SJ44236 is a BET PROTAC degrader capable of degrading BRD2 (DC50 = 0.127 nM), BRD3, and BRD4. It shows cytotoxicity in MV4-11 and HD-MB03 cells with IC50 values of 0.12 nM and 0.92 nM, respectively. The compound downregulates c-Myc expression and upregulates p53 expression. In mice, SJ44236 demonstrates good oral bioavailability (45%). [Pink: ligand for target protein JQ-1 carboxylic acid, Black: linker, Blue: ligand for E3 ligaseCereblonE3ligaseLigand 54]
Molekulargewicht:
753.36
Formel:
C40H45ClN8O3S
Target-Kategorie:
Epigenetic Reader Domain|||PROTACs
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