KDM4A/KDM4B Inhibitor, NSC636819-Calbiochem

C₂₂H₁₂Cl₄N₂O₄

510.15

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.
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.

Cell permeable: yes
Primary Target
KDM4A/B
Reversible: yes

Toxicity: Standard Handling (A)

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

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

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

100

≥97% (HPLC)

solid

3.0 μM K_i

Calbiochem^®

OK to freeze
protect from light

brown

DMSO: 10 mg/mL

2-8℃

Packaged under inert gas

11 - Combustible Solids

WGK 3