产品描述:
FR900359 is a cyclic depsipeptide that has been found in A. crenata and is an inhibitor of Gαq, Gα11, and Gα14 (IC50s = 13.18, 10.47, and 10 nM, respectively).{57721,57722} It is selective for these Gα subunits over a panel of additional Gα subunits, including Gαs and Gαi, in bioluminescence resonance energy transfer (BRET) assays at 1 µM.{57723} FR900359 (1 µM) induces relaxation of precontracted isolated mouse tail arteries and inhibits platelet aggregation induced by U-46619 (Item No. 16450) in washed isolated human platelets cultured with aspirin (Item No. 70260) in a concentration-dependent manner.{57723,57724} It induces cell cycle arrest at the G1 phase and reduces proliferation and serum-induced migration of B16 melanoma cells.{57723} FR900359 (2.5 µg/animal) inhibits airway hyperresponsiveness in a mouse model of house dust mite-induced allergic asthma.{57725}