MS182 - CAS 3034773-62-8

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/+) .

MDM-2/p53

Apoptosis

3034703

C57H68FN7O7S

1014.26

O=C(NCCOC1=CC=C(C=C1F)CCC2=NC=3C=C(C=CC3N2CCN4CCOCC4)C=5C(=NOC5C)C)CCOCCOCCOCCNCC=6C=CC7=C(C6)C=8C=CC(=CC8N7CC)C=9SC=C(C9)C

-20°C

Ice Packs

Small Compound