5.31996

KDM4A/KDM4B Inhibitor, NSC636819

• Synonyme(s) : KDM4A/KDM4B Inhibitor, NSC636819, JMJD2 Inhibitor, Jumonji C-containing Histone Lysine Demethylase Inhibitor
• Formule empirique (notation de Hill): C₂₂H₁₂Cl₄N₂O₄
• Numéro CAS: 1618672-71-1
• Poids moléculaire : 510.15
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥97% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Puissance: 3.0 μM K_i
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: brown
• Solubilité: DMSO: 10 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

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.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
KDM4A/B

Reversible: yes

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable