SMARCA4 Degrader
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AU-15330
0 ImagesAU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity.
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AU-24118
0 ImagesAU-24118 is an orally active PROTAC degrader that recruits cereblon to target the degradation of SMARCA2, SMARCA4 and PBRM1. AU-24118 impairs the chromatin accessibility of oncogenic transcription factors, inhibits colony formation, dislodges chromatin-bound transcription factors, attenuates downstream signal transduction, induces apoptosis, and exerts antiproliferative and cytotoxic effects. AU-24118 can be used in research related to castration-resistant prostate cancer, colorectal cancer, small cell lung cancer and multiple myeloma (including the t (4;14) subtype).
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PRT3789
0 ImagesPRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer.
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YD54
0 ImagesYD54 is an orally active and selective SMARCA2 PROTAC degrader. YD54 induces SMARCA4 degradation but with low potency and selectivity. YD54 selectively inhibits the growth of various cancer cells and suppresses tumor growth in mouse xenograft models. YD54 can be used for the research of SMARCA4-mutant lung cancer.
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A947
0 ImagesCat. No.: HY-148381CAS No.: 2378056-80-3A947 is a VHL-based SMARCA2 PROTAC degrader with a DC50 of 39 pM and a Kd of 93 nM for human SMARCA2. A947 recruits SMARCA2 to the VHL E3 ubiquitin ligase for ubiquitination modification, mediates its degradation via the proteasome, and exerts selective degradation effects on SMARCA4 and PBRM1. A947 induces G1 cell cycle arrest, inhibits transcription, and exerts growth inhibitory effects in SMARCA4G12C-mutant cancer cells. A947 acts synergistically with MCL1 inhibitors to induce apoptosis in SMARCA4G12C-mutant cancer cells. A947 can be used in studies related to SMARCA4G12C-mutant non-small cell lung cancer and non-small cell lung cancer.
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PROTAC SMARCA2/4 degrader-6
0 ImagesCat. No.: HY-159457CAS No.: 2568277-87-0
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PROTAC SMARCA2/4 degrader-25
0 ImagesCat. No.: HY-162813PROTAC SMARCA2/4 degrader-25 is a selective SMARCA2/SMARCA4 PROTAC degrader with selective anti-tumor activity. PROTAC SMARCA2/4 degrader-25 is activated by endogenous GSH, forms a ternary complex with SMARCA2 or SMARCA4 and VHL E3 ubiquitin ligase, and mediates degradation via the proteasome pathway. PROTAC SMARCA2/4 degrader-25 induces DNA damage and apoptosis, and inhibits cancer cell proliferation. PROTAC SMARCA2/4 degrader-25 is applicable to lung cancer-related research.
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PROTAC SMARCA2/4 degrader-32
0 ImagesCat. No.: HY-159459CAS No.: 2568273-79-8
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PROTAC SMARCA2 degrader-32
0 ImagesCat. No.: HY-170343CAS No.: 3033586-50-1PROTAC SMARCA2 degrader-32 is a potent, selective SMARCA2 PROTAC degrader, with DC50 values of 1.3 nM and 94 nM against SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-32 exhibits IC50 against SMARCA2, SMARCA4 and the VHL E3 ubiquitin ligase of 30 nM, 63 nM and 25 nM, respectively. PROTAC SMARCA2 degrader-32 inhibits the growth of SMARCA4-deficient cancer cells. It can be used in research on cancers such as fibrosarcoma.
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PROTAC SMARCA2/4 degrader-28
0 ImagesCat. No.: HY-162835CAS No.: 2409844-88-6PROTAC SMARCA2/4 degrader-28 is a heterobifunctional PROTAC degrader targeting SMARCA2 and SMARCA4. PROTAC SMARCA2/4 degrader-28 forms a ternary complex with CRL2VHL E3 ligase and SMARCA2 or SMARCA4, mediating the ubiquitination and degradation of SMARCA2, while acting as a partial degrader of SMARCA4. PROTAC SMARCA2/4-degrader-28 can be used in cancer-related research.
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PROTAC SMARCA2/4 degrader-27
0 ImagesCat. No.: HY-162834CAS No.: 2375564-54-6PROTAC SMARCA2/4 degrader-27 is a VHL-recruiting PROTAC degrader targeting SMARCA2 and SMARCA4, derived from structure-guided modification of PROTAC SMARCA2/4 degrader-28 (HY-162835). PROTAC SMARCA2/4-degrader-27 forms a cooperative ternary complex with CRL2VHL E3 ligase to induce ubiquitination and degradation. PROTAC SMARCA2/4-degrader-27 induces a novel protein-protein interaction between VHL and SMARCA2/SMARCA4, thereby stabilizing ternary complex formation and promoting proteasomal degradation of target proteins. PROTAC SMARCA2/4-degrader-27 exhibits enhanced cell permeability and stronger ternary complex formation ability, leading to improved degradation activity. PROTAC SMARCA2/4-degrader-27 can be used in cancer-related research[1].
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