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.

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

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…

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