NVS-PAK1-1 [1783816-74-9]
Référence T16367-1mg
Conditionnement : 1mg
Marque : TargetMol
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NVS-PAK1-1
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NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
Cas No. 1783816-74-9
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.35%
Appearance:Solid
Color:White
COA HNMR LCMS
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM). |
| Targets & IC50 | PAK1:5 nM |
| In vitro | NVS-PAK1-1 inhibits the proliferation of the Su86.86 cell line only above a concentration of 2 μM, consistent with the observation. NVS-PAK1-1 (6-20 μM) inhibits the phosphorylation of the downstream substrate MEK1 Ser289. Inhibition of downstream signaling, by applying a mixture of NVS-PAK1-1 and PAK2 shRNA, and cell proliferation at a significantly lower 0.21 μM concentration is achieved. NVS-PAK1-1 shows 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 displays excellent activity in biochemical assays and an exceptional selectivity profile against other known kinases . |
| In vivo | NVS-PAK1-1 displays relatively poor stability in rat liver microsomes (RLM). This would limit its application for in vivo studies (t1/2 in RLM 3.5 min). |
| Molecular Weight | 479.93 |
| Formula | C23H25ClF3N5O |
| Cas No. | 1783816-74-9 |
| Smiles | CC(C)NC(=O)N1CC[C@@H](C1)NC1=Nc2cc(F)ccc2N(CC(F)F)c2ccc(Cl)cc12 |
| Relative Density. | 1.42 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 145 mg/mL (302.13 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 10 mg/mL (20.84 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (20.84 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||