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Alobresib is a novel and potent BET bromodomain inhibitor for recurrent/chemotherapy resistant uterine serous carcinoma overexpressing c-Myc.
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MT-802 is a potent BTK degrader based on PROTAC technology, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia.
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GSK3368715 is an orally active and SAM uncompetitive type I PRMT inhibitor that produces a shift in arginine methylation states.
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MBM-55 is a potent, selective Nek2 inhibitor with an IC50 of 1 nM. MBM-55 shows antitumor activities and induces cell cycle arrest and apoptosis.
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APG-115 is an orally active MDM2 protein inhibitor binding to MDM2 protein. APG-115 blocks the interaction of MDM2 and p53 and induces apoptosis.
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M-89 is a specific menin inhibitor, with a Kd of 1.4 nM. M-89 inhibits the Menin-MLL protein-protein interaction and has potential to treat MLL leukemia.
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GSK2643943A is a novel deubiquitylating enzyme (DUB) inhibitor. GSK2643943A targets USP20/Ub-Rho and shows an IC50 of 160 nM.
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FGTI-2734 is a dual farnesyl and geranylgeranyl transferase-1 inhibitor. FGTI-2734 prevents membrane localization of KRAS and mutant KRAS pancreatic tumors.
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SAR-260301 is a selective PI3Kβ inhibitor with an IC50 of 23 nM. SAR-260301 is a potent and highly selective PI3Kβ inhibitor for melanoma.
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dBET6 is a potent PROTAC degrader of BET, shows high affinity to BRD4(1), and possess good efficacy in T cell acute lymphoblastic leukemia activity.
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