FTO-IN-18
FTO-IN-18 is a selective FTO inhibitor with an IC50 of 5.3 µM and a Kd of 3.25 µM. FTO-IN-18 increases global m6A modification levels, upregulates ASB2 and RARA expression, inhibits c-Myc expression, and induces Apoptosis. FTO-IN-18 inhibits the growth of acute myeloid leukemia xenograft tumors in mice.
For research use only. We do not sell to patients.
- CAS No.: 3144292-81-6
- Formula: C15H12N4O2
- Molecular Weight:280.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
RARA |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | IC50 |
6.9 μM
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Antiproliferative activity against human MOLM-13 cells assessed as viability reduction incubated 48 hrs and measured by CCK-8 assay.
Antiproliferative activity against human MOLM-13 cells assessed as viability reduction incubated 48 hrs and measured by CCK-8 assay.
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42911701 |
| THP-1 | IC50 |
3.7 μM
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Antiproliferative activity against human THP-1 cells assessed as viability reduction incubated 48 hrs and measured by CCK-8 assay.
Antiproliferative activity against human THP-1 cells assessed as viability reduction incubated 48 hrs and measured by CCK-8 assay.
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42911701 |
| MV4-11 | IC50 |
10.3 μM
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Antiproliferative activity against human MV4-11 cells assessed as viability reduction incubated 48 hrs and measured by CCK-8 assay.
Antiproliferative activity against human MV4-11 cells assessed as viability reduction incubated 48 hrs and measured by CCK-8 assay.
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42911701 |
In Vitro
FTO-IN-18 (10 µM; 6 h) stabilizes FTO protein in MOLM-13 cells[1].
FTO-IN-18 (1-100 µM) protects wild-type FTO, but not the S229A/K216A/P93A mutant, from Pronase-mediated proteolysis in MOLM-13 lysates[1].
FTO-IN-18 (2.5-10 µM) increases global m6A abundance in MOLM-13 and THP-1 AML cells[1].
FTO-IN-18 (2.5-10 µM; 48 h) upregulates ASB2 and RARA and downregulates c-Myc protein in MOLM-13 cells[1].
FTO-IN-18 (2.5-10 µM) upregulates ASB2 and RARA mRNA and downregulates c-Myc mRNA in MOLM-13 cells[1].
FTO-IN-18 binds wild-type FTO with a KD of 3.25 µM but does not bind the S229A/K216A/P93A mutant[1].
FTO-IN-18 (below 100 µM) shows selectivity over ALKBH3 and ALKBH5[1].
FTO-IN-18 has moderate CYP2D6 inhibitory activity (IC50 14.1 µM) and negligible inhibition of CYP1A2, CYP2C9, CYP2C19, and CYP3A4/5[1].
FTO-IN-18 (2 µM; 120 min) is highly permeable in Caco-2 monolayers with low P-gp-mediated efflux liability[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLM-13, THP-1, and MV4-11
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Concentration:Varying concentrations
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Incubation Time:48 h; 2 h (CCK-8 at 37 °C)
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Result:Proliferation IC50 values were 6.9 µM for MOLM-13, 3.7 µM for THP-1, and 10.3 µM for MV4-11.
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Cell Line:MOLM-13 cells
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Concentration:2.5, 5, and 10 µM
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Incubation Time:48 h
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Result:ASB2 and RARA protein levels were dose-dependently upregulated, and c-Myc protein was reduced.
GAPDH was used as the loading control.
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Cell Line:MOLM-13 cells
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Concentration:2.5, 5, and 10 µM
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Incubation Time:24 h
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Result:At 2.5 µM, Q1 was 0.29%, Q2 was 2.08%, Q3 was 10.5%, and Q4 was 87.1%.
At 5 µM, Q1 was 0.28%, Q2 was 4.18%, Q3 was 16.0%, and Q4 was 79.5%.
At 10 µM, Q1 was 0.16%, Q2 was 10.4%, Q3 was 22.0%, and Q4 was 67.4%.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 5-7 weeks old)[1]
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Dosage:20 mg/kg; 40 mg/kg; 80 mg/kg
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Administration:i.p.; once daily; 14 days
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Result:Tumor growth was reduced dose-dependently compared with vehicle, shown by decreased tumor volume over the study period and lower tumor weight at sacrifice.
At 80 mg/kg, a tumor growth inhibition rate of 51% was achieved.
Representative excised tumors showed dose-dependent size reduction.
In tumor tissues, ASB2 and RARA expression increased and c-Myc expression decreased by Western blot.
Immunohistochemical staining showed reduced c-Myc and Ki-67 signals at 20, 40, and 80 mg/kg.
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 3144292-81-6
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Molecular Weight 280.28
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Formula C15H12N4O2
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SMILES
O=C(NC1=NN=CC=C1)C2=CN=C(C3=CC=C(C)O3)C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FTO-IN-18 Related Classifications
HY-190752 Related Classifications
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