1. Cell Cycle/DNA Damage
    Epigenetics
    Metabolic Enzyme/Protease
  2. HDAC
    HIF/HIF Prolyl-Hydroxylase
  3. PHD2/HDACs-IN-1

PHD2/HDACs-IN-1 

Cat. No.: HY-144332
Handling Instructions

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).

For research use only. We do not sell to patients.

PHD2/HDACs-IN-1 Chemical Structure

PHD2/HDACs-IN-1 Chemical Structure

CAS No. : 2339867-53-5

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Description

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)

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].

MCE 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.
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].

MCE 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.
Molecular Weight

425.40

Formula

C18H19N9O4

CAS No.
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PHD2/HDACs-IN-1
Cat. No.:
HY-144332
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