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.

• Sinônimo(s): JMJD2 Inhibitor, 5-carboxy-8HQ, JHDM Inhibitor I, Histone Lysine Demethylase Inhibitor II, 5-carboxy-8HQ, IOX1
• Fórmula empírica (Notação de Hill): C₁₀H₇NO₃
• Número CAS: 5852-78-8
• Peso molecular: 189.17
• Número MDL: MFCD18417145
• Código UNSPSC: 12352200

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: orange
• solubilidade: DMSO: 50 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 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)
• chave InChI: JGRPKOGHYBAVMW-UHFFFAOYSA-N

Descrição

Descrição geral

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.

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.

Embalagem

Packaged under inert gas

Advertência

Toxicity: Regulatory Review (Z)

Reconstituição

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable