5.31996

KDM4A/KDM4B Inhibitor, NSC636819

• Synonym(s): KDM4A/KDM4B Inhibitor, NSC636819, JMJD2 Inhibitor, Jumonji C-containing Histone Lysine Demethylase Inhibitor
• Empirical Formula (Hill Notation): C₂₂H₁₂Cl₄N₂O₄
• CAS Number: 1618672-71-1
• Molecular Weight: 510.15
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥97% (HPLC)
• Quality Level: 100
• form: solid
• potency: 3.0 μM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: brown
• solubility: DMSO: 10 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC₅₀ = 6.4 µM; K_i = 5.5 µM) and KDM4B (IC₅₀ = 9.3 µM; K_i = 3.0 µM) and completely blocks their demethylating activity toward H3K9me3 (~ 5 µM). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC₅₀ = 16.5 µM after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 µM over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.

A cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC₅₀ = 6.4 µM; K_i = 5.5 µM) and KDM4B (IC₅₀ = 9.3 µM; K_i = 3.0 µM) and completely blocks their demethylating activity toward H3K9me3 (~ 5 µM). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC₅₀ = 16.5 µM after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 µM over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
KDM4A/B

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Chu, C.H., et al. 2014. Journ. Med. Chem.57, 5975.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable