Bromodomains are a family of evolutionarily conserved protein modules of approximately 110 amino acids that have been found in chromatin-associated proteins as well as nuclear histone acetyltransferases (HATs). Besides its role in chromatin remodeling, recent studies have identified that bromodomains, as acetyl-lysine binding domains, are able to recognize and bind ε–N-acetylated lysine residues in histone and non-histone proteins. The nuclear magnetic resonance (NMR) spectroscopic analysis reveals that the chemical structure of bromodomains, consisting of four left-handed α-helices (including αZ, αA, αB and αC) connected by two loops (ZA and BC loops), forms a deep hydrophobic cavity serving as the acetyl-lysine recognition site.
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A potent, highly selective inhibitor of the CBP and p300 bromodomains with IC50 of 125 nM and 363 nM, respectively; displays >100-fold selectivity for the bromodomain of CBP over those of BRD4 and a panel of other proteins; reduces the expression of inflammatory cytokines by LPS-stimulated primary macrophages, also suppresses the expression of RGS4 in primary cortical neurons.
A selective TAF1 second bromodomain inhibitor with IC50 of 2.1 uM; shows high selectivity for the TAF1 (2) bromodomain over BRD4 (1), BRD9, CREBBP, EP300 and TAF1 (2) bromodomains (IC50>10 uM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.
JQ-1 carboxylic acid
JQ-1 carboxylic acid is an inhibitor of bromodomain and extra terminal domain (BET) family proteins with Kd of 128, 59.5, 49.0, and 190 nM for JQ1 binding to bromodomains of BRD2, BRD3, BRD4, and BRDT, respectively, blocking their interaction with acetylated histones; a chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis.
A potent and selective CBP/p300 bromodomain inhibitor with Kd of 134 nM for CBP bromodomain, displays excellent selectivity over other bromodomains (>30-fold over BRD4 (1)); targets the CBP bromodomain in the nucleus and is capable of competing with acetyl-lysine mediated interactions of the CBP bromodomain in cellular environments.
A potent and selective the bromodomains of CBP/EP300 inhibitor with IC50 of 0.02 and 0.03 uM for CBP and EP300, respectively; displays high selectivity over BRD4 (1) and other BRDs (>10 uM); shows antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo; exhibits excellent in vivo PK and antitumor activity in an AML tumor model.
A potent, highly selective and cell-active BRPF1 bromodomain inhibitor with TR-FRET pIC50 of 8.1; displays>1600-fold selectivity over others bromodomains (BRPF2/3, BRD4 BD1/BD2); displaces NanoLuc-tagged BRPF1 bromodomain from Halo-tagged histone H3.3 (IC50=20 nM) and disrupts chromatin binding in cell assays; demonstrates properties suitable for cellular and in vivo studies.
AZD5153 6-Hydroxy-2-naphthoic acid
A potent, selective, bivalent and orally available BET/BRD4 bromodomain with IC50 of 5 nM; simultaneously binds to two bromodomains in BRD4; exhibits antitumor activity in multiple xenograft models of acute myeloid leukemia, multiple myeloma, and diffuse large B cell lymphoma.
IACS-9571 is a potent, selective dual TRIM24-BRPF1 bromodomain inhibitor with Kd of 31 and 14 nM, respectively; displays 9- and 21-fold selectivity against BRPF2 and BRPF3, weaker affinities with BAZ2B (Kd= 400 nM) and the second domain of TAF1 (Kd=1,800 nM), and >7,700-fold selectivity versus BRD4 BD1 and BD2; demonstrates excellent cellular potency (EC50= 50 nM) and favorable pharmacokinetic properties; IACS-9571 is a chemical probe to investigate biological and pharmacological role of TRIM24 and/or BRPF1 bromodomain inhibition in vitro and in vivo.
BMS-986158 (BMS986158) is a potent and selective BET inhibitor, disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes, resulting in an inhibition of tumor cell growth.
BET-BAY 002 is a potent BET bromodomain inhibitor; shows efficacy in a multiple myeloma model.
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