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SML0666 Sigma-Aldrich

GSK1210151A

≥98% (HPLC)

Synonym: 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

  • CAS Number 1300031-49-5

  • Empirical Formula (Hill Notation) C23H21N5O3

  • Molecular Weight 415.44

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, G,
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

Description

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.

Packaging

5, 25 mg in glass bottle

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.

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.

Legal Information

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

Safety & Documentation

Safety Information

Symbol 
GHS06  GHS06
Signal word 
Danger
Hazard statements 
Precautionary statements 
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
3

Documents

Certificate of Analysis


Milli-Q® Water Purification Solutions
Protocols & Articles
Peer-Reviewed Papers
15

References

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