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Cat. Number
066001748431625
Chemical Name
LSD1 Inhibitor Screening Assay Kit
References

 

Synonyms
  • Lysine-Specific Demethylase 1
Stability 6 months
Storage -80°C
Shipping Dry ice in continental US; may vary elsewhere

Background Reading

Shi, Y., Lan, F., Matson, C., et al. Histone demethylation mediated by the nuclear amine oxidase homolog LSD1. Cell 119 941-953 (2004).

Shi, Y., Matson, C., Lan, F., et al. Regulation of LSD1 histone demethylase activity by its associated factors. Mol Cell 19 864 (2005).

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

Forneris, F., Binda, C., Vanoni, M.A., et al. Human histone demethylase LSD1 reads the histone code. J Biol Chem 280(50) 41360-41365 (2005).

Huang, J., Sengupta, R., Espejo, A.B., et al. p53 is regulated by the lysine demethylase LSD1. Nature 449 105-108 (2007).

Scoumanne, A., and Chen, X. The lysine-specific demethylase 1 is required for cell proliferation in both p53-dependent and -independent manners. J Biol Chem 282(21) 15471-15475 (2007).

Tsai, W., Nguyen, T.T., Shi, Y., et al. p53-targeted LSD1 functions in repression of chromatin structure and transcription in vivo. Mol Cell Biol 28(17) 5139-5146 (2008).

Scoumanne, A., and Chen, X. Protein methylation: A new mechanism of p53 tumor suppressor regulation. Histol Histopathol 23 1143-1149 (2008).

Schmidt, D.M.Z., and McCafferty, D.G. trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1. Biochemistry 46 4408-4416 (2007).

Gooden, D.M., Schmidt, D.M.Z., Pollock, J.A., et al. Facile synthesis of substituted trans-2-arylcyclopropylamine inhibitors of the human histone demethylase LSD1 and monoamine oxidases A and B. Bioorg Med Chem Lett 18 3047-3051 (2008).

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700120-96well
96-Well Solid Plate (black)
LSD1 Assay Buffer (10X) 1 ea
LSD1 (human recombinant) Assay Reagent 2 × 1 ea
LSD1 Assay Fluorometric Substrate 3 × 1 ea
LSD1 Assay Horseradish Peroxidase 2 × 1 ea
LSD1 Assay Peptide 2 × 1 ea
LSD1 Assay DMSO 1 ea
Size Global Purchasing
96 wells  

Description

Lysine-specific demethylase 1 (LSD1) is a histone demethylase whose actions on specific lysine residues repress transcription of chromosomal DNA. LSD1 also inhibits the tumor suppressor activity of p53 by demethylating a specific lysine residue. Inhibitors of LSD1 are important tools used to elucidate mechanisms of transcription and cell cycle progression and have therapeutic potential for treating cancer. Cayman’s LSD1 Inhibitor Screening Assay Kit provides a convenient fluorescence-based method for screening LSD1-specific inhibitors. The assay is based on the multistep enzymatic reaction in which LSD1 first produces H2O2 during the demethylation of lysine 4 on a peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3. In the presence of horseradish peroxidase, H2O2 reacts with ADHP to produce the highly fluorescent compound resorufin that can be analyzed with an excitation wavelength of 530-540 nm and an emission wavelength of 585-595 nm.

 

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