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.
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- CAS No.: 2763577-75-7
- Formule: C23H18Cl2N6O6
- Masse moléculaire:545.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Help & FAQs
Activité biologique
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.
Chemical Information
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CAS No. 2763577-75-7
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Masse moléculaire 545.33
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FTO-IN-5 Related Classifications
HY-139821 Related Classifications
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