中文名称: IPA-3
英文名称: IPA-3
CAS No: 42521-82-4
分子式: C20H14O2S2
分子量: 350.45
I10746 IPA-3 ≥98% (psaitong)
包装规格:
100mg in glass bottle
溶解性:
溶于DMSO(≥100mg/mL)
产品描述:

基本信息

产品编号:I10746

产品名称:IPA-3

CAS:

42521-82-4

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C20H14O2S2

溶于液体

-80℃

六个月

分子量

350.45

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

70mg/mL (199.74mM)

Ethanol

70mg/mL (199.74mM)

Water

Insoluble

1mg/ml表示微溶或不溶。

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。

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
(Cell-free assay)

2.5μM

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:

 

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.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量,填写另外两个变量

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 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:
  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):