G-5555 is a selective PAK1 inhibitor (Ki=3.7 nM).

IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC50 of 2.5 μM, no inhibition to group II PAKs (PAKs 4-6).

FRAX597, a small-molecule pyridopyrimidinone, is a potent and ATP competitive inhibitor of the group I PAKs (PAK1 IC50= 8 nM, PAK2 IC50= 13 nM, PAK3 IC50= 19 nM).

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.

LCH-7749944 is a novel and potent p21-activated kinase 4 (PAK4) inhibitor that suppresses proliferation and invasion in human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and causes successful inhibition of EGFR activity.

FRAX-1036 is a potent and selective PAK1 inhibitor.

APTO-253 is a small molecule with potent anti-tumor activity in cancer cells via induction of the gene that expresses the Kruppel-like factor 4 (KLF4) master transcription factor, leading to cell cycle inhibition and programmed cell death.

FRAX486 is a selective inhibitor of group I PAKs with IC50s of 8.25/39.5, /55.3 nM for PAK1/PAK2/PAK3 respectivelt and less potent for PAK4 (IC50=779 nM).

MYCMI-6 (NSC354961) is a potent and selective endogenous MYC:MAX protein interactions inhibitor. MYCMI-6 blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with a Kd of 1.6 μM. MYCMI-6 inhibits tumor cell growth in a MYC-dependent manner (IC50<0.5 μM). MYCMI-6 is not cytotoxic to normal human cells. MYCMI-6 induces apoptosis .

PAK4-IN-1 is an inhibitor of p21-activated kinases (PAKs), with IC50 of ≤100 nM in MTT assay.

PF-3758309 is an inhbitor of PAKs with IC50 of 1.3 nM for PAK4, which inhbits tumor growth in HCT116, A549, M24met and other xenograft tumor models.

CFSE is a fluorescent cell staining dye. CFSE is cell permeable and covalently couples, via its succinimidyl group, to intracellular molecules, notably, to intracellular lysine residues and other amine sources.

CFSE is a fluorescent cell staining dye. CFSE is cell permeable and covalently couples, via its succinimidyl group, to intracellular molecules, notably, to intracellular lysine residues and other amine sources.