BRD 8899

Names

[ Name ]:
BRD 8899

[Synonym ]:
N-[[(2S,4R)-4-[(4-methyl-5-isoquinolinyl)sulfonylamino]-2-pyrrolidinyl]methyl]acetamide
Acetamide, N-[[(2S,4R)-4-[[(4-methyl-5-isoquinolinyl)sulfonyl]amino]-2-pyrrolidinyl]methyl]-
N-{[(2S,4R)-4-{[(4-Methyl-5-isoquinolinyl)sulfonyl]amino}-2-pyrrolidinyl]methyl}acetamide

Biological Activity

[Description]:

BRD 8899 is a potent and selective inhibitor of the serine/threonine kinase STK33 with IC50 of 0.11 nM (25 uM ATP); exhibits significant off-target inhibition of a few other kinases, including RIOK1 (97% inhibition), MST4 (96%), RSK4 (89%), ATK1 (85%), KITD816V (85%), ROCK1 (84%), and FLT3 (81%), while STK33 is inhibited by 89%; shows no effect cell viability in 35 cancer cell lines, fails to kill KRAS-dependent cells.

[References]

References 1. Luo T, et al. Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2860-5. View Related Products by Target Other Targets

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₁₇H₂₂N₄O₃S

[ Molecular Weight ]:
362.447

[ Exact Mass ]:
362.141266

[ LogP ]:
-0.22

[ Index of Refraction ]:
1.640

Related Compounds

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