country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Cat. No.: HY-125243

Copy Link Print Information

KDM5A-IN-2

KDM5A-IN-2 is a KDM5A inhibitor. The human IC₅₀ values of KDM5A-IN-2 for KDM5A, KDM5B, and KDM4A are 0.11 μM, 0.22 μM, and 5.3 μM, respectively. KDM5A-IN-2 inhibits KDM5B- and KDM4A-mediated histone lysine demethylation.

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

CAS No.: 2281766-67-2
Formula: C₂₈H₃₄N₄O₄S
Molecular Weight:522.66

Storage:

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

KDM5A-IN-2 Chemical Structure

CAS No.: 2281766-67-2

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

KDM5A

0.11 μM (IC₅₀)

KDM5B

0.22 μM (IC₅₀)

KDM4A

5.3 μM (IC₅₀)

All Histone Demethylase Isoforms :

In Vitro

KDM5A-IN-2 (N71) inhibits KDM5B (1-755)ΔAP with an IC₅₀ of 0.22 μM, showing 24-fold selectivity over KDM4A (1-350) in AlphaLISA^[1].
KDM5A-IN-2 (preincubation 20 min; reaction 10 min) inhibits KDM5A (1-739)ΔAP with an IC₅₀ of 0.10-0.18 μM across a range of 10-1000 μM αKG, exhibiting enzyme concentration-dependent and time-dependent inhibition^[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. 2281766-67-2
Molecular Weight 522.66
Formula C₂₈H₃₄N₄O₄S
SMILES

O=C(C1=C2C(C=C(C(C3=CC=CC(NC(/C=C/CN(C)C)=O)=C3)OCCN4CCCCC4)S2)=NC=C1)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

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.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Horton JR, et al. Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A. Journal of medicinal chemistry. 2018 Dec 13;61(23):10588-10601.

Calculators

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Get Quote In-stock

Other size

Get Quote