BRD9 Degrader

FHD-609 is a BRD9 PROTAC degrader. FHD-609 induces BRD9 degradation, downregulates primary transcripts of HBG/HBD, Myc expression and proliferation gene sets, reduces the levels of synovial sarcoma tumor proliferation markers, and inhibits tumor growth. FHD-609 can be used in research related to advanced synovial sarcoma, SMARCB1-deficient tumors and adrenocortical carcinoma.

DBr-1 is a potent BRD9 PROTAC degrader with a DC₅₀ of 90 nM. DBr-1 mediates the ubiquitination and proteasomal degradation of BRD9 via the ubiquitin-proteasome pathway. DBr-1 is applicable to research related to renal cell carcinoma and synovial sarcoma.

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).

dBRD9 is a BRD9 PROTAC degrader. dBRD9 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 can be used in research related to acute myeloid leukemia.

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.

PROTAC BRD9 Degrader-4 is a BRD9 PROTAC degrader with a DC₅₀ of 1 nM. PROTAC BRD9 Degrader-4 is applicable to research related to synovial sarcoma and acute myeloid leukemia.

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.

dBRD9 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.

PROTAC 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.

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).

BRD9 Degrader-4 is a bifunctional targeted degrader of the BRD9 protein, which promotes proteasomal degradation of BRD9 via a non-canonical PROTAC mechanism independent of the CRBN or VHL E3 ligases.

PROTAC BRD9 Degrader-6 (Compound D1) is a racemic PROTAC degrader that recruits cereblon to induce targeted degradation of BRD9. PROTAC BRD9 Degrader-6 has an IC₅₀ of 0.13 nM in SYO-1 cells. It can be used in research on BAF complex-related diseases, such as cancer, infections and synovial sarcoma.

PROTAC 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.

ZZ7-23-022 (ZZ7) is a selective BRD9 molecule glue degrader. ZZ7-23-022 effectively degrades BRD9 in synovial sarcoma cells, but does not affect cardiomyocytes. ZZ7-23-022 can be used for the research of cancer.

BI 7271 is a BRD9 ligand, which can be used for the synthesis of PROTACs, such as PROTAC BRD9 Degrader-7 (HY-155361).

BRD9 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.

PROTAC 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.

EA-89 is a potent and selective BRD9 inhibitor with antitumor activity. EA-89 is a Ligand for Target Protein for PROTAC. EA-89 can be used to synthesize PROTAC QA-68 (HY-150797).

BRD9 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.

BRD9 Degrader-1 is a selective BRD9 PROTAC degrader with a DC₅₀ of 108 nM. BRD9 Degrader-1 induces the formation of a ternary complex between BRD9 and VHL, with an EC₅₀ of 17 nM, and shows no hook effect at high concentrations. BRD9 Degrader-1 can be used for the research of synovial sarcoma.