GW779439X (2 μM) biochemically inhibits Stk1. GW779439X (5 μM) potentiates ceftaroline activity against a ceftaroline-resistant MRSA strain. GW779439X is able to potentiate the activity of oxacillin against various S. aureus isolates, including both MRSA and MSSA isolates, but the potentiation is clearly strongest in PBP2A-containing strains[1]. GW779439X has growth inhibition effects on the AGP-01 cell line (IC50= 0.57 μM). GW779439X (1μM) significantly blockS the cell cycle at the G0/G1 phase and sub-G1 phase. GW779439X (1μM; 72 hours; AGP-01 cells) significantly decreases expression levels of genes involved in proliferation progression (c-MYC, NRAS, and CDC25A) and increases expression levels of genes involved in cell cycle blocking (CDKN1A and TP53)[2].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Mesquita FP, et al. Kinase inhibitor screening reveals aurora-a kinase is a potential therapeutic and prognostic biomarker of gastric cancer [published online ahead of print, 2021 Jun 23]. J Cell Biochem. 2021;10.1002/jcb.30015.
[2]. Schaenzer AJ, et al. GW779439X and Its Pyrazolopyridazine Derivatives Inhibit the Serine/Threonine Kinase Stk1 and Act As Antibiotic Adjuvants against β-Lactam-Resistant Staphylococcus aureus. ACS Infect Dis. 2018;4(10):1508-1518.
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
