JMJD2D Inhibitor Screening Assay Kit

Cayman Chemical Item Number 700370

Jumonji Domain Containing 2D Inhibitor Screening Assay Kit

Description

Jumonji Domain Containing 2D (JMJD2D) is a Jumonji C (JmjC) histone demethylase that catalyzes the demethylation of mono-, di-, and trimethylated lysine 9 of histone H3. Cayman’s JMJD2D Inhibitor Screening Assay Kit provides a convenient fluorescence-based method for screening JMJD2D inhibitors. The assay is based on the multistep reaction in which JMJD2D first produces formaldehyde during the demethylation of the trimethylated peptide substrate, histone H3 trimethyl lys9, with the concomitant oxidation/decarboxylation of 2-oxoglutarate. The detection reaction involves the cyclization between formaldehyde and acetoacetanilide in the presence of ammonia. The resulting fluorescent product is analyzed using an excitation wavelength between 365-375 nm and an emission wavelength between 465-475 nm.

Synonyms

Jumonji Domain Containing 2D Inhibitor Screening Assay Kit

Stability

6 months

Storage

-80°C

Shipping

Dry ice in continental US; may vary elsewhere

Background Reading

Rose, N.R., Ng, S.S., Mecinovic, J., et al. Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases. J Med Chem 51 7053-7056 (2008).

Strahl, B.D., and Allis, D. The language of covalent histone modifications. Nature 403 41-45 (2000 Jan 6).

Shin, S., and Janknecht, R. Activation of androgen receptor by histone demethylases JMJD2A and JMJD2D. Biochem Biophys Res Commun 359 742-746 (2007).

Tsukada, Y., Fang, J., Erdjument-Bromage, H., et al. Histone demethylation by a family of JmjC domain-containing proteins. Nature 439(16) 811-816 (2006).

Li, Q., Sritharathikhun, P., and Motomizu, S. Development of novel reagent for Hantzsch reaction for the determination of formaldehyde by spectrophotometry and fluorometry. Anal Sci 23 413-417 (2007).

Rose, N.R., Woon, E.C.Y., Kingham, G.L., et al. Selective inhibitors of the JMJD2 histone demethylases: Combined nondenaturing mass spectrometric screening and crystallographic approaches. J Med Chem 53 1810-1818 (2010).

Shin, S., and Janknecht, R. Diversity within the JMJD2 histone demethylase family. Biochem Biophys Res Commun 353 973-977 (2007).

Couture, J., Collazo, E., Ortiz-Tello, P.A., et al. Specificity and mechanism of JMJD2A, a trimethyllysine-specific histone demethylase. Nat Struct Mol Biol 14(8) 689-695 (2007).

Katoh, M., and Katoh, M. Identification and characterization of JMJD2 family genes in silico. Int J Oncol 24 1623-1628 (2004).

Schneider, J., and Shilatifard, A. Histone demethylation by hydroxylation: Chemistry in action. ACS Chem Biol 1(2) 75-81 (2006).

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700370-96well

96-Well Cover Sheet