A first generation histamine H1 receptor antagonist (Ki = 2.6 nM) that also inhibits muscarinic acetylcholine receptors (Ki = 22 nM); penetrates the CNS, depressing central H1 receptor activity, which may relate to its sedative properties.

A selective, orally available inhibitor of MEK1 (IC₅₀ = 4.2 nM); induces differentiation and apoptosis in cancer cells lines.

Benzo[a]pyrene is a polycyclic aromatic hydrocarbon (PAH) originally found in coal tar, cigarette smoke, and wood smoke. Metabolites of this compound bind DNA and induce mutations. Benzo[a]pyrene is highly carcinogenic and is used in research models to induce carcinogenesis and tumor formation.…

ICI 192605 is a potent antagonist of the thromboxane A₂ receptor (TP) that blocks contraction of isolated guinea pig trachea induced by U-46619 (Item No. 16450; K_d = 0.398 nM). It is used to study the role of TP signaling in tissues and animals.

Diethylstilbestrol (DES) is a synthetic estrogen receptor agonist that was prescribed to pregnant women in the late 1930s. It was banned in 1971 because of possible links to increased risk of breast cancer in mothers along with congenital abnormalities and increased risk of cancer in offspring. DES…

A cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC₅₀ = 15 μM); inhibits clathrin-dependent vesicle formation and endocytosis; can also augment the release of neurotransmitters and secreted cytokines.

A selective sEH inhibitor with IC50 values of 160 and 90 nM for recombinant human and mouse sEH, respectively; at 10 µM, blocks the hydrolysis of cis- and trans-EETs and completely inhibits 14,(15)-EET-induced PPAR activation.

An orally bioavailable Smac/DIABLO mimetic and antagonist of IAPs (Kis = 66.4, 1.9, and 5.1 nM for XIAP, cIAP1, and cIAP2, respectively); inhibits cancer cell growth in various human cancer cell lines and induces apoptosis in xenograft tumors in mice.

A synthetic analog of 17β-estradiol

A prodrug of the potent, long-acting, and selective AT1 receptor antagonist, candesartan; 4-16 mg/day effectively reduces diastolic blood pressure and has proved useful in the treatment of hypertension and diabetes.

An antifungal compound clinically used to treat nail and skin infections; inhibits ergosterol synthesis at the stage of squalene epoxidation (IC50 = 30 nM for C. albicans); induces cell cycle arrest at the G0/G1 stage in COLO 205 tumor cells and human vascular endothelial cells.

A cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol or the GPER-selective agonist G-1 (IC₅₀ = 112 and 165 nM, respectively); has no detectable binding activity to either ERα or ERβ.

A partial CB receptor agonist isolated from the bark of M. officinalis that has been used in Asian traditional medicine for the treatment of anxiety, sleep disorders, and allergic diseases; demonstrates selectivity for the peripheral CB2 receptor subtype (EC₅₀ = 3.28 μM; Ki = 1.44…

An non-nucleoside reverse transcriptase inhibitor that prevents RNA plus-strand initiation (IC₅₀ = 17 nM); also inhibits the late stages of HIV-1 replication by interfering with HIV-1 Gag-Pol polyprotein processing.

A rotenoid that exhibits antineoplastic and piscicidal activities; inhibits the NADH:ubiquinone oxidoreductase (IC₅₀ = 98 nM) and induces ornithine decarboxylase activity (IC₅₀ = 147 nM).

Amitraz is an agonist at a-adrenergic receptors that displays insecticide activity. Amitraz also inhibits monoamine oxidase (MAO) and synthesis of prostaglandins. Additionally, amitraz may act on octopamine receptors. Amitraz acts as an acaricide and is commonly used in veterinary prophylaxis…

A thiazide-like diuretic that inhibits sodium/chloride cotransporters in the proximal convoluted tubule of the kidney, which prevents the reabsorption of sodium and chloride.

An NSAID that reduces edema in certain types of acute inflammation in animal models; a poor inhibitor of prostaglandin synthesis, but, like other NSAIDs, it inhibits OAT1 (Ki = 32 µM).

G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a Ki value of 11 nM. Competitive binding studies in endoplasmic reticulum α- (ERα-) and ERβ-expressing cells yielded Ki values for estradiol of 0.30 and 0.38 nM, respectively, with no substantial…

A copper and zinc chelator and an irreversible inhibitor of aldehyde dehydrogenase (IC₅₀ = 0.1 mM) that has been indicated for the treatment of alcohol dependence; targets the ubiquitin-proteasome pathway, induces ROS, activates JNK and p38 pathways, and inhibits NF-κB activity in…

A natural product with diverse therapeutic effects, including acting as an anxiolytic in mice; inhibits NF-κB and PI3K/Akt signaling, preventing inflammation; interferes with angiogenesis while preventing tumor growth in vivo; scavenges superoxide and peroxyl radicals.

A natural metabolite formed by CYP450-mediated hydroxylation followed by catechol-O-methyltransferase (COMT) methylation of estradiol; has anticancer agent activity as an angiogenesis inhibitor via the HIF-1α pathway; levels are significantly lower in women with severe pre-eclampsia.

An orally available, selective inhibitor of LSD1 (IC₅₀ < 20 nM); targets AML stem cells.