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

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.