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(s):
JMJD2 Inhibitor, 5-carboxy-8HQ - CAS 5852-78-8 - Calbiochem, JHDM Inhibitor I, Histone Lysine Demethylase Inhibitor II, 5-carboxy-8HQ, IOX1
Empirical Formula (Hill Notation):
C10H7NO3
CAS Number:
Molecular Weight:
189.17
MDL number:

storage conditions

+2C to +8C

Quality Level

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

orange

solubility

DMSO: 50 mg/mL

shipped in

ambient

storage temp.

2-8°C

General description

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.
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.

Packaging

5 mg in Glass bottle
Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

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

Other Notes

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

Legal Information

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

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis

Certificate of Origin

Shohei Hamada et al.
Journal of medicinal chemistry, 53(15), 5629-5638 (2010-08-06)
Selective inhibitors of Jumonji domain-containing protein (JMJD) histone demethylases are candidate anticancer agents as well as potential tools for elucidating the biological functions of JMJDs. On the basis of the crystal structure of JMJD2A and a homology model of JMJD2C...
Oliver N F King et al.
PloS one, 5(11), e15535-e15535 (2010-12-03)
Small molecule modulators of epigenetic processes are currently sought as basic probes for biochemical mechanisms, and as starting points for development of therapeutic agents. N(ε)-Methylation of lysine residues on histone tails is one of a number of post-translational modifications that...

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service

Social Media

LinkedIn icon
Twitter icon
Facebook Icon
Instagram Icon

MilliporeSigma

Research. Development. Production.

We are a leading supplier to the global Life Science industry with solutions and services for research, biotechnology development and production, and pharmaceutical drug therapy development and production.

© 2021 Merck KGaA, Darmstadt, Germany and/or its affiliates. All Rights Reserved.

Reproduction of any materials from the site is strictly forbidden without permission.