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  3. NVS-PAK1-1

NVS-PAK1-1 

Cat. No.: HY-100519 Purity: 99.82%
Handling Instructions

NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.

For research use only. We do not sell to patients.

NVS-PAK1-1 Chemical Structure

NVS-PAK1-1 Chemical Structure

CAS No. : 1783816-74-9

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10 mM * 1 mL in DMSO USD 132 In-stock
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50 mg USD 828 In-stock
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100 mg USD 1488 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

NVS-PAK1-1 is a potent and selective allosteric PAK1 inhibitor with an IC50 of 5 nM.

IC50 & Target

IC50: 5 nM (PAK1)[1]

In Vitro

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].

In Vivo

NVS-PAK1-1 shows a relatively poor stability in rat liver microsomes (RLM) and this would limit its application for in vivo studies (t1/2 in RLM 3.5 min)[1].

Molecular Weight

479.93

Formula

C₂₃H₂₅ClF₃N₅O

CAS No.

1783816-74-9

SMILES

FC1=CC2=C(C=C1)N(CC(F)F)C3=C(C=C(Cl)C=C3)C(N[[email protected]]4CCN(C(NC(C)C)=O)C4)=N2

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (260.45 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0836 mL 10.4182 mL 20.8364 mL
5 mM 0.4167 mL 2.0836 mL 4.1673 mL
10 mM 0.2084 mL 1.0418 mL 2.0836 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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NVS-PAK1-1
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