| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H23ClF3N5O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe, with IC50 values of 5 nM for dephosphorylated PAK1 and 6 nM for phosphorylated PAK1. It also acts against PAK2, with IC50 values of 270 nM for the dephosphorylated form and 720 nM for the phosphorylated form[1]. It is supplied as a white to off-white solid (C22H23ClF3N5O, MW 465.90) at 99.2% purity.
Physical & Chemical Properties
| CAS Number | 2250019-95-3 |
|---|---|
| Molecular Formula | C22H23ClF3N5O |
| Molecular Weight | 465.90 g/mol |
| Purity | 99.2% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(N1C[C@@H](NC2=NC3=CC(F)=CC=C3N(CC(F)F)C4=CC=C(Cl)C=C42)CC1)N(C)C |
| Target | PAK1, PAK2 |
| Signaling Pathway | Cell Cycle/DNA Damage; Cytoskeleton |
| Solubility | In Vitro: DMSO: ≥ 50 mg/mL (107.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| Storage | Powder: -20°C, 3 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
PAK1 0.007 μM (Kd) |
PAK2 0.4 μM (Kd) |
PAK1 5 nM (IC50) |
PAK2 270 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[1]. NVS-PAK1-1 A Chemical Probe For PAK1
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | ≥ 50 mg/mL (107.32 mM) | use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
In the Su86.86 cell line, NVS-PAK1-1 potently inhibits PAK1 (S144) autophosphorylation at 0.25 μM, and blocks MEK S289 phosphorylation (IC50=0.21 μM) in Su86.86 cells where PAK2 is downregulated[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Network analysis of α-synuclein pathology progression reveals p21-activated kinases as regulators of vulnerability. bioRxiv 2024 Oct 22:2024.10.22.619411. PMID: 39484617
