| E1103 |
AU-15330
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AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4, which can induce potent inhibition of tumor growth in xenograft models of prostate cancer.
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DNA Repair, 2025, 103884
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EMBO J, 2024, 10.1038/s44318-024-00206-1
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| S9612 |
ACBI1
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ACBI1 is a potent and cooperative PROTAC degrader of SMARCA2, SMARCA4 and PBRM1 with DC50 of 6 nM, 11 nM and 32 nM for SMARCA2, SMARCA4 and PBRM1 in MV-4-11 cells, respectively. ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase VHL. ACBI1 induces anti-proliferative effects and apoptosis.
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Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2054
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Cancer Research, 2025, 1997-2013
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Mol Metab, 2025, 93:102107
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| E8293New |
YD54
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YD54 is a potent, selective and orally bioavailable PROTAC and a degrader of SMARCA2 with DC50 of 8.1 nM at 24 hours. It exhibits antitumor activity in SMARCA4-mutant lung cancer xenograft models and can be used in research on non-small cell lung cancer.
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| E1985 |
YD23
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YD23 is a PROTAC which induces the degradation of SMARCA2. It reduces chromatin accessibility in SMARCA4-deficient cells, affecting gene enhancers related to cell cycle and growth regulation, which leads to the downregulation of several cell cycle genes. It also selectively inhibits the growth of SMARCA4 mutant lung cancer cells in vitro.
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| E8059 |
VH032-cyclopropane-F
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VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4.
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