NVS PAK1 1

Name: NVS PAK1 1
Brand: Tocris Bioscience
SKU: 6132

Tocris Bioscience, part of Bio-Techne | Catalog # 6132

Citations (14)

COA / SDS

Potent and selective PAK1 inhibitor

Key Product Details

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)
Molecular Weight:	479.93

View Full Technical Details for NVS PAK1 1

Technical Data
Citations

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.

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.

External Portal Information

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.

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
InChi Key	OINGHOPGNMYCAB-INIZCTEOSA-N
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 for NVS PAK1 1

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

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 Optimization of a dibenzodiazepine hit to a potent and selective allosteric PAK1 inhibitor. ACS Med.Chem.Lett. 2015 PMID: 26191365