I-BET762
- Molibresib - GSK525762
- Optical Purity: >99% e.e.
- Soluble in DMSO
- MF: C22H22ClN5O2
- MW: 423.9
Description
I-BET762 is a cell-permeable benzodiazepine-based inhibitor of 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, displacing 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.
More Information
| Parent CAS No. | 1260907-17-2 |
|---|---|
| Chemical Name | (S)-2-(6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1C2N3C(C)=NN=C3[C@H](CC(=O)NCC)N=C(C3C=CC(Cl)=CC=3)C=2C=C(OC)C=1 |&1:8,r| |
| MFCD | N.A. |
| InChi | N.A. |
| InChiKey | N.A. |
| CID | N.A. |
| Short Description | BET bromodomain inhibitor |
References
- O Mirguet et al. Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains. J Med Chem. 2013 Oct 10;56(19):7501-15.
- A Chaidos et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705.
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