For research use only. Not for therapeutic Use.
GSK2801 (Cat No.:I002077) is a potent and selective inhibitor of BAZ2A and BAZ2B bromodomains, which play a role in chromatin biology. It competitively binds to the acetyl-lysine binding site of BAZ2 bromodomains, with dissociation constants (KD) of 257 nM for BAZ2A and 136 nM for BAZ2B. Crystal structure analysis confirmed the acetyl-lysine competitive binding mode. In cellular studies, GSK2801 displaced GFP-BAZ2A from acetylated chromatin, demonstrating its cellular activity. Pharmacokinetic studies in mice revealed reasonable exposure after oral administration, with moderate clearance and plasma stability. GSK2801 serves as a valuable tool compound for investigating the function of BAZ2 bromodomains in chromatin biology through cellular and in vivo studies.
| Catalog Number | I002077 |
| CAS Number | 1619994-68-1 |
| Synonyms | 1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone |
| Molecular Formula | C₂₀H₂₁NO₄S |
| Purity | ≥95% |
| Target | Bromodomain |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IC50 | 136 nM/257 nM(Kd, BAZ2A/BAZ2B) |
| IUPAC Name | 1-[1-(2-methylsulfonylphenyl)-7-propoxyindolizin-3-yl]ethanone |
| InChI | InChI=1S/C20H21NO4S/c1-4-11-25-15-9-10-21-18(14(2)22)13-17(19(21)12-15)16-7-5-6-8-20(16)26(3,23)24/h5-10,12-13H,4,11H2,1-3H3 |
| InChIKey | KHWCPNJRJCNVRI-UHFFFAOYSA-N |
| SMILES | CCCOC1=CC2=C(C=C(N2C=C1)C(=O)C)C3=CC=CC=C3S(=O)(=O)C |
| Reference | 1: Yang X, Wu X, Zhang J, Zhang X, Xu C, Liao S, Tu X. Recognition of hyperacetylated N-terminus of H2AZ by TbBDF2 from Trypanosoma brucei. Biochem J. 2017 Nov 9;474(22):3817-3830. doi: 10.1042/BCJ20170619. PubMed PMID: 29025975.<br /> |
