- PF-3758309
- FRAX597
| IPA-3Non-ATP competitive Pak1 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Description | PA-3 is a selective non-ATP competitive inhibitor of Pak1 with an IC50 value of 2.5 μM. | |||||
| Targets | Pak1 | |||||
| IC50 | 2.5 μM | |||||
| Kinase experiment [1]: | |
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]: | |
Cell lines | Mouse embryonic fibroblasts |
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. |
Reacting condition | 30 μM for 10 min |
Applications | IPA-3 selectively inhibits Pak1 activation in mammalian cells, and can inhibit activation of Group I Paks in cells. |
| Animal experiment [2]: | |
Animal models | CD-1 mice |
Dosage form | 3.5 mg/kg, i.p. |
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. |
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. |
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 | Download SDF |
| Synonyms | N/A | ||
| 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 |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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如题，试剂商推荐这家的，然后网上查了一下就是武汉三鹰啊，国产的，有点虚啊？请前辈指点迷津啊
尽量使用已经用荧光素标记好的单克隆抗体。
如果是单色实验，荧光素的亮度越强越好，比如标记了APC的抗体就要比标记了pacific blue的在相同抗原量，抗体用量相同的情况下，要亮很多
如果是多色实验，除了不要使用光谱重叠度高的荧光素以外，还要搭配染色指数。简单的说，就是用亮度强的荧光素标记的抗体来染水平低的抗原，而用较弱的荧光素标记的抗体来染高表达的抗原。
高保真生物技术有限公司~~实验整体外包服务商~~~
anti-mouse TCR γ/δ Antibody
anti-human TCR γ/δ Antibody
利用CD3/CD4/IL-17的抗体组合（不同荧光素标记），具体步骤可按照淋巴细胞TH1/2亚型分析的protocol！
一般都是先做CD4的surface staining
然后再做IFN-gamma和IL-17的intrecellular staining
