2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain
  5. BRPF3 Isoform

BRPF3

BRPF3 (bromodomain and PHD finger-containing protein 3) is a chromatin-associated scaffold protein that functions within the HBO1/KAT7 histone acetyltransferase complex and contributes to the regulation of DNA replication initiation through histone modification mechanisms[1]. Mechanistically, BRPF3 directs HBO1 substrate specificity toward histone H3 lysine 14 acetylation (H3K14ac), resulting in enrichment of BRPF3, HBO1, and H3K14ac at ORC1-binding sites and replication origins located near transcription start sites[1]. This chromatin-regulatory activity promotes efficient replication origin activation, as BRPF3 depletion reduces H3K14 acetylation at selected origins and impairs CDC45 recruitment required for origin firing[1]. Therefore, BRPF3 represents an important epigenetic regulator linking histone acetylation, replication origin activation, and genome duplication programs[1]. In experimental models, BRPF3 deficiency decreases replication origin activation while preserving MCM2-7 loading, supporting a specific role in origin activation rather than replication licensing[1]. Compared with the related paralogs BRPF1 and BRPF2, BRPF3 forms a functional HBO1-containing complex with distinct biological properties and is not required for mouse development or survival, indicating functional divergence within the BRPF family[2]. This isoform-specific activity makes BRPF3 particularly useful for studies investigating chromatin-dependent replication control and replication stress responses[1][2]. Currently, BRPF3-directed pharmacological modulators remain limited, and research applications primarily rely on genetic perturbation approaches to dissect BRPF3-HBO1-dependent H3K14 acetylation and replication origin regulation[1].

BRPF3 Related Products (2):

Cat. No. Product Name Effect Purity
  • HY-107424
    BAY-299
    		Inhibitor 99.40%
    BAY-299, a chemical probe, is a very potent, dual inhibitor with IC50s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.
  • HY-101121
    NI-42
    		Inhibitor 99.53%
    NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins.