pak1

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

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.

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.

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.

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].

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

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.

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).

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.

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

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.

PIR 3.5 (6,6′-Dithiodi(2-naphthol)) is a negative control of IPA 3 which is a Pak1 inhibitor.

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

KT D606 is a PAK kinase family inhibitor with an IC50 of 4 μM. It selectively inhibits the proliferation of cancer cells transformed by oncogenic RAS mutants, making it useful for studying RAS PAK1-induced cancers.

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).

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

CZh226 is a potent and selective PAK4 inhibitor (PAK4 Ki = 9 nM; PAK1 Ki = 3112 nM). CZh226 potently inhibits the migration and invasion of A549 tumor cells by regulating the PAK4-directed downstream signaling pathways in vitro.

Mesalamine impurity P is an impurity of Mesalamine. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB [1].

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).

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.