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).

IPA-3化学構造

CAS No. 42521-82-4

サイズ 価格(税別) 在庫状況
JPY 13600 国内在庫あり
JPY 63400 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(46)

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
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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
PAK1 [1]
(Cell-free assay)
2.5 μM
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
Batch:

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
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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

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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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/

Tags: IPA-3を買う | IPA-3 ic50 | IPA-3供給者 | IPA-3を購入する | IPA-3費用 | IPA-3生産者 | オーダーIPA-3 | IPA-3化学構造 | IPA-3分子量 | IPA-3代理店