IPA-3
IPA-3是一种选择性的，非ATP竞争性Pak1抑制剂，无细胞试验中IC50为2.5 μM，对第II组PAKs(PAKs 4-6)没有抑制作用。
IPA-3 Chemical Structure
CAS: 42521-82-4
产品质控
IPA-3相关产品
| 相关靶点 | PAK1 PAK3 PAK2 PAK4 PAK5 PAK6 | 点击展开 |
|---|---|---|
| 相关产品 | FRAX597 PF-3758309 FRAX486 FRAX1036 NVS-PAK1-1 LCH-7749944 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 血管生成相关化合物库 TGF-beta/Smad信号通路库 细胞骨架信号通路化合物库 抗心血管疾病化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| human NALM-6 cell | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.97694 μM | SANGER | ||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.17833 μM | SANGER | ||
| human YT cell | Growth inhibition assay | Inhibition of human YT cell growth in a cell viability assay, IC50=1.39036 μM | SANGER | ||
| human BL-70 cell | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay, IC50=2.03796 μM | SANGER | ||
| human SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=2.10219 μM | SANGER | ||
| human MCF7 cell | Growth inhibition assay | Inhibition of human MCF7 cell growth in a cell viability assay, IC50=2.1807 μM | SANGER | ||
| human GB-1 cell | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50=2.63494 μM | SANGER | ||
| human KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.7595 μM | SANGER | ||
| human QIMR-WIL cell | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=2.90891 μM | SANGER | ||
| human BL-41 cell | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay, IC50=3.09844 μM | SANGER | ||
| human CMK cell | Growth inhibition assay | Inhibition of human CMK cell growth in a cell viability assay, IC50=3.14599 μM | SANGER | ||
| human U-698-M cell | Growth inhibition assay | Inhibition of human U-698-M cell growth in a cell viability assay, IC50=3.23856 μM | SANGER | ||
| human Daoy cell | Growth inhibition assay | Inhibition of human Daoy cell growth in a cell viability assay, IC50=3.24662 μM | SANGER | ||
| 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 REH cell | Growth inhibition assay | Inhibition of human REH cell growth in a cell viability assay, IC50=3.36655 μM | SANGER | ||
| human MHH-PREB-1 cell | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=3.46687 μM | SANGER | ||
| human KE-37 cell growth | Growth inhibition assay | Inhibition of human KE-37 cell growth in a cell viability assay, IC50=3.50231 μM | SANGER | ||
| human CAL-51 cell | Growth inhibition assay | Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=3.54519 μM | SANGER | ||
| human CA46 cell | Growth inhibition assay | Inhibition of human CA46 cell growth in a cell viability assay, IC50=3.6618 μM | SANGER | ||
| human HEL cell | Growth inhibition assay | Inhibition of human HEL cell growth in a cell viability assay, IC50=3.72768 μM | SANGER | ||
| human NB6 cell | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50=3.83751 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 EW-13 cell | Growth inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50=4.20148 μM | SANGER | ||
| human NB13 cell | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50=4.2256 μM | SANGER | ||
| human EB2 cell | Growth inhibition assay | Inhibition of human EB2 cell growth in a cell viability assay, IC50=4.49142 μM | SANGER | ||
| human HOS cell | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay | SANGER | ||
| human HLE cell | Growth inhibition assay | Inhibition of human HLE cell growth in a cell viability assay, IC50=4.52149 μM | SANGER | ||
| human ST486 cell | Growth inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50=4.8654 μM | SANGER | ||
| human NCI-H2009 cell | Growth inhibition assay | Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=5.04354 μM | SANGER | ||
| human NH-12 cell | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50=5.1176 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 | ||
| human RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=5.28471 μM | SANGER | ||
| human PF-382 | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay, IC50=5.35226 μM | SANGER | ||
| human SR cell | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay, IC50=5.37256 μM | SANGER | ||
| human WSU-NHL cell | Growth inhibition assay | Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=5.52067 μM | SANGER | ||
| human CAL-12T cell | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=5.6414 μM | SANGER | ||
| human Daudi cell | Growth inhibition assay | Inhibition of human Daudi cell growth in a cell viability assay, IC50=5.68477 μM | SANGER | ||
| human MC-CAR cell | Growth inhibition assay | Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=5.70644 μM | SANGER | ||
| human RPMI-8402 cell | Growth inhibition assay | Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=5.76876 μM | SANGER | ||
| human CCRF-CEM cell | Growth inhibition assay | Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=5.97667 μM | SANGER | ||
| human CHP-126 cell | Growth inhibition assay | Inhibition of human CHP-126 cell growth in a cell viability assay, IC50=6.74268 μM | SANGER | ||
| human NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50=6.76352 μM | SANGER | ||
| human KS-1 cell | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50=6.88549 μM | SANGER | ||
| human J82 cell | Growth inhibition assay | Inhibition of human J82 cell growth in a cell viability assay, IC50=7.04965 μM | SANGER | ||
| human SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50=7.83558 μM | SANGER | ||
| human HC-1 cell | Growth inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay, IC50=8.06805 μM | SANGER | ||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=8.21464 μM | SANGER | ||
| human HL-60 cell | Growth inhibition assay | Inhibition of human HL-60 cell growth in a cell viability assay, IC50=8.84605 μM | SANGER | ||
| human MV-4-11 cell | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=9.1649 μM | SANGER | ||
| human SK-N-DZ cell | Growth inhibition assay | Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=9.20423 μM | SANGER | ||
| human HT-1197 cell | Growth inhibition assay | Inhibition of human HT-1197 cell growth in a cell viability assay, IC50=10.3073 μM | SANGER | ||
| human NOS-1 cell | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=11.7152 μM | SANGER | ||
| human HT-1080 cell | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=18.6283 μM | SANGER | ||
| human SK-LU-1 cell | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50=18.8731 μM | SANGER | ||
| human SW48 cell | Growth inhibition assay | Inhibition of human SW48 cell growth in a cell viability assay, IC50=21.8897 μM | SANGER | ||
| human A2780 cell | Growth inhibition assay | Inhibition of human A2780 cell growth in a cell viability assay, IC50=28.371 μM | SANGER | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | IPA-3是一种选择性的，非ATP竞争性Pak1抑制剂，无细胞试验中IC50为2.5 μM，对第II组PAKs(PAKs 4-6)没有抑制作用。 | ||
|---|---|---|---|
| 特性 | IPA-3共价结合到Pak1的调节域，并抑制结合到Cdc42的上游活化剂。 | ||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | IPA-3是非ATP竞争性的p21-激活激酶1(Pak1)的变构抑制剂。IPA-3抑制Cdc42刺激的Pak1在Thr423位点自磷酸化。IPA-3也抑制鞘氨醇依赖性的Pak1自磷酸化。IPA-3不靶向作用于暴露的Pak1的半胱氨酸残基。IPA-3的二硫键对抑制Pak1是至关重要的，且通过还原剂二硫苏糖醇（DTT）废除IPA-3对Pak1的抑制。IPA-3通过不同的活化剂抑制Pak1激活, 但不抑制预活化的Pak1。IPA-3作用于小鼠胚胎成纤维细胞，抑制PDGF刺激的Pak激活。[1]IPA-3通过共价结合到Pak1的调节域抑制Pak1活化。IPA-3与Pak1共价结合，这种作用存在时间和温度依赖性。IPA-3抑制Pak1活化剂Cdc42的结合。IPA-3直接结合到Pak1的自动调节域。IPA-3 作用于细胞，可逆抑制PMA诱导的膜皱裂。[2] | |||
|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-PAK1 / PAK1 / p-PAK2 / PAK2 / p-Raf1 / Raf1 / p-MEK1 / MEK1 / p-ERK / ERK |
|
30971268 | |
| Growth inhibition assay | Cell viability |
|
30971268 | |
| Immunofluorescence | Paxillin NF-κB BiP |
|
23894351 | |
化学信息&溶解度
| 分子量 | 350.45 | 分子式 | C20H14O2S2 |
| CAS号 | 42521-82-4 | SDF | Download IPA-3 SDF |
| Smiles | C1=CC=C2C(=C1)C=CC(=C2SSC3=C(C=CC4=CC=CC=C43)O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 70 mg/mL ( (199.74 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 7 mg/mL (19.97 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
If this product is cell membrane permeable and would it be suitable for PAK1 inhibition on a pancreatic beta cell line?
回答：
Based on the reference, I think IPA-3 is able to penetrate the cell membrane, it's likely to inhibit PAK1 on a pancreatic beta cell line although there is no reference confirming it: Figure 3: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3963893/; http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4353635/
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