(2S,3R)-LP99

Names

[ CAS No. ]:
1808948-28-8

[ Name ]:
(2S,3R)-LP99

Biological Activity

[Description]:

(2S,3R)-LP99 is a potent and selective BRD7 and BRD9 inhibitor with an KD of 99 nM for BRD9. (2S,3R)-LP99 inhibits the association of BRD7 and BRD9 to acetylated histones in vitro and in cells. (2S,3R)-LP99 demonstrates that BRD7/9 plays a role in regulating pro-inflammatory cytokine secretion[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRD7

BRD9:99 nM (Kd)


[In Vitro]

(2S,3R)-LP99 (compound 60) (0-100 µM) inhibits the expression of IL6 in LPS-stimulated (100 ng/mL) THP-1 cells[1].

[References]

[1]. Clark PG, et al. LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor. Angew Chem Int Ed Engl. 2015 May 18;54(21):6217-21.

Chemical & Physical Properties

[ Molecular Formula ]:
C26H30ClN3O4S

[ Molecular Weight ]:
516.05

Related Compounds