Name: IPA-3
Brand: Selleck Chemicals
SKU: S7093
Rating: 5 (49 reviews)

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Contrôle Qualité

Lot : S709301 DMSO]70 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false Pureté : 99.66%

Cité dans Nature Medicine pour sa qualité supérieure
COA
NMR
SDS
Fiche technique

99.66

Cibles apparentées	Akt Wnt/beta-catenin PKC HSP ROCK Microtubule Associated Integrin Bcr-Abl Actin FAK
Autre PAK Inhibiteurs	FRAX597 PF-3758309 FRAX486 FRAX1036 LCH-7749944 NVS-PAK1-1 Hydrastine GNE 2861 G-5555

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Description de lactivité
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
Cliquez pour voir plus de données expérimentales sur la lignée cellulaire

Informations chimiques, stockage et stabilité

Poids moléculaire	350.45	Formule	C₂₀H₁₄O₂S₂	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	42521-82-4	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	C1=CC=C2C(=C1)C=CC(=C2SSC3=C(C=CC4=CC=CC=C43)O)O

Solubilité

In vitro
Lot:

DMSO : 70 mg/mL (199.74 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 7 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	2.500mg/ml (7.13mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Caractéristiques	IPA-3 binds covalently to the Pak1 regulatory domain and prevents binding to the upstream activator Cdc42.
Targets/IC₅₀/Ki	PAK1 (Cell-free assay) 2.5 μM
In vitro	IPA-3 est un inhibiteur allostérique non compétitif de l'ATP de la p21-activated kinase 1 (Pak1). Le PIR3.5 est le composé de contrôle de ce composé. Il empêche l'autophosphorylation de Pak1 stimulée par Cdc42 sur Thr423. Ce composé empêche également l'autophosphorylation de Pak1 dépendante de la sphingosine. Il ne cible pas les résidus cystéine exposés sur Pak1. La liaison disulfure de cet inhibiteur est essentielle pour l'inhibition de Pak1 et la réduction in vitro par l'agent réducteur dithiothreitol (DTT) abolit l'inhibition de Pak1 par ce produit chimique. Il inhibe l'activation de Pak1 par divers activateurs, mais n'inhibe pas le Pak1 préactivé. Ce composé inhibe l'activation de Pak stimulée par le PDGF dans les fibroblastes embryonnaires de souris. Il inhibe l'activation de Pak1 en partie en se liant de manière covalente au domaine régulateur de Pak1. Ce produit chimique se lie à Pak1 de manière covalente d'une manière dépendante du temps et de la température. Il empêche la liaison de l'activateur de Pak1, Cdc42. Cet inhibiteur se lie directement au domaine autorégulateur de Pak1. Il inhibe de manière réversible le ruffling membranaire induit par le PMA dans les cellules.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/18420139/ [2] https://pubmed.ncbi.nlm.nih.gov/19723886/

Applications

Méthodes	Biomarqueurs	PMID
Growth inhibition assay	Cell viability	30971268
Western blot	p-PAK1 / PAK1 / p-PAK2 / PAK2 / p-Raf1 / Raf1 / p-MEK1 / MEK1 / p-ERK / ERK	30971268
Immunofluorescence	BiP NF-κB Paxillin	24844382

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

Foire aux questions

Question 1:
If this compound is cell membrane permeable, would it be suitable for PAK1 inhibition on a pancreatic beta cell line?

Réponse :
Based on the reference, this compound is able to penetrate the cell membrane, and it is 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/

C1=C0/X	C1:	LOG(C1):
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C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

IPA-3 PAK Inhibiteur

Structure chimique

Poids moléculaire: 350.45