pak2

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

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).

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].

PQA-18, an inhibitor of p21-activated kinase 2 (PAK2; IC50 = 10 nM), is derived from Ppc-1 and exhibits immunosuppressive properties. It inhibits IL-2 production in Jurkat T cells induced by Concanavalin A (product number 14951) with an IC50 of 400 nM. Topically applied at 0.1%, PQA-18 reduces the severity of atopic dermatitis, serum IgE levels, and skin thickness in the NC/Nga mouse model. A lower concentration of 0.05% also decreases skin nerve fiber density in NC/Nga mice. Additionally, PQA-18 administered at 4 mg/kg improves graft survival in a rat small intestine transplantation model.

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

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.

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.

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

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.

G-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.

PAK1-IN-3 is a PAK1 inhibitor with an IC50 of 10 nM for PAK1, 20 nM for PAK2, and 1079 nM for the hERG potassium channel. It can form a salt bridge with Asp106 in PAK1 through a correctly positioned tertiary amine. PAK1-IN-3 also inhibits PAK2 and the hERG potassium channel.

MRIA9, an ATP-competitive inhibitor targeting pan Salt-Inducible Kinases (SIK) and PAK2/3, demonstrates IC50 values of 516 nM, 180 nM, and 127 nM for SIK1, SIK2, and SIK3, respectively [1].

FRAX486 HCL 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.