420201

JMJD2 Inhibitor, 5-carboxy-8HQ

The JMJD2 Inhibitor, 5-carboxy-8HQ, also referenced under CAS 5852-78-8, controls the biological activity of JMJD2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonyme(s) : JMJD2 Inhibitor, 5-carboxy-8HQ, JHDM Inhibitor I, Histone Lysine Demethylase Inhibitor II, 5-carboxy-8HQ, IOX1
• Formule empirique (notation de Hill): C₁₀H₇NO₃
• Numéro CAS: 5852-78-8
• Poids moléculaire : 189.17
• Numéro MDL: MFCD18417145
• Code UNSPSC : 12352200

Propriétés

• Niveau de qualité: 100
• Essai: ≥95% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: orange
• Solubilité: DMSO: 50 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C10H7NO3/c12-8-4-3-7(10(13)14)6-2-1-5-11-9(6)8/h1-5,12H,(H,13,14)
• Clé InChI: JGRPKOGHYBAVMW-UHFFFAOYSA-N

Description

Description générale

A cell-permeable, 5-carboxy-8-hydroxyquinoline that acts as a 2-oxoglutarate competitive inhibitor of JMJD (IC₅₀ = 200 nM against JMJD2E in a FDH coupled assay). It demonstrates higher selectivity than 2.4-PDCA against other 2-OG oxygenases (IC₅₀ = 2.4 µM, 1.7 µM, 20.5 µM, and 14.3 µM for JMJD2E, JMJD2A, FIH, and PHD2, respectively, in a MALDI-TOF MS assay). Additionally, it is shown to inhibit H3K9me3 demethylation (IC₅₀ = 86.5 µM) in JMJD2A-transfected HeLa cells in a cellular demethylase assay, dose-dependently.




This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the IOX1 probe summary on the SGC website.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Regulatory Review (Z)

Reconstitution

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

Autres remarques

Hamada, S., et al. 2010. J. Med. Chem.53, 5629.
King, D.N.F., et al. 2010. PLoS One5, e15535.

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