Chemical Structure : DK-5070
货号: PC-27736Not For Human Use, Lab Use Only.
DK-5070 is a potent, selective UHRF1-recruiting degrader of GPX4 with DC50 of 17.4 nM, Dmax of 84% in in HT1080 cells (24 h).
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DK-5070 is a potent, selective UHRF1-recruiting degrader of GPX4 with DC50 of 17.4 nM, Dmax of 84% in in HT1080 cells (24 h).
DK-5070 induced pronounced GPX4 degradation following 24 h treatment at 50 nM.
DK-5070 (20 nM) achieved greater GPX4 degradation than dGPX4 at 200 nM.
DK-5070 exhibits antiproliferative activity against with IC50 of 47 nM in HT1080 cells.
DK-5070 induces rapid and durable GPX4 degradation via the ubiquitin-proteasome system.
DK-5070 covalently recruits UHRF1 to mediate the degradation of GPX4 via the proteasome pathway, enhances the GPX4-UHRF1 interaction with Kd of 1.02 uM.
DK-5070 suppresses cell proliferation primarily through GPX4 degradation-induced ferroptosis.
DK-5070 (10-30 mg/kg) significantly suppressed tumor growth in a dose-dependent manner in HT1080 xenograft mouse models.
| 分子量 | 532.44 | |
| 分子式 | C24H23Cl2N5O3S | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Lin Z, et al. Adv Sci (Weinh). 2026 Aug 19:e77201.
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