DC-PGKI is an orally active ATP-competitive inhibitor of PGK1, with an IC50 of 0.16 µM and a Kd of 99.08 nM. It stabilizes PGK1 both in vitro and in vivo, inhibiting glycolytic activity and PGK1s kinase function. This inhibition induces the accumulation of NRF2 (nuclear factor erythroid 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1beta and IL-6 genes, and inhibits their LPS-induced expression. DC-PGKI is applicable for research in colitis.
Molecular Weight:
558.46
CAS Number:
[2829198-49-2]
Formula:
C26H29Cl2N7O3
Target:
PGK1|||Nrf2|||Interleukin
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