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Chemical Structure : HKB99
Catalog No.: PC-72381Not For Human Use, Lab Use Only.
HKB99 (PGAM1 allosteric inhibitor HKB99) is a novel potent, cellularly active PGAM1 (Phosphoglycerate mutase 1) allosteric inhibitor, HKB99 is noncompetitive with the substrate 3-PG with IC50 of 0.85 uM in in vitro enzyme assays.
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HKB99 (PGAM1 allosteric inhibitor HKB99) is a novel potent, cellularly active PGAM1 (Phosphoglycerate mutase 1) allosteric inhibitor, HKB99 is noncompetitive with the substrate 3-PG with IC50 of 0.85 uM in in vitro enzyme assays.
HKB99 significantly inhibited the proliferation of NSCLC cells (PC9, HCC827, H1975, and A549) in a concentration-dependent manner with the IC50 of 17-67 uM.
HKB99 allosterically block conformational change of PGAM1 during catalytic process and PGAM1-ACTA2 interaction, disrupts cellular migration and induces apoptosis in NSCLC cells.
HKB99 resensitizes the erlotinib-resistant NSCLC cells to erlotinib treatment. HKB99 (100 mg/kg, i.p.) significantly suppresses tumor growth and augments the tumoricidal effect of erlotinib in mouse xenografts
| M.Wt | 450.465 | |
| Formula | C23H18N2O6S | |
| Appearance | Solid | |
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1. Huang K, et al. Cell Metab. 2019 Dec 3;30(6):1107-1119.e8.
2. Liang Q, et al. Acta Pharmacol Sin. 2021 Jan;42(1):115-119.
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