| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G655324-1ml |
1ml |
期货  |
|
| 规格或纯度 | 10mM in DMSO |
|---|---|
| 英文名称 | GW779439X |
| 生化机理 | GW779439X 是一种吡唑并哒嗪，被确认为金黄色葡萄球菌 PASTA 激酶 Stk1 的抑制剂。GW779439X 能增强β-内酰胺类抗生素对各种 MRSA 和 MSSA 分离物的活性，有些甚至跨越了从耐药到敏感的分界点。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
GW779439X，吡唑并吡啶类化合物，是一种金黄色葡萄球菌 PASTA 激酶 Stk1 抑制剂。GW779439X 增强 β-内酰胺类抗生素对各种 MRSA 和 MSSA 的分离株，有的甚至跨越了从耐药到敏感的断点。GW779439X 是一种 AURKA 抑制剂，可通过 caspases 3/7 诱导细胞凋亡 (apoptosis)。
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1 . GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway MRSA:methicillin-resistant S. aureus ; MSSA: methicillin-sensitive S. aureus In Vitro 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. GW779439X has growth inhibition effects on the AGP-01 cell line (IC 50 = 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:Aurora A|Stk1|apoptosis |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CN1CCN(CC1)C2=C(C=C(C=C2)NC3=NC=CC(=N3)C4=C5C=CC=NN5N=C4)C(F)(F)F |
| PubChem CID | 10173796 |
| 分子量 | 454.46 |
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