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HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.
KT-474 is a highly active and selective, orally bioavailable IRAK4 degrader being developed for the treatment of toll-like receptor (TLR)/interleukin-1 receptor (IL-1R)-driven immune-inflammatory diseases.
HJM-561 is a potent, selective and orally bioavailable EGFR PROTAC degrader, selectively degrades the EGFR C797S-containing triple mutants Del19/T790M/C797S and L858R/T790M/C797S with DC50 values of 9.2 nM and 5.8 nM, respectively.
GNE-0011 is a monovalent, JQ1-based BRD4 degrader that is not linked to an E3 ligase binder, triggers proteasomal and ubiquitin-dependent selective degradation of BRD4 over BRD2 and BRD3.
JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
PROTAC SGK3 degrader-1 (SGK3-PROTAC1), is a potent SKG3 degrader based on PROTAC. PROTAC SGK3 degrader-1 (0.3 μM) induces 50% degradation of endogenous SGK3 within 2 hours, with maximal 80% degradation observed within 8 hours, accompanied by a loss of phosphorylation of NDRG1 (an SGK3 substrate).
TD165(TD 165) is a PROTAC-based cereblon (CRBN) degrader that degrads Cav1.2α with the DC50 of 20.4 nM, comprising a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.
ARD2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer.
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