Acetylated Lysine
BRPFs (bromodomain and PHD finger-containing proteins) are multidomain proteins of the Trithorax group (TrxG): regulatory proteins composed of diverse, evolutionary conserved units that form chromatin-associated complexes accounting for epigenetic transcriptional memory. Three BRPFs are known to date, sharing >65% homology in their ~100 amino acid counting sequences, all sharing an acetylated lysine (KAc) recognition site that closely resembles other bromodomains, including those of the BETs[1]. BRPF1 (also known as Br140 and Peregrin) is a component of complexes containing the MOZ/MORF transcriptional coactivators, that links the catalytic HATs to the other subunits ING5 and hEAF6. Furthermore, BRPF1 contains PHD fingers, a bromodomain and a PWWP domain[2]. It has been shown that BRPF1 has a central role during development, since mutations have shown to display anterior transformations of pharyngeal arches due to progressive loss of anterior Hox gene expression. What’s more, translocations of MOZ are associated with aggressive subtypes of leukemia, and make BRPF1 an interesting target in oncology related research[3].
[1] E.H. Demont et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5.
[2] K. Laue et al. The multidomain protein Brpf1 binds histones and is required for Hox gene expression and segmental identity. Development. 2008 Jun;135(11):1935-46.
[3] L. You et al. The chromatin regulator brpf1 regulates embryo development and cell proliferation. J Biol Chem. 2015 May 1;290(18):11349-64.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
1989 | (+)-JQ1 |
Potent and selective BET bromodomain inhibitor |
€60.00 | |
3822 | (+)-JQ1 carboxylic acid | (+)-JQ1 derivative; PROTAC precursor | €110.00 | |
3873 | (-)-JQ-1 | Inactive enantiomer of (+)-JQ1 | Recently added | €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 | |
3933 | CCS-1477 | Potent, selective and orally bioavailable inhibitor of the Bromodomain of p300 and CBP | 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 | |
3769 | FHD-286 | Selective inhibitor of the BAF chromatin remodeling complex ATPases (BRG1/BRM) | Inquire | |
2410 | GSK 5959 | Potent, cell permeable inhibitor of BRPF1 bromodomain | €135.00 | |
3921 | GSK046 | Domain-selective and orally active inhibitor of BET with immunomodulatory activity | Inquire | |
3860 | I-BET726 | Potent and selective, tetrahydroquinoline-based small molecule ligand binding to BET proteins | Inquire | |
3186 | NVS-BPTF-1 | Potent, selective and cell active chemical probe for BPTF | €180.00 | |
3329 | ODM-207 | Highly potent, selective and orally active pan-BET inhibitor | €140.00 | |
2442 | OF-1 | Potent bromodomain inhibitor (BRPF1 and BRPF2 selective) | €80.00 | |
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 | |
3623 | SGC-SMARCA-BRDVIII | Potent, highly selective and cell-active SMARCA2/4 and PB1(5) bromodomain inhibitor | €90.00 |