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 Related Products (55)
Related Products (55)
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QA-68
0 ImagesCat. No.: HY-150797Synonyms: QA-68-ZU81QA-68 (QA-68-ZU81) is an effective PROTAC-class BRD9 degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines
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BRD9 Degrader-3
0 ImagesCat. No.: HY-163810CAS No.: 3033018-77-5BRD9 Degrader-3 is a selective BRD9 BRD9 molecular glue degrader degrader. BRD9 Degrader-3 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-3 can be used in cancer research, including studies of malignant rhabdoid tumors, specific sarcomas, and acute myeloid leukemia.
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PROTAC BRD9 Degrader-8
0 ImagesCat. No.: HY-162651CAS No.: 3081180-48-2PROTAC BRD9 Degrader-8 is a selective, orally active BRD9 PROTAC degrader with a DC50 of 16 pM.\nPROTAC BRD9 Degrader-8 induces cell cycle arrest at the G1 phase and promotes apoptosis. PROTAC BRD9 Degrader-8 can be used for research on acute myeloid leukemia and diffuse large B-cell lymphoma.
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TP-238
0 ImagesCat. No.: HY-114205CAS No.: 2415263-04-4
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PROTAC BRD9 Degrader-10
0 ImagesCat. No.: HY-181949PROTAC BRD9 Degrader-10 is a PROTAC degrader targeting BRD9, with an IC50 of 2.97 μM against BRD9. PROTAC BRD9 Degrader-10 induces BRD9 degradation via the ubiquitin-proteasome system by recruiting the VHL E3 ubiquitin ligase. PROTAC BRD9 Degrader-10 reduces the viability and inhibits the proliferation of myeloid leukemia cells. PROTAC BRD9 Degrader-10 is applicable for the research of acute myeloid leukemia.
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(S,R)-CFT8634
0 ImagesCat. No.: HY-145925CCAS No.: 2704617-95-6(S,R)-CFT8634 is a BRD9 PROTAC degrader that exerts activity via the ubiquitin-proteasome pathway. (S,R)-CFT8634 can be used in the research of acute myeloid leukemia, malignant rhabdoid tumor, synovial sarcoma, and multiple myeloma.
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BRD9 ligand-12
0 ImagesCat. No.: HY-182084BRD9 ligand-12 is a BRD9 ligand. BRD9 ligand-12 can be used as a ligand for target protein for PROTAC to develop and design degradative agents for PROTAC BRD9, such as XYD270 (HY-182082). XYD270 inhibits tumor growth in a mouse model of acute myeloid leukemia. XYD270 can be used in research related to synovial sarcoma and acute myeloid leukemia.
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BRD9 ligand-13
0 ImagesCat. No.: HY-175915CAS No.: 2704619-67-8BRD9 ligand-13 (Compound 5) is a BRD9 ligand that can be used for the synthesis of PROTACs, such as PROTAC BRD9 Degrader-8 (HY-162651).
