Quality Segment
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
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)
InChI key
JGRPKOGHYBAVMW-UHFFFAOYSA-N
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.
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
Preparation Note
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.
King, D.N.F., et al. 2010. PLoS One5, e15535.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Regulatory Review (Z)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable