2. PROTAC Epigenetics
  3. LYTACs Epigenetic Reader Domain
  4. MrTAC-8

MrTAC-8 是甲基精氨酸靶向嵌合体 (MrTAC)，同时也是一种 BRD4 降解剂，其在 HeLa 细胞中的 DC50 值为 46 nM。MrTAC-8 可招募 PRMT1、PRMT3、PRMT4、PRMT5 和 PRMT7 至靶蛋白，诱导精氨酸甲基化以触发溶酶体降解。MrTAC-8 可降解分布于不同亚细胞定位的蛋白质，且不依赖于天然蛋白水解途径。MrTAC-8 可用于宫颈癌、胶质母细胞瘤的研究。

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MrTAC-8

MrTAC-8 Chemical Structure

1.  客户无需承担相应的运输费用。

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MrTAC-8 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

MrTAC-8, methylarginine-targeting chimera (MrTAC), is a BRD4 degrader with DC50 values of 46 nM in HeLa cells. MrTAC-8 recruits PRMT1, PRMT3, PRMT4, PRMT5, and PRMT7 to target proteins, inducing arginine methylation that triggers lysosomal degradation. MrTAC-8 degrades proteins across diverse subcellular localizations and independent of native proteolytic routes. MrTAC-8 can be used for the research of cervical cancer, glioblastoma[1].

IC50 & Target[1]

BRD4

 

体外研究
(In Vitro)

MrTAC-8 (0.01 nM-10 μM；24 小时) 可通过招募具有催化活性的 PRMT5，强效诱导内源性 BRD4 的溶酶体降解，在 HeLa 细胞中的 DC50 值为 46 nM，在 U87 细胞中为 67 nM，在 HEK293 细胞中为 4.8 μM[1]。
MrTAC-8 (1 μM；2 小时) 在 HeLa 细胞中可阻断 BRD4 降解，当用溶酶体抑制剂 bafilomycin 和 Chloroquine (HY-17589A) 预处理时，BRD4 水平可恢复至 DMSO 对照组的 110%[1]。

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

MrTAC-8 相关抗体:

Western Blot Analysis[1]

Cell Line: HEK293, HeLa, U87 human cancer cells
Concentration: 0.01 nM; 0.1 nM; 1 nM; 10 nM; 100 nM; 1 μM; 10 μM
Incubation Time: 24 h
Result: Reduced BRD4 levels to 39% of DMSO control in HEK293 cells at 1 μM.
Reduced BRD4 levels to 13% of DMSO control in HEK293 cells at 10 μM.
Demonstrated cell line-specific potency, with DC50 values of 46 nM in HeLa cells, 67 nM in U87 cells, and 4.8 μM in HEK293 cells.

Western Blot Analysis[1]

Cell Line: HeLa human cervical cancer cells
Concentration: 1 μM plus 500 nM bafilomycin and 10 μM Chloroquine
Incubation Time: 2 h
Result: Blocked BRD4 degradation when pre-treated with lysosomal inhibitors bafilomycin and Chloroquine, restoring BRD4 levels to 110% of DMSO control.
Reduced BRD4 levels to 100% of DMSO control in cells expressing catalytically dead (E444Q) PRMT5 at 1 μM, compared to 15% reduction in cells expressing wild-type PRMT5.
Enriched BRD4 in SDMA-positive fractions after treatment, confirming proximity-induced arginine methylation.
分子量

1017.68

Formula

C54H65ClN10O6S
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

MrTAC-8 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

MrTAC-8MrTAC8MrTAC 8LYTACsEpigenetic Reader DomainLysosome-targeting chimerasPRMT1PRMT4PRMT5glioblastomaPRMT7arginine methylationPRMT3cervical cancerlysosomal degradationHeLa cellsInhibitorinhibitorinhibit

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产品名称：
MrTAC-8
目录号：
HY-183061
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