NVS-PAK1-1
Based on 5 publication(s) in Google Scholar
NVS-PAK1-1, a chemical probe, is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 1783816-74-9
- Formula: C23H25ClF3N5O
- Molecular Weight:479.93
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NVS-PAK1-1
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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Flow Cytometry
Biological Activity
IC50: 5 nM (PAK1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.25 μM
Compound: 3, NOV-3
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Growth inhibition of human A549 cells
Growth inhibition of human A549 cells
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[PMID: 28814374] |
NVS-PAK1-1 demonstrates high selectivity for inhibition of PAK1 over other PAK isoforms and the kinome in general. NVS-PAK1-1 has a biochemical PAK1 Kd of 7 nM and a PAK2 Kd of 400 nM. NVS-PAK1-1 shows excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases. NVS-PAK1-1 at 6-20 μM inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Consistent with the observation, NVS-PAK1-1 inhibits proliferation of Su86.86 cell line only above a concentration of 2 μM. In contrast, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, inhibition of downstream signaling and cell proliferation at a significantly lower 0.21 μM concentration are achieved[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1783816-74-9
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Appearance Solid
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Molecular Weight 479.93
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Formula C23H25ClF3N5O
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Color Off-white to light yellow
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SMILES
FC1=CC2=C(C=C1)N(CC(F)F)C3=C(C=C(Cl)C=C3)C(N[C@H]4CCN(C(NC(C)C)=O)C4)=N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell
2026 May 28;189(11):3444-3464.e28. PMID: 41923641 -
Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
PLoS One
Synergistic effect of PAK and Hippo pathway inhibitor combination in NF2-deficient Schwannoma. [Abstract]2024 Jul 31;19(7):e0305121. PMID: 39083549
NVS-PAK1-1 purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Jul 31;19(7):e0305121. [Abstract]
NVS-PAK1-1 (0-10 μM; 72 h) inhibited HEI-193 cell viability by CellTiter-Glo.
NVS-PAK1-1 purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Jul 31;19(7):e0305121. [Abstract]
NVS-PAK1-1 (2, 5 μM; 4, 72 h) decreased the protein expression of phospho-PAK1/2 (S144/S141) in HEI-193 cells.
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bioRxiv
Network analysis of α-synuclein pathology progression reveals p21-activated kinases as regulators of vulnerability. [Abstract]2024 Oct 22:2024.10.22.619411. PMID: 39484617 -
NVS-PAK1-1 purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Jun 11.
Measure of protein expression by median fluorescence intensity (MFI) of CD137 or CD69 surface markers in flow cytometry of T cells treated with NVS-PAK1-1 (10uM or 20uM) or DMSO for 5 days.
Solvent & Solubility
DMSO : 100 mg/mL (208.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Inhibition of PAK1 kinase activity is measured using the Caliper assay. The assay is performed using 384-well microtiter plates. Compounds (NVS-PAK1-1) are tested as 8-point dose responses. The assays are prepared by addition of 50 nL of compound solution in 90% DMSO directly into the empty plate. Subsequently, 4.5 µL of the enzyme solution is added to each well and the resulting solution is pre-incubated at 30°C for 60 min, followed by addition of 4.5 µL of the peptide/ATP-solution. After 60 min incubation at 30°C, reactions are terminated by addition of 16 μL per well of the stop solution. Plates with terminated kinase reactions are transferred to the Caliper LC3000 workstations for reading. Product formation is measured in a microfluidic mobility shift assay. IC50 values are derived from percent inhibition values at different compound concentrations by non-linear regression analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0836 mL | 10.4182 mL | 20.8364 mL | 52.0909 mL |
| 5 mM | 0.4167 mL | 2.0836 mL | 4.1673 mL | 10.4182 mL | |
| 10 mM | 0.2084 mL | 1.0418 mL | 2.0836 mL | 5.2091 mL | |
| 15 mM | 0.1389 mL | 0.6945 mL | 1.3891 mL | 3.4727 mL | |
| 20 mM | 0.1042 mL | 0.5209 mL | 1.0418 mL | 2.6045 mL | |
| 25 mM | 0.0833 mL | 0.4167 mL | 0.8335 mL | 2.0836 mL | |
| 30 mM | 0.0695 mL | 0.3473 mL | 0.6945 mL | 1.7364 mL | |
| 40 mM | 0.0521 mL | 0.2605 mL | 0.5209 mL | 1.3023 mL | |
| 50 mM | 0.0417 mL | 0.2084 mL | 0.4167 mL | 1.0418 mL | |
| 60 mM | 0.0347 mL | 0.1736 mL | 0.3473 mL | 0.8682 mL | |
| 80 mM | 0.0260 mL | 0.1302 mL | 0.2605 mL | 0.6511 mL | |
| 100 mM | 0.0208 mL | 0.1042 mL | 0.2084 mL | 0.5209 mL |
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