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製品番号: HY-189308

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AZ137

AZ137 is a selective, ATP-competitive type I HIPK4 inhibitor with an IC₅₀ of 11 nM for hHIPK4. AZ137 inhibits HIPK4-dependent F-actin remodeling. AZ137 can be used for research on cutaneous squamous cell carcinoma.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

分子式: C₂₂H₂₁N₃O₅
分子量:407.42

保管条件:

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

AZ137 構造式

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性

製品説明

Cellular Effect

Cell Line	Type	Value	Description	References
HEK-293T	EC50	76 nM	Cellular target engagement of HIPK4 in intact HEK293T cells overexpressing HIPK4-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of HIPK4 in intact HEK293T cells overexpressing HIPK4-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483
HEK-293T	EC50	16069 nM	Cellular target engagement of HIPK1 in intact HEK293T cells overexpressing HIPK1-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of HIPK1 in intact HEK293T cells overexpressing HIPK1-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483
HEK-293T	EC50	11054 nM	Cellular target engagement of HIPK2 in intact HEK293T cells overexpressing HIPK2-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of HIPK2 in intact HEK293T cells overexpressing HIPK2-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483
HEK-293T	EC50	15613 nM	Cellular target engagement of HIPK3 in intact HEK293T cells overexpressing HIPK3-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of HIPK3 in intact HEK293T cells overexpressing HIPK3-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483
HEK-293T	EC50	2299 nM	Cellular target engagement of CLK1 in intact HEK293T cells overexpressing CLK1-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of CLK1 in intact HEK293T cells overexpressing CLK1-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483
HEK-293T	EC50	4102 nM	Cellular target engagement of CLK2 in intact HEK293T cells overexpressing CLK2-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of CLK2 in intact HEK293T cells overexpressing CLK2-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483
HEK-293T	EC50	6209 nM	Cellular target engagement of CLK4 in intact HEK293T cells overexpressing CLK4-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of CLK4 in intact HEK293T cells overexpressing CLK4-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483
HEK-293T	EC50	11830 nM	Cellular target engagement of BMP2K in intact HEK293T cells overexpressing BMP2K-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of BMP2K in intact HEK293T cells overexpressing BMP2K-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483
HEK-293T	EC50	912 nM	Cellular target engagement of DYRK2 in intact HEK293T cells overexpressing DYRK2-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound. Cellular target engagement of DYRK2 in intact HEK293T cells overexpressing DYRK2-NanoLuciferase fusion constructs assessed by NanoBRET assay after 2.5 hrs incubation with tracer and compound.	42720483

体外実験

AZ137 is a potent inhibitor of recombinant hHIPK4 with an IC₅₀ of 11 nM^[1].
AZ137 (2.5 h) acts on HIPK4 with an EC₅₀ of 76 nM in intact HEK293T cells^[1].
AZ137 (2.5 h) demonstrates high selectivity for HIPK4 over HIPK1-3, CLK1/2/4, YSK4, BMP2K, and DYRK2 in cellular target engagement assays^[1].
AZ137 (1.25 nM-25 μM; 24 h) has no significant effect on HEK293T cell viability at concentrations up to 25 μM^[1].
AZ137 (0.2-5 μM) reverses HIPK4-driven F-actin remodeling in NIH-3T3 cells in a dose-dependent manner and restores normal actin architecture at 1 and 5 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:

HEK293T cells
Concentration:

1.25 nM-25 μM
Incubation Time:

24 h
Result:

Exhibited no significant cytotoxicity at compound concentrations up to 25 μM.

Related Protocols :

Phalloidin F-actin cytoskeleton staining

化学情報

分子量 407.42
分子式 C₂₂H₂₁N₃O₅
SMILES

COC1=C2C=C3C(N=CC(C#N)=C3NC4=CC=CC(OC)=C4OCCOCCO2)=C1
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]. Zerva A, et al. Macrocyclization of Broad-Spectrum Kinase Inhibitor Bosutinib Leads to Potent and Selective Quinoline-Based HIPK4 Inhibitor AZ137. Journal of medicinal chemistry. 2026 Sep 10;69(17):20616-20638. [Content Brief]

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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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MOQ

Minimum order quantity

100 mg

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