PGAM1 inhibitor KH3 | PGAM1 inhibitor | Probechem Biochemicals

Chemical Structure : PGAM1 inhibitor KH3

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PGAM1 inhibitor KH3 (KH3)

货号: PC-73135Not For Human Use, Lab Use Only.

PGAM1 inhibitor KH3 is a potent, allosteric small molecule inhibitor of phosphoglycerate mutase 1 (PGAM1) with IC50 of 105 nM.

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生物&药学活性

PGAM1 inhibitor KH3 is a potent, allosteric small molecule inhibitor of phosphoglycerate mutase 1 (PGAM1) with IC50 of 105 nM.
KH3 binds to PGAM1 with Kd of 890 nM.
KH3 effectively suppresses pancreatic cancer cell proliferation (SW1990, PANC-1, AsPC-1, and MIA PaCa-2) with EC50 ranging from 0.27 to 0.70 uM, the primary pancreatic cancer cells are slightly more sensitive to KH3 with EC50 ranging from 0.22 to 0.43 uM.
KH3 inhibits PDAC cell growth by reducing glycolysis and mitochondrial respiration via targeting PGAM1.
KH3 targets similar signaling pathways in PANC-1 PDAC cells compared to PGAM1 knockdown.
KH3 attenuates PDAC growth in patient-derived xenograft (PDX) models.

物理化学性质&存储条件

分子量	464.492
分子式	C24H20N2O6S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(3,4-dihydroxy-9,10-dioxo-9,10-dihydroanthracen-2-yl)-4-(pyrrolidin-1-yl)benzenesulfonamide

参考文献

1. Wen CL, et al. Proc Natl Acad Sci U S A. 2019 Nov 12;116(46):23264-23273.

PGAM1 inhibitor KH3 (KH3)

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物理化学性质&存储条件

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PGAM1 inhibitor KH3 (KH3)

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