2. PROTAC EZH2 Degrader-38

PROTAC EZH2 Degrader-38 (Compound 17) 是一种 EZH2 PROTAC 降解剂，IC50 为 165.00 nM。PROTAC EZH2 Degrader-38 可在功能上抑制 EZH2 甲基转移酶活性，竞争结合 EZH2 SET 结构域的 SAM 结合口袋。
(粉色: Histone Methyltransferase 配体 (HY-147230)；蓝色: Cereblon 配体 (HY-103596)；黑色: )。

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PROTAC EZH2 Degrader-38

PROTAC EZH2 Degrader-38 Chemical Structure

CAS No. : 2653338-74-8

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PROTAC EZH2 Degrader-38 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EZH2 Degrader-38 (Compound 17) is a EZH2 PROTAC degrader with an IC50 of 165.00 nM. PROTAC EZH2 Degrader-38 functionally inhibits the methyltransferase activity of EZH2 and competitively binds to the SAM-binding pocket of the EZH2 SET domain[1]. (Pink: Histone Methyltransferase ligand (HY-147230); Blue: Cereblon ligand (HY-103596); Black: ).

体外研究
(In Vitro)

EZH2 是组蛋白甲基转移酶 (histone methyltransferase)，也是多梳抑制复合物 2（PRC2）的催化亚基。它通过转录抑制肿瘤抑制基因，在肿瘤表观遗传学中发挥“关键作用” (pivotal role)。EZH2 是一个在肿瘤发生发展中起核心调控作用的表观遗传酶，既是现有疗法的靶点，也是新一代蛋白降解技术 (PROTACs) 的重点研究对象[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PROTAC EZH2 Degrader-38 相关抗体:
分子量

998.26

Formula

C58H75N7O8
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

PROTAC EZH2 Degrader-38 相关分类

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Keywords:

PROTAC EZH2 Degrader-382653338-74-8EZH2 methyltransferase activityrecombinant EZH2 enzymatic activitySAM-binding pocketEZH2EZH2 SET domainInhibitorinhibitorinhibit

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