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]^[7]. 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^[7]. 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]^[8].

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]

BRD9 Related Products (44):

By Type:	Pan (9) Selective (14)
By Effects:	Inhibitors (18) Degraders (14) Ligands (4)

Cat. No.	Product Name	Effect	Purity

HY-153367

FHD-609	Inhibitor	98.95%
FHD-609 is a PROTAC degrader and inhibitor of BRD9 (Bromodomain-containing protein 9). FHD-609 targets to ncBAF, can be used for research of wide range of cancers that contain a mutation in a BAF complex subunit. FHD-609 in combination with Telomelysin or INO5401, may play a role in adrenocortical carcinoma (ACC) treatment. (Blue: BRD9 ligand-6 (HY-49393), Black: linker (HY-168309); Pink: (S)-Deoxy-thalidomide-Br (HY-168308) ).

HY-100351

BI-7273	Inhibitor	99.75%
BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC₅₀ and a K_d of 19 and 0.75 nM; also shows high effect on BRD7, with an IC₅₀ and a K_d of 117 nM and 0.3 nM.

HY-114322

VZ185	Inhibitor	99.95%
VZ185 is a potent, fast, and selective von Hippel-Lindau based dual degrader probe of BRD9 and BRD7 with DC₅₀s of 4.5 and 1.8 nM, respectively. VZ185 is cytotoxic in EOL-1 and A-402 cells, with EC₅₀s of 3 nM and 40 nM, respectively.

HY-100352

BI-9564	Inhibitor	98.96%
BI-9564, a chemical probe, is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC₅₀s of 75 nM and 3.4 μM and K_ds of 14 nM and 239 nM, respectively. BI-9564 has an IC₅₀ of > 100 μM for BET family.

HY-117690

dBRD9	Degrader	99.75%
dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family.

HY-182082

XYD270
XYD270 is an orally active BRD9 PROTAC degrader. XYD270 inhibits the proliferation of cancer cells. XYD270 suppresses tumor growth in a mouse model of acute myeloid leukemia. XYD270 can be used in research related to synovial sarcoma and acute myeloid leukemia.

HY-182766

AMX-883	Degrader
AMX-883 a selective and orally active BRD9 molecular glue degrader that drives differentiation in acute myeloid leukaemia. AMX-883 shows selectivity over all other bromodomain containing proteins and proteome wide. AMX-883 does not employ the commonly used E3 ligases (cereblon, VHL) but instead drives degradation via DCAF16 as a targeted glue. AMX-883 can be used for the study of acute myeloid leukaemia (AML).

HY-184210

XYD224	Degrader
XYD224 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).

HY-110374

NVS-CECR2-1	Inhibitor	99.40%
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC₅₀=47 nM; K_D=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism. NVS-CECR2-1 is a chemical probe.

HY-100517

TP-472	Inhibitor	99.54%
TP-472, a chemical probe, is a selective BRD9/7 inhibitor, with K_ds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells.

HY-149420

BRD7-IN-2	Inhibitor	99.29%
BRD7-IN-2 (compound 2-77) is a potent inhibitor of bromodomain-containing protein 7 (BRD7), targeting to prostate cancer cells. BRD7-IN-2 is selective for BRD7 rather than BRD9, with IC50s of 5.4 μM, and >300 μM, respectively.

HY-148739

dBRD 9-A	Degrader	99.50%
dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma.

HY-103632

PROTAC BRD9 Degrader-1	Inhibitor	99.16%
PROTAC BRD9 Degrader-1 is a PROTAC connected by ligands for Cereblon and BRD9 (IC₅₀=13.5 nM), which can be used as a selective probe useful for the study of BAF complex biology.

HY-107477

GSK8573		99.53%
GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a K_d value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments.

HY-155361

PROTAC BRD9 Degrader-7	Degrader	99.29%
PROTAC BRD9 Degrader-7 is an orally active, selective BRD9 PROTAC degrader (DC₅₀ = 1.02 nM). PROTAC BRD9 Degrader-7 mediates BRD9 degradation via the ubiquitin-proteasome system. PROTAC BRD9 Degrader-7 exhibits proliferation inhibitory activity in the MV4-11 cells. PROTAC BRD9 Degrader-7 can be used in the research of acute myeloid leukemia and other related malignancies. (Pink: BI 7271: HY-123616, Blue: 5-Aminothalidomide: HY-W023573, Blue + Black: Thalidomide-5-piperazine: HY-W834174, Black: N,N'-Dimethylpiperazine: HY-W539783).

HY-159579

CW-3308		99.43%
CW-3308 is an orally active BRD9 PROTAC degrader with an DC₅₀ of 92 nM. CW-3308 forms a ternary complex with BRD9 and cereblon to mediate BRD9 degradation. CW-3308 inhibits the viability of synovial sarcoma and rhabdoid tumor cells. CW-3308 reduces BRD9 protein levels in xenograft tumor tissues and suppresses tumor growth in xenograft models. CW-3308 can be used for the research of synovial sarcoma and rhabdoid tumors.

HY-145403

PROTAC BRD9 Degrader-4	Degrader	99.06%
PROTAC BRD9 Degrader-4 is a BRD9 bifunctional PROTAC degrader for researching cancer.

HY-123621

GNE-375	Inhibitor	99.93%
GNE-375 is a potent and highly selective BRD9 inhibitor with an IC₅₀ of 5 nM. GNE-375 shows >100-fold selective for BRD9 over BRD4, TAF1, and CECR2. GNE-375 decreases BRD9 binding to chromatin.

HY-114205A

TP-238 hydrochloride	Inhibitor	≥99.0%
TP-238 hydrochloride is a potent and selective dual CECR2/BPTF probe with IC₅₀ values of 30 nM and 350 nM, respectively. TP-238 hydrochloride also inhibits BRD9 with a pIC₅₀ of 5.9 and is less active against other 338 kinases.

HY-49393

BRD9 ligand-6
BRD9 ligand-6 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BRD9 ligand-6 can be utilized for the synthesis of FHD-609 (HY-153367).

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