PROTAC GPX4 degrader-1

• CAT Number: I041191
• CAS Number: 2916433-81-1
• Molecular Formula: C50H57ClN10O10
• Molecular Weight: 993.50
• Purity: ≥95%
• Synonyms: 4-[3-[4-[[1-[2-[4-[(4-chlorophenyl)-[4-(5-methyl-4-nitro-1,2-oxazole-3-carbonyl)piperazin-1-yl]methyl]phenoxy]acetyl]piperidin-4-yl]methyl]piperazin-1-yl]propylamino]-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
• InChI: InChI=1S/C50H57ClN10O10/c1-32-45(61(68)69)44(54-71-32)50(67)59-28-26-58(27-29-59)46(34-6-10-36(51)11-7-34)35-8-12-37(13-9-35)70-31-42(63)57-20-16-33(17-21-57)30-56-24-22-55(23-25-56)19-3-18-52-39-5-2-4-38-43(39)49(66)60(48(38)65)40-14-15-41(62)53-47(40)64/h2,4-13,33,40,46,52H,3,14-31H2,1H3,(H,53,62,64)
• InChIKey: HMSNFNLFZRKDIO-UHFFFAOYSA-N
• SMILES: CC1=C(C(=NO1)C(=O)N2CCN(CC2)C(C3=CC=C(C=C3)OCC(=O)N4CCC(CC4)CN5CCN(CC5)CCCNC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O)C9=CC=C(C=C9)Cl)[N+](=O)[O-]

PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC50 of 0.03 μM in HT1080 cells[1].
PROTAC GPX4 degrader-1 (DC-2) has been found to induce GPX4 degradation and subsequent ferroptosis[1].

Reference

[1]. Han Wang, et al. Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells. Eur J Med Chem. 2023 Jun 5;254:115343.
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