1. Stem Cell/Wnt
  2. Smo
  3. LEQ506

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 506 In-stock
Solution
10 mM * 1 mL in DMSO USD 506 In-stock
Solid
5 mg USD 460 In-stock
10 mg USD 680 In-stock
25 mg USD 1160 In-stock
50 mg USD 1560 In-stock
100 mg USD 2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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]

Cellular Effect
Cell Line Type Value Description References
C3H 10T1/2 IC50
< 100 nM
Compound: 19, NVP-LEQ506
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
10.1039/C3MD00334E
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].

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

Clinical Trial
Molecular Weight

432.56

Formula

C25H32N6O

CAS No.
Appearance

Solid

Color

White to yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.15% ee.: 98.93%

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

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
LEQ506
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