pak

NVS-PAK1-1 is an effective and selective allosteric PAK1 inhibitor (IC50: 5 nM).

5-Aminosalicylic Acid (5-ASA) is a specific PPARγ agonist and also inhibits P21-activated kinase 1(PAK1) and NF-Κb. 5-Aminosalicylic Acid has anti-cancer and anti-inflammatory activities. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

G-5555 is a potent inhibitor of p21-activated kinase 1 (PAK1) (Kis: 3.7 nM and 11 nM for PAK1 and PAK2, respectively).

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

Fingolimod (FTY-720A) is an antagonist of sphingosine 1-phosphate (S1P) (IC50 of 0.033 nM in K562 and NK cells).

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM, effectively suppressing the proliferation of human gastric cancer cells by downregulating the PAK4/c-Src/EGFR/cyclin D1 pathway and inducing apoptosis.

GNE 2861 inhibits PAK4, PAK5, and PAK6 (IC50s: 7.5, 36, 126 nM, respectively). GNE 2861 is a PAK inhibitor that shows group II selectivity.

PF-3758309 hydrochloride (PF-03758309 hydrochloride) , is a PAK4 inhibitor, is also a n orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PF-3758309 hydrochloride binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

FRAX597 is an effective, ATP-competitive inhibitor of group I PAKs, and for PAK1(IC50=8 nM), PAK2(IC50=13 nM), and PAK3 (IC50=19 nM).

IPA-3 is a selective, non-ATP competitive Pak1 inhibitor with an IC50 of 2.5 μM, and it does not inhibit group II PAKs (PAKs 4-6).

PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition.

FRAX-1036 is a effective and selective PAK1 inhibitor.

FRAX486 is a potent p21-activated kinase (PAK) inhibitor with IC50 values of 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively.

NVS-PAK1-1 is a potent allosteric inhibitor of PAK1 with an IC 50 of 5 nM for dephosphorylated PAK1 and 6 nM for phosphorylated PAK1 as assessed. Inhibition is ATP-competitive, most likely due to indirect competition due to incompatibility of ATP binding with the DFG-out binding conformation of the allosteric compound. NVS-PAK1-1 has an IC50 of 270 nM against dephosphorylated PAK2 and 720 nM against phosphorylated PAK2 respectively [1].

TAT-PAK18 inhibitory peptide is a cell-permeable PAK inhibitor peptide. It is capable of reducing F-actin clusters and interfering with Shank3 knockdown effects.

PAK4-IN-5 (Compound 12i) is a potent inhibitor of PAK4 (IC50: PAK4 at 7.68 nM, PAK1 at 1872.01 nM) that forms stable interactions with the PAK4 enzyme. This compound effectively inhibits the proliferation and migration potential of MDA-MB-231 cells by hindering the phosphorylation of PAK4 and LIMK1. Additionally, PAK4-IN-5 arrests the cell cycle in the G0/G1 phase, induces apoptosis, and prompts the production of reactive oxygen species. The LD50 in mice is greater than 500 mg/kg (oral).

PAK4-IN-6 is a selective degrader of PAK4 and can be utilized in the synthesis of PROTACs, such as CPS-021.

PAK4-IN-2 is a potent and selective PAK4 inhibitor (IC50 = 23 nM). It suppresses migration and invasion by blocking PAK4-mediated cytoskeleton remodeling and survival signaling in cancer research.

PAK1-IN-1 is a selective and potent inhibitor of PAK1 (IC50: 9.8 nM). PAK1-IN-1 inhibits PAK1-associated tumour cell migration and invasion in a dose-dependent manner.

PAK4-IN-1 is a selective, potent, orally active PAK4 inhibitor that is stable under both acidic and neutral conditions.PAK4-IN-1 exhibits good anti-tumour effects in vivo.

PAK4-IN-3 (compound 27e) is a PAK4 inhibitor with an IC50 of 10 nM, demonstrating antiproliferative effects on A549 cells with an IC50 of 0.61μM. It induces concentration-dependent apoptosis in A549 cells and halts the cell cycle at the G0/G1 phase [1].

Carbamic acid, (3-(hexyloxy)phenyl)-, 1-butyl-4-piperidinyl ester, monohydrochloride is a bioactive chemical.

PAK1-IN-2 (Compound 35) is a selective PAK1 inhibitor with a Ki of 7.3 nM. It inhibits MEK phosphorylation and shows significant inhibitory effects on cancer cell lines with amplified PAK1/4. PAK1-IN-2 is applicable in tumor research.

AZA197 (AZA-197) is a selective Cdc42 inhibitor. It acts by inhibiting primary colon cancer growth and prolonging survival in a preclinical mouse xenograft model by downregulation of PAK1 activity.