Comparison

GSK2801

Item no. CS-4188-5mg
Manufacturer ChemScene
Amount 5mg
Category
Type Molecules
Specific against other
ECLASS 10.1 32169090
ECLASS 11.0 32169090
UNSPSC 12000000
Similar products 1619994-68-1
Available
CAS
1619994-68-1
Purity
>98%
Formula
C20H21NO4S
MWt
371.45
Solubility
H2O : < 0.1 mg/mL (insoluble); DMSO : 50 mg/mL (134.61 mM; Need ultrasonic)
Clinical Information
No Development Reported
Pathway
Epigenetics
Target
Epigenetic Reader Domain
Biological Activity
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 inhibitor 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.

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 5mg
Available: In stock
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