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G6PDi-1

Chemical Structure : G6PDi-1

CAS No.: 2457232-14-1

G6PDi-1 (G6PD inhibitor 1)

Catalog No.: PC-72918Not For Human Use, Lab Use Only.

G6PDi-1 is a non-steroidal, potent cell active small molecule inhibitor of glucose-6-phosphate dehydrogenase (G6PD) with IC50 of 70 nM (hG6PD).

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Biological Activity

G6PDi-1 is a non-steroidal, potent cell active small molecule inhibitor of glucose-6-phosphate dehydrogenase (G6PD) with IC50 of 70 nM (hG6PD).
G6PDi-1 binds to G6PD reversibly and non-competitively, binds to G6PD at an allosteric site and inhibits enzyme catalytic activity.
G6PDi-1 dose-dependently decreases 6-PG levels in HepG2 cells with IC50 of 13 uM, decreases 2H transfer from [1-2H]-glucose to NADPH's active hydride in treated HCT116 cells (IC50=31 uM).
G6PDi-1 dose-dependently increases NADP+/NADPH ratio in T cells, suppresses T cell cytokine production while having a minimal effect on initial activation or proliferation, suppresses oxidative burst in bone marrow derived macrophages.

Physicochemical Properties

M.Wt 284.377
Formula C14H12N4OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((5-oxo-6,7,8,9-tetrahydro-5H-cyclohepta[d]pyrimidin-2-yl)amino)thiophene-2-carbonitrile

References

1. Ghergurovich JM, et al. Nat Chem Biol. 2020 Jul;16(7):731-739.

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