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SML1867 Sigma-Aldrich

NVS-PAK1-1

≥98% (HPLC)

Synonym: (S)-3-(2-Chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-ylamino)-N-isopropylpyrrolidine-1-carboxamide

  • CAS Number 1783816-74-9

  • Empirical Formula (Hill Notation) C23H25ClF3N5O

  • Molecular Weight 479.93

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Properties

Related Categories Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, Kinase/Phosphatase Biology,
assay   ≥98% (HPLC)
form   powder
color   white to beige
solubility   DMSO: 30 mg/mL, clear
storage temp.   2-8°C

Description

Packaging

5, 25 mg in glass bottle

Biochem/physiol Actions

NVS-PAK1-1 is a potent allosteric inhibitor of p21-activated kinase PAK1, a serine-threonine kinase that is upregulated in many cancers. NVS-PAK1-1 has an IC50 value of 5 nM for dephoshorylated PAK1 and 6 nM for phosphorylated PAK1 in an in vitro dephosphorylation assay. NVS-PAK1-1 showed good selectivity against 442 other kinases including PAK2. NVS-PAK1-1 has generally good physicochemical properties, but was metabolized by rat liver microsomes, so may not be useful for in vivo work. For full characterization details, please visit the NVS-PAK1-1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for protein targets, visit sigma.com/sgc

Features and Benefits

NVS-PAK1-1 is a chemical probe available through a partnership between Sigma Life Science and the Structural Genomics Consortium (SGC). To learn more and view other SGC chemical probes, visit sigma.com/SGC

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm

Safety & Documentation

Safety Information

RIDADR 
NONH for all modes of transport

Documents

Certificate of Analysis (COA)

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Protocols & Articles

Articles

Discover Bioactive Small Molecules for Kinase Phosphatase Biology

Phosphorylation is a ubiquitous cellular regulatory mechanism that mediates signal transduction pathways, which carry signals from the cell surface to the nucleus or cytoplasm, by altering the activi...
Keywords: Apoptosis, Bioactive small molecules, Cancer, Diseases, Inflammation, Metabolism, Neurodegenerative Diseases, Phosphorylations, Transduction

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