MS453 | SETD8 inhibitor | ProbeChem Biochemicals

Chemical Structure : MS453

Catalog No.: PC-60300Not For Human Use, Lab Use Only.

MS453 (MS-453) is a potent, selective and covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM.

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Biological Activity

MS453 (MS-453) is a potent, selective and covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM.

MS453 exhibits selectivity for SETD8 against 28 other methyltransferases.

MS453 does not causes significant reduction in the H4K20me in HeLa cells at up to 10 uM.

MS453 shows poor membrane permeability (4.4 nm/s) and high efflux ratio (137).

M.Wt	385.468
Formula	C20H27N5O3
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(3-((6,7-dimethoxy-2-(pyrrolidin-1-yl)quinazolin-4-yl)amino)propyl)acrylamide

1. Butler KV, et al. J Med Chem. 2016 Nov 10;59(21):9881-9889.