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NVS-PAK1-1

NVS-PAK1-1
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Purity:99.74%
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NVS-PAK1-1

Catalog No. T16367Cas No. 1783816-74-9
NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Pack SizePrice/USDAvailabilityQuantity
1 mg$44In Stock
5 mg$97In Stock
10 mg$177In Stock
25 mg$387In Stock
50 mg$579In Stock
100 mg$828In Stock
1 mL x 10 mM (in DMSO)$97In Stock
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Product Introduction

Bioactivity
Description
NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 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).
Chemical Properties
Molecular Weight479.93
FormulaC23H25ClF3N5O
Cas No.1783816-74-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 125 mg/mL (260.45 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0836 mL10.4182 mL20.8364 mL104.1819 mL
5 mM0.4167 mL2.0836 mL4.1673 mL20.8364 mL
10 mM0.2084 mL1.0418 mL2.0836 mL10.4182 mL
20 mM0.1042 mL0.5209 mL1.0418 mL5.2091 mL
50 mM0.0417 mL0.2084 mL0.4167 mL2.0836 mL
100 mM0.0208 mL0.1042 mL0.2084 mL1.0418 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μLDMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μLDMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μLTween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify.
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