中文名称: | IPA-3 | ||||
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英文名称: | IPA-3 | ||||
别名: | IPA-3 国华试剂;二(2-羟基-1-萘基)二硫醚 1,1'-disulfanediylbis(naphthalen-2-ol);2-Naphthalenol, 1,1'-dithiobis- | ||||
CAS No: | 42521-82-4 | 分子式: | C20H14O2S2 | 分子量: | 350.45 |
CAS No: | 42521-82-4 | ||||
分子式: | C20H14O2S2 | ||||
分子量: | 350.45 |
基本信息
产品编号:I10746 |
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产品名称:IPA-3 |
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CAS: |
42521-82-4 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
350.45 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
70mg/mL (199.74mM) |
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Ethanol |
70mg/mL (199.74mM) |
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Water |
Insoluble |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.8535mL |
14.2674mL |
28.5347mL |
5mM |
0.5707mL |
2.8535mL |
5.7069mL |
10mM |
0.2853mL |
1.4267mL |
2.8535mL |
50mM |
0.0571mL |
0.2853mL |
0.5707mL |
生物活性
产品描述 |
一种选择性的,ATP 非竞争的 PAK1 抑制剂,IC50 值为 2.5μM,对 PAKs 4-6 没有抑制作用。 |
靶点/IC50 |
PAK1 |
2.5μM |
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体外研究 |
IPA-3 inhibits Pak1 activation in part by binding covalently to the regulatory domain of Pak1. IPA-3 binds Pak1 covalently in a time- and temperature-dependent manner. IPA-3 prevents binding of the Pak1 activator Cdc42. IPA-3 binds directly to the Pak1 autoregulatory domain. IPA-3 reversibly inhibits PMA-induced membrane ruffling in cells. IPA-3 (2µM, 5µM or 20µM) reduces cell spreading in human primary Schwann and schwannoma cells. IPA-3 treatment significantly reduces the number of adherent Schwann and schwannoma cells in a dose-dependent manner. IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1).PIR3.5 is the control compound of IPA-3.IPA-3 prevents Cdc42-stimulated Pak1 autophosphorylation on Thr423. IPA-3 also prevents sphingosine-dependent Pak1 autophosphorylation. IPA-3 does not target exposed cysteine residues on Pak1. The disulfide bond of IPA-3 is critical for inhibition of Pak1 and in vitro reduction by the reducing agent dithiothreitol (DTT) abolishes Pak1 inhibition by IPA-3. IPA-3 inhibits activation of Pak1 by diverse activators, but does not inhibit preactivated Pak1. IPA-3 inhibits PDGF-stimulated Pak activation in mouse embryonic fibroblasts.IPA-3 inhibits Pak1 activation in part by binding covalently to the regulatory domain of Pak1. IPA-3 binds Pak1 covalently in a time- and temperature-dependent manner. IPA-3 prevents binding of the Pak1 activator Cdc42. IPA-3 binds directly to the Pak1 autoregulatory domain. IPA-3 reversibly inhibits PMA-induced membrane ruffling in cells. IPA-3 (2µM, 5µM or 20µM) reduces cell spreading in human primary Schwann and schwannoma cells. IPA-3 treatment significantly reduces the number of adherent Schwann and schwannoma cells in a dose-dependent manner. IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1).PIR3.5 is the control compound of IPA-3.IPA-3 prevents Cdc42-stimulated Pak1 autophosphorylation on Thr423. IPA-3 also prevents sphingosine-dependent Pak1 autophosphorylation. IPA-3 does not target exposed cysteine residues on Pak1. The disulfide bond of IPA-3 is critical for inhibition of Pak1 and in vitro reduction by the reducing agent dithiothreitol (DTT) abolishes Pak1 inhibition by IPA-3. IPA-3 inhibits activation of Pak1 by diverse activators, but does not inhibit preactivated Pak1. IPA-3 inhibits PDGF-stimulated Pak activation in mouse embryonic fibroblasts. |
推荐实验方法(仅供参考)
激酶实验: |
Pak1 (150nM final) is pre-incubated with MBP (8.3μM), indicated proteins, and IPA-3 or DMSO in Kinase buffer for 20 minutes at 4℃. Cdc42-GTPγS (3.2μM) is then added and the reaction is pre-equilibrated 10 minutes at 30℃. Kinase reactions are started by the addition of ATP (to 30μM) containing [32P]ATP and are incubated 10 min and analyzed by SDSPAGE and autoradiography. |
细胞实验: |
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Human primary schwannoma cells are grown on 96 well plates for 2 days. Cells are left untreated or treated with 5µM IPA-3,20µM IPA-3 or 20µM PIR-3.5 for 24 hours. The MTS-solution is left on the cells for 3 hours, before the absorbance at 490 nm is measured. The experiments are conducted three times and mean and standard error of the mean is calculated with Excel. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )