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细胞周期
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/ PAK / IPA-3

IPA-3 {[allProObj[0].p_purity_real_show]}

货号：A427173

IPA-3是一种选择性的非ATP竞争性PAK1抑制剂，IC50为2.5 μM，对PAK组II（PAKs 4-6）无抑制作用。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
IPA-3 化学结构 CAS号：42521-82-4
IPA-3 化学结构
CAS号：42521-82-4
IPA-3 3D分子结构
CAS号：42521-82-4
IPA-3 化学结构 CAS号：42521-82-4
IPA-3 3D分子结构 CAS号：42521-82-4
规格 价格 会员价 库存 数量
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IPA-3 纯度/质量文件 产品仅供科研

货号：A427173 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 PAK ↓ PAK1 ↓ PAK2 ↓ PAK3 ↓ PAK4 ↓ PAK5 ↓ PAK6 ↓ 其他靶点 纯度
IPA-3 +

PAK1, IC50: 2.5 μM

 		+

PAK1, IC50: 2.5 μM

 		99%+
FRAX486 +++

PAK4, IC50: 39 nM

PAK1, IC50: 14 nM

 		+++

PAK1, IC50: 14 nM

 		++

PAK2, IC50: 33 nM

 		++

PAK3, IC50: 39 nM

 		+

PAK4, IC50: 575 nM

 		99%+
FRAX1036 ++

PAK2, Ki: 72.4 nM

PAK4, Ki: 23.3 nM

 		++

PAK1, Ki: 23.3 nM

 		++

PAK2, Ki: 72.4 nM

 		+

PAK4, Ki: 2.4 μM

 		99%+
FRAX597 ++++

PAK2, IC50: 13 nM

PAK3, IC50: 13 nM

 		++++

PAK1, IC50: 8 nM

 		++++

PAK2, IC50: 13 nM

 		+++

PAK3, IC50: 19 nM

 		98+%
PF-3758309 ++++

PAK6, Ki: 17.1 nM

PAK3, IC50: 190 nM

 		++++

PAK1, Ki: 13.7 nM

 		+

PAK2, IC50: 190 nM

 		++

PAK3, IC50: 99 nM

 		+++

PAK4, Ki: 18.7 nM

 		+++

PAK5, Ki: 18.1 nM

 		+++

PAK6, Ki: 17.1 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

IPA-3 生物活性

靶点

  • PAK

    PAK1, IC50:2.5 μM

  • PAK1

    PAK1, IC50:2.5 μM
描述 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[3]. IPA-3 (2 µM, 5 µM or 20 µM) 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[4]. 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[5]. Targeting PAK1 using IPA-3, significantly inhibits the murine metastatic PCa (RM1) cell proliferation and motility in vitro, and metastasis to the lungs in vivo[6]. Compared with spinal cord injury SCI + vehicle mice, IPA-3 treatment showed decreased p-PAK1, MMP-2, MMP-9, cleaved caspase-3, TNF-α, and IL-1β expression. Moreover, inhibition of PAK1 by IPA-3 reduced spinal cord water content and Evans blue extravasation, increased neuronal survival, and reduced TUNEL-positive cells at 24 hours after SCI[7].

IPA-3 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 数据源
human 786-0 cell Growth inhibition assay Inhibition of human 786-0 cell growth in a cell viability assay, IC50=3.31805 μM SANGER
human 8305C cell Growth inhibition assay Inhibition of human 8305C cell growth in a cell viability assay, IC50=4.16758 μM SANGER
human A2780 cell Growth inhibition assay Inhibition of human A2780 cell growth in a cell viability assay, IC50=28.371 μM SANGER
human BFTC-905 cell Growth inhibition assay Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.14768 μM SANGER

IPA-3 参考文献

[1]Viaud J, Peterson JR. An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently. Mol Cancer Ther. 2009 Sep;8(9):2559-65.

[2]Deacon SW, Beeser A, et al. An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chem Biol. 2008 Apr;15(4):322-31.

[3]Viaud J, et al. An allosteric kinase inhibitor binds the p21-activated kinase autoregulatory domain covalently. Mol Cancer Ther. 2009 Sep;8(9):2559-65.

[4]Flaiz C, et al. PAK kinase regulates Rac GTPase and is a potential target in human schwannomas. Exp Neurol. 2009 Jul;218(1):137-44.

[5]Deacon SW, et al. An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chem Biol. 2008 Apr;15(4):322-31

[6]Arti Verma,et al. PAK1 inhibitor IPA-3 mitigates metastatic prostate cancer-induced bone remodeling. Biochem Pharmacol. 2020 Jul;177:113943.

[7]Xinran Ji,et al. Inhibition of p21-Activated Kinase 1 by IPA-3 Promotes Locomotor Recovery After Spinal Cord Injury in Mice. Spine (Phila Pa 1976). 2016 Jun;41(11):919-925.

IPA-3 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.85mL

0.57mL

0.29mL

14.27mL

2.85mL

1.43mL

28.53mL

5.71mL

2.85mL

IPA-3 技术信息

CAS号42521-82-4
分子式C20H14O2S2
分子量 350.45
SMILES Code OC1=CC=C2C=CC=CC2=C1SSC3=C4C=CC=CC4=CC=C3O
MDL No. MFCD00388917
别名
运输蓝冰
InChI Key RFAXLXKIAKIUDT-UHFFFAOYSA-N
Pubchem ID 521106
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C
溶解方案

DMSO: 40 mg/mL(114.14 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: IPA-3 | 42521-82-4 | IPA3 | IPA 3 | PAK Inhibitor | Cell Cycle/DNA Damage | Cytoskeleton | PAK | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | IPA-3 纯度/质量文件 | IPA-3 亚型比较 | IPA-3 生物活性 | IPA-3 细胞研究 | IPA-3 参考文献 | IPA-3 实验方案 | IPA-3 技术信息

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