1. PROTAC Epigenetics Apoptosis
  2. PROTACs METTL3 Apoptosis Bcl-2 Family
  3. AF151

AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875)).

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AF151 Chemical Structure

AF151 Chemical Structure

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Description

AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875))[1].

IC50 & Target

Bcl-2

 

VHL

 

Mcl-1

 

In Vitro

AF151 (0-10 μM, 0-72 h) can efficiently degrade METTL3 protein in a time-dependent manner and significantly inhibit cell growth of MOLM-13 cells (DC50 = 0.43 μM, IC50 = 0.45 μM)[1].
AF151 (2 μM, 24-48 h) can significantly reduce m6A levels in MOLM-13 cells[1].
AF151 (0.1-5 μM, 48 h) can dose dependently induce cell apoptosis and reduce the level of anti apoptotic proteins in MOLM-13 cells[1].
AF151 (72 h) can work synergistically with Venetoclax (HY-15531) in MOLM-13 cells[1].
AF151 (0.001-10 μM) can promote the binding of METTL3 and VHL (AF151 = 363 nM, AF151-METTL3 = 79.9 nM)[1].

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

Cell Viability Assay[1]

Cell Line: MOLM-13 cells
Concentration: 0.1-10 μM
Incubation Time: 72 h
Result: Significantly inhibited cell growth with the IC50 of 0.45 μM, superior to STM2457 (HY-134836) (IC50 = 1.82 μM) and WD6305 (HY-160415) (IC50 = 0.78 μM).

Western Blot Analysis[1]

Cell Line: MOLM-13 cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Decreased the protein level of Mcl-1 and Bcl-2.

RT-PCR[1]

Cell Line: MOLM-13 cells
Concentration: 2 μM
Incubation Time: 24-48 h
Result: Did not cause significant changes in the expression of METTL3 and METTL14 genes.
Molecular Weight

1043.32

Formula

C61H70N8O6S

SMILES

CC1=C(C2=CC=C(CNC([C@H]3N(C([C@@H](NC(CCC4=CC=C(C5=CC=C(COC6=CN=CC(C(NCC7=CC(NC(CN8CCC(C)(C)CC8)=C9)=C9C=C7)=O)=C6)C=C5)C=C4)=O)C(C)(C)C)=O)C[C@H](O)C3)=O)C=C2)SC=N1

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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    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.

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AF151
Cat. No.:
HY-174873
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