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PHD2/HDACs-IN-1
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
PHD2/HDACs-IN-1图片
CAS NO:2339867-53-5
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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)。
生物活性

PHD2/HDACs-IN-1 is a potentPHD2/HDACshybrid inhibitor (IC50s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2,HDAC1,HDAC2andHDAC6, 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].

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].

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.