pak

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

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).

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

Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).

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

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.

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

PAK4-IN-3 (compound 27e) is a PAK4 inhibitor with an IC50 of 10 nM, demonstrating antiproliferative effects on A549 cells with an IC50 of 0.61μM. It induces concentration-dependent apoptosis in A549 cells and halts the cell cycle at the G0 G1 phase [1].

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).

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.

Opakalim is an activator of potassium channels (potassium channel) and exhibits anticonvulsant activity.

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].

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.

PAK4-IN-1 is a selective, potent, orally active PAK4 inhibitor that is stable under both acidic and neutral conditions.PAK4-IN-1 exhibits good anti-tumour effects in vivo.

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.

XY221 (Compound 16o) selectively inhibits BRD4 BD2 with an IC50 of 5.8 nM. It demonstrates high selectivity for pan-BD2 and BRD4 BD2 domains, being 667 times more selective than for BRD4 BD1, and 9-32 times more selective than for BRD2 3 T BD2. XY221 can induce apoptosis in MV4-11 cells and exhibits anti-cancer activity.

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.

KPT9274 (PAK4-IN-1) is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.

ZMF-23, a PAK1 HDAC6 dual inhibitor, suppresses PAK1 and HDAC6-mediated aerobic glycolysis and cellular migration while inducing TNF-α-regulated necroptosis and augmenting apoptosis. The compound effectively hampers the Warburg effect and cell motility, positioning it as a potential research tool for triple-negative breast cancer (TNBC) [1].

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