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  3. MS182

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.

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MS182 Chemical Structure

MS182 Chemical Structure

CAS No. : 3034773-62-8

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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].

IC50 & Target

ACE50: 1.52 μM (p53Y220C)[1]

Molecular Weight

1014.26

Formula

C57H68FN7O7S

CAS No.
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

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HY-159606
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