| Identification | Back Directory | [Name]
5-Pyrimidinecarboxamide, 2-[4-[[[1,6-dihydro-6-oxo-2-(1H-pyrazol-1-yl)-5-pyrimidinyl]carbonyl]amino]-1-piperidinyl]-N-hydroxy- | [CAS]
2339867-53-5 | [Synonyms]
PHD2/HDACs-IN-1
5-Pyrimidinecarboxamide, 2-[4-[[[1,6-dihydro-6-oxo-2-(1H-pyrazol-1-yl)-5-pyrimidinyl]carbonyl]amino]-1-piperidinyl]-N-hydroxy- | [Molecular Formula]
C18H19N9O4 | [MOL File]
2339867-53-5.mol | [Molecular Weight]
425.4 |
| Hazard Information | Back Directory | [Uses]
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]. | [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. |
| [IC 50]
HDAC1: 19.75 μM (IC50); HDAC2: 26.60 μM (IC50); HDAC6: 15.98 μM (IC50); PHD2: 1.15 μM (IC50) | [References]
[1] Wei H, et al. Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury. Eur J Med Chem. 2022;230:114115. DOI:10.1016/j.ejmech.2022.114115 |
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