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420201 Sigma-Aldrich

JMJD2 Inhibitor, 5-carboxy-8HQ - CAS 5852-78-8 - Calbiochem

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.

Synonym: JHDM Inhibitor I, Histone Lysine Demethylase Inhibitor II, 5-carboxy-8HQ, IOX1

  • CAS Number 5852-78-8

  • Linear Formula C10H7NO3

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Properties

Related Categories Bioactive Small Molecules for Epigenetic Research, Biochemicals and Reagents, Epigenetics, Histone Methylation Modulators, Molecular Biology More...
brand family   Calbiochem
packaging   5 mg in Glass bottle (420201-5MG)
form   Orange solid
purity   ≥95% by HPLC
toxicity   Regulatory Review
shipped in   ambient
storage temp.   +2C to +8C
storage conditions   Protect from light
  Ok to freeze

Description

Overview

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.

Packaging

Packaged under inert gas

Storage and Shipping Instructions

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

Safety & Documentation

Safety Information

Safety Information for this product is unavailable at this time.
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