Chemical Structure : NCOA4 PROTAC V3
CAS No.:
NCOA4 PROTAC V3
(NCOA4 degrader V3)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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1141.44
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Formula
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C62H80N10O9S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Ji J, et al. J Med Chem. 2024 Jul 24. doi: 10.1021/acs.jmedchem.4c00403.
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