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MS182

Product Specifications

CAS Number

3034773-62-8

UNSPSC Description

MS182 (compound 11) is an acetylation targeting chimera (AceTAC) designed based on p53Y220C stabilizer and targeting p53Y220C. MS182 is composed of p53Y220C and p300/CBP binders, respectively, coupled by a linker. MS182 forms a ternary complex with p300/CBP acetyltransferase and p53Y220C in a time- and concentration-dependent manner, effectively acetylating lysine at position 382 of p53Y220C (ACE50: 1.52 μM). MS182 also exhibited considerable bioavailability in mice, with GI50 values of 2.16 μM and 1.83 μM for BxPC3 (p53Y220C/-) and NUGC (p53Y220C/+), respectively[1].

Target Antigen

MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis

Field of Research

cancer

Assay Protocol

https://www.medchemexpress.com/ms182.html

Smiles

O=C(NCCOC1=CC=C(CCC2=NC3=CC(C4=C(C)ON=C4C)=CC=C3N2CCN5CCOCC5)C=C1F)CCOCCOCCOCCNCC6=CC7=C(C=C6)N(CC)C8=C7C=CC(C9=CC(C)=CS9)=C8

Molecular Weight

1014.26

References & Citations

[1]Design, Synthesis, and Evaluation of p53Y220C Acetylation Targeting Chimeras (AceTACs)

Shipping Conditions

Room temperature

Clinical Information

No Development Reported

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