PAK Inhibitor

5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

IPA-3 is a selective non-ATP competitive PAK1 inhibitor with IC₅₀ of 2.5 μM, and shows no inhibition to group II PAKs (PAKs 4-6).

LDN-0028574 is a PAK3 inhibitor. LDN-0028574 can be used in the research of p53-deficient cancers.

SIK2/3-IN-2 (compound 12, compound I-200) is a potent SIK2/3 inhibitor (SIK2 IC₅₀ = 65 nM, SIK3 IC₅₀ = 14 nM). SIK2/3-IN-2 is also a p21-activated protein kinase (PAK) 1 inhibitor with a K_i of 20.7 nM. SIK2/3-IN-2 can be used for hyperproliferative diseases and cancer research, such as Paclitaxel (HY-B0015)-resistant ovarian cancer.

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.

Padnarsertib (KPT-9274) is an orally bioavailable, dual PAK4/Nicotinamide phosphoribosyltransferase (Nampt) inhibitor, with IC₅₀s of <100 nM and 120 nM, respectively.

NVS-PAK1-1, a chemical probe, is a potent and selective allosteric PAK1 inhibitor with an IC₅₀ of 5 nM.

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.

PRT062607 (P505-15) Hydrochloride is an orally available Syk inhibitor (IC₅₀: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 Hydrochloride exerts potent antitumor activity in tumor xenograft mouse models.

GNE 2861 is a PAK inhibitor that displays group II selectivity. GNE 2861 inhibits PAK4, PAK5 and PAK6 with IC₅₀s of 7.5, 36, 126 nM, 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.

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.

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC₅₀ of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis.

PAK4-IN-2 is a highly potent PAK4 inhibitor with IC₅₀ value of 2.7 nM. PAK4-IN-2 can arrest MV4-11 cells at G0/G1 phase and induce cell apoptosis. PAK4-IN-2 can be used for researching cancer.

DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a K_i value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research.

st-Ht31 ammonium is a membrane-permeable peptide inhibitor of?protein kinase A (PKA) anchoring. st-Ht31 ammonium induces robust cholesterol/phospholipid efflux. st-Ht31 ammonium completely reverses foam cell formation and restores the metabolic health of macrophage.