pak4

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

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

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).

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].

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.

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].

DB07268 is a potent and selective JNK1 inhibitor. It exhibits a strong affinity for the JNK1 enzyme, effectively inhibiting its activity and providing potential therapeutic benefits in conditions where JNK1 is implicated. This compound has demonstrated selective binding to JNK1 over other kinases, underscoring its specificity and promising application in targeted therapies.

GSK-690693 is a pan-Akt inhibitor targeting Akt1 2 3 with IC50 of 2 nM 13 nM 9 nM, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. Phase 1.

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM, effectively suppressing the proliferation of human gastric cancer cells by downregulating the PAK4 c-Src EGFR cyclin D1 pathway and inducing apoptosis.

GNE 2861 inhibits PAK4, PAK5, and PAK6 (IC50s: 7.5, 36, 126 nM, respectively). GNE 2861 is a PAK inhibitor that shows group II selectivity.

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.

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.

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.

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.

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.

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.

SPU-106 is a novel specific PAK4 inhibitor, effectively inhibiting the invasion of SGC7901 cells without cytotoxicity, regulating the PAK4 LIMK1 cofilin and PAK4 SCG10 signaling pathways.

KY-04045 is a PAK4 inhibitor.