Z57346765 is a novel small-molecule inhibitor targeting phosphoglycerate kinase 1 (PGK1), a key enzyme in glycolysis, and has demonstrated significant in vitro antitumor activity against kidney renal clear cell carcinoma (KIRC) cells. Treatment with Z57346765 led to a dose-dependent reduction in KIRC cell proliferation by decreasing PGK1's metabolic enzyme activity, thereby inhibiting glucose consumption and lactate production. Additionally, Z57346765 suppressed DNA replication activity, impaired DNA damage repair capacity, and induced cell cycle arrest at the G1/S phase. These effects were associated with downregulation of cell cycle-related proteins, including cyclin B1, cyclin D1, CDK1, and CDK2, as well as DNA replication-associated proteins such as MCM3, MCM5, and POLD1. Furthermore, Z57346765 altered the expression of genes related to cell metabolism, DNA replication, and the cell cycle, underscoring its potential as a therapeutic agent for KIRC.
MedKoo Cat#: 556385
Name: Z57346765
CAS#: 1016340-64-9
Chemical Formula: C17H18N4O
Exact Mass: 294.1481
Molecular Weight: 294.36
Elemental Analysis: C, 69.37; H, 6.16; N, 19.03; O, 5.44
The following data is based on the product molecular weight 294.36 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
