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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Bacterial-GW779439X
GW779439X

Chemical Structure : GW779439X

CAS No.: 551919-98-3

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GW779439X (GW 779439X)

货号: 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.

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5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3780 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 454.461
分子式 C22H21F3N8
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-[4-(4-Methylpiperazin-1-yl)-3-(trifluoromethyl)phenyl]-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amine

参考文献

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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