Sigma-Aldrich Kdm4a/Kdm4b Inhibitor Nsc6

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

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: yesPrimary Target
KDM4A/BReversible: 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.CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany