Home Cytoskeletal Signaling PAK inhibitor IPA-3 For research use only.

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 Chemical Structure

IPA-3 Chemical Structure

CAS No. 42521-82-4

Purity & Quality Control

Batch: S709301 DMSO]70 mg/mL]false]Ethanol]7 mg/mL]false]Water]Insoluble]false Purity: 99.66%
99.66

IPA-3 Related Products

Signaling Pathway

PAK Signaling Pathways

PAK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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
Click to View More Cell Line Experimental Data

Biological Activity

Description 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).
Features 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]
Experimental Result Images Methods Biomarkers Images 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

Chemical Information & Solubility

Molecular Weight 350.45 Formula

C20H14O2S2
CAS No. 42521-82-4 SDF Download IPA-3 SDF
Smiles C1=CC=C2C(=C1)C=CC(=C2SSC3=C(C=CC4=CC=CC=C43)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 70 mg/mL ( (199.74 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

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

Answer:
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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