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LP 99

Names

[ CAS No. ]:
1808951-93-0

[ Name ]:
LP 99

[Synonym ]:
1-Propanesulfonamide, N-[(2R,3S)-2-(4-chlorophenyl)-1-(1,2-dihydro-1,4-dimethyl-2-oxo-7-quinolinyl)-6-oxo-3-piperidinyl]-2-methyl-
N-(2R,3S)-2-(4-Chlorophenyl)-1-(1,4-dimethyl-2-oxo-1,2-dihydroquinolin-7-yl)-6-oxopiperidin-3-yl)-2-methylpropane-1-sulfonamide
(2R,3S)-LP99
LP99
MFCD28969655
N-[(2R,3S)-2-(4-Chlorophenyl)-1-(1,4-dimethyl-2-oxo-1,2-dihydro-7-quinolinyl)-6-oxo-3-piperidinyl]-2-methyl-1-propanesulfonamide

Biological Activity

[Description]:

LP99 is the first potent and selective BRD7/9 bromodomain inhibitor with Kd of 99 nM for BRD9; inhibits IL‐6 secretion from THP‐1 cells in a dose‐dependent manner; decreases BRET for both BRD7 and BRD9 in both the H3.3 and H4 systems in a dose‐dependent manner, with cellular IC50 values in the low micromolar range for both histones.

[References]

References 1. Clark PG, et al. Angew Chem Weinheim Bergstr Ger. 2015 May 18;127(21):6315-6319. View Related Products by Target Bromodomain

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
726.6±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H30ClN3O4S

[ Molecular Weight ]:
516.052

[ Flash Point ]:
393.2±35.7 °C

[ Exact Mass ]:
515.164551

[ LogP ]:
4.15

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.644

Related Compounds