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 (Compound 8a-1), 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.

For research use only. We do not sell to patients.

FTO-IN-16

FTO-IN-16 Chemical Structure

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FTO-IN-16 Related Antibodies

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Description

FTO-IN-16 (Compound 8a-1), 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].

In Vitro

FTO-IN-16 (0-8 μM; 48 h) downregulates c-Myc and CEBPA (protein and mRNA), and upregulates ASB2 and RARA in multiple AML cells (NB4, MOLM13, MV4-11, HEL, OCI-AML3, NOMO-1, KG-1)[1].
FTO-IN-16 (0-20 μM; 48 h) induces dose-dependent apoptosis in NB4 cells[1].
FTO-IN-16 (0-8 μM; 48 h) downregulates c-Myc and CEBPA (protein and mRNA), and upregulates ASB2 and RARA in multiple AML cells (NB4, MOLM13, MV4-11, HEL, OCI-AML3, NOMO-1, KG-1)[1].
FTO-IN-16 (72 h) exhibits potent antileukemic activity across a panel of AML cell lines, with IC50 values of 5.5 (NB4), 2.3 (MOLM13), 4.4 (KG-1), 3.6 (MV4-11), 4.6 (HEL), 5.2 (OCI-AML3), and 4.7 μM (NOMO-1), respectively[1].

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

FTO-IN-16 Related Antibodies

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.
In Vivo

FTO-IN-16 (30 and 60 mg/kg; i.p.; daily for 9 days) impairs AML progression through m6A-mediated transcriptional regulation in an AML mouse xenograft model[1].

MedChemExpress (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.
Molecular Weight

508.35

Formula

C23H23Cl2N3O6
SMILES

O=C(C1=CC=CC=C1NC2=C(C=C(C=C2Cl)C(NCCNC(/C=C/C(OCC)=O)=O)=O)Cl)OC
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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FTO-IN-16 Related Classifications

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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:

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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