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

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)。

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PHD2/HDACs-IN-1 Chemical Structure

PHD2/HDACs-IN-1 Chemical Structure

CAS No. : 2339867-53-5

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PHD2/HDACs-IN-1 相关抗体

Top Publications Citing Use of Products

查看 HDAC 亚型特异性产品:

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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HIF-1α HIF

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PHD2/HDACs-IN-1 相关抗体:

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].

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.
分子量

425.40

Formula

C18H19N9O4
CAS 号
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.
纯度 & 产品资料
参考文献

PHD2/HDACs-IN-1 相关分类

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Keywords:

PHD2/HDACs-IN-12339867-53-5HDACHIF/HIF Prolyl-HydroxylaseHistone deacetylasesHypoxia-inducible factorsHIFsHIF-PHAcute kidney injuryRenal protectingCancerHDACsPHD2Hybrid inhibitorInhibitorinhibitorinhibit

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