FTO-IN-5
FTO-IN-5 is a potent and selective FTO inhibitor, with an IC50 of 0.087 μM for FTO demethylase activity and a Kd of 28.0 nM for direct binding to FTO. The IC50 of FTO-IN-5 for ALKBH5 is 8.98 μM. FTO-IN-5 can be used in studies related to FTO demethylase activity and cancer.
For research use only. We do not sell to patients.
- CAS No.: 2763577-75-7
- Formula: C23H18Cl2N6O6
- Molecular Weight:545.33
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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]|
FTO 0.087 μM (IC50) |
FTO 28 μM (Kd) |
ALKBH5 8.98 μM (IC50) |
In Vitro
FTO-IN-5 (compound 11b) (50 μM) inhibits FTO demethylase activity by 94% in an in vitro HPLC enzymatic activity assay[1].
FTO-IN-5 inhibits FTO demethylase activity in a dose-dependent manner, with an IC50 of 0.087 μM[1].
FTO-IN-5 directly binds to FTO in ITC assays, with a Kd of 28.0 nM[1].
FTO-IN-5 inhibits the demethylase activity of ALKBH5 with an IC50 of 8.98 μM; its selectivity index for FTO relative to ALKBH5 is 103[1].
FTO-IN-5 (10 μM) does not inhibit KDM4C, whereas the control compound 2,4-PDCA (HY-W017132) (10 μM) exhibits an inhibition rate of 49% against KDM4C, which further supports the FTO selectivity of FTO-IN-5[1].
FTO-IN-5 exerts a minor effect on cell growth in NOMO-1 acute monocytic leukemia cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 2763577-75-7
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Molecular Weight 545.33
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Formula C23H18Cl2N6O6
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SMILES
OC(/C=C/C(NNC(C1=CN=CC=C1NC(C=C2Cl)=C(C)C(Cl)=C2NC3=CC=CC=C3[N+]([O-])=O)=O)=O)=O
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FTO-IN-5 Related Classifications
HY-139821 Related Classifications
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