SML0768
GSK2801
≥98% (HPLC)
Synonym(s):
1-(7-(2-Methylsulfonyl-phenyl)-4-propoxy-1-aza-bicyclo[4.3.0]nona-2,4,6,8-tetraen-9-yl)-ethanone
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About This Item
Empirical Formula (Hill Notation):
C20H21NO4S
CAS Number:
Molecular Weight:
371.45
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
storage condition
protect from light
color
, white to pink to light brown
solubility
DMSO: 10 mg/mL, clear
storage temp.
−20°C
SMILES string
CCCOC1=CC2=C(C3=CC=CC=C3S(=O)(C)=O)C=C(C(C)=O)N2C=C1
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
InChI key
KHWCPNJRJCNVRI-UHFFFAOYSA-N
Biochem/physiol Actions
GSK2801 is a potent inhibitor of the BAZ2 family of bromodomain containing proteins. BAZ2A is an essential component of the nucleolar remodeling complex (NoRC), which mediates recruitment of histone modifying enzymes and DNA methylase involved in the silencing of ribosomal RNA transcription. BAZ2B is believed to be involved in regulating nucleosome mobilization along linear DNA. For full characterization details, please visit the GSK2801 probe summary on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins (BAZ2B/A).
Features and Benefits
GSK2801 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
Other Notes
GSK2801 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK2801 probe summary on the Chemical Probes Portal website.
Light sensitive
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Natali Abeywickrama-Samarakoon et al.
Nature communications, 11(1), 419-419 (2020-01-23)
Hepatitis Delta virus (HDV) is a satellite of Hepatitis B virus with a single-stranded circular RNA genome. HDV RNA genome synthesis is carried out in infected cells by cellular RNA polymerases with the assistance of the small hepatitis delta antigen
Nathaniel W Mabe et al.
Cell reports, 33(5), 108341-108341 (2020-11-05)
Dysregulated gene expression is a common feature of cancer and may underlie some aspects of tumor progression, including tumor relapse. Here, we show that recurrent mammary tumors exhibit global changes in gene expression and histone modifications and acquire dependence on