Chemical Structure : DEL-I25
CAS No.:
3036889-54-7
DEL-I25
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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393.45
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Formula
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C21H23N5O3
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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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3-(5-aminopyridin-2-yl)-N-(1-(2-(1-oxoisoindolin-2-yl)acetyl)azetidin-3-yl)propanamide
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References
1. Liu H, et al. ACS Chem Biol. 2025 May 5. doi: 10.1021/acschembio.5c00158.
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