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Cat. No.: HY-208740

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PKCζ-IN-2

PKCζ-IN-2 is an orally active, selective PKCζ inhibitor with an IC₅₀ of 0.1 nM. As an anti-inflammatory agent, PKCζ-IN-2 reduces joint swelling and ameliorates disease progression in a mouse collagen-induced arthritis model. PKCζ-IN-2 can be used for the research of rheumatoid arthritis.

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

CAS No.: 2488951-93-3
Formula: C₂₁H₂₃FN₄
Molecular Weight:350.43

Storage:

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

PKCζ-IN-2 Chemical Structure

CAS No.: 2488951-93-3

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Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

PKCζ

0.1 nM (IC₅₀)

All PKC Isoforms :

In Vitro

PKCζ-IN-2 (Compound 37) potently inhibits purified PKCζ kinase activity with an IC₅₀ of 0.0001 μM and exhibits 210-fold selectivity over PKA^[1].
PKCζ-IN-2 exhibits high selectivity against a panel of 381 kinases, with only partial inhibition of FYN (50%) and TrkB (49%) observed^[1].
PKCζ-IN-2 inhibits LPS-stimulated TNFα production in THP-1 human acute monocytic leukemia cells with an IC₅₀ of 0.045 μM^[1].

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

In Vivo

PKCζ-IN-2 (3-30 mg/kg; twice daily; p.o.) reduces joint swelling and ameliorates disease progression in a mouse collagen-induced arthritis model^[1].

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

Animal Model:

Collagen-induced arthritis model^[1]
Dosage:

3, 10, 30 mg/kg
Administration:

twice daily; p.o.
Result:

Dose-dependently
ameliorated CIA progression, with reduced joint swelling in a
dose-dependent manner.

Chemical Information

CAS No. 2488951-93-3
Molecular Weight 350.43
Formula C₂₁H₂₃FN₄
SMILES

NC1=CC(F)=C(C2=CC3=CN=CC=C3C(N[C@H]4CCCCNC4)=C2)C=C1
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]. Atobe M, et al. Discovery of 4,6- and 5,7-Disubstituted Isoquinoline Derivatives as a Novel Class of Protein Kinase C ζ Inhibitors with Fragment-Merging Strategy. Journal of medicinal chemistry. 2020 Jul 09;63(13):7143-7162. [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
- In Vivo
Chemical Information
Purity & Documentation
References

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PKCζ-IN-2

All PKC Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PKCζ-IN-2 Related Classifications

HY-208740 Related Classifications