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LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC₅₀s of 2 and 4 nM in human and mouse, respectively.

LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC₅₀s of 2 and 4 nM in human and mouse, respectively. LEQ506 inhibits Hedgehog (Hh) signaling in a human cell line (HEPM) as measured by the amount of Gli mRNA with an IC₅₀ ~6-fold lower than that of Compound 2. LEQ506 is an efficacious compound by consistently decreasing Gli1 mRNA by about 70 to 80%. LEQ506 shows a tendency to preferentially inhibit Gli1 rather than Ptch1 mRNA. LEQ506 (at 1%) is also an efficacious compound with an inhibition of 80 to 90% for Gli1 and of 60 to 70% for Ptch1.

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