PROTAC sEH degrader-4
PROTAC sEH degrader-4 is a highly efficient PROTAC degrader that targets soluble epoxide hydrolase (sEH) (pDC50 = 10.3). PROTAC sEH degrader-4 can be used for research on inflammation-related diseases.
(Pink: sEH ligand (HY-179169); Blue: Cereblon ligand (HY-179168); Black: linker).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C45H49F3N10O8
- 分子量:914.93
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
体外実験
PROTAC sEH degrader-4 (Compound P4) (300 nM, 18 h) exhibits extreme degradation activity, with a pDC50 of 10.3 after 18 hours of incubation and a maximum degradation efficiency (Dmax = 96 %) in HeLa cells stably overexpressing the sEH-HiBiT fusion protein (HeLasEH-HiBiT). Significant degradation is also observed after a shorter incubation period of 6 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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分子量 914.93
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分子式 C45H49F3N10O8
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SMILES
O=C(NCCCC1=CN(CCN2CCN(C3=CC4=C(C(N(C(CC5)C(NC5=O)=O)C4=O)=O)C=C3)CC2)N=N1)C6=CC=C(O[C@H]7CC[C@H](NC(NC8=CC=C(OC(F)(F)F)C=C8)=O)CC7)C=C6
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)