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SML1272 Sigma-Aldrich

I-BET762

≥98% (HPLC)

Synonym: (4S)- 6-(4-Chlorophenyl)-N-ethyl-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, GSK525762, GSK525762A, I-BET

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Gene Regulation,
InChI Key   AAAQFGUYHFJNHI-SFHVURJKSA-N
assay   ≥98% (HPLC)
form   powder
optical activity   [α]/D +80 to +90°, c = 0.3 in methanol
drug control   regulated under CDSA - not available from Sigma-Aldrich Canada
color   white to beige
solubility   DMSO: 10 mg/mL, clear
storage temp.   2-8°C

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

I-BET762 (GSK525762) is a selective inhibitor of bromodomain and extra terminal (BET) domain proteins BRD2, BRD3 and BRD4 with IC50 values of 32.5–42.5 nM and no interaction with other bromodomain-containing proteins. I-BET mimicks acetylated histone, preventing the protein-protein interaction between acetyl-lysines and the BET reader protein. This was shown to block expression of inflammatory genes in activated macrophages and confer protection against endotoxic shock and bacterial sepsis. I-BET762 also showed potent anti-myeloma activity in vitro and in vivo.

I-BET762 possesses anti-inflammatory property by controlling the pro-inflammatory gene expression. I-BET762 hinders the MYC (proto-oncogene) expression in cellular models. This action of I-BET762 might serve as an effective therapy in treating prostate cancer.

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis


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

References

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