1. PROTAC Metabolic Enzyme/Protease Apoptosis Cell Cycle/DNA Damage Epigenetics
  2. PROTACs Fat Mass and Obesity-associated Protein (FTO) Apoptosis Caspase PARP YTHDF
  3. PROTAC FTO degrader 1

PROTAC FTO degrader 1 是一种脂肪量和肥胖相关蛋白 (FTO) 的 PROTAC 降解剂。PROTAC FTO degrader 1 依赖于 VHL E3 连接酶和泛素-蛋白酶体系统选择性降解 FTO。PROTAC FTO degrader 1 可增加与核糖体生物发生相关的 mRNA 上的 m6A 修饰,并促进其由 YTHDF2 介导的降解。PROTAC FTO degrader 1 能够抑制癌细胞增殖并诱导凋亡 (apoptosis)。PROTAC FTO degrader 1 可用于癌症研究,如急性髓系白血病 (AML)。(结构:粉色:FTO 配体 (HY-175886);蓝色:VHL 连接酶配体 (HY-112078);黑色:连接子 (HY-W002042);VHL 配体-Linker: (HY-139218))

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PROTAC FTO degrader 1

PROTAC FTO degrader 1 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

PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m6A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML)[1]. (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))

IC50 & Target[1]

VHL

 

PARP1

 

Caspase 3

 

YTHDF2

 

体外研究
(In Vitro)

PROTAC FTO degrader 1 (Compound FP54) (0.08-2.5 μM, 48 h) 在 NB4 和 MOLM-13 细胞中以剂量依赖性方式降解 FTO,最大降解率 >95%[1]
PROTAC FTO degrader 1 抑制多种急性髓系白血病细胞系的增殖, IC50 值为 0.48-2.44 μM[1]
PROTAC FTO degrader 1 (2-5 μM, 48 h) 显著诱导 MOLM-13 和 NB4 细胞凋亡[1]
PROTAC FTO degrader 1 (5 μM) 促进 MOLM-13 细胞分化[1]
PROTAC FTO degrader 1 (2 μM, 48 h) 提高 NB4 细胞中整体 mRNA 的 m6A 修饰水平[1]
PROTAC FTO degrader 1 (2 μM, 48 h) 降低 MOLM-13 细胞中的多核糖体/80S 单核糖体比率,并抑制整体翻译[1]
PROTAC FTO degrader 1 (2 μM) 在 MOLM-13 细胞中会使 YTHDF2 中富集核糖体生物发生相关 mRNA MRPL36 和 LYAR,降低其 mRNA 稳定性,并促进 YTHDF2 介导的降解[1]

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

Apoptosis Analysis[1]

Cell Line: MOLM-13 and NB4 cells
Concentration: 2 and 5 μM
Incubation Time: 48 h
Result: Increased apoptotic cells.
Induced cleavage of caspase-3 and PARP1.
体内研究
(In Vivo)

PROTAC FTO degrader 1 (Compound FP54) (25 mg/kg,静脉注射,每周 3 次) 可延缓 MA9.3Ras/MOLM13/AML-0148 肿瘤小鼠中的疾病发作,并延长其生存期[1]

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

Animal Model: MA9.3Ras/ MOLM13/AML-0148 tumor mice models[1]
Dosage: 25 mg/kg
Administration: Intraperitoneally injection, 3 times a week
Result: Reduced AML cell engraftment in peripheral blood and bone marrow.
Decreased leukemia burden and delayed disease onset.
Prolonged survival.
Showed no obvious toxicity to mouse body weight, blood routine, or major organs.
分子量

1173.25

Formula

C59H75Cl2N9O10S

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

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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.

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产品名称:
PROTAC FTO degrader 1
目录号:
HY-175885
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