1783816-74-9 Usage
Uses
NVS PAK1 1 is one of potent and selective allosteric PAK1 inhibitors.
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
Check Digit Verification of cas no
The CAS Registry Mumber 1783816-74-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,7,8,3,8,1 and 6 respectively; the second part has 2 digits, 7 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1783816-74:
(9*1)+(8*7)+(7*8)+(6*3)+(5*8)+(4*1)+(3*6)+(2*7)+(1*4)=219
219 % 10 = 9
So 1783816-74-9 is a valid CAS Registry Number.
1783816-74-9Relevant articles and documents
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor
Karpov, Alexei S.,Amiri, Payman,Bellamacina, Cornelia,Bellance, Marie-Helene,Breitenstein, Werner,Daniel, Dylan,Denay, Regis,Fabbro, Doriano,Fernandez, Cesar,Galuba, Inga,Guerro-Lagasse, Stephanie,Gutmann, Sascha,Hinh, Linda,Jahnke, Wolfgang,Klopp, Julia,Lai, Albert,Lindvall, Mika K.,Ma, Sylvia,M?bitz, Henrik,Pecchi, Sabina,Rummel, Gabriele,Shoemaker, Kevin,Trappe, Joerg,Voliva, Charles,Cowan-Jacob, Sandra W.,Marzinzik, Andreas L.
, p. 776 - 781 (2015)
The discovery of inhibitors targeting novel allosteric kinase sites is very challenging. Such compounds, however, once identified could offer exquisite levels of selectivity across the kinome. Herein we report our structure-based optimization strategy of
