1. Apoptosis
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  3. MS182

MS182 (compound 11) 是一种基于 p53Y220C 稳定剂设计的、靶向 p53Y220C 的乙酰化靶向嵌合体 (AceTAC)。MS182 由 p53Y220C 和 p300/CBP 分别的结合剂、通过 Linker 偶联而成。MS182 呈时间和浓度依赖性地与 p300/CBP 乙酰转移酶和 p53Y220C 形成三元复合物,有效乙酰化 p53Y220C 382 位点的赖氨酸 (ACE50: 1.52 μM)。MS182 还在小鼠体内表现出可观的生物利用度,对 BxPC3 (p53Y220C/-) 和 NUGC (p53Y220C/+) 的 GI50 分别为 2.16 μM 和 1.83 μM。

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MS182 Chemical Structure

MS182 Chemical Structure

CAS No. : 3034773-62-8

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  • 生物活性

  • 纯度 & 产品资料

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生物活性

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]

分子量

1014.26

Formula

C57H68FN7O7S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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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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