BRD9
BRD9 (bromodomain-containing protein 9) is an epigenetic reader that recognizes acetylated lysine residues and functions as a core component of the non-canonical BAF (ncBAF) chromatin-remodeling complex, thereby regulating transcriptional programs linked to chromatin accessibility and cell identity[1][2]. Mechanistically, BRD9 contributes to chromatin-dependent gene regulation through its bromodomain-mediated recognition of acetylated proteins and its integration within SWI/SNF-family remodeling complexes[1][3]. In disease-relevant settings, BRD9 has emerged as a functional dependency in several cancer models, including acute myeloid leukemia (AML) and colorectal cancer, where genetic depletion or pharmacological inhibition impairs proliferation and promotes apoptosis or growth suppression[4][5][6]. Compared with the closely related bromodomain protein BRD7, BRD9 displays distinct biological activities within ncBAF complexes, and selective targeting of BRD9 has therefore become an important strategy for dissecting ncBAF-specific functions without broadly perturbing related chromatin-remodeling pathways[2][1]. For experimental applications, highly selective BRD9 chemical probes such as I-BRD9 have enabled interrogation of BRD9-dependent transcriptional programs, showing substantial selectivity over BRD7 and BET-family bromodomains while identifying BRD9-sensitive genes involved in oncology and immune-response pathways[1]. In addition, next-generation BRD9 inhibitors and degraders, including BI-7273, BI-9564, and BRD9-directed PROTAC degraders, have provided valuable tools for mechanistic studies and target-validation experiments in cancer biology[3][7].
References:
- [1]. Theodoulou NH, et al. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem. 2016 Feb 25;59(4):1425-39. [Content Brief]
- [2]. Uniprotkb.
- [3]. Remillard D, et al. Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angew Chem Int Ed Engl. 2017 May 15;56(21):5738-5743. [Content Brief]
- [4]. Zhou L, et al. Targeting BRD9 by I-BRD9 efficiently inhibits growth of acute myeloid leukemia cells. Transl Cancer Res. 2021 Jul;10(7):3364-3372. [Content Brief]
- [5]. Chen P, et al. Bromodomain-containing protein 9 activates proliferation and epithelial-mesenchymal transition of colorectal cancer via the estrogen pathway in vivo and in vitro. J Gastrointest Oncol. 2023 Apr 29;14(2):980-996. [Content Brief]
- [6]. Zhu X, et al. Targeting BRD9 for Cancer Treatment: A New Strategy. Onco Targets Ther. 2020 Dec 24;13:13191-13200. [Content Brief]
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BRD9 관련 제품 (55)
관련 제품 (55)
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dBRD9 dihydrochloride
0 ImagesdBRD9 dihydrochloride is a BRD9 PROTAC degrader. dBRD9 dihydrochloride reduces the binding of the ISGF3 complex to ISG promoters, decreases the level of ISG induction downstream of IFNAR signaling, and reduces the chromatin binding of BRD4 at BRD9 co-binding sites. dBRD9 dihydrochloride can be used in research related to acute myeloid leukemia.
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BRD7-IN-1 free base
0 ImagesCat. No.: HY-111905ACAS No.: 2305379-66-0BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).
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PROTAC BRD9 Degrader-5
0 ImagesCat. No.: HY-145947CAS No.: 2704616-86-2PROTAC BRD9 Degrader-5 is a BRD9 PROTAC degrader. PROTAC BRD9 Degrader-5 is used in research on acute myeloid leukemia, rhabdoid tumor, synovial sarcoma, and multiple myeloma.
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XYD224
0 ImagesCat. No.: HY-184210XYD224 is a selective BRD9 PROTAC degrader with a DC50 of 7.3 nM. XYD224 inhibits the proliferation of acute myeloid leukemia cells. XYD224 suppresses tumor growth in xenograft models. XYD224 is applicable for the research of acute myeloid leukemia (AML).
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PROTAC BRD9 Degrader-12
0 ImagesCat. No.: HY-189226PROTAC BRD9 Degrader-12 is a BRD9 PROTAC degrader, with DC50 values of 57 pM and 62 pM against BRD9 and IKZF1, respectively. PROTAC BRD9 Degrader-12 promotes CRL-CRBN-dependent ubiquitination and proteasome-mediated BRD9 degradation by simultaneously binding to BRD9 and CRBN, and concurrently recruits IKZF1 as a neosubstrate via CRBN to induce its degradation. PROTAC BRD9 Degrader-12 selectively degrades BRD9 and IKZF1. The synergistic degradation of BRD9/IKZF1 downregulates MYC-related signaling, induces apoptosis and S-phase cell cycle arrest, and thereby inhibits the proliferation of hematological malignant cells. PROTAC BRD9 Degrader-12 is used for research related to hematological malignancies.
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BRD9 Degrader-2
0 ImagesCat. No.: HY-163809CAS No.: 3033018-68-4BRD9 Degrader-2 is a selective BRD9 molecular glue degrader. BRD9 Degrader-2 consists of a BRD9-binding ligand, a linker, and a warhead that promotes proteasomal degradation of BRD9 via a non-canonical PROTAC mechanism independent of CRBN or VHL E3 ligases. BRD9 Degrader-2 can be used in cancer research, including studies of malignant rhabdoid tumors, specific sarcomas, and acute myeloid leukemia.
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BRD9 ligand-14
0 ImagesCat. No.: HY-184211CAS No.: 3126237-28-0
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PROTAC BRD9 Degrader-11
0 ImagesCat. No.: HY-181951PROTAC BRD9 Degrader-11 is a VHL-based BRD9 PROTAC degraderwith an IC50 of 0.66 μM. PROTAC BRD9 Degrader-11 induces selective, proteasome-dependent degradation of BRD9 via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-11 impairs cell viability, suppresses proliferation, and arrests growth of acute myeloid leukemia cells. PROTAC BRD9 Degrader-11 can be used for the research of acute myeloid leukemia.
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BRD9 ligand-5
0 ImagesCat. No.: HY-169988CAS No.: 2633634-64-5
