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PROTAC(H-PGDS)-7 是一种造血前列腺素 D 合酶 (H-PGDS) PROTAC 降解剂,DC50 为 17.3 pM。
PROTAC(H-PGDS)-7 is a proteolysis-targeting chimera (PROTAC) comprised of the hematopoietic prostaglandin D synthase (H-PGDS) inhibitor TFC-007 and the cereblon inhibitor pomalidomide .1 It induces degradation of H-PGDS in KU812 cells with a 50% degradation concentration (DC50) value of 17.3 pM, as well as decreases the production of prostaglandin D2 (PGD2) in the same cells.
1.Yokoo, H., Shibata, N., Endo, A., et al.Discovery of a highly potent and selective degrader targeting hematopoietic prostaglandin D synthase via in silico designJ. Med. Chem.64(21)15868-15882(2021)
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