LEQ506
Based on 1 Customer Validation
LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.
For research use only. We do not sell to patients.
- Purity: 98.92%
- CAS No.: 1204975-42-7
- Formula: C25H32N6O
- Molecular Weight:432.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 2 nM (human smo), 4 nM (mouse smo)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C3H 10T1/2 | IC50 |
<100 nM
Compound: 19, NVP-LEQ506
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Inhibition of Smo D473H mutant (unknown origin) expressed in mouse C3H10T1/2 cells by luciferase assay
Inhibition of Smo D473H mutant (unknown origin) expressed in mouse C3H10T1/2 cells by luciferase assay
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10.1039/C3MD00334E |
LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively. LEQ506 inhibits Hedgehog (Hh) signaling in a human cell line (HEPM) as measured by the amount of Gli mRNA with an IC50 ~6-fold lower than that of Compound 2[1]. LEQ506 is an efficacious compound by consistently decreasing Gli1 mRNA by about 70 to 80%. LEQ506 shows a tendency to preferentially inhibit Gli1 rather than Ptch1 mRNA. LEQ506 (at 1%) is also an efficacious compound with an inhibition of 80 to 90% for Gli1 and of 60 to 70% for Ptch1[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1204975-42-7
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Appearance Solid
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Molecular Weight 432.56
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Formula C25H32N6O
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Color White to yellow
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SMILES
OC(C)(C)C1=NC=C(N2[C@H](C)CN(C3=NN=C(CC4=CC=CC=C4)C(C)=C3C)CC2)N=C1
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Synonyms
NVP-LEQ506
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 100 mg/mL (231.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
DAOY cells are serum starved 16 h before experiments and subsequently incubated for 24 h with sonic Hedgehog (SHH) (50 nM) and LEQ506 at different concentrations. Cells are then washed twice with PBS and stored at -80°C until RNA isolation. Total RNA is isolated using the RNeasy Mini Kit. The amount and quality of extracted RNA are determined using the 2100 Bioanalyzer[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Peukert S, et al. Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened. ChemMedChem. 2013 Aug;8(8):1261-5. [Content Brief]
[2]. Lauressergues E, et al. Pharmacological evaluation of a series of smoothened antagonists in signaling pathways and after topical application in a depilated mouse model. Pharmacol Res Perspect. 2016 Mar 4;4(2):e00214. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3118 mL | 11.5591 mL | 23.1182 mL | 57.7955 mL |
| 5 mM | 0.4624 mL | 2.3118 mL | 4.6236 mL | 11.5591 mL | |
| 10 mM | 0.2312 mL | 1.1559 mL | 2.3118 mL | 5.7795 mL | |
| 15 mM | 0.1541 mL | 0.7706 mL | 1.5412 mL | 3.8530 mL | |
| 20 mM | 0.1156 mL | 0.5780 mL | 1.1559 mL | 2.8898 mL | |
| 25 mM | 0.0925 mL | 0.4624 mL | 0.9247 mL | 2.3118 mL | |
| 30 mM | 0.0771 mL | 0.3853 mL | 0.7706 mL | 1.9265 mL | |
| 40 mM | 0.0578 mL | 0.2890 mL | 0.5780 mL | 1.4449 mL | |
| 50 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1559 mL | |
| 60 mM | 0.0385 mL | 0.1927 mL | 0.3853 mL | 0.9633 mL | |
| 80 mM | 0.0289 mL | 0.1445 mL | 0.2890 mL | 0.7224 mL | |
| 100 mM | 0.0231 mL | 0.1156 mL | 0.2312 mL | 0.5780 mL |
LEQ506 Related Classifications
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