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Chemical Structure : GW779439X
CAS No.: 551919-98-3
Catalog No.: PC-38471Not For Human Use, Lab Use Only.
GW779439X is a small-molecule kinase inhibitor that sensitizes methicillin-resistant Staphylococcus aureus (MRSA) to β-lactam antibiotics via inhibition of the PASTA kinase Stk1.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $138 | In stock | |
| 10 mg | $218 | In stock | |
| 25 mg | $378 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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GW779439X is a small-molecule kinase inhibitor that sensitizes methicillin-resistant Staphylococcus aureus (MRSA) to β-lactam antibiotics via inhibition of the PASTA kinase Stk1.
GW779439X potentiates β-lactam activity against multiple MRSA and MSSA isolates, including the sensitization of a ceftaroline-resistant isolate to ceftaroline.
GW779439X potentiates β-lactam activity via direct inhibition of Stk1.
GW779439X also interacts in the active site of the Aurora-a kinase (AURKA) enzyme.
GW779439X was originally designed for human CDK4 but failed to progress clinically because of high toxicity and low specificity.
The penicillin-binding-protein and serine/threonine kinase-associated (PASTA) kinases has attracted attention as targets for antibiotic adjuvants for β-lactams.
| M.Wt | 454.461 | |
| Formula | C22H21F3N8 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-[4-(4-Methylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine |
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1. Schaenzer AJ, et al. ACS Infect Dis. 2018 Oct 12;4(10):1508-1518.
2. Mesquita FP, et al. J Cell Biochem. 2021 Oct;122(10):1376-1388.
3. Wlodarchak N, et al. ACS Med Chem Lett. 2021 Jan 13;12(2):228-235.
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