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Cat. No.: 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.

For research use only. We do not sell to patients.

Formula: C₂₂H₂₁N₃O₅
Molecular Weight:407.42

Storage:

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

AZ137 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Protocols (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

In Vitro

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. Further protocols information, click here.

Cell Viability Assay^[1]

View Protocol

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.

Chemical Information

Molecular Weight 407.42
Formula C₂₂H₂₁N₃O₅
SMILES

COC1=C2C=C3C(N=CC(C#N)=C3NC4=CC=CC(OC)=C4OCCOCCO2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Phalloidin F-actin cytoskeleton staining
Phalloidin F-actin staining detects polymerized filamentous actin in fixed and permeabilized specimens by using fluorescent phalloidin or phalloidin-derived phallotoxins that bind actin filaments and generate a fluorescence microscopy readout corresponding to F-actin organization, including stress fibers, cortical actin, filament bundles, and tissue-specific actin networks. Phalloidin stabilizes F-actin by reducing actin subunit dissociation from filament ends, and fluorescent phallotoxins were established as tools for visualizing actin-containing structures in eukaryotic cells.

Purity & Documentation

Handling Instructions (2659 KB)

References

[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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