2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Phosphoglycerate Kinase (PGK) Keap1-Nrf2 Interleukin Related
  4. DC-PGKI

DC-PGKI is an orally active ATP-competitive PGK1 inhibitor(IC50 = 0.16 Μm, Kd = 99.08 nM). DC-PGKI stabilizes PGK1 in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. DC-PGKI-mediated inhibition of PGK1 leads to the accumulation of NRF2 (nuclear factor-erythroid factor 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1β and IL-6 genes, and suppresses the LPS-induced expression of these genes. DC-PGKI can be used for the study of colitis.

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

DC-PGKI

DC-PGKI Chemical Structure

CAS No. : 2829198-49-2

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.

DC-PGKI Related Antibodies

Top Publications Citing Use of Products

View All Phosphoglycerate Kinase (PGK) Isoform Specific Products:

View All Isoforms
PGK1

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DC-PGKI is an orally active ATP-competitive PGK1 inhibitor(IC50 = 0.16 Μm, Kd = 99.08 nM). DC-PGKI stabilizes PGK1 in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. DC-PGKI-mediated inhibition of PGK1 leads to the accumulation of NRF2 (nuclear factor-erythroid factor 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1β and IL-6 genes, and suppresses the LPS-induced expression of these genes. DC-PGKI can be used for the study of colitis[1].

IC50 & Target[1]

PGK1

0.16 μM (IC50)

PGK1

99.08 nM (Kd)

IL-6

 

IL-1β

 

In Vitro

DC-PGKI (0.1-30 μM, 3 h) can increase RAW264.7 cells' PGK1 thermal stability in a concentration-dependent manner[1].
DC-PGKI (5-10 μM, 10 h) inhibits PGK1 glycolytic metabolic activity in the resting and activated in RAW264.7 cells[1].
DC-PGKI (10-20 μM) notably decreases the Ser30 phosphorylation level of Beclin1 in RAW246.7 cells, indicating that DC-PGKI also impairs PGK1’s kinase function[1].
DC-PGKI (5-20 μM) inhibits LPS-induced IL-1β and IL-6 mRNA in a concentration-dependent manner in RAW246.7 cells[1].
DC-PGKI (0-20 μM) significantly inhibits Lipopolysaccharides (HY-D1056) (LPS)-induced precursor of IL-1β and IL-6 in RAW264.7 cells[1].
DC-PGKI (5-20 μM, 7 h) results in a significant reduction in KEAP1 protein level, accumulation of NRF2, as well as upregulation of both the mRNA and protein levels of HMOX1 in LPS-induced RAW264.7 cells[1].
DC-PGKI (5-20 μM, 7 h) upregulates other downstream target genes of NRF2, including Txnrd1, Prdx1, Gclc, Sod1, Fth1, and Ephx1, in both LPS-treated and untreated conditions in RAW264.7 cells[1].

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

DC-PGKI Related Antibodies

Western Blot Analysis[1]

Cell Line: RAW264.7 cells
Concentration: 0 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM, 20 μM, 30 μM
Incubation Time: 3 h
Result: Increased RAW264.7 cells' PGK1 thermal stability in a concentration-dependent manner.

Real Time qPCR[1]

Cell Line: RAW264.7 cells were stimulated with LPS (1 μg/mL) for 4 hours.
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 7 h
Result: Inhibited the mRNA expression of IL-1β and IL-6.
Resulted in a significant reduction in KEAP1 protein level, accumulation of NRF2, as well as upregulation of both the mRNA and protein levels of HMOX1.
Upregulated other downstream target genes of NRF2, including Txnrd1, Prdx1, Gclc, Sod1, Fth1, and Ephx1.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUClast MRTINF_obs F AUCINF_obs Vss_obs
Mice 10 mg/kg p.o. 5.29 h 4 h 38 ng/mL 253 ng·h/mL 8.1 h 11.2 % / /
Mice 3 mg/kg i.v. 4.35 h / / 676 ng·h/mL 5.36 h / 755 ng·h/mL 22362 mL/kg
In Vivo

DC-PGKI (5-10 mg/kg, p.o., once daily for 8 days) significantly alleviates dextran sulfate sodium (DSS)-induced colitis symptoms in mice by inhibiting PGK1 and activating the NRF2 pathway[1].

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

Animal Model: 8-week-old C57BL/6 male mice were given 5%(w/v) DSS for 7 days to induce acute colitis, followed by drinking water for one day[1].
Dosage: 5 mg/kg, 10 mg/kg
Administration: P.o., once daily for 8 days
Result: Significantly reduced weight loss induced by DSS.
The disease activity index (DAI) decreased compared to the DSS group.
Reduced colonic tissue damage, lymphocyte infiltration, and crypt destruction.
Lowered serum and tissue protein and mRNA levels of IL-1β and IL-6.
Increased NRF2 protein accumulation in colonic tissue.
Molecular Weight

558.46

Formula

C26H29Cl2N7O3
CAS No.
SMILES

O=C(N1CCN(C2=NC3=C(N=C2C(OCC)=O)C=C(Cl)C(Cl)=C3)CC1)NC(C=C4)=CC=C4N5CCNCC5
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.

DC-PGKI 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:

DC-PGKI2829198-49-2Phosphoglycerate Kinase (PGK)Keap1-Nrf2Interleukin RelatedPhosphoglycerate KinaseILGlycolysisPhosphoglycerate kinase1MacrophagesNRF2InflammationInhibitorinhibitorinhibit

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:
DC-PGKI
Cat. No.:
HY-177944
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.