上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。
NVS-PAK1-1 纯度: 99.91%
NVS-PAK1-1是有效,选择性的 PAK1 变构抑制剂,IC50值为5 nM。
NVS-PAK1-1 Chemical Structure
CAS No. : 1783816-74-9
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Free Sample (0.1-0.5 mg) | Apply now | ||
10 mM * 1 mL in DMSO | ¥1210 | In-stock | |
5 mg | ¥1100 | In-stock | |
10 mg | ¥1950 | In-stock | |
25 mg | ¥4250 | In-stock | |
50 mg | ¥7550 | In-stock | |
100 mg | ¥13500 | In-stock | |
200 mg | 询价 | ||
500 mg | 询价 |
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NVS-PAK1-1 相关产品
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生物活性 |
NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM. |
IC50 & Target |
IC50: 5 nM (PAK1)[1] |
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体外研究 (In Vitro) |
NVS-PAK1-1 demonstrates 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 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t1/2 in RLM 3.5 min)[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
479.93 |
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Formula |
C23H25ClF3N5O |
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CAS 号 |
1783816-74-9 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 125 mg/mL (260.45 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Kinase Assay [1] |
Inhibition of PAK1 kinase activity is measured using the Caliper assay. The assay is performed using 384-well microtiter plates. Compounds (NVS-PAK1-1) are tested as 8-point dose responses. The assays are prepared by addition of 50 nL of compound solution in 90% DMSO directly into the empty plate. Subsequently, 4.5 µL of the enzyme solution is added to each well and the resulting solution is pre-incubated at 30°C for 60 min, followed by addition of 4.5 µL of the peptide/ATP-solution. After 60 min incubation at 30°C, reactions are terminated by addition of 16 μL per well of the stop solution. Plates with terminated kinase reactions are transferred to the Caliper LC3000 workstations for reading. Product formation is measured in a microfluidic mobility shift assay. IC50 values are derived from percent inhibition values at different compound concentrations by non-linear regression analysis[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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