Hedgehog/Smoothened

Inhibitory Selectivity

Isoform-specific Inhibitors

Hedgehog/Smoothened Products

New Hedgehog/Smoothened Products
Catalog No. Information Product Use Citations Product Validations
S8075

GANT61

GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.

S9743New

Ciliobrevin D

Ciliobrevin D (compound 5) is a cell-permeable, reversible and specific antagonist of AAA+ (ATPases associated with diverse cellular activities) ATPase motor cytoplasmic dynein. Ciliobrevin D perturbs primary cilia formation and blocks Hedgehog (Hh) signaling.

S8249

HPI-4 (Ciliobrevin A)

HPI-4 (Ciliobrevin A, Hedgehog Pathway Inhibitor 4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.

S6565

JK184

JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.

S1146

Cyclopamine

Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

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.

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
S8075

GANT61

GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.

S9743New

Ciliobrevin D

Ciliobrevin D (compound 5) is a cell-permeable, reversible and specific antagonist of AAA+ (ATPases associated with diverse cellular activities) ATPase motor cytoplasmic dynein. Ciliobrevin D perturbs primary cilia formation and blocks Hedgehog (Hh) signaling.

S8249

HPI-4 (Ciliobrevin A)

HPI-4 (Ciliobrevin A, Hedgehog Pathway Inhibitor 4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.

S6565

JK184

JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.

Catalog No. Information Product Use Citations Product Validations
S1146

Cyclopamine

Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

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.

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.

Catalog No. Information Product Use Citations Product Validations
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.

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.