PHD2/HDACs-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PHD2/HDACs-IN-1 

PHD2/HDACs-IN-1 是一种有效的 PHD2/HDACs 混合抑制剂 (PHD2 和 HDAC1、 HDAC2、 HDAC16 的 IC50 分别为1.15 μM、19.75 μM、26.60 μM、15.98 μM)。PHD2/HDACs-IN-1 是一种低毒性肾保护剂，可用于研究顺铂诱导的急性肾损伤 (AKI)。

PHD2/HDACs-IN-1

PHD2/HDACs-IN-1 Chemical Structure

CAS No. : 2339867-53-5

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生物活性

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)[1].

IC50 & TargetWei 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)

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: MCF7 and A549[1]
Concentration: 50 μM
Incubation Time: 24 hours
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.

Cell Viability Assay

Cell Line: HK-2 cells[1]
Concentration: 0.78-100 μM
Incubation Time: 24 hours
Result: No evident inhibitions on HK-2 cell viabilities up to 100 μM dosing.

体内研究
(In Vivo)

PHD2/HDACs-IN-1 (10 mg/kg/day; i.p.; 2 days) has significant renal protecting effects on alleviating pathological injuries with considerably decreased tubular injury scores[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 mice (8 weeks; n=5) (Cisplatin-induced AKI)[1]
Dosage: 10 mg/kg/day
Administration: i.p., 2 days
Result: Showed significant renal protecting effects on alleviating pathological injuries with considerably decreased tubular injury scores.

分子量

425.40

Formula

C18H19N9O4
CAS 号

2339867-53-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wei H, et al. Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. Eur J Med Chem. 2022;230:114115.

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