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Cat. No.: HY-182103

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ZAK-IN-2

ZAK-IN-2 (Compound 8) is a selective, covalent ZAK inhibitor with an IC₅₀ of 11.5 nM. ZAK-IN-2 forms a covalent bond with Cys22 in the P-loop of ZAK to inhibit its kinase activity. ZAK-IN-2 inhibits the phosphorylation of the downstream target p38. ZAK-IN-2 blocks Doxorubicin (HY-15142A)-induced cleavage of Caspase 3. ZAK-IN-2 is applicable to research related to myocardial hypertrophy.

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

CAS No.: 3033697-19-4
Formula: C₃₃H₂₆F₂N₈O₄S
Molecular Weight:668.67

Storage:

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

ZAK-IN-2 Chemical Structure

CAS No.: 3033697-19-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

p38

Caspase 3

All MAP3K Isoforms :

All Caspase Isoforms :

All p38 MAPK Isoforms :

In Vitro

ZAK-IN-2 (60 min) potently inhibits recombinant ZAK kinase with an IC₅₀ of 11.5 nM, and exhibits high selectivity over B-raf^V600E^[1].
ZAK-IN-2 (0.01-10 μM; 1 h) dose-dependently inhibits ZAKα kinase activity in U2OS cells, which is verified by the reduced phosphorylation level of downstream p38^[1].

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

Western Blot Analysis^[1]

Cell Line:

Human U2OS osteosarcoma cells, CRISPR-generated ZAK knockout U2OS cells
Concentration:

10 μM
Incubation Time:

Undefined
Result:

Prevented doxorubicin-induced caspase 3 cleavage in U2OS cells, matching the effect seen in ZAK knockout cells.
Inhibited doxorubicin-induced phosphorylation of p38 and JNK.
Prevented massive cell death induced by 24 h doxorubicin treatment in U2OS cells, matching the protection seen in ZAK knockout cells.

Chemical Information

CAS No. 3033697-19-4
Molecular Weight 668.67
Formula C₃₃H₂₆F₂N₈O₄S
SMILES

O=C(N1CCC(C1)OC2=NNC3=C2C=C(C4=CN(C5=C(F)C(NS(=O)(C6=CC=CC(C7=CC=CC=C7)=C6)=O)=CC=C5F)N=N4)C=N3)C=C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhou Y, et al. Rational Design of Covalent Kinase Inhibitors by an Integrated Computational Workflow (Kin-Cov). J Med Chem. 2023;66(11):7405-7420. [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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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ZAK-IN-2

All MAP3K Isoforms

All Caspase Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

ZAK-IN-2 Related Classifications

HY-182103 Related Classifications