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MS182

CAT: 0931-T200153-01Size: 10 mgDry Ice: NoHazardous: No
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CAT#:0931-T200153-01Size:10 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
3034773-62-8
Target
MDM-2/p53
Related Pathways
Apoptosis
Bioactivity
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/+) .
Smiles
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
Molecular Formula
C57H68FN7O7S
Molecular Weight
1014.26
Shipping Conditions
Ice Packs
Storage Temperature
-20°C

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