For research use only. Not for therapeutic Use.
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM for human G6PD. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells[1].
G6PDi-1 (10 μM, 2 h) increases the NADP+/NADPH ratio in mouse CD8+ and CD4+ T cells[1].
G6PDi-1 (50 μM, 0-300 min) inhibits mouse and human neutrophil oxidative burst[1].
G6PDi-1 inhibits the activity of G6PDH in lysates of cultured astrocytes with an IC50 of 102 nM, and lowers the total cellular WST1 reduction (0-100 μM, 60 min)[2].
G6PDi-1 (0-100 μM,) in combination with CB-839 (0-48 nM) shows synergistic cytotoxicity against A549 (KEAP1 mutant) cells and KPK (Keap1 KO) cells[3].
| Catalog Number | I027890 |
| CAS Number | 2457232-14-1 |
| Synonyms | 4-[(5-oxo-6,7,8,9-tetrahydrocyclohepta[d]pyrimidin-2-yl)amino]thiophene-2-carbonitrile |
| Molecular Formula | C14H12N4OS |
| Purity | ≥95% |
| InChI | InChI=1S/C14H12N4OS/c15-6-10-5-9(8-20-10)17-14-16-7-11-12(18-14)3-1-2-4-13(11)19/h5,7-8H,1-4H2,(H,16,17,18) |
| InChIKey | USWCHVCZOGGQQA-UHFFFAOYSA-N |
| SMILES | C1CCC(=O)C2=CN=C(N=C2C1)NC3=CSC(=C3)C#N |
| Reference | [1]. Jonathan M Ghergurovich, et al. A small molecule G6PD inhibitor reveals immune dependence on pentose phosphate pathway. Nat Chem Biol. 2020 Jul;16(7):731-739. [2]. Watermann P, et al. G6PDi-1 is a Potent Inhibitor of G6PDH and of Pentose Phosphate pathway-dependent Metabolic Processes in Cultured Primary Astrocytes. Neurochem Res. 2023 Oct;48(10):3177-3189. [3]. Ding H, et al. Activation of the NRF2 antioxidant program sensitizes tumors to G6PD inhibition. Sci Adv. 2021 Nov 19;7(47):eabk1023. |
