2. Stem Cell/Wnt
  3. YAP
  4. TEAD ligand-Linker Conjugate 3

TEAD ligand-Linker Conjugate 3 (文献中 A536 的蓝色结构+黑色结构) 是一种靶向 TEAD1 的配体和 linker 偶联物，能够耦连 IAP 配体 (HY-181531) 后，形成 IAP 招募型双功能蛋白降解剂 (IPD) (HY-181594)，即 SNIPER 降解剂。该 TEAD SNIPER 可同时结合 TEAD1 棕榈酰化口袋和 cIAP1 的 BIR3 结构域形成三元复合物，高效诱导 TEAD1 及 cIAP1 的泛素化降解 (DC50=110 nM，Dmax=51%；对 cIAP1 IC50=122 nM)。TEAD ligand-Linker Conjugate 3 及其合成的 SENIPER 分子可用于 NF2 突变型肿瘤等 Hippo 异常疾病的研究。

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TEAD ligand-Linker Conjugate 3

TEAD ligand-Linker Conjugate 3 Chemical Structure

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TEAD ligand-Linker Conjugate 3 相关抗体

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YAP/TAZ YAP/TAZ-TEAD TEAD YAP1

  • 生物活性

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生物活性

TEAD ligand-Linker Conjugate 3 (the blue structure + black structure of A536 in the literature) is a conjugate of a TEAD1-targeting ligand and a linker. TEAD ligand-Linker Conjugate 3 can be coupled with an IAP ligand (HY-181531) to form an IAP-recruiting bifunctional protein degrader (IPD) (HY-181594), also known as a SNIPER degrader. This TEAD SNIPER simultaneously binds to the TEAD1 palmitoylation pocket and the BIR3 domain of cIAP1 to form a ternary complex, efficiently inducing the ubiquitination and degradation of both TEAD1 and cIAP1 (DC50=110 nM, Dmax=51%; IC50=122 nM for cIAP1). TEAD ligand-Linker Conjugate 3 and its synthesized SENIPER molecule can be utilized in research on Hippo pathway dysregulation-related diseases, such as NF2-mutant tumors[1].

IC50 & Target1

TEAD1

 

分子量

608.05

Formula

C32H29ClF3N5O2
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

TEAD ligand-Linker Conjugate 3 相关分类

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Keywords:

TEAD ligand-Linker Conjugate 3YAPYes-associated proteinInhibitorinhibitorinhibit

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