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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（48）
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 | 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 | ||
| 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 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. [1] 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. [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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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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