2. Metabolic Enzyme/Protease
  3. Phosphoglycerate Kinase (PGK)
  4. PGK1-IN-3

PGK1-IN-3 is an orally active PGK1 inhibitor with human PGK1 IC50 values of 0.48 μM and human PGK1 Kd of 63 nM. PGK1-IN-3 binds to the ADP-binding pocket of PGK1, inhibits glycolysis, and reduces glucose consumption and lactate production. PGK1-IN-3 can be used for the research of pancreatic cancer.

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

PGK1-IN-3

PGK1-IN-3 Chemical Structure

CAS No. : 1185003-32-0

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.

PGK1-IN-3 Related Antibodies

Top Publications Citing Use of Products

View All Phosphoglycerate Kinase (PGK) Isoform Specific Products:

View All Isoforms
PGK1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PGK1-IN-3 is an orally active PGK1 inhibitor with human PGK1 IC50 values of 0.48 μM and human PGK1 Kd of 63 nM. PGK1-IN-3 binds to the ADP-binding pocket of PGK1, inhibits glycolysis, and reduces glucose consumption and lactate production. PGK1-IN-3 can be used for the research of pancreatic cancer[1].

IC50 & Target[1]

PGK1

0.48 μM (IC50)

PGK1

63 nM (Kd)

In Vitro

PGK1-IN-3 (Compound C67-47) (15 min) potently inhibits purified recombinant PGK1 enzyme activity with an IC50 of 0.48 μM and glycolysis activity with an IC50 of 0.37 μM[1].
PGK1-IN-3 binds directly to PGK1 protein with a dissociation constant of 63 nM[1].
PGK1-IN-3 exhibits an IC50 of 2.86 μM for PLK1[1].
PGK1-IN-3 (0.5-1 μM; 24 h) dose-dependently inhibits glucose consumption in PANC-1 human pancreatic cancer cells[1].
PGK1-IN-3 (0.5-1 μM; 24 h) dose-dependently inhibits lactate production in PANC-1 human pancreatic cancer cells[1].
PGK1-IN-3 (2-fold serial dilutions; 72 h) inhibits the viability of human (MiaPaCa-2, PANC-1, Capan-1, AsPC-1, CFPAC-1) and murine (KPC1199, Panc02) pancreatic cancer cell lines with IC50 values ranging from 0.48 μM to 2.00 μM[1].

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

PGK1-IN-3 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t F CL Vss
Mice[1] 2 mg/kg i.v. 0.3 h / 953 ng·h/mL / 35.1 mL/min/kg 0.93 L/kg
Mice[1] 10 mg/kg p.o. 3.1 h 798 ng/mL 2297 ng·h/mL 56 % / /
Rat[1] 2 mg/kg i.v. 2.9 h / 12908 ng·h/mL / 2.6 mL/min/kg 0.2 L/kg
Rat[1] 10 mg/kg p.o. 3.2 h 7360 ng/mL 37351 ng·h/mL 58 % / /
In Vivo

PGK1-IN-3 (Compound C67-47) (50 mg/kg; p.o.; daily for 24 days) achieves 80% tumor growth inhibition in Panc02 pancreatic cancer xenograft mice, with no associated body weight loss[1].

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

Animal Model: C57BL/6 (6-week-old male; subcutaneously injected with 1 × 106 Panc02 murine pancreatic cancer cells to establish a pancreatic cancer xenograft model)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily for 24 days
Result: Achieved 80% tumor growth inhibition (TGI) after 15 days.
Showed no observable impact on mouse body weight relative to vehicle controls.
Reduced tumor volumes and weights significantly compared to controls.
Molecular Weight

403.48

Formula

C18H17N3O4S2
CAS No.
SMILES

O=C1NC2=C(C(NC3CCCCC3)=O)SC(N2C4=CC5=C(C=C14)OCO5)=S
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.

PGK1-IN-3 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:

PGK1-IN-31185003-32-0Phosphoglycerate Kinase (PGK)Phosphoglycerate KinaseADP-binding pocketPGK1glycolysisCapan-1AsPC-1PANC-1PLK1pancreatic cancerMiaPaCa-2CFPAC-1Inhibitorinhibitorinhibit

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:
PGK1-IN-3
Cat. No.:
HY-184191
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.