BET (BRD)
Acetylation of lysine residues is a post-translational modification with broad relevance to cellular signaling and disease biology. Enzymes that ‘write’ (histone acetyltransferases, HATs) and ‘erase’ (histone deacetylases, HDACs) acetylation sites are an area of extensive research in current drug development. The principal readers of ɛ-N-acetyl lysine (Kac) marks are Bromo and extra terminal (BET) proteins (BRD2, BRD3, BRD4 and BRDT), which are in turn transcriptional regulators required for efficient expression of several growth promoting and anti-apoptotic genes as well as for cell cycle progression[1]. Moreover, they have an important role in the targeting of chromatin-modifying enzymes to specific sites. Often they act with other protein-interaction modules to guarantee a high level of targeting specificity for these essential enzymes[2].
[1] PFI-1 - A highly Selective Protein Interaction Inhibitor TargetingBET bromodomains. S. Picaud et al. Cancer Res. 2013, 73, 3336-3346.
[2] Bromodomains as therapeutic targets. S. Muller, P. Filippakopoulos, S. Knapp. Expert Rev. Mol. Med. 2011, 13, e29.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
1989 | (+)-JQ1 |
Potent and selective BET bromodomain inhibitor |
€60.00 | |
3822 | (+)-JQ1 carboxylic acid | (+)-JQ1 derivative; PROTAC precursor | Recently added | €110.00 |
3696 | ABBV-075 | Highly potent and orally bioavailable BET bromodomain (BRD) inhibitor | €110.00 | |
3833 | AZD5153 HNT salt | Potent, selective, and orally available BET/BRD4 bromodomain inhibitor | Recently added | Inquire |
3037 | BI-894999 | Potent, selective and orally active BET inhibitor | €165.00 | |
3716 | BMS-986158 | BET bromodomain (BRD) inhibitor | Inquire | |
2776 | CD161 | Potent, selective, and orally active BET bromodomain inhibitor | €135.00 | |
2594 | CPI 0610 | Selective and metabolically stable inhibitor of BET bromodomains | Inquire | |
3860 | I-BET726 | Potent and selective, tetrahydroquinoline-based small molecule ligand binding to BET proteins | Recently added | Inquire |
3329 | ODM-207 | Highly potent, selective and orally active pan-BET inhibitor | €140.00 | |
2530 | OTX 015 | Potent inhibitor of BRD2, BRD3, and BRD4 with clear anti-proliferative activity | €110.00 | |
1887 | PFI-1 | BET bromodomain (BRD) inhibitor | €75.00 | |
2245 | RVX 208 | BET bromodomain inhibitor specific for second bromodomains (BD2s) | €65.00 |