2. Metabolic Enzyme/Protease Apoptosis Vitamin D Related/Nuclear Receptor
  3. Fat Mass and Obesity-associated Protein (FTO) c-Myc RAR/RXR Apoptosis
  4. FTO-IN-16

FTO-IN-16，FTO-IN-15 (HY-179266) 的前药，是一种强效 FTO 抑制剂。FTO-IN-16 可抑制急性髓系白血病 (AML) 细胞的活力，增加 m6A 水平，下调 c-Myc 和 CEBPA 的表达，并上调 ASB2 和 RARA 的表达。FTO-IN-16 诱导细胞凋亡 (apoptosis)。FTO-IN-16 在 AML 小鼠异种移植模型中显示出显著的体内活性。FTO-IN-16 可用于 AML 的研究。

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FTO-IN-16

FTO-IN-16 Chemical Structure

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FTO-IN-16 相关抗体

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RXRα RXRβ RXRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FTO-IN-16, a FTO-IN-15 (HY-179266) prodrug, is a potent FTO inhibitor. FTO-IN-16 suppresses acute myeloid leukemia (AML) cell viability, increases m6A levels, downregulates c-Myc and CEBPA, and upregulates ASB2 and RARA. FTO-IN-16 induces apoptosis. FTO-IN-16 demonstrates strong in vivo efficacy in AML mouse xenografts. FTO-IN-16 can be used for the research of AML[1].

体外研究
(In Vitro)

FTO-IN-16 (0-8 μM; 48 小时) 下调 c-Myc 和 CEBPA (蛋白质和 mRNA)，并上调多种 AML 细胞 (NB4、MOLM13、MV4-11、HEL、OCI-AML3、NOMO-1、KG-1) 中的 ASB2 和 RARA[1]。
FTO-IN-16 (0-20 μM; 48 小时) 可诱导 NB4 细胞发生剂量依赖性凋亡[1]。
FTO-IN-16 (0-8 μM; 48 小时) 下调 c-Myc 和 CEBPA (蛋白质和 mRNA)，并上调多种 AML 细胞 (NB4、MOLM13、MV4-11、HEL、OCI-AML3、NOMO-1、KG-1) 中的 ASB2 和 RARA[1]。
FTO-IN-16 (72 小时) 对一系列 AML 细胞系表现出强大的抗白血病活性，IC50 值分别为 5.5 (NB4)、2.3 (MOLM13)、4.4 (KG-1)、3.6 (MV4-11)、4.6 (HEL)、5.2 (OCI-AML3) 和 4.7 μM (NOMO-1)[1]。

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

FTO-IN-16 相关抗体:

Cell Viability Assay[1]

Cell Line: MOLM13
Concentration: 0, 2, 4, 8 μM
Incubation Time: 24, 48, 72 h
Result: Induced time-dependent growth inhibition. Significantly inhibited cell growth after 72 h treatment at 8 μM compared to the control.

Cell Proliferation Assay[1]

Cell Line: NB4
Concentration: 0, 1, 2, 4 μM
Incubation Time: 7 days
Result: Induced dose-dependent suppression of colony formation.

Apoptosis Analysis[1]

Cell Line: NB4
Concentration: 0, 5, 10, 20 μM
Incubation Time: 48 h
Result: Induced dose-dependent apoptosis.

Western Blot Analysis[1]

Cell Line: NB4, MOLM13, MV4-11, HEL, OCI-AML3, NOMO-1, KG-1
Concentration: 0, 2, 4, 8 μM
Incubation Time: 48 h
Result: Upregulated tumor suppressors RARA and ASB2. Reduced protein levels of the oncoproteins CEBPA and c-Myc. The downregulation of c-Myc protein was consistently observed across 7 tested AML cell lines. Did not alter the protein levels of FTO itself or other major m6A regulators, including ALKBH5 and METTL3.

Real Time qPCR[1]

Cell Line: NB4
Concentration: 0, 4, 8 μM
Incubation Time: 48 h
Result: Increased ASB2 expression accompanied by decreased c-Myc and CEBPA transcripts.
体内研究
(In Vivo)

FTO-IN-16 (30 和 60 mg/kg；腹腔注射；每天一次，持续 9 天) 在 AML 小鼠异种移植模型中通过 m6A 介导的转录调控来抑制 AML 的进展[1]。

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

Animal Model: Female BALB/c nude mice subcutaneously injected with NB4 AML cells[1]
Dosage: 30 and 60 mg/kg
Administration: i.p.; daily for 9 days
Result: Significantly suppressed tumor growth in a dose-dependent manner. Showed no significant body weight loss or organ toxicity. Resulted in upregulation of tumor suppressors (RARA, ASB2) and downregulation of oncoproteins (CEBPA, c-Myc). Showed a marked increase in global RNA m6A modifications.
分子量

508.35

Formula

C23H23Cl2N3O6
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

FTO-IN-16 相关分类

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  • 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:

FTO-IN-16Fat Mass and Obesity-associated Protein (FTO)c-MycRAR/RXRApoptosisMycRetinoic acid receptorsRetinoid X receptorsNB4 MOLM13 MV4-11 HEL OCI-AML3 NOMO-1 KG-1 FTO AML mouse xenograftsInhibitorinhibitorinhibit

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