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.

For research use only. We do not sell to patients.

PARP1/PKM2-IN-1

PARP1/PKM2-IN-1 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

PARP1/PKM2-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)

In Vitro

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 Related Antibodies

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.
Molecular Weight

929.18

Formula

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-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • 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)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PARP1/PKM2-IN-1
Cat. No.:
HY-183765
Quantity:
MCE Japan Authorized Agent:

Customer Review

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.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

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