NCOA4 PROTAC V3 | NCOA4 PROTAC | Probechem Biochemicals

Chemical Structure : NCOA4 PROTAC V3

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NCOA4 PROTAC V3 (NCOA4 degrader V3)

货号: PC-22832Not For Human Use, Lab Use Only.

NCOA4 PROTAC V3 is a highly efficient VHL-based nuclear receptor coactivator 4 (NCOA4) PROTAC degrader (DC50=3 nM, HeLa cells) and potent ferroptosis inhibitor.

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生物&药学活性

NCOA4 PROTAC V3 is a highly efficient VHL-based nuclear receptor coactivator 4 (NCOA4) PROTAC degrader (DC50=3 nM, HeLa cells) and potent ferroptosis inhibitor.
NCOA4 PROTAC V3 induces the degradation of NCOA4 via the UPS system in HeLa cells.
NCOA4 PROTAC V3 exhibits a concentration-and time-dependent capacity to attenuate the intracellular levels of NCOA4 in AML12 cells, with a calculated DC50 of 202 nM.
NCOA4 PROTAC V3 upregulates FTH1 and FTL levels in AML12 cells in a concentration-dependent manner, with no significant changes in the mRNA levels of FTH1 and FTL.
NCOA4 PROTAC V3 inhibits ferritinophagy and thus reduces the intracellular ferrous iron (Fe2+) level, induces elevation of ferritin.
NCOA4 PROTAC V3 inhibits the ferroptosis induced by CCl4 in AML12 cells, and in livers of CCl4-induced mice acute liver injury model. ameliorated liver damage in a CCl4-induced acute liver injury model.

物理化学性质&存储条件

分子量	1141.44
分子式	C62H80N10O9S
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	N1-((R)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-N5-(2-(2-(2-(2-((2-(3-(6-(4-methylpiperazin-1-yl)-1H-benzo[d]imidazol-2-yl)phenyl)-1,2,3,4-tetrahydroisoquinolin-6-yl)oxy)ethoxy)ethoxy)ethoxy)ethyl)glutaramide

参考文献

1. Ji J, et al. J Med Chem. 2024 Jul 24. doi: 10.1021/acs.jmedchem.4c00403.

NCOA4 PROTAC V3 (NCOA4 degrader V3)

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NCOA4 PROTAC V3 (NCOA4 degrader V3)

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