A PAK1 inhibitor (Ki =3.7 nM); selective for PAK1 over the majority of targets in a panel of 235 kinases but does inhibit PAK2

G-5555 – 10 mg

Brand:
Cayman
CAS:
1648863-90-4
Storage:
-20
UN-No:
Non-Hazardous - /

G-5555 is an inhibitor of p21-activated kinase 1 (PAK1; Ki = 3.7 nM), a non-receptor serine/threonine kinase involved in tumorigenesis.{37400} It is selective for PAK1 over the majority of targets in a panel of 235 kinases but does inhibit PAK2, PAK3, KHS1, LCK, MST3, MST4, SIK2, and YSK1 by greater than 70% with IC50 values ranging from 9 to 52 nM. G-5555 inhibits phosphorylation of MEK, a downstream target of PAK1, in EBC1 cells (IC50 = 69 nM). G-5555 (10, 20, and 30 mg/kg) dose-dependently reduces phosphorylation of MEK in tumors from an H292 non-small cell lung cancer (NSCLC) mouse xenograft model. G-5555 inhibits hERG channels less than 50% at a concentration of 10 μM, indicating the potential for a low risk of QT interval prolongation and potentially fatal arrhythmias.{37401}  

 

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Description

A PAK1 inhibitor (Ki =3.7 nM); selective for PAK1 over the majority of targets in a panel of 235 kinases but does inhibit PAK2, PAK3, KHS1, LCK, MST3, MST4, SIK2, and YSK1 by greater than 70% (IC50s = 9-52 nM); inhibits phosphorylation of MEK (IC50 = 69 nM in EBC1 cells); reduces phosphorylation of MEK in tumors from an H292 NSCLC mouse xenograft model (10, 20, and 30 mg/kg); inhibits hERG channels by less than 50% at a concentration of 10 μM

Formal name: 8-[(trans-5-amino-1,3-dioxan-2-yl)methyl]-6-[2-chloro-4-(6-methyl-2-pyridinyl)phenyl]-2-(methylamino)-pyrido[2,3-d]pyrimidin-7(8H)-one

Synonyms: 

Molecular weight: 493

CAS: 1648863-90-4

Purity: ≥98%

Formulation: A crystalline solid

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

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