2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. PROTAC EZH2 Degrader-35

PROTAC EZH2 Degrader-35 (compound U3i (44)) 是一款靶向 EZH2 的 PROTAC 蛋白降解剂，其对人源 EZH2 的 Ka 为 16.19 nM。PROTAC EZH2 Degrader-35 在三阴性乳腺癌细胞中表现出抗增殖活性，而在正常人源上皮细胞、肝细胞及肾细胞中的细胞毒性极低。PROTAC EZH2 Degrader-35 可用于三阴性乳腺癌的相关研究。
(粉色: Histone Methyltransferase 配体 (HY-181393)；蓝色: Cereblon 配体 (HY-10984)；黑色: 连接子)。

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PROTAC EZH2 Degrader-35

PROTAC EZH2 Degrader-35 Chemical Structure

CAS No. : 3034875-56-1

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PROTAC EZH2 Degrader-35 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Histone Methyltransferase 亚型特异性产品:

查看所有亚型
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC EZH2 Degrader-35 (compound U3i (44)) is a PROTAC protein degrader targeting EZH2 with a human EZH2 Ka of 16.19 nM. PROTAC EZH2 Degrader-35 exhibits antiproliferative activity in triple-negative breast cancer cells and minimal cytotoxicity in normal human epithelial, hepatic, renal cells.PROTAC EZH2 Degrader-35 can be used for the research of triple-negative breast cancer[1]. (Pink: Histone Methyltransferase ligand (HY-181393); Blue: Cereblon ligand (HY-10984); Black: linker).

体外研究
(In Vitro)

PROTAC EZH2 Degrader-35 可高亲和力结合 PRC2 复合物，其 Kd 值为 16.19 nM[1]。
PROTAC EZH2 Degrader-35 可强效抑制 MDA-MB-231 和 MDA-MB-468 三阴性乳腺癌细胞的增殖，其 IC50 值分别为 0.57 μM 和 0.38 μM[1]。
PROTAC EZH2 Degrader-35 可诱导依赖于 CRBN 和蛋白酶体的 PRC2 复合物组分降解，减少致癌组蛋白修饰，引发癌细胞的线粒体功能障碍和凋亡，且对正常人源细胞的毒性极低[1]。

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

PROTAC EZH2 Degrader-35 相关抗体:
分子量

1270.48

Formula

C66H87N13O13
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-35 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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.

Keywords:

PROTAC EZH2 Degrader-353034875-56-1PROTACsHistone MethyltransferaseCRBNtriple-negative breast cancer cellsEZH2apoptosisMDA-MB-231EEDMDA-MB-468PRC2 complexproteasomeSUZ12Inhibitorinhibitorinhibit

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HY-181392
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