pak-1

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

ZINC194100678 is an effective PAK1 inhibitor with IC50 of 8.37μM. ZINC194100678 showed strong anti-proliferation activity, with IC50 value of 40.16μM against MDA-MB-231.

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

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-231 and MDA-MB-435 cells, equally effective inhibition for Rac3.

AZ13705339 is an effective inhibitor of PAK1 with an IC50 of 0.33 nM and a Kd of 0.28 nM. AZ13705339 binds PAK2 with a Kd of 0.32 nM. AZ13705339 can be used in studies about cancers.

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].

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.

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.

7-Chloro-5-methyl-2-(4-methylphenyl)[1,2,4]triazolo[1,5-a]pyrimidine is a chemical intermediate that can be used to synthesize benzopyrimidine thioethers.

NVS PAK1 C is a negative control of NVS PAK1 1, a potent and selective PAK1 inhibitor.

G-9791 is an effective and selective inhibitor of group-I PAK.

ZMF-10 is a potent inhibitor of PAK1, and can act on PAK1 (IC50:174 nM), PAK2 (IC50:1.038 μM) and PAK3 (IC50:1.372 μM). ZMF-10 inhibited PAK1 activity and affected Pak1-regulated apoptosis, endoplasmic reticulum stress and migration in MDA-MB-231 cells. ZMF-10 can be used to study cancer.

G-5555 hydrochloride is a potent and selective inhibitor of PAK1 [Ki: 3.7 nM].

PF-3758309 dihydrochloride is a potent, reversible, orally active, ATP-competitive PAK4 inhibitor with a Kd value of 2.7 nM and a Ki value of 18.7 nM. PF-3758309 dihydrochloride exhibits the expected cellular functions of a PAK4 inhibitor, with the ability to inhibit anchorage independent growth, induction of apoptosis, cytoskeletal remodelling and inhibition of proliferation.

AZ13705339 hemihydrate is a hemihydrate form of AZ13705339, exhibiting high potency and selectivity as a PAK1 inhibitor, demonstrating IC50 values of 0.33 nM for PAK1 and 59 nM for pPAK1. It also shows strong binding affinities with Kd values of 0.28 nM for PAK1 and 0.32 nM for PAK2. This compound is utilized in cancer research.

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.

TAT-PAK18 R192A is an inactive Tat-Pak peptide. It does not influence Rac1 translocation triggered by any tested proteins.

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