2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. Pyruvate Kinase PDK-1 Akt EGFR Apoptosis
  4. PKM2/PDK1-IN-1

PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway.

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

PKM2/PDK1-IN-1 Chemical Structure

PKM2/PDK1-IN-1 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

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

PKM2/PDK1-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway[1].

IC50 & Target

PKM2, PDK-1[1]
In Vitro

PKM2/PDK1-IN-1 (compound E5) (0.5-4 μM; 24 h) shows a synergistic anticancer effects with Gefitinib (HY-50895)[1].
PKM2/PDK1-IN-1 (0.5 μM; 24 h) regulates the apoptotic proteins of both mitochondrial and death receptor pathway[1].
PKM2/PDK1-IN-1 (0.5 μM, 1 μM; 24 h) causes the mitochondria transmembrane potential (ΔΨm) dissipation and intracellular ROS accumulation in lung cancer cells[1].
PKM2/PDK1-IN-1 (1 μM, 2 μM; 24 h) inhibits PDK1 and enhances the downstream PDH activity in H1975 cells[1].
PKM2/PDK1-IN-1 inhibits intracellular NADPH concentration and increases ATP production of H1975 cells[1].

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

PKM2/PDK1-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: H1975 cells
Concentration: 0.5 μM, 1 μM, 2 μM, 4 μM24 h; with 2.5-20 μM Gefitinib
Incubation Time: 24 h
Result: Synergistically induced cell apoptosis.

Western Blot Analysis[1]

Cell Line: H1975 cells
Concentration: 0.5 μM
Incubation Time: 24 h; with 10 μM Gefitinib
Result: Increased the protein levels of Cleaved Caspase-9, -3, and Cytochrome c. Deceased the protein levels of p-AKT, p-EGFR, Bcl-2.
In Vivo

PKM2/PDK1-IN-1 (compound E5) (2.4 mg/kg, 4.8 mg/kg; 6 times in 2 days) suppress the growth of H1975 xenograft tumor in nude mice in vivo with low toxic side effects[1].

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

Animal Model: Nude mice with H1975 xenograft tumor (6-week-old)[1]
Dosage: 4.8 mg/kg; dispersed in 20% DMSO
Administration: IP; every two days for a total of 6 times, for 11 days
Result: Inhibited tumor growth.
Animal Model: For acute toxicity in ICR mice (8-week-old)[1]
Dosage: 2.4, 4.8, 9.6, 19.2, 38.4 mg/kg; dissolved in 20% DMSO
Administration: IP; singel dose; observed for 14 days
Result: Exhibited little side effect in mice.
Molecular Weight

697.92

Formula

C36H43NO7S3
SMILES

COC([C@@H](NC(CCCC[C@@H]1CCSC(S1)C2=C(C=CC=C2)C)=O)CS[C@@H](C3=CC(C4=C(C=CC(O)=C4C3=O)O)=O)C/C=C(C)\C)=O
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.

PKM2/PDK1-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:

PKM2/PDK1-IN-1Pyruvate KinasePDK-1AktEGFRApoptosis3-Phosphoinositide-dependent protein kinase 1PKBProtein kinase BEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PKM2/PDK1-IN-1
Cat. No.:
HY-149275
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

Request for HNMR Report

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