KY0418 | GPX4 inhibitor | Probechem Biochemicals

Chemical Structure : KY0418

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KY0418 (KY-0418)

货号: PC-28747Not For Human Use, Lab Use Only.

KY0418 is a specific covalent and orally bioavailable inhibitor of glutathione peroxidase 4 (GPX4) with inhibitory constant (Ki) of 0.3 uM, specifically targets GPX4SeCys46 to induce ferroptosis.

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生物&药学活性

KY0418 is a specific covalent and orally bioavailable inhibitor of glutathione peroxidase 4 (GPX4) with inhibitory constant (Ki) of 0.3 uM, specifically targets GPX4SeCys46 to induce ferroptosis.
KY0418 strongly suppressed the activity of purified GPX4-mediated reduction of tert-butyl hydroperoxide (TBHP) or cumene hydroperoxide in vitro.
KY0418 targets GPX4SeCys46 with superior selectivity over established covalent inhibitors.
KY0418 demonstrates near-nanomolar potency in most CCLs, fully rescued by Lip-1 and deferoxamine (DFO).
KY0418 shows strong cytotoxicity in mouse cancer cells, including MC-38 from the colorectum, 4T1 from breast, a T cell lymphoma EL4 line, and Lewis lung carcinoma (LLC1) cells in 2-D and 3-D cultures.
KY0418 also triggers GPX4 destabilization and degradation in CCLs, ensuring irreversible GPX4 blockade.
KY0418 acutely induces hallmarks of ferroptosis in ML210-pv-ALI model.
KY0418 remodels tissue metabolism in vivo via GPX4 inhibition, and a hydroxyl radical probe reports ferroptosis ex vivo.
KY0418 suppresses bulk tumor growth variably and kills CTCs in MC-38 subcutaneous allografts mouse models.

物理化学性质&存储条件

分子量	588.62
分子式	C28H35F3N8O3
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	(4'-amino-7'-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-6'-oxo-6',7'-dihydrospiro[cyclopentane-1,5'-pyrrolo[2,3-d]pyrimidin]-2'-yl)methyl (R)-2-(trifluoromethyl)pyrrolidine-1-carbimidate

参考文献

1. Naowarojna N, et al. Cell. 2026 Oct 21:S0092-8674(26)01200-6.

KY0418 (KY-0418)

生物&药学活性

物理化学性质&存储条件

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KY0418 (KY-0418)

生物&药学活性

物理化学性质&存储条件

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