Hedgehog/Smoothened
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S1082 | Vismodegib (GDC-0449) | <1 mg/mL | 84 mg/mL | <1 mg/mL |
| S2157 | Taladegib (LY2940680) | <1 mg/mL | 5 mg/mL | 2 mg/mL |
| S7160 | Glasdegib (PF-04449913) | <1 mg/mL | 47 mg/mL | <1 mg/mL |
| S8075 | GANT61 | <1 mg/mL | <1 mg/mL | 12 mg/mL |
| S8200 | MK-4101 | <1 mg/mL | 98 mg/mL | 60 mg/mL |
| S8249 | HPI-4 (Ciliobrevin A) | <1 mg/mL | 71 mg/mL | 1 mg/mL |
| S4747 | Jervine | <1 mg/mL | 5 mg/mL | 2 mg/mL |
| S1146 | Cyclopamine | <1 mg/mL | <1 mg/mL | 2 mg/mL |
| S2151 | Sonidegib (Erismodegib, NVP-LDE225) | <1 mg/mL | 97 mg/mL | 97 mg/mL |
| S2777 | PF-5274857 | 93 mg/mL | 93 mg/mL | <1 mg/mL |
| S7092 | SANT-1 | <1 mg/mL | 21 mg/mL | 20 mg/mL |
| S7138 | BMS-833923 | <1 mg/mL | 95 mg/mL | <1 mg/mL |
| S3042 | Purmorphamine | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S8597 | LYN-1604 | 100 mg/mL | 50 mg/mL | 100 mg/mL |
| S7779 | Smoothened Agonist (SAG) HCl | 100 mg/mL | 71 mg/mL | 40 mg/mL |
Isoform-specific Inhibitors
- Hedgehog/Smoothened Inhibitors (15)
- New Hedgehog/Smoothened Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| 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. |
SMOΔC captured on cholesterol beads in the presence of increasing concentrations of free vismodegib or 20(S)-OHC (h). Results from one of two independent pull-down experiments are shown. |
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| S2157 |
Taladegib (LY2940680)Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2. |
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| S7160New |
Glasdegib (PF-04449913)Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2. |
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| S8075 |
GANT61GANT61 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. |
Apoptosis evaluation of UACC62R, SK-MEL-28 R and R3 cells treated with Gant61 (10 μM) for 48 h by flow cytometry detection of Annexin V staining. |
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| S8200 |
MK-4101MK-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. |
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| S8249 |
HPI-4 (Ciliobrevin A)HPI-4 (Ciliobrevin A) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo. |
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| S4747 |
JervineJervine is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened. |
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| S1146 |
CyclopamineCyclopamine is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. |
(A)[3H]thymidine incorporation assay of B16F10 melanoma cells treated with DMSO or cyclopamine after incubation with SA-CM from WT and Cav1KO dermal fibroblasts. Representative phase-contrast images of B16F10 cells treated with SA-CM from WT and Cav1KO fibroblasts with cyclopamine are shown on the right. Similar experiments (B) were done with A-375 cells incubated with SA-CM from hTBJ1-shCtrl and hTBJ1-shCAV1 cells. |
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| S2151 |
Sonidegib (Erismodegib, 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. |
RU-SKI 43 blocks Shh signaling. (a) RU-SKI 43 blocks Gli activation. NIH 3T3 cells were cotransfected with vectors encoding 8× Gli-binding site (GliBS)-Firefly luciferase (unless indicated otherwise), Renilla luciferase reporter (pRL-TK) and Shh. Confluent cells were treated with DMSO, 10 μM LDE225, 10 μM RU-SKI 43 or 10 μM C-2. The firefly luciferase (FL)/Renilla luciferase (RL) ratio in cell lysates was calculated and normalized to that measured in DMSO-treated samples; error bars represent mean ± s.d. (n = 2–3). |
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| S2777 |
PF-5274857PF-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. |
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| S7092 |
SANT-1SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM. |
(D) Percentage cell death of OCI-AML3 cells was measured using the CellTiter-Glo® viability assay following 24 hours treatment with either sequential treatment of 1 μM Vorinostat with low (0.1 μM) or high dose (2.5 μM) SANT-1, or single agents. Data represents a biological replicate of 3, with data presented relative to the DMSO control (0% cell death). (E) Protein expression of SHH was measured following 24 hours treated with the four treatment strategies in OCI-AML3 cells. Equal loading was confirmed with β-Actin |
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| S7138 |
BMS-833923BMS-833923 is an orally bioavailable Smoothened antagonist. Phase 2. |
Cell viability assays performed on H1650 and H1975 cells with various concentrations of BMS-833923 (B).
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| S3042 |
PurmorphaminePurmorphamine, 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. |
a-d) LoVo cells were separately or simultaneously treated with 1 μM purmorphamine and 1 μM thiostrepton for the indicated time. a The Gli1, FoxM1, and CCNB1 protein expression levels were examined by immunoblotting after drug treatment for 48 h. b Cell viability was detected after 6 days using an MTT assay. c LoVo cells treated with indicated drugs were cultured for 2 weeks, and outgrowth colonies were stained with crystal violet. d The matched colony count of (c). Error bars represent the mean and S.D. of three independent experiments. **, p < 0.01.
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| S8597New |
LYN-1604LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants. |
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| S7779 |
Smoothened Agonist (SAG) HClSmoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. |
