PHD2/HDACs-IN-1
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.
- CAS No.: 2339867-53-5
- Formula: C18H19N9O4
- Molecular Weight:425.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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HDAC1 19.75 μM (IC50) |
HDAC2 26.60 μM (IC50) |
HDAC6 15.98 μM (IC50) |
PHD2 1.15 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 and A549[1]
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Concentration:50 μM
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Incubation Time:24 hours
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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.
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Cell Line:HK-2 cells[1]
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Concentration:0.78-100 μM
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Incubation Time:24 hours
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Result:No evident inhibitions on HK-2 cell viabilities up to 100 μM dosing.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (8 weeks; n=5) (Cisplatin-induced AKI)[1]
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Dosage:10 mg/kg/day
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Administration:i.p., 2 days
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Result:Showed significant renal protecting effects on alleviating pathological injuries with considerably decreased tubular injury scores.
Chemical Information
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CAS No. 2339867-53-5
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Molecular Weight 425.40
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Formula C18H19N9O4
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SMILES
O=C(C1=CN=C(N2CCC(NC(C3=CN=C(N4N=CC=C4)NC3=O)=O)CC2)N=C1)NO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)