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Merck
CN

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:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
protect from light
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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
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


pictograms

Exclamation mark

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

Regulatory Information

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Articles

We offer a variety of small molecule research tools, such as transcription factor modulators, inhibitors of chromatin modifying enzymes, and agonists/antagonists for target identification and validation in gene regulation research; a selection of these research tools is shown below.


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



Global Trade Item Number

SKUGTIN
SML0768-5MG04061832824840
SML0768-25MG04061832824833