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LDE225 (NVP-LDE225, also known as Sonidegib or erismodegib) is a potent and selective Hedgehog signaling pathway inhibitor (Smoothened antagonist) reduces melanoma growth in vitro and in vivo. NVP-LDE225 was potent in reducing cell proliferation and inducing tumor growth arrest in vitro and in vivo, respectively. Pharmacologic inhibition of BRAF(V600E) in human melanoma cell lines resulted in decreased expression of GLI1 thus demonstrating interaction of SHH-GLI and MAPK pathways. Inhibition of SHH-GLI pathway by the novel small molecule inhibitor of smoothened NVP-LDE225 was followed by inhibition of cell growth and induction of apoptosis in human melanoma cell lines, interestingly with both BRAF(V600E) and BRAF(Wild Type) status.
Cell Res. 2023 Jun;33(6):464-478.
SCUBE2 mediates bone metastasis of luminal breast cancer by modulating immune-suppressive osteoblastic niches
LDE225 purchased from AbMole
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Source | BMC Cancer (2017). Figure 4. LDE225 |
| Method | western blot | |
| Cell Lines | BALB/c nude mice | |
| Concentrations | 80 mg/kg | |
| Incubation Time | 41 day | |
| Results | Western blotting showed increased amounts of GLI1 in tumors from animals treated with 177Lu-octreotate monotherapy and combination treatment, and increased amounts of GLI2 in tumors from the combination therapy group, compared with controls |
| Molecular Weight | 485.5 |
| Formula | C26H26F3N3O3 |
| CAS Number | 956697-53-3 |
| Solubility (25°C) | DMSO 60 mg/mL Ethanol 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Hedgehog Products |
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TPB15 is an orally potent Hh (Hedgehog) signaling inhibitor that significantly induces MDA-MB-468 cell cycle arrest and apoptosis. TPB15 also blocks Smo (Smoothened) translocation into cilia and reduces Smo protein and mRNA expression. In addition, TPB15 can inhibit the expression of downstream regulator Glioma-associated oncogene 1 (Gli1). TPB15 has good anti-tumor activity and low toxicity. |
| Hedgehog IN-3
Hedgehog IN-3 is a hedgehog pathway inhibitor (IC50 = 0.01 µM). |
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| Physalin H
Physalin H is an inhibitor of Hedgehog (Hh) signaling and it disrupts GLI1-DNA-complex formation. Physalin H inhibits GLI1 transcription with an IC50 value of 0.7 μM. Physalin H shows cytotoxicity to PANC1 and DU145 cells with IC50 values of 5.7 and 6.8 μM, respectively. |
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Products are for research use only. Not for human use. We do not sell to patients.
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