1. PROTAC Epigenetics Apoptosis
  2. PROTACs METTL3 Apoptosis Bcl-2 Family
  3. AF151

AF151 是一种 METTL3 PROTAC 降解剂,在 MOLM-13 细胞中的 DC50 为 0.43 μM。AF151 通过显著降解 METTL3 蛋白和降低 m6A 水平来抑制细胞生长。AF151 可诱导细胞凋亡 (apoptosis) 并降低 Bcl-2 蛋白水平。AF151 可用于癌症如急性白血病 (AML) 的研究。(粉色:METTL3 配体 (HY-174874);蓝色:VHL 配体 (HY-125845);黑色:连接子;VHL 配体+连接子 (HY-174875)) 。

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AF151 Chemical Structure

AF151 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875))[1].

IC50 & Target

Bcl-2

 

VHL

 

Mcl-1

 

体外研究
(In Vitro)

AF151 (0-10 μM,0-72 小时) 可以以时间依赖的方式有效降解 METTL3 蛋白,并显著抑制 MOLM-13 细胞的生长 (DC50 = 0.43 μM,IC50 = 0.45 μM)[1]
AF151 (2 μM,24-48 小时) 可以显著降低 MOLM-13 细胞中的 m6A 水平[1]
AF151 (0.1-5 μM,48 小时) 可以剂量依赖性地诱导 MOLM-13 细胞凋亡并降低抗凋亡蛋白的水平[1]
AF151 (72 小时) 可以在 MOLM-13 细胞中与 Venetoclax (HY-15531) 发挥协同作用[1]
AF151 (0.001-10 μM) 可以促进 METTL3 和 VHL 的结合 (AF151 = 363 nM,AF151-METTL3 = 79.9 nM)[1]

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

Cell Viability Assay[1]

Cell Line: MOLM-13 cells
Concentration: 0.1-10 μM
Incubation Time: 72 h
Result: Significantly inhibited cell growth with the IC50 of 0.45 μM, superior to STM2457 (HY-134836) (IC50 = 1.82 μM) and WD6305 (HY-160415) (IC50 = 0.78 μM).

Western Blot Analysis[1]

Cell Line: MOLM-13 cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Decreased the protein level of Mcl-1 and Bcl-2.

RT-PCR[1]

Cell Line: MOLM-13 cells
Concentration: 2 μM
Incubation Time: 24-48 h
Result: Did not cause significant changes in the expression of METTL3 and METTL14 genes.
分子量

1043.32

Formula

C61H70N8O6S

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
  • 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 *
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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.

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产品名称:
AF151
目录号:
HY-174873
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