Cyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo).

Purmorphamine, which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo.

GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription.

Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist.

Silmitasertib is a potent and selective inhibitor of CK2 (casein kinase 2).

Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively.

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling.

PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.