Chemical Structure : 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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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.
分子量 | 393.45 | |
分子式 | C21H23N5O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Liu H, et al. ACS Chem Biol. 2025 May 5. doi: 10.1021/acschembio.5c00158.
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