PAK2 Inhibitor

PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC₅₀ of 8, 13 and 19 nM for PAK1, 2 and 3.

FRAX486 is a p21-activated kinase (PAK) inhibitor with IC₅₀s of 14, 33 and 39 nM for PAK1, PAK2 and PAK3, respectively.

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

FRAX1036 is a PAK inhibitor with K_is of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.

RN193 is a type II kinase inhibitor with a human PAK1 IC₅₀ of 4.28 μM. RN193 functionally inhibits kinase activity of PAK1, PAK2, and PAK3, and engages with their kinase domains in live cells. RN193 induces thermal shifts in CLK1, GSK3B, ULK1, MELK, MAPK13, BRAF, and STK10, indicating binding and stabilization of these proteins. RN193 induces formation of PAK3:PAK2 heterodimers and displaces PAK2 homodimers in live cells. RN193 acts as a tool compound for studying group I PAK conformational states.

PAK1-IN-3 is a PAK1 inhibitor with an IC₅₀ of 10 nM, an IC₅₀ of 20 nM against PAK2, and an IC₅₀ of 1079 nM against hERG potassium channels. PAK1-IN-3 forms a salt bridge with Asp106 in PAK1 via a properly positioned tertiary amine. PAK1-IN-3 inhibits PAK2 and hERG potassium channels.

AZ13705339 is a highly potent and selective PAK1 inhibitor with IC₅₀s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 has binding affinities to PAK1 and PAK2, with K_ds of 0.28 nM and 0.32 nM, respectively. AZ13705339 can be used in the research of cancers.

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

PQA-18 is a unique PAK2 inhibitor (IC₅₀: 10 nM). PQA-18 has immunosuppressing effects. PQA-18 suppresses IL2, IL4, IL6, and TNFα. PQA-18 inhibits the population of a subset of regulatory T cells and the immunoglobulin (Ig) production against T cell-dependent antigens as well as alleviates dermatitis in mice.

NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC₅₀ values of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively. NVS-PAK1-C is also against dephosphorylated PAK2 (IC₅₀=270 nM) and phosphorylated PAK2 (IC₅₀=720 nM).

AZ13705339 hemihydrate is a highly potent and selective PAK1 inhibitor with IC₅₀s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 hemihydrate has binding affinities to PAK1 and PAK2, with K_ds of 0.28 nM and 0.32 nM, respectively. AZ13705339 hemihydrate can be used in the research of cancers.

PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (K_d= 2.7 nM; K_i=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.

G-9791, a poyridone side chain analogue, is a potent PAK inhibitor with K_i values of 0.95 nM and 2.0 nM for PAK1 and PAK2, respectively.

ZMF-10 is a highly potent PAK1 inhibitor, with IC₅₀s of 174 nM, 1.038 μM and 1.372 μM for PAK1, PAK2 and PAK3, respectively. ZMF-10 can inhibit PAK1 activity to affect PAK1-regulated apoptosis, ER-Stress and migration in MDA-MB-231 cells. ZMF-10 can be used for researching anticancer.