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[1].
Product Specifications
CAS Number
[2829198-49-2]
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
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