MS-453
Names
[ CAS No. ]:
2059892-29-2
[ Name ]:
MS-453
[Synonym ]:
2-Propenamide, N-[3-[[6,7-dimethoxy-2-(1-pyrrolidinyl)-4-quinazolinyl]amino]propyl]-
N-(3-{[6,7-Dimethoxy-2-(1-pyrrolidinyl)-4-quinazolinyl]amino}propyl)acrylamide
Biological Activity
[Description]:
A potent, selective. covalent protein lysine methyltransferase SETD8 inhibitor with IC50 of 804 nM; exhibits selectivity for SETD8 against 28 other methyltransferases; does not causes significant reduction in the H4K20me in HeLa cells at up to 10 uM; poor membrane permeability (4.4 nm/s) and high efflux ratio (137).
[References]
References 1. Butler KV, et al. J Med Chem. 2016 Nov 10;59(21):9881-9889. View Related Products by Target Histone Methyltransferase (HMTase)
Chemical & Physical Properties
[ Density]:
1.2±0.1 g/cm3
[ Molecular Formula ]:
C20H27N5O3
[ Molecular Weight ]:
385.460
[ Exact Mass ]:
385.211395
[ LogP ]:
0.59
[ Index of Refraction ]:
1.614