LEQ506(Synonyms: NVP-LEQ506)

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LEQ506 (Synonyms: NVP-LEQ506) 纯度: ≥98.0%

LEQ506 是第二代 smoothened (smo) 抑制剂，在人类和小鼠中的 IC50 值分别为 2 和 4 nM。

LEQ506(Synonyms: NVP-LEQ506)

LEQ506 Chemical Structure

CAS No. : 1204975-42-7

规格 价格 是否有货 数量
5 mg ￥5000 In-stock
10 mg ￥8500 In-stock
50 mg   询价  
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生物活性

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]
体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

432.56

Formula

C25H32N6O
CAS 号

1204975-42-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (231.18 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [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.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [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.

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