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IPA-3
IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM in a cell-free assay, no inhibition to group II PAKs (PAKs 4-6).
CAS No. 42521-82-4
文献中Selleckの製品使用例（49）
製品安全説明書
現在のバッチを見る：
S709301
DMSO]
70 mg/mL]
false]
Ethanol]
7 mg/mL]
false]
Water]
Insoluble]
false
純度：
99.66%
99.66
IPA-3関連製品
シグナル伝達経路
PAK阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| human NALM-6 cell | Growth inhibition assay | Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=0.97694 μM | |||
| human SW1710 cell | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50=1.17833 μM | |||
| human YT cell | Growth inhibition assay | Inhibition of human YT cell growth in a cell viability assay, IC50=1.39036 μM | |||
| human BL-70 cell | Growth inhibition assay | Inhibition of human BL-70 cell growth in a cell viability assay, IC50=2.03796 μM | |||
| human SIG-M5 cell | Growth inhibition assay | Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=2.10219 μM | |||
| human MCF7 cell | Growth inhibition assay | Inhibition of human MCF7 cell growth in a cell viability assay, IC50=2.1807 μM | |||
| human GB-1 cell | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50=2.63494 μM | |||
| human KU812 cell | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50=2.7595 μM | |||
| human QIMR-WIL cell | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=2.90891 μM | |||
| human BL-41 cell | Growth inhibition assay | Inhibition of human BL-41 cell growth in a cell viability assay, IC50=3.09844 μM | |||
| human CMK cell | Growth inhibition assay | Inhibition of human CMK cell growth in a cell viability assay, IC50=3.14599 μM | |||
| 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 | |||
| human Daoy cell | Growth inhibition assay | Inhibition of human Daoy cell growth in a cell viability assay, IC50=3.24662 μM | |||
| human 786-0 cell | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=3.31805 μM | |||
| human REH cell | Growth inhibition assay | Inhibition of human REH cell growth in a cell viability assay, IC50=3.36655 μM | |||
| 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 | |||
| human KE-37 cell growth | Growth inhibition assay | Inhibition of human KE-37 cell growth in a cell viability assay, IC50=3.50231 μM | |||
| human CAL-51 cell | Growth inhibition assay | Inhibition of human CAL-51 cell growth in a cell viability assay, IC50=3.54519 μM | |||
| human CA46 cell | Growth inhibition assay | Inhibition of human CA46 cell growth in a cell viability assay, IC50=3.6618 μM | |||
| human HEL cell | Growth inhibition assay | Inhibition of human HEL cell growth in a cell viability assay, IC50=3.72768 μM | |||
| human NB6 cell | Growth inhibition assay | Inhibition of human NB6 cell growth in a cell viability assay, IC50=3.83751 μM | |||
| human 8305C cell | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50=4.16758 μM | |||
| human EW-13 cell | Growth inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50=4.20148 μM | |||
| human NB13 cell | Growth inhibition assay | Inhibition of human NB13 cell growth in a cell viability assay, IC50=4.2256 μM | |||
| human EB2 cell | Growth inhibition assay | Inhibition of human EB2 cell growth in a cell viability assay, IC50=4.49142 μM | |||
| human HOS cell | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay | |||
| human HLE cell | Growth inhibition assay | Inhibition of human HLE cell growth in a cell viability assay, IC50=4.52149 μM | |||
| human ST486 cell | Growth inhibition assay | Inhibition of human ST486 cell growth in a cell viability assay, IC50=4.8654 μM | |||
| human NCI-H2009 cell | Growth inhibition assay | Inhibition of human NCI-H2009 cell growth in a cell viability assay, IC50=5.04354 μM | |||
| human NH-12 cell | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50=5.1176 μM | |||
| human BFTC-905 cell | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.14768 μM | |||
| human RKO cell | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50=5.28471 μM | |||
| human PF-382 | Growth inhibition assay | Inhibition of human PF-382 cell growth in a cell viability assay, IC50=5.35226 μM | |||
| human SR cell | Growth inhibition assay | Inhibition of human SR cell growth in a cell viability assay, IC50=5.37256 μM | |||
| human WSU-NHL cell | Growth inhibition assay | Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=5.52067 μM | |||
| human CAL-12T cell | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50=5.6414 μM | |||
| human Daudi cell | Growth inhibition assay | Inhibition of human Daudi cell growth in a cell viability assay, IC50=5.68477 μM | |||
| human MC-CAR cell | Growth inhibition assay | Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=5.70644 μM | |||
| human RPMI-8402 cell | Growth inhibition assay | Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=5.76876 μM | |||
| human CCRF-CEM cell | Growth inhibition assay | Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=5.97667 μM | |||
| human CHP-126 cell | Growth inhibition assay | Inhibition of human CHP-126 cell growth in a cell viability assay, IC50=6.74268 μM | |||
| human NB69 cell | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50=6.76352 μM | |||
| human KS-1 cell | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50=6.88549 μM | |||
| human J82 cell | Growth inhibition assay | Inhibition of human J82 cell growth in a cell viability assay, IC50=7.04965 μM | |||
| human SW872 cell | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50=7.83558 μM | |||
| human HC-1 cell | Growth inhibition assay | Inhibition of human HC-1 cell growth in a cell viability assay, IC50=8.06805 μM | |||
| human DU-145 cell | Growth inhibition assay | Inhibition of human DU-145 cell growth in a cell viability assay, IC50=8.21464 μM | |||
| human HL-60 cell | Growth inhibition assay | Inhibition of human HL-60 cell growth in a cell viability assay, IC50=8.84605 μM | |||
| 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 | |||
| 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 | |||
| human HT-1197 cell | Growth inhibition assay | Inhibition of human HT-1197 cell growth in a cell viability assay, IC50=10.3073 μM | |||
| human NOS-1 cell | Growth inhibition assay | Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=11.7152 μM | |||
| human HT-1080 cell | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=18.6283 μM | |||
| 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 | |||
| human SW48 cell | Growth inhibition assay | Inhibition of human SW48 cell growth in a cell viability assay, IC50=21.8897 μM | |||
| human A2780 cell | Growth inhibition assay | Inhibition of human A2780 cell growth in a cell viability assay, IC50=28.371 μM | |||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | IPA-3 is a selective non-ATP competitive Pak1 inhibitor with IC50 of 2.5 μM in a cell-free assay, no inhibition to group II PAKs (PAKs 4-6). | ||
|---|---|---|---|
| 特性 | IPA-3 binds covalently to the Pak1 regulatory domain and prevents binding to the upstream activator Cdc42. | ||
| Targets |
|
| In Vitro | ||||
| In vitro | IPA-3 is a non ATP-competitive, allosteric inhibitor of p21-activated kinase 1 (Pak1). PIR3.5 is the control compound of this compound. It prevents Cdc42-stimulated Pak1 autophosphorylation on Thr423. This compound also prevents sphingosine-dependent Pak1 autophosphorylation. It does not target exposed cysteine residues on Pak1. The disulfide bond of this inhibitor is critical for inhibition of Pak1 and in vitro reduction by the reducing agent dithiothreitol (DTT) abolishes Pak1 inhibition by this chemical. It inhibits activation of Pak1 by diverse activators, but does not inhibit preactivated Pak1. This compound inhibits PDGF-stimulated Pak activation in mouse embryonic fibroblasts. [1] It inhibits Pak1 activation in part by binding covalently to the regulatory domain of Pak1. This chemical binds Pak1 covalently in a time- and temperature-dependent manner. It prevents binding of the Pak1 activator Cdc42. This inhibitor binds directly to the Pak1 autoregulatory domain. It reversibly inhibits PMA-induced membrane ruffling in cells. [2] | |||
|---|---|---|---|---|
| 実験結果図 | Methods | Biomarkers | 結果図 | 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 | |
|
化学情報
| 分子量 | 350.45 | 化学式 | C20H14O2S2 |
| CAS No. | 42521-82-4 | SDF | Download IPA-3 SDFをダウンロードする |
| Smiles | C1=CC=C2C(=C1)C=CC(=C2SSC3=C(C=CC4=CC=CC=C43)O)O | ||
| 保管 | |||
|
In vitro |
DMSO : 70 mg/mL ( (199.74 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 7 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | |||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
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よくある質問（FAQ）
質問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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