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Description: Potent and selective PAK1 inhibitor
Chemical Name: (3S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide
Purity: ≥98% (HPLC)
Citations (1)

Biological Activity for NVS PAK1 1

NVS PAK1 1 is a potent and selective PAK1 inhibitor (IC50 = 5 nM) that displays selective for PAK1 over PAK2 and a panel of 442 kinases. NVS PAK1 1 inhibits autophosphorylation of PAK1 in KRAS-mutated pancreatic cancer cell lines.

A negative control for NVS PAK1 1 is also available; NVS PAK1 C.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the NVS-PAK1-1 probe summary on the SGC website.

External Portal Information for NVS PAK1 1

Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of NVS-PAK1-1 is reviewed on the chemical probes website.

Compound Libraries for NVS PAK1 1

NVS PAK1 1 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for NVS PAK1 1

M. Wt 479.93
Formula C23H25ClF3N5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1783816-74-9
PubChem ID 122187564
Smiles FC(F)CN(C(C=CC(F)=C1)=C1N=C2N[C@H]3CCN(C(NC(C)C)=O)C3)C4=C2C=C(Cl)C=C4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for NVS PAK1 1

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 47.99 100
1eq. HCl 47.99 100

Preparing Stock Solutions for NVS PAK1 1

The following data is based on the product molecular weight 479.93. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.08 mL 10.42 mL 20.84 mL
5 mM 0.42 mL 2.08 mL 4.17 mL
10 mM 0.21 mL 1.04 mL 2.08 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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References for NVS PAK1 1

References are publications that support the biological activity of the product.

Karpov et al (2015) Optimization of a dibenzodiazepine hit to a potent and selective allosteric PAK1 inhibitor. ACS Med.Chem.Lett. 6 776 PMID: 26191365

If you know of a relevant reference for NVS PAK1 1, please let us know.

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Keywords: NVS PAK1 1, NVS PAK1 1 supplier, NVSPAK11, P21-activated, kinases, PAK1, inhibitors, inhibits, potent, selective, Kinases, 6132, Tocris Bioscience

1 Citation for NVS PAK1 1

Citations are publications that use Tocris products. Selected citations for NVS PAK1 1 include:

Teresa L et al (2021) PAK1 Positively Regulates Oligodendrocyte Morphology and Myelination. J Neurosci 41 1864-1877 PMID: 33478987

Do you know of a great paper that uses NVS PAK1 1 from Tocris? Please let us know.

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