AF151 | METTL3 PROTAC | Probechem Biochemicals

Chemical Structure : AF151

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AF151 (AF-151)

货号: PC-28783Not For Human Use, Lab Use Only.

AF151 is a potent, efficient, VHL-based METTL3 PROTAC degrader with DC50 of 430 nM in AML cell line MOLM-13, Dmax=95%.

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生物&药学活性

AF151 is a potent, efficient, VHL-based METTL3 PROTAC degrader with DC50 of 430 nM in AML cell line MOLM-13, Dmax=95%.
AF151 induces rapid METTL3 degradation, achieving over 50% METTL3 reduction within the first 6 h of treatment, reaching maximal effect at 24 h, and maintaining it for at least 48 h.
AF151 binds to the SAM-binding site of METTL3, shows high VHL affinity with KD of 363 nM.
AF151 is able to form a stable ternary complex between VHL and METTL3, exhibiting positive cooperativity and effectively reducing METTL3 levels in MOLM-13 cells in a concentration-, time-, and UPS-dependent manner.
AF151 reduces cell viability with IC50 of 0.45 uM in MOLM-13 cells, effectively promotes apoptosis in cancer cell lines, induces pronounced m6A reduction than the competitive inhibitor STM245.
AF151 is sensitizing MOLM-13 cells for treatment with venetoclax as the apoptosis-inducing effector, possibly by downregulation of Bcl-2 family proteins.

物理化学性质&存储条件

分子量	1043.34
分子式	C61H70N8O6S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-((2-((4,4-dimethylpiperidin-1-yl)methyl)-1H-indol-6-yl)methyl)-5-((4'-(3-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-3-oxopropyl)-[1,1'-biphenyl]-4-yl)methoxy)nicotinamide

参考文献

1. Weldert AC, et al. RSC Med Chem. 2025 Jun 19;16(9):4194-4207.

AF151 (AF-151)

生物&药学活性

物理化学性质&存储条件

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AF151 (AF-151)

生物&药学活性

物理化学性质&存储条件

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