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187-1, N-WASP inhibitor

187-1, N-WASP inhibitor

Catalog No. BCC5866
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1mg $226.00 Ship Within 7 Days
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Quality Control of 187-1, N-WASP inhibitor

Chemical structure

187-1, N-WASP inhibitor

Biological Activity of 187-1, N-WASP inhibitor

Inhibits neural Wiskott-Aldrich syndrome protein (N-WASP) by stabilizing the autoinhibited state of the protein. Blocks phosphatidylinositol 4,5-bisphosphate (PIP2)-stimulated actin assembly (IC50 ~ 2 μM) but does not directly inhibit actin polymerization.

187-1, N-WASP inhibitor Dilution Calculator

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187-1, N-WASP inhibitor Molarity Calculator



Chemical Properties of 187-1, N-WASP inhibitor

Cas No. 380488-27-7 SDF Download SDF

(Modifications: Phe-2 = D-Phe, Pro-3 = D-Pro, Phe-4 = D-Phe, Pro-6 = D-Pro, Cyclized)

Standard InChI InChI=1S/C96H122N18O16/c97-49-21-19-39-67-83(117)107-73(57-63-31-11-3-12-32-63)93(127)113-53-25-43-79(113)91(125)105-71(55-61-27-7-1-8-28-61)87(121)109-75(59-65-35-15-5-16-36-65)95(129)111-51-23-41-77(111)89(123)103-69(45-47-81(99)115)85(119)102-68(40-20-22-50-98)84(118)108-74(58-64-33-13-4-14-34-64)94(128)114-54-26-44-80(114)92(126)106-72(56-62-29-9-2-10-30-62)88(122)110-76(60-66-37-17-6-18-38-66)96(130)112-52-24-42-78(112)90(124)104-70(86(120)101-67)46-48-82(100)116/h1-18,27-38,67-80H,19-26,39-60,97-98H2,(H2,99,115)(H2,100,116)(H,101,120)(H,102,119)(H,103,123)(H,104,124)(H,105,125)(H,106,126)(H,107,117)(H,108,118)(H,109,121)(H,110,122)/t67-,68-,69-,70-,71+,72+,73+,74+,75-,76-,77+,78+,79+,80+/m0/s1
Formula C96H122N18O16 M.Wt 1784.13
Solubility Soluble to 2 mg/ml in water
Storage Desiccate at -20°C
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.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other courier with RT , or blue ice upon request.

Preparing Stock Solutions of 187-1, N-WASP inhibitor

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 0.5605 mL 2.8025 mL 5.605 mL 11.2099 mL 14.0124 mL
5 mM 0.1121 mL 0.5605 mL 1.121 mL 2.242 mL 2.8025 mL
10 mM 0.056 mL 0.2802 mL 0.5605 mL 1.121 mL 1.4012 mL
50 mM 0.0112 mL 0.056 mL 0.1121 mL 0.2242 mL 0.2802 mL
100 mM 0.0056 mL 0.028 mL 0.056 mL 0.1121 mL 0.1401 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

References on 187-1, N-WASP inhibitor

N-WASP inhibitor wiskostatin nonselectively perturbs membrane transport by decreasing cellular ATP levels.[Pubmed: 17092993]

Wiskott-Aldrich syndrome protein (WASP) and WAVE stimulate actin-related protein (Arp)2/3-mediated actin polymerization, leading to diverse downstream effects, including the formation and remodeling of cell surface protrusions, modulation of cell migration, and intracytoplasmic propulsion of organelles and pathogens. Selective inhibitors of individual Arp2/3 activators would enable more exact dissection of WASP- and WAVE-dependent cellular pathways and are potential therapeutic targets for viral pathogenesis. Wiskostatin is a recently described chemical inhibitor that selectively inhibits neuronal WASP (N-WASP)-mediated actin polymerization in vitro. A growing number of recent studies have utilized this drug in vivo to uncover novel cellular functions for N-WASP; however, the selectivity of wiskostatin in intact cells has not been carefully explored. In our studies with this drug, we observed rapid and dose-dependent inhibition of N-WASP-dependent membrane trafficking steps. Additionally, however, we found that addition of wiskostatin inhibited numerous other cellular functions that are not believed to be N-WASP dependent. Further studies revealed that wiskostatin treatment caused a rapid, profound, and irreversible decrease in cellular ATP levels, consistent with its global effects on cell function. Our data caution against the use of this drug as a selective perturbant of N-WASP-dependent actin dynamics in vivo.

A chemical inhibitor of N-WASP reveals a new mechanism for targeting protein interactions.[Pubmed: 11553809]

Cell morphology and motility are governed largely by complex signaling networks that ultimately engage the actin cytoskeleton. Understanding how individual circuits contribute to the process of forming cellular structures would be aided greatly by the availability of specific chemical inhibitors. We have used a novel chemical screen in Xenopus cell-free extracts to identify compounds that inhibit signaling pathways regulating actin polymerization. Here we report the results of a high-throughput screen for compounds that inhibit phosphatidylinositol 4,5-bisphosphate (PIP(2))-induced actin assembly and the identification of the first compound, a cyclic peptide, known to block actin assembly by inhibiting an upstream signaling component. We identify the target of this compound as N-WASP, a protein that has been investigated for its role as a node interconnecting various actin signaling networks. We show that this compound prevents activation of the Arp2/3 complex by N-WASP by allosterically stabilizing the autoinhibited conformation of N-WASP.


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