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Key Documents

420202

Sigma-Aldrich

JMJD Histone Demethylase Inhibitor III

The JMJD Histone Demethylase Inhibitor III controls the biological activity of JMJD Histone Demethylase. This small molecule/inhibitor is primarily used for Cell Structure applications.

Sinónimos:

JMJD Histone Demethylase Inhibitor III, JHDM Inhibitor III, Histone Lysine Demethylase Inhibitor X, ( E)-4-(Hydroxy(4-(4-((naphthalen-1-ylcarbamoyloxy)methyl)benzylamino)butyl)amino)-4-oxobut-2-enoic acid

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About This Item

Fórmula empírica (notación de Hill):
C27H29N3O6
Número de CAS:
Peso molecular:
491.54
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.32

Quality Level

assay

≥95% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

O=C(NC1=CC=CC2=C1C=CC=C2)OCC3=CC=C(CNCCCCN(O)C(/C=C/C(O)=O)=O)C=C3

General description

A substrate (methyl lysine) and cofactor (α-ketoglutarate) mimicking bivalent benzylamino-butylamino-N-hydroxybutenoic acid compound that acts as a selective in vitro inhibitor of Jumonji domain-containing histone demethylases (JHDMs; IC50 = 4.3, 3.4, 5.9, 10 and 43 µM for JMJD2A, JMJD2C, JMJD2E, PHF8 and JMJD3, respectively) over LSD1, asparaginyl and prolyl hydroxylases, and histone deacetylases (IC50 = 54, 83, 31, 22, 620, 680 and >800 µM for PHD1, PHD2, PHD3, FIH, LSD1 and HDACs, respectively). The cellular active JHDM Inhibitor, Methylstat is also available (Cat. No. 420203).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Luo, X., et al. 2011. J. Am. Chem. Soc.133, 9451.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Xuelai Luo et al.
Journal of the American Chemical Society, 133(24), 9451-9456 (2011-05-19)
Histone methylations are important chromatin marks that regulate gene expression, genomic stability, DNA repair, and genomic imprinting. Histone demethylases are the most recent family of histone-modifying enzymes discovered. Here, we report the characterization of a small-molecule inhibitor of Jumonji C

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