MS182 (compound 11), an acetylation targeting chimera (AceTAC), incorporates p53 Y220C stabilizers with p300/CBP binders, connected via a linker. This design enables MS182 to selectively form a ternary complex with p300/CBP acetyltransferase and the mutant p53 Y220C, subsequently catalyzing specific acetylation of lysine at position 382 in a time- and concentration-dependent manner, achieving an ACE 50 of 1.52 µM. Additionally, MS182 demonstrated significant bioavailability in mice, with GI 50 values recorded at 2.16 µM for BxPC3 (p53 Y220C/-) and 1.83 µM for NUGC (p53 Y220C/+).
Molekulargewicht:
1014.26
CAS Nummer:
[3034773-62-8]
Formel:
C57H68FN7O7S
Target-Kategorie:
MDM-2/p53
T200153
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