PHD2/HDACs-IN-1

立即咨询

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。

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.