pak3

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

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.

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.

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.

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).

PAK4-IN-2 is an exceptionally effective inhibitor of PAK4, exhibiting an IC 50 value of 2.7 nM. This compound is capable of arresting MV4-11 cells at the G0 G1 phase and inducing cell apoptosis. It holds significant potential in cancer research [1].

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.

LDN-0044878 is an inhibitor of PAK3 kinase that acts by inhibiting p53- inactivated cancers.

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.