| I-BET762 |
| 4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)- |
| (CAS 1260907-17-2) |
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| Description： |
I-BET-762 is an inhibitor for BET proteins with IC50 of ~35 nM, suppresses the production of proinflammatory proteins by macrophages and blocks acute inflammation, highly selective over other bromodomain-containing proteins.
I-BET-762 is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains of BET with Kd of 50.5–61.3 nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5–42.5 nM in FRET analysis. I-BET-762 occupies the acetyl-lysine binding pocket of BET proteins and inhibits binding of BET proteins to acetylated histones, thus disrupts the formation of the chromatin complexes essential for expression of inflammatory genes.I-BET-762 treatment during the first 2 d of differentiation alters CD4+ T-cell cytokine production, up-regulated expression of several antiinflammatory gene products and down-regulated expression of several proinflammatory cytokines. |
| Product No. |
KT00621 |
| Product Name |
I-BET762 |
| Synonyms |
GSK 525762A |
| Formal Name |
4H-[1,2,4]Triazolo[4,3-a][1,4]benzodiazepine-4-acetamide, 6-(4-chlorophenyl)-N-ethyl-8-methoxy-1-methyl-, (4S)- |
| CAS Number |
1260907-17-2 |
| Molecular Formula |
C22H22ClN5O2 |
| Formula Weight |
423.9 |
| Formulation |
A crystalline solid |
| Purity |
98%min |
| Stability |
2 years |
| Storage |
-20°C |
| Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500 |
| Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
| Price & Availability |
In Stock. Price Negotiated. |
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