Bromodomains

Bromodomains (BRDs) are epigenetic "reader" domains that selectively recognize acetylated lysine residues on the tails of histone proteins, and are the only known protein modules that can target acetylated lysine residues.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
5970 BAY 299
Potent and selective BRD1 and TAF1 inhibitor
5266 BAZ2-ICR
Selective BAZ2 inhibitor
5590 BI 9564
Potent and selective BRD9 and BRD7 inhibitor; orally active
4758 Bromosporine
Broad spectrum bromodomain inhibitor
5331 CPI 203
BET bromodomain inhibitor; arrests cell cycle at G1 phase
5635 GSK 2801
Selective BAZ2A and BAZ2B inhibitor
5385 GSK 5959
Potent and selective BRPF1 inhibitor
4650 I-BET 151 dihydrochloride
BET bromodomain inhibitor; also promotes differentiation of hiPSCs into megakaryocytes
5591 I-BRD9
Potent and selective BRD9 inhibitor
4891 I-CBP 112
Selective CBP/p300 BRD inhibitor
4695 Ischemin sodium salt
CBP inhibitor; cell permeable
5806 ISOX DUAL
Dual BRD4 and CBP/p300 bromodomain inhibitor
4499 (+)-JQ1
Potent, selective BET bromodomain inhibitor; cell permeable
6251 L Moses dihydrochloride
High affinity and selective PCAF bromodomain inhibitor
6068 Lin28 1632
Bromodomain inhibitor; also RNA binding protein Lin28 inhibitor and promotes mESC differentiation
2418 LY 303511
BRD2, BRD3 and BRD4 inhibitor; also negative control of LY 294002 (Cat. No. 1130)
5173 MS 436
Potent and selective BRD4(1) inhibitor
5786 NI 42
High affinity BRPF inhibitor
5546 NI 57
Potent and selective BRPF bromodomain inhibitor
5744 NVS-CECR2-1
Potent and selective inhibitor of cat eye syndrome chromosome region, candidate 2 (CECR2)
5289 OF 1
Selective BRPF1B and BRPF2 inhibitor
6181 OTX 015
BET bromodomain inhibitor; orally bioavailable
4928 OXF BD 02
Selective BRD4(1) inhibitor
5801 PF CBP1
Selective CBP/p300 bromodomain inhibitor
4445 PFI 1
BET bromodomain inhibitor
5072 PFI 3
Potent and selective SMARCA2/4 and polybromo 1 inhibitor
5576 PFI 4
Potent and selective BRPF1 bromodomain inhibitor
4889 SGC-CBP30
Potent CBP/p300 BRD inhibitor
6000 TP 472
Potent BRD9/7 inhibitor
5489 XD 14
BET bromodomain inhibitor
4132 XMD 8-92
BRD4 inhibitor; also ERK5/BMK1 inhibitor

Other

Cat No Product Name / Activity
6155 cis MZ 1
Negative Control for MZ1
6327 dBET1
(+)-JQ1 based PROTAC that selectively degrades BRD4 in cells
5808 ISOX INACT
Negative control for PF-CBP1 (Cat. No. 5801)
5603 (-)-JQ1
Inactive control for (+)-JQ1 (Cat. No. 4499)
6154 MZ 1
(+)-JQ1 based PROTAC that selectively degrades BRD4 in cells
6105 TC AC 28
High affinity BET bromodomain ligand
5999 TP 472N
Negative control for TP 472 (Cat. No. 6000).

Bromodomains (BRDs) are epigenetic "readers" that selectively recognize acetylated lysine (Kac) residues on histone protein tails, and are the only known protein modules that target Kac residues. There are approximately 62 unique human bromodomains, most of which can be classified according to sequence identity into nine groups.

Bromodomains are found in a wide range of proteins, from the histone acetyltransferase PCAF to the ATP-dependent helicase SNF2L2. This diversity makes it difficult to characterize the function of a given BRD-containing protein, particularly as some proteins may contain one or more additional epigenetic "reader" domains. However, some bromodomains have been implicated in diseases such as cancer and inflammation.

Of particular interest is the BET (bromodomain and extra-terminal) bromodomain family, which comprises the ubiquitously expressed proteins BRD2, BRD3, BRD4; and the testis-specific protein, BRDT. Due to the binding of BRD4 to transcriptional sites of genes expressed during the M/G1 cell cycle transition, BRD4 is currently under investigation as a therapeutic target for cancer. BRD4 has also been implicated in a rare but lethal form of cancer - NUT midline carcinoma (NUC) - which is caused by a rearrangement of the nuclear protein in testis gene (NUT), causing the formation of a BRD4-NUT fusion gene. In addition, BRD4 has been reported to function as a coactivator for the transcriptional activation of NFκB.

Literature for Bromodomains

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Cell Cycle & DNA Damage Repair

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Bromodomain Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
BRD2 Human BRD2 NM_001113182 P25440
Mouse Brd2 NM_001204973 Q7JJ13
Rat Brd2 NM_212495 Q6MGA9
BRD3 Human BRD3 NM_007371 Q15059
Mouse Brd3 NM_023336 Q8K2F0
Rat Brd3 NM_001108575 NP_001102045
BRD4 Human BRD4 NM_058243 O60885
Mouse Brd4 NM_020508 Q9ESU6
Rat Brd4 NM_001100903 NP_001094373
BRDT Human BRDT NM_207189 Q58F21
Mouse Brdt NM_054054 Q91Y44
Rat - - -