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MS2177

Catalog No. T28114   CAS T28114
Synonyms: MS 2177, MS-2177

MS2177 is a potent and selective inhibitor of SETD8, the only methyltransferase known to catalyze monomethylation of histone H4 lysine 20 (H4K20). MS2177 has an in vitro IC50 of 1.9 μM (σ = 1.05 μM, n = 4) in ascintillation proximity assay. Binding of MS2177 to SETD8 was confirmed by isothermal titration calorimetry (ITC), having a KD of 1.3 μM.

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MS2177 Chemical Structure
MS2177, CAS T28114
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MS2177 is a potent and selective inhibitor of SETD8, the only methyltransferase known to catalyze monomethylation of histone H4 lysine 20 (H4K20). MS2177 has an in vitro IC50 of 1.9 μM (σ = 1.05 μM, n = 4) in ascintillation proximity assay. Binding of MS2177 to SETD8 was confirmed by isothermal titration calorimetry (ITC), having a KD of 1.3 μM.
Synonyms MS 2177, MS-2177
Molecular Weight 442.61
Formula C24H38N6O2
CAS No. T28114

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase Kyle V. Butler, Anqi Ma, Wenyu Yu, Fengling Li, Wolfram Tempel, Nicolas Babault, Fabio Pittella-Silva, Jason Shao, Junyi Wang, Minkui Luo, Masoud Vedadi, Peter J. Brown, Cheryl H. Arrowsmith, and Jian Jin Publication Date (Web): November 2, 2016 (Article) doi: 10.1021/acs.jmedchem.6b01244

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Keywords

MS2177 T28114 MS 2177 MS-2177 inhibitor inhibit

 

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