An allosteric inhibitor of PAK1 (Kd = 7 nM); has an IC50 value of 5.2 nM in a PAK1 dephosphorylation assay; selective for PAK1 over PAK2 (Kd = 400 nM) and over a panel of 442 kinases; inhibits phosphorylation of MEK Ser289 at 6-20 µM but does not inhibit proliferation of Su86.86 cells at concentrations lower than 2 µM

NVS-PAK1-1 – 5 mg

Brand:
Cayman
CAS:
1783816-74-9
Storage:
-20
UN-No:
Non-Hazardous - /

NVS-PAK1-1 is an allosteric inhibitor of p21-activated kinase 1 (PAK1), a non-receptor serine/threonine kinase involved in tumorigenesis (Kd = 7 nM).{39819} It has an IC50 value of 5.2 nM in a PAK1 dephosphorylation assay. NVS-PAK1-1 is selective for PAK1 over PAK2 (Kd = 400 nM) and over a panel of 442 kinases, where it did not inhibit any other kinases by greater than 80%.{39819,39820} It inhibits phosphorylation of MEK Ser289 when used at concentrations ranging from 6 to 20 µM but does not inhibit proliferation of Su86.86 cells at concentrations lower than 2 µM.{39819} See the Structural Genomics Consortium (SGC) website for more information.  

 

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SKU: 19964 - Category:

Description

An allosteric inhibitor of PAK1 (Kd = 7 nM); has an IC50 value of 5.2 nM in a PAK1 dephosphorylation assay; selective for PAK1 over PAK2 (Kd = 400 nM) and over a panel of 442 kinases; inhibits phosphorylation of MEK Ser289 at 6-20 µM but does not inhibit proliferation of Su86.86 cells at concentrations lower than 2 µM

Formal name: (3S)-3-[[2-chloro-5-(2,2-difluoroethyl)-8-fluoro-5H-dibenzo[b,e][1,4]diazepin-11-yl]amino]-N-(1-methylethyl)-1-pyrrolidinecarboxamide

Synonyms: 

Molecular weight: 479.9

CAS: 1783816-74-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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