1619994-68-1

1619994-68-1 structure

Name: GSK 2801
Chemical Name: 1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone
CAS Number: 1619994-68-1
Molecular Formula: C₂₀H₂₁NO₄S
Molecular Weight: 371.450
Catalog: Signaling Pathways Epigenetics Epigenetic Reader Domain
Create Date: 2018-12-20 18:24:30
Modify Date: 2024-01-02 19:36:05
GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains.IC50 value: 136 nM/257 nM(Kd, BAZ2A/BAZ2B) [1]Target: BAZ2A/2B inhibitorGSK2801 binds to BAZ2 bromodomains with dissociation constants (KD) of 136 and 257 nM for BAZ2B and BAZ2A, respectively. Crystal structures demonstrated a canonical acetyl-lysine competitive binding mode. Cellular activity was demonstrated using fluorescent recovery after photobleaching (FRAP) monitoring displacement of GFP-BAZ2A from acetylated chromatin. A pharmacokinetic study in mice showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability. Thus, GSK2801 represents a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology.

Name	1-[1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]ethanone
Synonyms	1-{1-[2-(Methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl}ethanone Ethanone, 1-[1-[2-(methylsulfonyl)phenyl]-7-propoxy-3-indolizinyl]- GSK 2801 GSK2801

Description	GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains.IC50 value: 136 nM/257 nM(Kd, BAZ2A/BAZ2B) [1]Target: BAZ2A/2B inhibitorGSK2801 binds to BAZ2 bromodomains with dissociation constants (KD) of 136 and 257 nM for BAZ2B and BAZ2A, respectively. Crystal structures demonstrated a canonical acetyl-lysine competitive binding mode. Cellular activity was demonstrated using fluorescent recovery after photobleaching (FRAP) monitoring displacement of GFP-BAZ2A from acetylated chromatin. A pharmacokinetic study in mice showed that GSK2801 had reasonable in vivo exposure after oral dosing, with modest clearance and reasonable plasma stability. Thus, GSK2801 represents a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology.
Related Catalog	Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain Research Areas >> Cancer
References	[1]. Chen P, et al. Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B. J Med Chem. 2015 Apr 6.