IPA-3 |
Catalog No.GC16225
One-Click Copy Product Info
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Non-ATP competitive Pak1 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 42521-82-4
Sample solution is provided at 25 µL, 10mM.
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IPA-3 is an autoregulatory domain inhibitor of p21-activated kinase (Pak) with IC50 value of 2.5μM [1].
IPA-3 is a highly selective and non-ATP-competitive inhibitor that targets the autoregulatory mechanism of group I Paks. IPA-3 is screened out as an inhibitor of Pak1 by measuring ATP hydrolysis. In the in vitro assays, IPA-3 inhibits Pak1 autophosphorylation stimulated by Cdc42 or sphingosine. It shows an IC50 value of 2.5μM in the kinase assay. This inhibition of Pak1 is reported to be noncompetitive with ATP. Besides that, IPA-3 is found to remarkably inhibit the kinase activity of other group I Pak members, Pak2 and 3 at concentration of 10μM. Furthermore, 30μM IPA-3 can prevent both basal and PDGF-stimulated Pak activities in mouse embryonic fibroblasts [1].
References:
[1] Deacon S W, Beeser A, Fukui J A, et al. An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chemistry & biology, 2008, 15(4): 322-331.
| Kinase experiment [1]: | |
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Kinase assays |
Pak1 (571 nM final) in Assay buffer was mixed with IPA-3 for 5 min at room temp, followed by addition of 4 μM Cdc42 and 8.3 μM MBP for an additional 5 min. Kinase reactions were started by addition of unlabeled ATP and 1–10 μCi [32P]-γ-ATP per reaction for 10 min at 30°C. Kinase reactions were stopped on dry ice. Under these conditions, MBP phosphorylation was linear with time. |
| Cell experiment [1]: | |
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Cell lines |
Mouse embryonic fibroblasts |
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Preparation method |
The solubility of this compound in DMSO is >16.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
30 μM for 10 min |
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Applications |
IPA-3 selectively inhibits Pak1 activation in mammalian cells, and can inhibit activation of Group I Paks in cells. |
| Animal experiment [2]: | |
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Animal models |
CD-1 mice |
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Dosage form |
3.5 mg/kg, i.p. |
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Application |
Inhibition of PAK1 by IPA-3 promoted recovery of neurological function, possibly by downregulating the expression of MMP-2, MMP-9, TNF-α, and IL-1β. IPA-3 may be a potential therapeutic drug for spinal cord injury. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Deacon S W, Beeser A, Fukui J A, et al. An isoform-selective, small-molecule inhibitor targets the autoregulatory mechanism of p21-activated kinase. Chemistry & biology, 2008, 15(4): 322 - 331. [2] Ji X, Zhang Y, Zhang L, Chen H, Peng Y, Tang P. Inhibition of p21-Activated Kinase 1 by IPA-3 Promotes Locomotor Recovery After Spinal Cord Injury in Mice. Spine (Phila Pa 1976). 2016 Jun;41(11):919-25. |
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| Cas No. | 42521-82-4 | SDF | |
| Chemical Name | 1-[(2-hydroxynaphthalen-1-yl)disulfanyl]naphthalen-2-ol | ||
| Canonical SMILES | C1=CC=C2C(=C1)C=CC(=C2SSC3=C(C=CC4=CC=CC=C43)O)O | ||
| Formula | C20H14O2S2 | M.Wt | 350.45 |
| Solubility | ≥ 16.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8535 mL | 14.2674 mL | 28.5347 mL |
| 5 mM | 570.7 μL | 2.8535 mL | 5.7069 mL |
| 10 mM | 285.3 μL | 1.4267 mL | 2.8535 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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 saline, 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)