L-858,051 is a water-soluble analog of forskolin , a cell-permeant activator of adenylate cyclase.
1 L-858,051 activates adenylate cyclase (EC
50 = 3 μM), inhibits glucose transport, and blocks cytochalasin B binding in rat adipocyte membranes.
2 L-858,051 is used to activate adenylate cyclase and initiate signaling through elevated cAMP synthesis in a variety of cell types in culture.
3,4,5
1. Laurenza, A., Khandelwal, Y., De Souza, N.J., et al. Stimulation of adenylate cyclase by water-soluble analogues of forskolin Mol. Pharmacol. 32(1),133-139(1987).
2. Joost, H.G., Habberfield, A.D., Simpson, I.A., et al. Activation of adenylate cyclase and inhibition of glucose transport in rat adipocytes by forskolin analogues: structural determinants for distinct sites of action Mol. Pharmacol. 33(4),449-453(1988).
3. Funaki, C., Hodges, R.R., and Dartt, D.A. Role of cAMP inhibition of p44/p42 mitogen-activated protein kinase in potentiation of protein secretion in rat lacrimal gland Am. J. Physiol. Cell Physiol. 293(5),C1551-C1560(2007).
4. Luo, S.-F., Chiu, C.-T., Tsao, H.-L., et al. Effect of forskolin on bradykinin-induced calcium mobilization in cultured canine tracheal smooth muscle cells Cell. Signal. 9(2),159-167(1997).
5. Haj Slimane, Z., Bedioune, I., Lechêne, P., et al. Control of cytoplasmic and nuclear protein kinase A by phosphodiesterases and phosphatases in cardiac myocytes Cardiovasc. Res. 102(1),97-106(2014).
