PHD2/HDACs-IN-1
PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI).
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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。
- CAS 番号: 2339867-53-5
- 分子式: C18H19N9O4
- 分子量:425.40
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
Wei H, et al. Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. Eur J Med Chem. 2022;230:114115.|
HDAC1 19.75 μM (IC50) |
HDAC2 26.60 μM (IC50) |
HDAC6 15.98 μM (IC50) |
PHD2 1.15 μM (IC50) |
体外実験
PHD2/HDACs-IN-1 (compound 31c) (50 μM; 24 hours) and cisplatin co-treatment can further downregulate the MCF7 and A549 cell viability compared to the treatment of cisplatin alone[1].
PHD2/HDACs-IN-1 (0.78-100 μM; 24 hours) has no evident inhibitions on HK-2 cell viabilities up to 100 μM dosing[1].
PHD2/HDACs-IN-1 (50 μM; 24 hours) not only has potent protective activity against cisplatin-induced inhibition for normal renal tubule epithelial cells without observable toxicities[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MCF7 and A549[1]
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Concentration:50 μM
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Incubation Time:24 hours
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Result:The combination treatment of PHD2/HDACs-IN-1 and cisplatin could further downregulate the MCF7 and A549 cell viability compared to the treatment of cisplatin alone.
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Cell Line:HK-2 cells[1]
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Concentration:0.78-100 μM
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Incubation Time:24 hours
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Result:No evident inhibitions on HK-2 cell viabilities up to 100 μM dosing.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (8 weeks; n=5) (Cisplatin-induced AKI)[1]
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Dosage:10 mg/kg/day
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Administration:i.p., 2 days
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Result:Showed significant renal protecting effects on alleviating pathological injuries with considerably decreased tubular injury scores.
化学情報
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CAS 番号 2339867-53-5
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分子量 425.40
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分子式 C18H19N9O4
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SMILES
O=C(C1=CN=C(N2CCC(NC(C3=CN=C(N4N=CC=C4)NC3=O)=O)CC2)N=C1)NO
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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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Nephrotoxicity Study
This protocol assesses nephrotoxicity by combining functional kidney injury readouts, urinary/tissue injury biomarkers, and renal histopathology. Serum creatinine and BUN reflect impaired kidney function, while KIM-1, NGAL, clusterin, osteopontin, IL-18, cystatin C, nephrin, Oat5, urinary protein, glucose, and alkaline phosphatase have been used to detect tubular injury in cisplatin-, gentamicin-, and acetaminophen-induced nephrotoxicity models.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
PHD2/HDACs-IN-1 関連分類
HY-144332 関連分類
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