DC-PGKI

• 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].

• UNSPSC :

  12352005

• Target :

  Interleukin Related; Keap1-Nrf2; Phosphoglycerate Kinase (PGK)

• Related Pathways :

  Immunology/Inflammation; Metabolic Enzyme/Protease; NF-κB

• Field of Research :

  Inflammation/Immunology

• Smiles :

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

• Molecular Formula :

  C26H29Cl2N7O3

• Molecular Weight :

  558.46

• References & Citations :

  [1]Liao L, et al. A potent PGK1 antagonist reveals PGK1 regulates the production of IL-1β and IL-6. Acta Pharm Sin B. 2022 Nov;12 (11) :4180-4192.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  IL-1; IL-6; PGK1

• CAS Number :

  [2829198-49-2]