ML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC₅₀s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…

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.

A time-dependent, non-specific COX inhibitor with IC₅₀ values of 1.5 and 9.7 µM for human recombinant COX-1 and COX-2, respectively.

A lipophilic, nontoxic, iron-chelating agent that shows high iron chelation efficacy both in vitro in cell culture models and also in vivo in rats and mice.

Azithromycin is an azalide macrolide antibiotic derived from erythromycin. Azithromycin binds the bacterial 50S ribosomal subunit, inhibiting protein translation. Azithromycin displays antibacterial, anti-fibrotic, and anti-inflammatory activities. In epithelial cells, azithromycin inhibits the…

A potent and selective EP4 receptor antagonist (Ki = 24 nM); reverses the anti-inflammatory action of PGE2 in LPS - activated human macrophages at 100 nM.

A melatonin receptor antagonist that preferentially targets MT1B over MT1A (Ki values = 10-27 and 158-513 nM, respectively); used both in vitro and in vivo to evaluate the roles of melatonin receptor signaling in diverse pathways.

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.

PGE2 p-acetamidophenyl ester is a crystalline derivative of PGE2. PGE2 is one of the primary COX products of arachidonic acid and one of the most widely investigated PGs. Its activity influences inflammation, fertility and parturition, gastric mucosal integrity, and immune modulation. The effects…

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…

A tricyclic antidepressant that inhibits the reuptake of serotonin and norepinephrine and acts as an antagonist at histamine, serotonin, adrenergic, and muscarinic receptors with Ki values in the nanomolar range.

A cytotoxic compound that at 1 µM activates aryl hydrocarbon receptor signaling, inducing transcription of cytochrome P450 1A1, which leads to the formation of DNA adducts and cell cycle arrest; can increase the levels of ROS as well as activate JNK, ERK, and p38MAPK in certain ovarian,…

ARRY-162 is an orally bioavailable noncompetitive inhibitor of MEK1/2 and ERK that shows anticancer chemotherapeutic activity. Inhibition of MEK inhibits downstream signaling by IL-1, IL-6, and TNF. ARRY-162 inhibits proliferation in melanoma, non-small-cell lung cancer (NSCLC), head/neck cancer,…

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;…

A monobactam antibiotic that is effective against Gram-negative bacteria but inactive against Gram-positive bacteria.

A potent ER antagonist that works by both down-regulating and degrading ERα; efficacious in the treatment of estrogen-sensitive breast cancer; fully activates ER on hippocampal neurons.

Inhibits several isoforms of protein kinase C (PKC; IC₅₀ = 7, 7, 6, 10, 60, and 20,000 nM for PKCα, PKCβ, PKCγ, PKCδ, PKCζ, and PKCμ, respectively); provides cardioprotective effects in myocardial ischemia/reperfusion.

A stable analog of PFT-α, formed by the condensation of PFT-α in solution; inhibits the growth of the cancer cell lines IGROV-1, A2780, and HCT116 (IC₅₀ = 23, 77, and 103 μM, respectively); induces autophagy in HCT116 cells and sensitizes IGROV-1 and H460 cells to…

A water soluble, irreversible, broad spectrum inhibitor of serine proteases, including trypsin, chymotrypsin, plasmin, thrombin, and kallikreins; also inhibits NADPH oxidase.

15(S)-15-methyl PGF2α is a metabolically stable analog of PGF2α. It is a potent uterine stimulant and abortifacient which can be administered intramuscularly to induce labor. It induces luteolysis and reduces serum progesterone concentrations when given as an intramuscular injection in…

A benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC₅₀ = 0.09 and 0.9 µM, respectively); dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β; dose-dependently reduces PGE2 synthesis and cell recruitment…

CAY10499 is a potent inhibitor of human HSL exhibiting an IC50 of 90 nM for the recombinant enzyme. The in vivo pharmacological efficacy of CAY10499 has not been reported.

A natural oxidative metabolic product of the mycotoxin aflatoxin B2.

Linolein hydroperoxides are a mixture of 132 possible isomers of mono-, di-, and tri-hydroperoxides produced from the autoxidation of trilinolein. Autoxidation of linoleic acid containing triglycerides (for example, trilinolein) in vivo could result in the formation of these hydroperoxides. Unlike…

Eltrombopag is a small molecule, nonpeptide agonist of the thrombopoietin receptor. It selectively binds to the transmembrane domain of the receptor and stimulates megakaryocytopoiesis in primary human bone marrow cells through the JAK/STAT signaling pathway. Eltrombopag is reported to increase…

A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

A glucosamine-nitrosourea which is commonly used to induce experimental diabetes in animals; specifically targets beta cells, entering via the glucose transporter GLUT2 and causing alkylation of DNA, leading to the destruction of beta cells.

Aflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin M1 is the hydroxylated metabolite of aflatoxin B1; it inhibits DNA synthesis and induces cell cycle arrest.

Key urinary metabolite of PGD2; represents approximately 1% and 4% of the infused radiolabeled dose in monkeys and humans, respectively.

A potent, non-ATP-competitive inhibitor of Plk1 (IC₅₀ = 9 nM); induces apoptosis in a wide array of tumor cell lines (GI50 = 50-200 nM); active in vivo when administered intraperitoneally and synergizes with chemotherapeutic agents.

A synthetic thyroid hormone mimetic that lowers total and LDL cholesterol up to 40% when administered to humans at a dose of 50-200 µg once daily for 14 days; stimulates cholesterol catabolism to bile acids without affecting cholesterol synthesis.

A specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.