الصفحة الرئيسية>>Signaling Pathways>> Stem Cell>> Smoothened>>LEQ506 (NVP-LEQ506)

LEQ506 (NVP-LEQ506) (Synonyms: NVP-LEQ506)

رقم الكتالوجGC32954

LEQ506 (NVP-LEQ506) هو مثبط من الجيل الثاني من (Smo) مع IC50s من 2 و 4 نانومتر في الإنسان والفأر ، على التوالي.

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LEQ506 (NVP-LEQ506) التركيب الكيميائي

Cas No.: 1204975-42-7

الحجم السعر المخزون الكميّة
5mg
450٫00
متوفر
10mg
765٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of LEQ506 (NVP-LEQ506)

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

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].

[1]. Peukert S, et al. Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened. ChemMedChem. 2013 Aug;8(8):1261-5. [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.

Protocol of LEQ506 (NVP-LEQ506)

Cell experiment:

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].

References:

[1]. Peukert S, et al. Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened. ChemMedChem. 2013 Aug;8(8):1261-5.
[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.

Chemical Properties of LEQ506 (NVP-LEQ506)

Cas No. 1204975-42-7 SDF
المرادفات NVP-LEQ506
Canonical 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
Formula C25H32N6O M.Wt 432.56
الذوبان DMSO : ≥ 100 mg/mL (231.18 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of LEQ506 (NVP-LEQ506)

Prepare stock solution
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
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Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

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