SML0666

Sigma-Aldrich

GSK1210151A

≥98% (HPLC)

Synonym(s):
7-(3,5-Dimethyl-4-isoxazolyl)-8-(methyloxy)-1-[(1R)-1-(2-pyridinyl)ethyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one, I-BET151
Empirical Formula (Hill Notation):
C23H21N5O3
CAS Number:
Molecular Weight:
415.44
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 20 mg/mL, clear

originator

GlaxoSmithKline

relevant disease(s)

cancer

storage temp.

2-8°C

Application

GSK1210151A or I-BET151 has been used to study its inhibitory effect on BET (bromodomain and extra terminal) recruitment to chromatin in treating MLL (mixed-lineage leukemia)-fusion leukemia.

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

GSK1210151A (I-BET151) is an inhibitor of the BET (bromodomain and extra terminal domain protein) family of acetyl-lysine recognizing, chromatin ′adaptor′ proteins. GSK1210151A displaces BRD3 and BRD4, PAFc and SEC components from chromatin resulting in inhibition of transcription at key genes (BCL2, C-MYC and CDK6) involved in the initiation of mixed lineage leukemia (MLL). GSK1210151A (I-BET151) showed good efficacy in 2 MLL animal models.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

Other Notes

GSK1210151A has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK1210151A probe summary on the Chemical Probes Portal website.

Legal Information

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC

Pictograms

Skull and crossbones

Signal Word

Danger

Hazard Statements

Precautionary Statements

hazcat

Acute Tox. 3 Oral

storage_class_code

6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects

WGK Germany

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis

Certificate of Origin

Zhongyuan Gao et al.
Cancer biology & therapy, 19(5), 407-415 (2018-01-16)
Lung cancer is the leading cause of cancer-related death worldwide. Bromodomain and extraterminal domain (BET) proteins act as epigenome readers for gene transcriptional regulation. Among BET family members, BRD4 was well studied, but for its mechanism in non-small cell lung...
Replication Study: Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
Shan X, et al.
eLife, 6, e25306-e25306 (2017)
Yan-Yi Jiang et al.
Gastroenterology, 159(4), 1311-1327 (2020-07-04)
We investigated the transcriptome of esophageal squamous cell carcinoma (ESCC) cells, activity of gene regulatory (enhancer and promoter regions), and the effects of blocking epigenetic regulatory proteins. We performed chromatin immunoprecipitation sequencing with antibodies against H3K4me1, H3K4me3, and H3K27ac and...
Leiming Wang et al.
The Journal of clinical investigation, 130(4), 1782-1792 (2019-12-25)
Recent findings have shown that inhibitors targeting bromodomain and extraterminal domain (BET) proteins, such as the small molecule JQ1, are potent growth inhibitors of many cancers and hold promise for cancer therapy. However, some reports have also revealed that JQ1...

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