DEL-I25 | GPX4 R152H activator | Probechem Biochemicals

Chemical Structure : DEL-I25

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DEL-I25 (DEL I25)

货号: PC-24537Not For Human Use, Lab Use Only.

DEL-I25 is a selective, small molecule activator of GPX4 R152H variant, selectively binds to GPX4 R152H (MST binding KD, 2 uM), restores GPX4R152H enzyme activity, and specifically rescues patient-derived lymphoblast cells.

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生物&药学活性

DEL-I25 is a selective, small molecule activator of GPX4 R152H variant, selectively binds to GPX4 R152H (MST binding KD, 2 uM), restores GPX4R152H enzyme activity, and specifically rescues patient-derived lymphoblast cells.
DEL-I25 shows little to no actiivty against GPX4 WT (MST KD, >100 uM)
DEL-I25 can boost the viability of patient lymphoblast RAG03 to 520%, with EC50 of 2 uM.
DEL-I25 (100 uM) fully restores the enzymatic activity of GPX4R152H to 96% of GPX4WT.
At the concentration of EC100 (10 μM), DEL-I25 is more therapeutically effective than general antioxidants α-tocopherol and CoQ10.
DEL-I25 can stabilize the G-loop in GPX4R152H, which contains residue W136 essential for GPX4 enzymatic activity and is disordered by the R152H mutation.

物理化学性质&存储条件

分子量	393.45
分子式	C21H23N5O3
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	3-(5-aminopyridin-2-yl)-N-(1-(2-(1-oxoisoindolin-2-yl)acetyl)azetidin-3-yl)propanamide

参考文献

1. Liu H, et al. ACS Chem Biol. 2025 May 5. doi: 10.1021/acschembio.5c00158.

DEL-I25 (DEL I25)

生物&药学活性

物理化学性质&存储条件

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DEL-I25 (DEL I25)

生物&药学活性

物理化学性质&存储条件

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