FR900359

FR900359 is a cyclic depsipeptide that has been found in A. crenata and is an inhibitor of Gα_q, Gα₁₁, and Gα₁₄ (IC₅₀s = 13.18, 10.47, and 10 nM, respectively).^1,2 It is selective for these Gα subunits over a panel of additional Gα subunits, including Gα_s and Gα_i, in bioluminescence resonance energy transfer (BRET) assays at 1 µM.³ 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.^3,4 It induces cell cycle arrest at the G₁ phase and reduces proliferation and serum-induced migration of B16 melanoma cells.³ FR900359 (2.5 µg/animal) inhibits airway hyperresponsiveness in a mouse model of house dust mite-induced allergic asthma.⁵

WARNING This product is not for human or veterinary use.

1. Fujioka, M., Koda, S., Morimoto, Y., et al. Structure of FR900359, a cyclic depsipeptide from Ardisia crenata sims. The Journal of Organic Chemistry 53(12), 2820–2825 (1988).

2. Kukkonen, J.P. G-protein inhibition profile of the reported G_q/11 inhibitor UBO-QIC. Biochem. Biophys. Res. Commun. 469(1), 101-107 (2016).

3. Schrage, R., Schmitz, A.-L., Gaffal, E., et al. The experimental power of FR900359 to study G_q-regulated biological processes. Nat. Commun. 6, 10156 (2015).

4. Inamdar, V., Patel, A., Manne, B.J., et al. Characterization of UBO-QIC as a Gα_q inhibitor in platelets. Platelets 26(8), 771-778 (2015).

5. Matthey, M., Roberts, R., Seidinger, A., et al. Targeted inhibition of G_q signaling induces airway relaxation in mouse models of asthma. Sci. Transl. Med. 9(407), eaag2288 (2017).