2829198-49-2
Chemical Structure
DC-PGKI
- CAS No.: 2829198-49-2
- Formula:C26H29Cl2N7O3
- Molecular Weight:558.46
InChIKey: VOMHLXVSFXLZDS-UHFFFAOYSA-N
SMILES: O=C(N1CCN(C2=NC3=C(N=C2C(OCC)=O)C=C(Cl)C(Cl)=C3)CC1)NC(C=C4)=CC=C4N5CCNCC5
Biological Activity: 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].
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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. | |||||||||||||||||||||
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