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 is a potent PHD2 / HDACs hybrid inhibitor ( IC 50 s 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].

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.

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.

2339867-53-5

C18H19N9O4

425.4

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years