Smoothened Selective Inhibitors | Agonists | Antagonists
|Catalog No.||Product Name||Information||Selective / Pan||IC50 / Ki|
MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.
SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.
|Selective||Smoothened receptor, Kd: 1.2 nM|
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. Phase 3.
|Selective||Smo (mouse), IC50: 1.3 nM; Smo (human), IC50: 2.5 nM|
|S7779||Smoothened Agonist (SAG) HCl||
Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
|Selective||Smoothened, EC50: 3 nM|
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.
|Selective||Smoothened, Ki: 4.6 nM; Smoothened, IC50: 5.8 nM|
Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
|Selective||Smoothened, IC50: 5 nM|
Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.
|Selective||Smoothened, IC50: 46 nM|
Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.
|Selective||Smoothened, IC50: ~1.5 μM|
Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.
BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.
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