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PGMI-004A

Chemical Structure : PGMI-004A

CAS No.: 1313738-90-7

PGMI-004A

Catalog No.: PC-23304Not For Human Use, Lab Use Only.

PGMI-004A is a specific small molecule inhibitor of glycolytic enzyme phosphoglycerate mutase 1 (PGAM1) with IC50 of 13.1 uM, Ki of 3.91 uM.

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Biological Activity

PGMI-004A is a specific small molecule inhibitor of glycolytic enzyme phosphoglycerate mutase 1 (PGAM1) with IC50 of 13.1 uM, Ki of 3.91 uM.
PGMI-004A directly binds to the protein with KD of 9.4 uM.
PGMI-004A treatment results in decreased 2-PG and increased 3-PG levels in H1299 cells, which could be rescued by treatment with methyl-2-PG.
PGMI-004A treatment results in decreased oxidative PPP flux and NADPH/NADP+ ratio as well as reduced biosynthesis of lipids and RNA and cell proliferation in H1299 cells.
PGMI-004A treatment inhibits cancer cell proliferation and tumor growth, and alters 3-PG and 2-PG levels in primary leukemia cells from human patients, leading to attenuated leukemia cell proliferation.

Physicochemical Properties

M.Wt 463.38
Formula C21H12F3NO6S
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

3,4-dihydroxy-9,10-dioxo-N-(4-(trifluoromethyl)phenyl)-9,10-dihydroanthracene-2-sulfonamide

References

1. Hitosugi T, et al. Cancer Cell. 2012 Nov 13;22(5):585-600.

2. Wang P, et al. Bioorg Med Chem. 2018 May 1;26(8):1961-1970.

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