AB3067 is a PROTAC degrader targeting BET protein, efficiently recruiting two distinct E3 ligases, Cereblon and VHL, with strong affinity (demonstrated by IC50 values of 559 nM for VHL and 190 nM for CRBN in vivo HEK293). It degrades BRD2, BRD3, BRD4, and CRBN with DC50 values of 2.1~2.3, 1.6, 15, and 75 nM, respectively. Additionally, AB3067 inhibits the proliferation of RKO cells, with an EC50 of 111 nM. (Pink: ligand for target protein, Black: linker, Blue: ligand for E3 ligase VHL and CRBN)
Molekulargewicht:
1525.16
Formel:
C74H91ClFN11O17S2
Target-Kategorie:
PROTACs|||Epigenetic Reader Domain
T204341
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