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.
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- Formule: C22H21N3O5
- Masse moléculaire:407.42
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Description
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[1].
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
76 nM
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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.
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42720483 |
| HEK-293T | EC50 |
16069 nM
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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.
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42720483 |
| HEK-293T | EC50 |
11054 nM
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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
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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.
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42720483 |
| HEK-293T | EC50 |
2299 nM
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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.
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42720483 |
| HEK-293T | EC50 |
4102 nM
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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
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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.
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42720483 |
| HEK-293T | EC50 |
11830 nM
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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.
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42720483 |
| HEK-293T | EC50 |
912 nM
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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.
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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].
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]
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Cell Line:HEK293T cells
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Concentration:1.25 nM-25 μM
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Incubation Time:24 h
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Result:Exhibited no significant cytotoxicity at compound concentrations up to 25 μM.
Related Protocols :
Chemical Information
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Masse moléculaire 407.42
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Formule C22H21N3O5
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SMILES
COC1=C2C=C3C(N=CC(C#N)=C3NC4=CC=CC(OC)=C4OCCOCCO2)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
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AZ137 Related Classifications
HY-189308 Related Classifications
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