| S8200 |
MK-4101 |
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. |
Selective |
|
| S7092 |
SANT-1 |
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 |
| S2151 |
Sonidegib |
Sonidegib 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 |
| S6384 |
SAG (Smoothened Agonist) |
SAG (Smoothened Agonist) is a potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.
|
Selective |
Smo, EC50: 3 nM |
| S7779 |
SAG (Smoothened Agonist) HCl |
SAG (Smoothened Agonist) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. |
Selective |
Smoothened, EC50: 3 nM |
| S2777 |
PF-5274857 |
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, IC50: 5.8 nM; Smoothened, Ki: 4.6 nM |
| S7160 |
Glasdegib (PF-04449913) |
Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
|
Selective |
Smoothened, IC50: 5 nM |
| S1146 |
Cyclopamine |
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 |
| S3042 |
Purmorphamine |
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 |
| S2157 |
Taladegib (LY2940680) |
Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2. |
Selective |
|
| S7138 |
BMS-833923 |
BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2. |
Selective |
|
