TargetMol

MS2177

Product Code:
 
TAR-T28114
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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TAR-T28114-100mg100mgEnquire
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TAR-T28114-500mg500mgEnquire
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Further Information

Bioactivity:
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 uM (σ = 1.05 uM, n = 4) in ascintillation proximity assay. Binding of MS2177 to SETD8 was confirmed by isothermal titration calorimetry (ITC), having a KD of 1.3 uM.
CAS:
T28114
Molecular Weight:
442.61
Purity:
0.98
SMILES:
COC1=C(OCCN)C=C(N=C(N2CCCC2)N=C3NCCCCCN4CCCC4)C3=C1

References

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