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Cat. No.: HY-183653

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AK442

AK442 is a selective PRMT4 (CARM1) inhibitor with an IC₅₀ of 2.6 nM against human targets. AK442 is applicable to breast cancer-related research.

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

CAS No.: 3062376-05-7
Formula: C₃₅H₄₀ClN₉O₄
Molecular Weight:686.20

Storage:

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

AK442 Chemical Structure

CAS No.: 3062376-05-7

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Protocols (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

AK442 is a selective PRMT4 (CARM1) inhibitor with an IC₅₀ of 2.6 nM against human targets. AK442 is applicable to breast cancer-related research^[1].

IC₅₀ & Target

^[1]

PRMT4

All Histone Methyltransferase Isoforms :

In Vitro

AK442 (10 μM; 6.5 h) binds to PRMT4 in MDA-MB-231 cells and increases the thermal stability of PRMT4 by 2 °C compared with the DMSO control group^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Chemical Information

CAS No. 3062376-05-7
Molecular Weight 686.20
Formula C₃₅H₄₀ClN₉O₄
SMILES

O[C@H]1[C@@H](O)[C@H](N2C(N=CN=C3N)=C3N=C2)O[C@@H]1CN(CCNCC4=CC(C5=CC=C(C=C5)Cl)=CC=C4)CCNC(NCC6=CC=CC=C6)=O
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 Animals and Diseases

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.
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Kulkarni AS, et al. Tailoring PRMT Inhibition: Shifting PRMT7 Selectivity to PRMT4 through "T-Shape" Strategy and "Linker-Specific" Preferences. J Med Chem. 2026 May 14;69(9):9977-9990. [Content Brief]

Calculators

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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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