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Wiskostatin

 
Catalog No.
B7666
神经Wiskott-Aldrich综合征蛋白(N-WASP)活性抑制剂
组合的产品项目
规格价格库存 数量
1mg
¥ 1,300.00
Ship with 10-15 days
5mg
¥ 2,220.00
Ship with 10-15 days
10mg
¥ 2,979.00
Ship with 10-15 days
50mg
¥ 8,937.00
Ship with 10-15 days

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A

背景

Wiskostatin is an N-WASP inhibitor, with an IC50 value slightly less than 10 μM. Wiskostatin interacts with a cleft in the regulatory GTPase-binding domain (GBD) of N-WASP and maintains N-WASP in an inactive conformation, thereby inhibiting Cdc42 and phosphatidylinositol 4,5-bisphosphate (PIP2) mediated N-WASP activation, as well as Arp2/3 complex activation. N-WASP, highly expressed in the brain, belongs to the WASP family in which member proteins initiate the nucleation of new actin filaments through activation of the Arp2/3 complex, and thus are emerging as critical regulators of the actin cytoskeleton. By inhibiting N-WASP, wiskostatin has been shown to interfere with the formation of dendritic spines and synapses in neurons.

References:

1. Peterson JR, Bickford LC, Morgan D, et al. Chemical inhibition of N-WASP by stabilization of a native autoinhibited conformation. Nature Structural & Molecular Biology, 2004, 11(8): 747-755.

2. Wegner AM, Nebhan CA, Hu L, et al. N-wasp and the arp2/3 complex are critical regulators of actin in the development of dendritic spines and synapses. Journal of Biological Chemistry, 2008, 283(23): 15912-15920.

化学属性

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt426.15
Cas No.253449-04-6
FormulaC17H18Br2N2O
SolubilitySoluble in DMSO
Chemical Name(R)-1-(3,6-dibromo-9H-carbazol-9-yl)-3-(dimethylamino)propan-2-ol
SDFDownload SDF
Canonical SMILESBrC1=CC=C(C2=C1)N(C(C2=C3)=CC=C3Br)C[C@@H](CN(C)C)O
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试验操作

Cell experiment:[2]

Cell lines

Hippocampal neurons

Reaction Conditions

2 or 5 μM wiskostatin

Applications

Wiskostatin caused a dose-dependent decrease in the number of dendritic spines and excitatory synapses. However, wiskostatin, even at the highest concentration (5 μM), did not significantly affect the number of inhibitory synapses. In addition, wiskostatin did not adversely affect the health of the neurons, because they were observed to develop normally and no detectable effects on the growth of axons or dendrites were seen at any of the wiskostatin concentrations used.

Note

The technical data provided above is for reference only.

References:

1. Peterson JR, Bickford LC, Morgan D, et al. Chemical inhibition of N-WASP by stabilization of a native autoinhibited conformation. Nature Structural & Molecular Biology, 2004, 11(8): 747-755.

2. Wegner AM, Nebhan CA, Hu L, et al. N-wasp and the arp2/3 complex are critical regulators of actin in the development of dendritic spines and synapses. Journal of Biological Chemistry, 2008, 283(23): 15912-15920.

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化学结构

Wiskostatin