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Hh-Ag1.5 is one of the most potent and selective small-molecule agonists of the Hedgehog pathway, targeting Smoothened (Smo) with an EC₅₀ ~1 nM. Studies showed that it has more potent activity than the recombinant Hh protein in activating Smo and hedgehog pathway.

How to Use:

• In vitro: Hh-Ag1.5 was used at 25 nM to induce Hh pathway activation in the reporter gene assay. It was suggested to use at 0.1 µM to replace recombinant Hh protein.
• In vivo: n/a

Reference:

• 1.  Frank-Kamenetsky M, et al. Small-molecule modulators of Hedgehog signaling: identification and characterization of Smoothened agonists and antagonists. (2002) Journal of Biology (1): 10.2-10.19.
• 2.  Borzillo GV, et al. The Hedgehog Signaling Pathway as a Target for Anticancer Drug Discovery. (2005) Current Topics in Medicinal Chemistry (5), 147-157.
• 3.  Pan S, et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med. Chem. Lett., 2010, 1 (3), pp 130–134.