2. PROTAC Metabolic Enzyme/Protease Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. PROTACs Fat Mass and Obesity-associated Protein (FTO) Apoptosis Caspase PARP YTHDF
  4. 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). (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))

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PROTAC FTO degrader 1

PROTAC FTO degrader 1 Chemical Structure

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PROTAC FTO degrader 1 Related Antibodies

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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YTHDF1 YTHDF3 YTHDF2 YTHDC1 YTHDC2

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Description

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)[1]. (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))

IC50 & Target[1]

VHL

 

PARP1

 

Caspase 3

 

YTHDF2

 

In Vitro

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.

PROTAC FTO degrader 1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MOLM-13 and NB4 cells
Concentration: 2 and 5 μM
Incubation Time: 48 h
Result: Increased apoptotic cells.
Induced cleavage of caspase-3 and PARP1.
In Vivo

PROTAC FTO degrader 1 (Compound FP54) (25 mg/kg, i.v., 3 times a week) delays disease onset, and prolongs survival in MA9.3Ras/ MOLM13/AML-0148 tumor mice models[1].

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

Animal Model: MA9.3Ras/ MOLM13/AML-0148 tumor mice models[1]
Dosage: 25 mg/kg
Administration: Intraperitoneally injection, 3 times a week
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.
Molecular Weight

1173.25

Formula

C59H75Cl2N9O10S
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
Shipping

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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PROTAC FTO degrader 1 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:

PROTAC FTO degrader 1PROTAC FTO degrader1PROTAC FTO degrader-1PROTACsFat Mass and Obesity-associated Protein (FTO)ApoptosisCaspasePARPYTHDFpoly ADP ribose polymerase (YTH) domain-containing family proteins (YTHDF)PROTACFTOYTHDF2AMLNB4MOLM-13,ApoptosisMA9.3RasMOLM13AML-0148Inhibitorinhibitorinhibit

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