1. Signaling Pathways
  2. Epigenetics
  3. Epigenetic Reader Domain
  4. BRPF2 Isoform

BRPF2

BRPF2 (also known as BRD1) is a bromodomain- and PHD finger-containing chromatin regulator that functions as a scaffold component of histone acetyltransferase complexes involved in epigenetic gene regulation[1]. Mechanistically, BRPF2 forms the HBO1-BRPF2 complex, which is responsible for global acetylation of histone H3 lysine 14 (H3K14ac), a chromatin modification associated with transcriptional regulation and chromatin accessibility[1]. Through control of H3K14 acetylation, BRPF2 participates in chromatin-dependent transcriptional programs that support cellular differentiation processes[1][2]. In experimental models, genetic disruption of the HBO1-BRPF2 complex markedly impairs fetal liver erythropoiesis, establishing a functional link between BRPF2-mediated histone acetylation and hematopoietic development[1]. BRPF2 is also associated with transcriptional activation of genes involved in erythrocyte differentiation, further supporting its role in lineage-specific gene regulation[2]. Compared with related BRPF family members, BRPF2 is distinguished by its documented requirement within the HBO1-BRPF2 complex for global H3K14 acetylation during erythropoietic development, whereas alternative BRPF-containing complexes have been linked to distinct biological contexts and acetyltransferase activities[1][3]. At the molecular level, the first PHD finger of BRPF2 recognizes unmodified histone H3, providing mechanistic insight into how BRPF2 contributes to chromatin targeting and regulation of MOZ/MORF-associated histone acetyltransferase activity[4].

BRPF2 Related Products (5):

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-100729
    GSK9311
    Inhibitor 99.33%
    GSK9311, a less active analogue of GSK6853, can be used as a negative control. GSK9311 inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
  • 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.
  • HY-100729A
    GSK9311 hydrochloride
    Inhibitor
    GSK9311 hydrochloride, a less active analogue of GSK6853, can be used as a negative control. GSK9311 hydrochloride inhibits BRPF bromodomain with pIC50 values of 6.0 and 4.3 for BRPF1 and BRPF2, respectively.
  • HY-122626
    BRPF1B/TRIM24-IN-1
    Inhibitor
    BRPF1B/TRIM24-IN-1 (compound 34) is a potent TRIM24/BRPF1/BRPF2 inhibitor, with IC50 values of 0.43, 0.34, 1.75 μM, respectively. BRPF1B/TRIM24-IN-1 binds the TRIM24 bromodomain with a KD of 222 nM and has a KD for the BRPF1 bromodomain of 137 nM and for BRD1 of 1130 nM.