PROTAC FTO degrader 1
PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m6A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML).
(Pink: Fat Mass and Obesity-associated Protein (FTO) ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042)).
For research use only. We do not sell to patients.
- Formula: C59H75Cl2N9O10S
- Molecular Weight:1173.25
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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VHL |
PARP1 |
Caspase 3 |
YTHDF2 |
PROTAC FTO degrader 1 (Compound FP54) (0.08-2.5 μM, 48 h) degrades FTO in a dose-dependent manner in NB4 and MOLM-13 cells with a maximum degradation rate (Dmax) > 95%[1].
PROTAC FTO degrader 1 inhibits proliferation in various AML cell lines with IC50 values of 0.48-2.44 μM[1].
PROTAC FTO degrader 1 (2-5 μM, 48 h) significantly induces apoptosis in MOLM-13 and NB4 cells[1].
PROTAC FTO degrader 1 (5 μM) promotes cell differentiation in MOLM-13 cells[1].
PROTAC FTO degrader 1 (2 μM, 48 h) increases the global mRNA m6A modification level in NB4 cells[1].
PROTAC FTO degrader 1 (2 μM, 48 h) reduces the polysome/80S monosome ratio and inhibits global translation in MOLM-13 cells[1].
PROTAC FTO degrader 1 (2 μM) enriches ribosome biogenesis-related mRNAs such as MRPL36 and LYAR in YTHDF2, reduces their mRNA stability, and promotes YTHDF2-mediated degradation in MOLM-13 cells[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 and NB4 cells
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Concentration:2 and 5 μM
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Incubation Time:48 h
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Result:Increased apoptotic cells.
Induced cleavage of caspase-3 and PARP1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MA9.3Ras/ MOLM13/AML-0148 tumor mice models[1]
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Dosage:25 mg/kg
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Administration:Intraperitoneally injection, 3 times a week
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Result:Reduced AML cell engraftment in peripheral blood and bone marrow.
Decreased leukemia burden and delayed disease onset.
Prolonged survival.
Showed no obvious toxicity to mouse body weight, blood routine, or major organs.
Chemical Information
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Molecular Weight 1173.25
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Formula C59H75Cl2N9O10S
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SMILES
CC(C(OCOC(C1=C(C=CC=C1NC(C(Cl)=CC(C(C(C)=NO2)=C2C)=C3)=C3Cl)N4CCN(CC(NCCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@H](O)C[C@H]5C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)=O)=O)CC4)=O)=O)C
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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)
PROTAC FTO degrader 1 Related Classifications
HY-175885 Related Classifications
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