Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 10,000 | |||
5 mg | 在庫あり | ¥ 22,500 | |||
10 mg | 在庫あり | ¥ 41,000 | |||
25 mg | 在庫あり | ¥ 89,000 | |||
50 mg | 在庫あり | ¥ 133,000 | |||
100 mg | 在庫あり | ¥ 190,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 22,500 |
説明 | NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM). |
ターゲット&IC50 | PAK1:5 nM |
In vitro | NVS-PAK1-1 inhibits the proliferation of the Su86.86 cell line only above a concentration of 2 μM, consistent with the observation. NVS-PAK1-1 (6-20 μM) inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Inhibition of downstream signaling, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, and cell proliferation at a significantly lower 0.21 μM concentration is achieved. NVS-PAK1-1 shows high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 displays excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases . |
In vivo | NVS-PAK1-1 displays relatively poor stability in rat liver microsomes (RLM). This would limit its application for in vivo studies (t1/2 in RLM 3.5 min). |
分子量 | 479.93 |
分子式 | C23H25ClF3N5O |
CAS No. | 1783816-74-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (260.45 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
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