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GSK2801

  Cat. No.:  DC7853   Featured
Chemical Structure
1619994-68-1
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More than 5000 active chemicals with high quality for research!
Field of application
GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins.
Cas No.: 1619994-68-1
Chemical Name: 1-(7-(2-Methylsulfonyl-phenyl)-4-propoxy-1-aza-bicyclo[4.3.0]nona-2,4,6,8-tetraen-9-yl)-ethanone
Synonyms: GSK2801,GSK-2801,GSK 2801
SMILES: C(=O)(C1N2C(=C(C3=CC=CC=C3S(C)(=O)=O)C=1)C=C(OCCC)C=C2)C
Formula: C20H21NO4S
M.Wt: 371.45
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains.GSK2801 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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