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

PNU-142586 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

PNU-142586

PNU-142586 構造式

CAS 番号 : 368891-70-7

容量 在庫状況
50 mg   お問い合わせ  
100 mg   お問い合わせ  
250 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

Other Forms of PNU-142586:

PNU-142586 関連抗体

Top Publications Citing Use of Products

Topoisomerase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Topoisomerase Topo I Topo II DNA gyrase

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

PNU-142586 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

 

体外実験

PNU-142586 (0.1-2.5 mM; 30 min) potently inhibits human TOP2A-mediated kDNA decatenation in a cell-free system with an IC50 of ~150 μM[1].
PNU-142586 (0.1-2.5 mM; 30 min) inhibits human TOP2A-mediated scDNA relaxation in a cell-free system with an IC50 of ~1.425 mM[1].
PNU-142586 (0.1-2.5 mM; 30 min) potently inhibits human TOP2B-mediated kDNA decatenation in a cell-free system with an IC50 of ~150 μM[1].
PNU-142586 (sodium) (0.1-2.5 mM; 30 min) inhibits human TOP2B-mediated scDNA relaxation in a cell-free system with an IC50 of ~1.875 mM[1].
PNU-142586 (31.25-500 μM) directly binds to the human TOP2A DNA binding domain with a Kd of 310.6 ± 89.2 μM, as measured by tryptophan fluorescence quenching[1].
PNU-142586 (31.25-500 μM) directly binds to the human TOP2A ATPase domain with a Kd of 300.8 ± 31.3 μM, as measured by tryptophan fluorescence quenching[1].
PNU-142586 (50 nM-100 μM; 144 hours) suppresses proliferation of human HL-60 promyelocytes in a concentration-dependent manner, with up to ~25% inhibition at 100 μM after 144 hours[1].
PNU-142586 (50 nM-100 μM; 144 h) induces concentration-dependent cytotoxicity and inhiibits proliferation in human HL-60 promyelocytes and THP-1 monocytes[1].
PNU-142586 (50 nM-100 μM; 0-120 h) suppresses mitochondrial MT-CO1 gene transcription, gene and protein expression in human HL-60 promyelocytes and and THP-1 monocytes at concentrations ≥5 μM and incubation times ≥48 h[1].

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

PNU-142586 関連抗体

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: 144 h
Result: Suppressed MT-CO1 protein levels, with a more pronounced effect than Linezolid.
体内実験

PNU-142586 (0.015625-1 mM; incubation; 168 h) induces dose-dependent morphological toxicity in Xenopus laevis oocytes and inhibits topoisomerase II-mediated kDNA decatenation, with ~43% of oocytes showing malformation at 0.5 mM[1].
PNU-142586 (0.0005-0.5 mM; incubation; from 24 hpf to 120 hpf) induces dose-dependent pericardial edema in Danio rerio embryos and suppresses mitochondrial mt-co1 gene expression at concentrations ≥0.5 μM[1].

MedChemExpress (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: 0.125 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)
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

369.34

分子式

C16H20FN3O6
CAS 番号
SMILES

O=C(CN(CCO)C1=CC=C(C=C1F)N2C(O[C@H](C2)CNC(C)=O)=O)O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

PNU-142586 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PNU-142586368891-70-7PNU142586PNU 142586TopoisomeraseLZDTOP2ATOP2BHL-60 cellsTHP-1 cellsCYP450Inhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
PNU-142586
製品番号:
HY-123393
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.