S1082 |
Vismodegib (GDC-0449)
|
Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay. |
-
Nat Commun, 2022, 13(1):1439
-
Neuro Oncol, 2022, noac001
-
Front Immunol, 2022, 13:841045
|
|
S2157 |
Taladegib (LY2940680)
|
Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2. |
-
Sci Rep, 2022, 12(1):7
-
Carcinogenesis, 2020, 41(7):993-1004
-
Sci Rep, 2019, 9(1):1897
|
|
S2476 |
Itraconazole (R 51211)
|
Itraconazole (R 51211) is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy. |
-
Microbiol Spectr, 2022, 10(1):e0200721
-
BMC Microbiol, 2022, 22(1):21
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S4747 |
Jervine
|
Jervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened. |
-
Sci Rep, 2022, 12(1):7
-
Neurochem Int, 2021, 146:105042
|
|
S6565 |
JK184
|
JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells. |
-
Cell Res, 2020, 10.1038/s41422-020-00426-0
|
|
S7160 |
Glasdegib (PF-04449913)
|
Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
|
-
Front Cell Dev Biol, 2021, 9:662868
-
Genome Med, 2020, 18;12(1):17
|
|
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. |
-
Cell Death Dis, 2022, 13(2):136
-
Front Immunol, 2022, 13:841045
-
Future Med Chem, 2022, 14(7):479-500
|
|
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. |
-
Sci Rep, 2022, 12(1):7
|
|
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. |
-
FASEB J, 2020, 10.1096/fj.201901852RR
-
Front Pharmacol, 2019, 10:290
-
PLoS One, 2019, 14(5):e0216642
|
|
S9743 |
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. |
|
|
A5208 |
ULK3 Rabbit Recombinant mAb
|
ULK3 Rabbit Recombinant mAb detects endogenous level of total ULK3. |
|
|
S1146 |
Cyclopamine
|
Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. |
-
Cell Rep, 2022, 38(7):110379
-
Cell Death Dis, 2022, 13(2):136
-
Oxid Med Cell Longev, 2022, 2022:9955677
|
|
S2151 |
Sonidegib (NVP-LDE225)
|
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. |
-
J Mol Cell Biol, 2022, mjab082
-
Biochem Pharmacol, 2022, 199:115009
-
CNS Neurosci Ther, 2022, 10.1111/cns.13835
|
|
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. |
-
Sci Rep, 2022, 12(1):7
-
Biol Reprod, 2021, ioab111
-
Carcinogenesis, 2020, 41(7):993-1004
|
|
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. |
-
Sci Rep, 2022, 12(1):7
-
Adv Sci (Weinh), 2021, e2103495
-
ACS Appl Mater Interfaces, 2021, 13(2):3199-3208
|
|
S7138 |
BMS-833923
|
BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2. |
-
Sci Rep, 2022, 12(1):7
-
Mol Cancer Res, 2021, molcanres.MCR-21-0257-A.2021
-
Carcinogenesis, 2020, 41(7):993-1004
|
|
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. |
-
Nat Commun, 2022, 13(1):1439
-
Oxid Med Cell Longev, 2022, 2022:9955677
-
Cancer Cell, 2021, 39(3):407-422.e13
|
|
S6384New |
Smoothened Agonist (SAG)
|
Smoothened Agonist (SAG) is potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.
|
-
Nat Commun, 2022, 13(1):2387
-
J Nat Med, 2022, 10.1007/s11418-022-01603-8
-
EMBO Rep, 2021, e53015
|
|
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. |
-
Nat Commun, 2022, 13(1):2387
-
EMBO Mol Med, 2022, e14990
-
Front Immunol, 2022, 13:841045
|
|
S1082 |
Vismodegib (GDC-0449)
|
Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay. |
- Nat Commun, 2022, 13(1):1439
- Neuro Oncol, 2022, noac001
- Front Immunol, 2022, 13:841045
|
|
S2157 |
Taladegib (LY2940680)
|
Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2. |
- Sci Rep, 2022, 12(1):7
- Carcinogenesis, 2020, 41(7):993-1004
- Sci Rep, 2019, 9(1):1897
|
|
S2476 |
Itraconazole (R 51211)
|
Itraconazole (R 51211) is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy. |
- Microbiol Spectr, 2022, 10(1):e0200721
- BMC Microbiol, 2022, 22(1):21
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S4747 |
Jervine
|
Jervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened. |
- Sci Rep, 2022, 12(1):7
- Neurochem Int, 2021, 146:105042
|
|
S6565 |
JK184
|
JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells. |
- Cell Res, 2020, 10.1038/s41422-020-00426-0
|
|
S7160 |
Glasdegib (PF-04449913)
|
Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
|
- Front Cell Dev Biol, 2021, 9:662868
- Genome Med, 2020, 18;12(1):17
|
|
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. |
- Cell Death Dis, 2022, 13(2):136
- Front Immunol, 2022, 13:841045
- Future Med Chem, 2022, 14(7):479-500
|
|
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. |
- Sci Rep, 2022, 12(1):7
|
|
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. |
- FASEB J, 2020, 10.1096/fj.201901852RR
- Front Pharmacol, 2019, 10:290
- PLoS One, 2019, 14(5):e0216642
|
|
S9743 |
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. |
|
|
S1146 |
Cyclopamine
|
Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. |
- Cell Rep, 2022, 38(7):110379
- Cell Death Dis, 2022, 13(2):136
- Oxid Med Cell Longev, 2022, 2022:9955677
|
|
S2151 |
Sonidegib (NVP-LDE225)
|
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. |
- J Mol Cell Biol, 2022, mjab082
- Biochem Pharmacol, 2022, 199:115009
- CNS Neurosci Ther, 2022, 10.1111/cns.13835
|
|
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. |
- Sci Rep, 2022, 12(1):7
- Biol Reprod, 2021, ioab111
- Carcinogenesis, 2020, 41(7):993-1004
|
|
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. |
- Sci Rep, 2022, 12(1):7
- Adv Sci (Weinh), 2021, e2103495
- ACS Appl Mater Interfaces, 2021, 13(2):3199-3208
|
|
S7138 |
BMS-833923
|
BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2. |
- Sci Rep, 2022, 12(1):7
- Mol Cancer Res, 2021, molcanres.MCR-21-0257-A.2021
- Carcinogenesis, 2020, 41(7):993-1004
|
|