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製品番号: HY-182402

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Notum-IN-2

Notum-IN-2 is a partially brain-penetrant Notum carboxyl-esterase inhibitor with an IC₅₀ of 18 nM. Notum-IN-2 can be used as a chemical tool for exploring Wnt signalling in cells.

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CAS 番号: 2411969-28-1
分子式: C₉H₄ClF₃N₂O₂
分子量:264.59

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Notum-IN-2 構造式

CAS 番号: 2411969-28-1

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数量

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

Notum-IN-2 is a partially brain-penetrant Notum carboxyl-esterase inhibitor with an IC₅₀ of 18 nM. Notum-IN-2 can be used as a chemical tool for exploring Wnt signalling in cells^[1]^[2].

Carboxylesterase (CES) アイソフォーム固有の製品をすべて表示 :

Wnt アイソフォーム固有の製品をすべて表示 :

体外実験

Notum-IN-2 (6ZVL) potently inhibits Notum carboxyl-esterase with an IC₅₀ of 0.018 μM, achieving a 640-fold potency increase from its parent fragment hit^[1].
Notum-IN-2 (0.3 nM- 10 μM) shows an activation of Wnt signaling (EC₅₀ = 3500 nM) in a cell-based TCF/LEF reporter gene (Luciferase) assay through the inhibition of Notum in a concentration-dependent manner^[2].

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

体内実験

Notum-IN-2 (6ZVL) (10 mg/kg; p.o.; single dose) has a rapid absorption and modest BBB penetration in male C57BL6 mice^[2].

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

Animal Model:

C57BL6 mice (male)^[2]
Dosage:

10 mg/kg
Administration:

p.o.; single dose
Result:

Had a rapid absorption and modest BBB penetration.

化学情報

CAS 番号 2411969-28-1
分子量 264.59
分子式 C₉H₄ClF₃N₂O₂
SMILES

O=C1OC(C2=CC(C(F)(F)F)=C(Cl)C=C2)=NN1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Li ASM, et al. Discovery of Nanomolar DCAF1 Small Molecule Ligands. J Med Chem. 2023;66(7):5041-5060. [Content Brief]

[2]. Mahy W, et al. 5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit. J Med Chem. 2020 Nov 12;63(21):12942-12956. [Content Brief]

Calculators

モル濃度計算機

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

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希釈計算機

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濃度 _(開始) 濃度 _(開始)

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濃度 _(終了) 濃度 _(終了)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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生物活性
- 製品説明
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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Notum-IN-2

Carboxylesterase (CES) アイソフォーム固有の製品をすべて表示

Wnt アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Notum-IN-2 関連分類

HY-182402 関連分類