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GSK2801(GSK-2801)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK2801(GSK-2801)图片
CAS NO:1619994-68-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)371.45
FormulaC20H21NO4S
CAS No.1619994-68-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 74 mg/mL (199.2 mM)
Water: <1 mg/mL
Ethanol: 7 mg/mL (18.8 mM)
Solubility (In vivo)0.5% CMC+1% Tween 80: 30mg/mL
Synonyms

GSK-2801; GSK 2801; GSK2801

Chemical Name: 1-(1-(2-(methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone

InChi Key: KHWCPNJRJCNVRI-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: CC(C1=CC(C2=CC=CC=C2S(=O)(C)=O)=C3C=C(OCCC)C=CN13)=O

实验参考方法
In Vitro

In vitro activity: In U2OS cells transfected with mutant BAZ2A (N1873F), GSK2801 (1 μM) accelerates FRAP half-recovery time by displacing BAZ2A from chromatin.


Kinase Assay: GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A(Kd=136 nM) and BAZ2B(Kd=257 nM) bromodomains.


Cell Assay: In U2OS cells, treatment with the SAHA induced hyperacetylated chromatin. In a GFP-BAZ2A fusion construct, the conserved asparagines that are essential for recognizing the acetylated lysine has been mutated. When a GFP-BAZ2A fusion construct was transfected into SAHA-treated U2OS cells, the mutant construct accelerated FRAP half-recovery time. Treatment with GSK2801 alone in U2OS cells also accelerated FRAP half-recovery time. Both acceleration extents are the same. This meant that GSK2801 can displace BAZ2A from chromatin.

In VivoIn male CD1 mice, GSK2801 (30 mg/kg, p.o. and i.p.) has reasonable in vivo exposure after oral dosing, modest clearance, and reasonable plasma stability.
Animal modelMale CD1 mice
Formulation & DosageFormulated in 0.5% CMC+1% Tween 80; 30 mg/kg; i.p. or p.o.
References

J Med Chem. 2016 Feb 25;59(4):1410-24.