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

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.

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.

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 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.