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  3. LEQ506

LEQ506 (Synonyms: NVP-LEQ506)

Cat. No.: HY-18636 Purity: 98.27% ee.: 98.93%
Handling Instructions

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.

LEQ506 Chemical Structure

LEQ506 Chemical Structure

CAS No. : 1204975-42-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 1144 In-stock
Estimated Time of Arrival: December 31
1 mg USD 751 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1202 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1923 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

LEQ506 is a second-generation inhibitor of smoothened (Smo) with IC50s of 2 and 4 nM in human and mouse, respectively.

IC50 & Target

IC50: 2 nM (human smo), 4 nM (mouse smo)[1]

In Vitro

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].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (231.18 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3118 mL 11.5591 mL 23.1182 mL
5 mM 0.4624 mL 2.3118 mL 4.6236 mL
10 mM 0.2312 mL 1.1559 mL 2.3118 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

432.56

Formula

C₂₅H₃₂N₆O

CAS No.

1204975-42-7

SMILES

OC(C)(C)C1=NC=C(N2[[email protected]](C)CN(C3=NN=C(CC4=CC=CC=C4)C(C)=C3C)CC2)N=C1

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.27% ee.: 98.93%

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LEQ506
Cat. No.:
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LEQ506

Cat. No.: HY-18636