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Wiskostatin
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 426.15 |
Cas No. | 253449-04-6 |
Formula | C17H18Br2N2O |
Solubility | Soluble in DMSO |
Chemical Name | (R)-1-(3,6-dibromo-9H-carbazol-9-yl)-3-(dimethylamino)propan-2-ol |
SDF | Download SDF |
Canonical SMILES | BrC1=CC=C(C2=C1)N(C(C2=C3)=CC=C3Br)C[C@@H](CN(C)C)O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
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. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)