells; effective in a number of animal tumor systems including LI210 leukemia, CD8F mammary adenocarcinoma, P388 leukemia, and human LX-1 lung tumor xenograft and displays anticancer activity against human hematological malignancies in vivo.

A cell-impermeable, negatively charged tetrazolium dye that produces a water-soluble formazan when reduced at the cell surface by cellular-derived NADH and an electron mediator.

A potent and selective inhibitor of Wip1 (IC₅₀ = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable, causing inhibition of lymphoma xenograft growth in mice.

A metabolite produced during GCDH deficiency and used as a biomarker of glutaric acidemia type 1.

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

A potent and selective inhibitor of DGAT-1 (IC₅₀ = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.

A selective inhibitor of PI3Kγ

The major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.

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 cell-permeable inhibitor of SCF-mediated c-kit activation, completely blocking phosphorylation of c-kit in human melanoma cells at a concentration between 1 and 5 µM; prevents SCF-mediated downstream phosphorylation of p44/p42 ERK.

An agonist of GPR81 (EC₅₀ = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor; stimulates lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks; blocks basal ghrelin secretion by primary gastric mucosal cells.

Spontaneously hypertensive rats fed a diet which includes γ-tocotrienol show significant reduction of systolic blood pressure and an increase of nitric oxide synthase activity in blood vessels. γ-Tocotrienol at 20 µM induces apoptosis of malignant sympathoadrenal (+SA) murine…

A selective agonist of S1P3 (EC₅₀ = 72-132 nM); less effectively activates S1P1 (EC₅₀ = 28-38 µM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.

An inhibitor of SRPK1 (Ki = 0.89 µM); suppresses the propagation of viruses in mammalian cells; modulates alternative splicing of VEGF, reducing neovascularization both in cells and in animals.

An imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC₅₀ = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.

A small molecule inhibitor of DNA ligase IV that prevents nonhomologous end-joining by interfering with the ligase binding and activating apoptosis; inhibits cancer cell growth in vitro (IC₅₀s = 8-120 µM) and in mouse models when co-administered with double-strand break-inducing…

A natural, potent and irreversible inhibitor of cysteine proteases; IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively; also inhibits papain, calpain, and cathepsins B and H.

An isomer of Vitamin E that has less potent antioxidant properties than α-tocotrienol.

A HSL compound produced in the marine bioluminescence bacterium V. fischeri.

An immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections.

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.

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 potent antagonist of the type III receptor tyrosine kinases PDGFRβ, FLT3, and c-Kit (IC₅₀ = 200, 220, and 170 nM, respectively); less potently inhibits CSF-1R (IC₅₀ = 3.4 µM) and does not significantly inhibit other tyrosine or serine/threonine kinases.

The racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.

A potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.