2. Cell Cycle/DNA Damage Epigenetics Metabolic Enzyme/Protease
  3. PARP Pyruvate Kinase
  4. PARP1/PKM2-IN-1

PARP1/PKM2-IN-1 is a dual PARP1/PKM2 inhibitor, with an IC50 of 39.5 nM against PARP1, and IC50 values of 261 nM (recombinant PKM2) and 50 nM (dimeric PKM2) against PKM2. PARP1/PKM2-IN-1 reduces the dimerization of PKM2 and decreases its nuclear accumulation level. PARP1/PKM2-IN-1 also selectively downregulates PKM2 mRNA and impairs poly (ADP-ribose)-mediated nuclear retention of PKM2. PARP1/PKM2-IN-1 exhibits antiproliferative activity and inhibits the formation of 3D cancer spheroids. PARP1/PKM2-IN-1 can be used in research related to mammary adenocarcinoma, triple-negative breast cancer, BRCA1-mutant triple-negative breast cancer, and prostate adenocarcinoma.

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。

PARP1/PKM2-IN-1

PARP1/PKM2-IN-1 構造式

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.

PARP1/PKM2-IN-1 関連抗体

Top Publications Citing Use of Products

PARP 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
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 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

PARP1/PKM2-IN-1 is a dual PARP1/PKM2 inhibitor, with an IC50 of 39.5 nM against PARP1, and IC50 values of 261 nM (recombinant PKM2) and 50 nM (dimeric PKM2) against PKM2. PARP1/PKM2-IN-1 reduces the dimerization of PKM2 and decreases its nuclear accumulation level. PARP1/PKM2-IN-1 also selectively downregulates PKM2 mRNA and impairs poly (ADP-ribose)-mediated nuclear retention of PKM2. PARP1/PKM2-IN-1 exhibits antiproliferative activity and inhibits the formation of 3D cancer spheroids. PARP1/PKM2-IN-1 can be used in research related to mammary adenocarcinoma, triple-negative breast cancer, BRCA1-mutant triple-negative breast cancer, and prostate adenocarcinoma[1].

IC50 & Target[1]

PARP1

39.5 nM (IC50)

PKM2

261 nM (IC50)

体外実験

PARP1/PKM2-IN-1 (compound 9f) binds to purified PKM2 protein via a conformational change binding model, with a dissociation constant Kd of 0.71 μM[1].
PARP1/PKM2-IN-1, a mixed inhibitor against purified PKM2, has a Ki value of 481 nM[1].
PARP1/PKM2-IN-1 (0.1-5 μM) induces a dose-dependent shift in the oligomer distribution of purified 50 nM PKM2, reducing dimers and increasing trimers and tetramers; in the presence of FBP in vitro, it reduces dimers and increases trimers without altering tetramer levels[1].
PARP1/PKM2-IN-1 (2 μM; 24 h) exhibits a better inhibitory effect on nuclear PKM2 aggregation than Olaparib (HY-10162) in CoCl2-stimulated 4T1 cells, and reduces the size of nuclear PAR aggregates by inhibiting PARP1 activity[1].
PARP1/PKM2-IN-1 (0.25-0.5 μM; 24 h) reduces PKM2 mRNA expression in a dose-dependent manner in 4T1 and HCC1937 cells without affecting the level of PKM1 mRNA[1].
PARP1/PKM2-IN-1 inhibits the proliferation of 4T1, HCC1937, MCF-7, MDA-MB-231 and PC-3 cancer cell lines in 2D culture systems, with IC50 values ranging from 3.19 μM to 4.57 μM[1].
PARP1/PKM2-IN-1 (0-12.5 μM; 72 h) inhibits the formation of 4T1 cancer spheroids with an IC50 of 3.83 μM; it also inhibits the viability of pre-formed spheroids with an IC50 of 4.72 μM, and a concentration of 12.5 μM completely blocks spheroid formation[1].

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

PARP1/PKM2-IN-1 関連抗体

Immunofluorescence[1]

Cell Line: 4T1 mouse triple-negative breast cancer cells
Concentration: 2 μM
Incubation Time: 24 h incubation, followed by 24 h CoCl2 stimulation
Result: Significantly reduced nuclear PKM2 signal count and relative nuclear volume occupied by PKM2 compared to control cells, with a greater reduction than that induced by Olaparib.
Increased nuclear PAr signal count but reduced relative nuclear volume occupied by PAr compared to controls, with smaller mean and median PAr volume than PD-128 or Olaparib.

Real Time qPCR[1]

Cell Line: 4T1 mouse triple-negative breast cancer cells, HCC1937 human BRCA1-mutated triple-negative breast cancer cells
Concentration: 0.25 μM, 0.5 μM
Incubation Time: 24 h
Result: In 4T1 cells, reduced PKM2 mRNA by 10% at 0.25 μM and 33% at 0.5 μM, with no change in PKM1 mRNA.
In HCC1937 cells, reduced PKM2 mRNA by 15% at 0.25 μM and 36% at 0.5 μM, with no change in PKM1 mRNA.

Cell Viability Assay[1]

Cell Line: 4T1 mouse triple-negative breast cancer cell spheroids
Concentration: 0-12.5 μM
Incubation Time: 72 h
Result: Inhibited spheroid formation with an IC50 of 3.83 μM in the pre-treatment setup, and completely prevented spheroid formation at 12.5 μM.
Inhibited viability of pre-formed spheroids with an IC50 of 4.72 μM in the direct treatment setup.
分子量

929.18

分子式

C42H47BrClFN6O5Se
SMILES

OC1(C2=C(Br)C3=CC(C(NCCCCCCCC(N4CCN(C(C5=CC(CC6=NNC(C7=C6C=CC=C7)=O)=CC=C5F)=O)CC4)=O)=O)=CC=[N+]3[Se]2)CCCCC1.[Cl-]
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.

PARP1/PKM2-IN-1 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:

PARP1/PKM2-IN-1PARPPyruvate Kinasepoly ADP ribose polymerasePC-3 cancer cell linestriple-negative breast cancer4T1 cellsHCC1937 cellsPKM2pyruvate kinase isoformsPARP1prostate adenocarcinomabreast adenocarcinomabrca1-mutated triple-negative breast cancerInhibitorinhibitorinhibit

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:
PARP1/PKM2-IN-1
製品番号:
HY-183765
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.