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GKI-1是 Greatwall (GWL)激酶抑制剂,对 hGWLFL 具有抑制,其 IC50为4.9。GKI-1对 hGWL-KinDom 也具有抑制作用,其 IC50 为 2.5 µM。GKI-1 对 ROCK1抑制效果比 hGWLFL 和hGWL-KinDom 好,其IC50为11 µM, 仅微弱抑制 PKA。
GKI-1是 Greatwall (GWL)激酶抑制剂,对 hGWLFL 具有抑制,其 IC50为4.9。GKI-1对 hGWL-KinDom 也具有抑制作用,其 IC50 为 2.5 µM。GKI-1 对 ROCK1抑制效果比 hGWLFL 和hGWL-KinDom 好,其IC50为11 µM, 仅微弱抑制 PKA。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 1,490 | 现货 | |
5 mg | ¥ 3,730 | 现货 | |
10 mg | ¥ 5,390 | 现货 | |
25 mg | ¥ 8,350 | 现货 | |
50 mg | ¥ 11,200 | 现货 | |
100 mg | ¥ 15,180 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 4,120 | 现货 |
产品描述 | GKI-1 is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL with an IC50 of 4.9. GKI-1 also inhibited hGWL-KinDom, and its IC50 was 2.5 µM. The inhibitory effect of GKI-1 on ROCK1 was better than that of hGWLFL and hGWL-KinDom, and its IC50 was 11 µM, which only weakly inhibited PKA. |
靶点活性 | GWL-KinDom (human):4.9 µM , GWLFL (human):4.9 µM , GWLFL (human):4.9 µM, GWL-KinDom (human):2.5 µM, ROCK1:11 µM |
体外活性 | Treatment of HeLa cells with GKI-1 (25 and 50µM, 0-8.5 h) reduced ENSA/ARPP19 phosphorylation levels, resulting in reduced mitotic events, mitotic arrest/cell death, and cell division failure. GKI-1 inhibited full-length human GWL and showed cellular effects[1] |
分子量 | 269.73 |
分子式 | C15H12ClN3 |
CAS No. | 2444764-03-6 |
Smiles | N(C=1C=C(C=CC1)C=2C=NNC2)C3=CC=C(Cl)C=C3 |
密度 | 1.320 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 180.0 mg/mL (667.3 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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