2. Metabolic Enzyme/Protease Immunology/Inflammation GPCR/G Protein Apoptosis
  3. Fat Mass and Obesity-associated Protein (FTO) CXCR TNF Receptor
  4. FTO-IN-17

FTO-IN-17 is an orally active and brain-penetrant FTO (m6A RNA demethylase) inhibitor with an IC50 of 1.1 μM. FTO-IN-17 stably binds the FTO catalytic pocket. FTO-IN-17 protects against Aβ1-42-induced toxicity while increasing global m6A levels and dampening pro-inflammatory gene (CXCL10, TNF-α) expression. FTO-IN-17 ameliorates anxiety-like behavior and rescues hippocampal-dependent spatial, recognition memory and neuroinflammation in Alzheimer's disease mice models.

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FTO-IN-17

FTO-IN-17 Chemical Structure

CAS No. : 1434867-98-7

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FTO-IN-17 Related Antibodies

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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Description

FTO-IN-17 is an orally active and brain-penetrant FTO (m6A RNA demethylase) inhibitor with an IC50 of 1.1 μM. FTO-IN-17 stably binds the FTO catalytic pocket. FTO-IN-17 protects against Aβ1-42-induced toxicity while increasing global m6A levels and dampening pro-inflammatory gene (CXCL10, TNF-α) expression. FTO-IN-17 ameliorates anxiety-like behavior and rescues hippocampal-dependent spatial, recognition memory and neuroinflammation in Alzheimer's disease mice models[1].

In Vitro

FTO-IN-17 (Compound VI) exhibits high in vitro blood-brain barrier permeability (Pe = 12.2 × 10-6 cm/s)[1].
FTO-IN-17 (0.01-50 μM; overnight) potently inhibits human FTO demethylase activity with an IC50 of 1.1 μM[1].
FTO-IN-17 (10 μM; overnight) is fully selective for human FTO over human ALKBH5 demethylase, showing no inhibition of ALKBH5 at 10 μM[1].
The (S)-stereoisomer of FTO-IN-17 exhibits significantly stronger, more stable binding to human FTO than the (R)-stereoisomer, with over 7 times higher calculated binding affinity[1].
FTO-IN-17 (0.001-50 μM; 30 min pre-incubation + 24 h co-incubation) provides sustained, dose-dependent neuroprotection against Aβ1-42-induced toxicity in differentiated SH-SY5Y cells, increases global m6A levels, and downregulates pro-inflammatory gene expression at 1 μM[1].

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

FTO-IN-17 Related Antibodies

Cell Viability Assay[1]

Cell Line: differentiated SH-SY5Y human neuroblastoma cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 50 μM
Incubation Time: 30 min pre-incubation, followed by 24 h co-incubation with 5 μM Aβ1-42
Result: Demonstrated dose-dependent neuroprotection, with 70-85% cell viability at 0.1-10 μM.
Significantly increased global m6A RNA methylation levels compared to Aβ1-42-treated cells at 1 μM.
Significantly downregulated mRNA expression of pro-inflammatory genes CXCL10, TNF-α, and HMOX1 at 1 μM.
Parmacokinetics
Species Dose Route Cmax Tmax Cmax (Brain) Tmax (Brain) Brain-Kp
Mice[1] 3 mg/kg p.o. 51.3 ng/mL 5 min 29.9 ng/g 5 min 58 %
In Vivo

FTO-IN-17 (3 mg/kg; I.g.,; daily; 28 days) ameliorates anxiety-like behavior and rescues spatial and recognition memory deficits in Alzheimer's disease mice models, concomitant with increased brain m6A levels, normalized synaptic plasticity markers, and reduced neuroinflammation[1].

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

Animal Model: Alzheimer's disease model (SAMP8, 5-month-old female; sporadic Alzheimer's disease model)[1]
Dosage: 3 mg/kg
Administration: p.o.; daily; 28 days
Result: Significantly reduced anxiety-like behavior via decreased rearing and grooming in the open field test.
Rescued hippocampal-dependent spatial memory, with object location test discrimination index recovered to levels comparable to SAMR1 control mice.
Significantly increased both short-term and long-term recognition memory relative to SAMP8 control mice via novel object recognition test discrimination indices.
Increased global m6A methylation levels in brain tissue.
Upregulated expression of synaptic plasticity genes Arc and Egr1 in brain tissue.
Downregulated expression of neuroinflammatory genes Cxcl10, iNOS, and Hmox1 in brain tissue.
Molecular Weight

370.42

Formula

C20H23FN4O2
CAS No.
SMILES

CC(C1=NOC(C2CCCN(C2)CC3=NC4=C(C=CC=C4C(O)=C3)F)=N1)C
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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-17 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-171434867-98-7Fat Mass and Obesity-associated Protein (FTO)CXCRTNF ReceptorCXC chemokine receptorsC-X-C motif chemokine receptorsTumor Necrosis Factor ReceptorTNFRsynaptic markersSH-SY5Y cellshERGhuman FTOalzheimer's diseasepro-inflammatory gene expressionSAMP8 miceAβ1-42ALKBH5m6A RNA demethylaseInhibitorinhibitorinhibit

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