2. Cell Cycle/DNA Damage
  3. Topoisomerase
  4. PNU-142586 sodium

PNU-142586 sodium 是 Linezolid (HY-10394) 的主要代谢产物。PNU-142586 可抑制 DNA 拓扑异构酶 2-α (TOP2A) 和 DNA 拓扑异构酶 2-β (TOP2B) 的活性。PNU-142586 通过阻断 DNA 与 TOP2 的结合并抑制 ATP 水解，干扰 DNA 的复制与转录，最终产生抗增殖和细胞毒性作用，包括线粒体功能障碍。PNU-142586 可用于研究利奈唑胺诱导的血液毒性及其分子机制。

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PNU-142586 sodium

PNU-142586 sodium Chemical Structure

CAS No. : 2468637-62-7

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Other Forms of PNU-142586 sodium:

PNU-142586 sodium 相关抗体

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Topoisomerase Topo I Topo II DNA gyrase

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PNU-142586 sodiu) is the major metabolite of Linezolid (HY-10394). PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis, ultimately leading to antiproliferative and cytotoxic effects, including mitochondrial dysfunction. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism[1].

IC50 & Target[1]

topoisomerase II alpha

 

topoisomerase II beta

 

体外研究
(In Vitro)

PNU-142586 sodium (0.1-2.5 mM; 30 min) 可在无细胞体系中强效抑制人源 TOP2A 介导的 kDNA 解连环作用，其 IC50 约为 150 μM[1]。
PNU-142586 sodium (0.1-2.5 mM; 30 min) 可在无细胞体系中抑制人 TOP2A 介导的 scDNA 松弛，其 IC50 约为 1.425 mM[1]。
PNU-142586 sodium (0.1-2.5 mM; 30 min) 可在无细胞体系中强效抑制人源 TOP2B 介导的 kDNA 解连环作用，其 IC50 约为 150 μM[1]。
PNU-142586 sodium (0.1-2.5 mM; 30 min) 在无细胞体系中抑制人源 TOP2B 介导的 scDNA 松弛，其 IC50 约为 1.875 mM[1]。
PNU-142586 sodium (31.25-500 μM) 可通过色氨酸荧光淬灭法检测到与人 TOP2A DNA 结合域直接结合，其 Kd 值为 310.6 ± 89.2 μM[1]。
PNU-142586 sodium (31.25-500 μM) 可通过色氨酸荧光淬灭法检测到直接结合人 TOP2A ATP 酶结构域，其 Kd 值为 300.8 ± 31.3 μM[1]。
PNU-142586 sodium (50 nM-100 μM; 144 hours) 可呈浓度依赖性抑制人 HL-60 早幼粒细胞的增殖，在 100 μM 作用 144 小时后，抑制率最高可达约 25%[1]。
PNU-142586 sodium (50 nM-100 μM; 144 h) 处理 144 h 后可在人 HL-60 早幼粒细胞和 THP-1 单核细胞中诱导浓度依赖性细胞毒性，并抑制增殖[1]。
PNU-142586 sodium (50 nM-100 μM; 0-120 h) 可在浓度 ≥5 μM、孵育时间 ≥48 h 时抑制人 HL-60 早幼粒细胞和 THP-1 单核细胞中线粒体 MT-CO1 基因的转录，基因和蛋白的表达[1]。

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

PNU-142586 sodium 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Human HL-60 promyelocytes, Human THP-1 monocytes
Concentration: 50, 500 nM, 5, 50, 100 μM
Incubation Time: 144 h
Result: Suppressed HL-60 and THP-1 cell proliferation in a concentration-dependent manner.

Real Time qPCR[1]

Cell Line: Human HL-60 promyelocytes, Human THP-1 monocytes
Concentration: 50, 500 nM, 5, 50, 100 μM
Incubation Time: 0-120 h
Result: Down-regulated MT-CO1 transcription at concentrations above 5 μM and after incubation periods of more than 48 h, with a more pronounced effect than Linezolid (HY-10394).

Western Blot Analysis[1]

Cell Line: Human HL-60 promyelocytes, Human THP-1 monocytes
Concentration: 50, 500 nM, 5, 50, 100 μM
Incubation Time: 0-120 h
Result: Suppressed MT-CO1 protein levels, with a more pronounced effect than Linezolid.
体内研究
(In Vivo)

PNU-142586 sodium (0.015625-1 mM; incubation; 168 h) 对 Xenopus laevis 卵母细胞具有剂量依赖性的形态学毒性，并抑制拓扑异构酶 II 介导的 kDNA 解连环作用；在 0.5 mM 浓度下，约 43% 的卵母细胞出现畸形[1]。
PNU-142586 sodium (0.0005-0.5 mM; incubation; from 24 hpf to 120 hpf) 会在斑马鱼胚胎中诱导剂量依赖性心包水肿，且在浓度 ≥0.5 μM 时会抑制线粒体 mt-co1 基因的表达[1]。

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

Animal Model: wild-type (female, V-VI X. laevis oocytes)[1]
Dosage: 0.015625 mM (5.77 mg/liter); 0.03125 mM (11.54 mg/liter); 0.0625 mM (23.08 mg/liter); 0.125 mM (46.17 mg/liter); 0.25 mM (92.34 mg/liter); 0.5 mM (184.67 mg/liter); 1 mM (369.34 mg/liter)
Administration: incubation; 168 h
Result: Induced a dose-dependent increase in oocyte malformation, with a ~43% malformation rate at 0.5 mM compared to no malformation in vehicle controls.
Dose-dependently inhibited kDNA decatenation activity in Xenopus oocyte extracts, with partial inhibition observed at 0.5 mM.
Animal Model: wild-type (embryos)[1]
Dosage: 0.0005 mM (0.18 mg/liter); 0.005 mM (1.85 mg/liter); 0.025 mM (9.23 mg/liter); 0.125 mM (46.17 mg/liter); 0.25 mM (92.34 mg/liter); 0.5 mM (184.67 mg/liter); ≥0.5 μM (0.19 mg/liter)
Administration: incubation; from 24 hpf to 120 hpf
Result: Induced a dose-dependent increase in pericardial edema in zebrafish embryos, with effects visible at 72 hpf and peaking at 96 hpf in the 0.125 to 0.25 mM groups.
Significantly down-regulated mt-co1 gene expression at both 72 and 120 hpf compared to vehicle controls, with stable expression levels between 72 and 120 hpf, at concentrations ≥0.5 μM.
分子量

391.33

Formula

C16H19FN3NaO6
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

PNU-142586 sodium 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

PNU-1425862468637-62-7PNU142586PNU 142586TopoisomeraseDNA topoisomerase inhibitorhuman THP-1 monocyteshuman TOP2AG2-M phase cell cycle arrestzebrafish embryoshuman HL-60 promyelocyteshuman TOP2BXenopus laevis oocyteshuman TOP1ATP hydrolysisInhibitorinhibitorinhibit

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