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.

21 Item(s)

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Axon ID Name Description From price
1989 (+)-JQ1

Potent and selective BET bromodomain inhibitor

3822 (+)-JQ1 carboxylic acid (+)-JQ1 derivative; PROTAC precursor €110.00
3873 (-)-JQ-1 Inactive enantiomer of (+)-JQ1 €120.00
3696 ABBV-075 Highly potent and orally bioavailable BET bromodomain (BRD) inhibitor €110.00
3956 ABBV-744 First-in-class highly BDII (Bromodomain II)-selective BET bromodomain inhibitor Inquire
3944 ARV-825 Potent and selective protein BRD4 degrader Inquire
3833 AZD5153 HNT salt Potent, selective, and orally available BET/BRD4 bromodomain inhibitor 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
3764 CFT-8634 Selective orally bioavailable BRD9 degrader Inquire
2594 CPI 0610 Selective and metabolically stable inhibitor of BET bromodomains Inquire
3922 dBET1 BET bromodomain degrader Inquire
3921 GSK046 Domain-selective and orally active inhibitor of BET with immunomodulatory activity Inquire
4135 I-BET151 BET bromodomain inhibitor Inquire
3860 I-BET726 Potent and selective, tetrahydroquinoline-based small molecule ligand binding to BET proteins Inquire
4134 I-BET762 BET bromodomain inhibitor 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

21 Item(s)

per page
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