PAKs (p21-activated kinases) are a family of six serine/threonine kinases that act as key effectors of RHO family GTPases in mammalian cells.Based on their domain architecture and regulation, PAKs are divided into two groups: group I (PAK1, PAK2, and PAK3) and group II (PAK4, PAK5, and PAK6). GTPases like Cdc42, Rac, TC10, CHP, and Wrch-1, as well as other GTPases independently of GTPases, activate Group I PAKs. Cdc42/Rac binding typically does not activate Group II PAKs. Members of the PAK family have been linked to a variety of diseases, including cancer, infectious diseases, and neurological disorders. PAK plays critical roles in cytoskeletal organization, cellular morphogenesis, and survival.

PAKs take part in a number of signaling networks. Along with NF-B, phosphorylating Raf1 by PAKs activates the MAPK pathway. Other cytoskeleton regulators phosphorylated by PAKs include MLCK, LIMK, filamin A, ILK, merlin, and Arpc1b. Additionally, PAKs control apoptotic and survival pathways by phosphorylating their effectors, like DLC1 and BimL. Gene transcription is directly impacted by PAKs after they move to the nucleus. PAK1 is a substrate for a number of transcription factors and transcriptional co-regulators, including FKHR, SHARP, CTBP1, and SNAI1. Through the phosphorylation of histone H3, Aurora A, and PlK1, PAKs also control the progression of the cell cycle.

PAK related products

Structure Cat No. Product Name CAS No. Product Description
FRAX1036 V21361 FRAX1036 1432908-05-8 FRAX1036 (FRAX-1036; FRAX 1036) is a selective p21-activated kinase 1 (PAK1) inhibitor with potential anticancer activity.
FRAX486 V21362 FRAX486 1232030-35-1 FRAX486 is a novel and potent p21-activated kinase (PAK) inhibitor (IC50 are 14, 33, 39 and 575 nM for PAK1, PAK2, PAK3 and PAK4 respectively).
G-5555 hydrochloride V76993 G-5555 hydrochloride G-5555 HCl is a potent and specific PAK1 inhibitor (antagonist) with Ki of 3.7 nM.
Hydrastine V16966 Hydrastine 118-08-1 Hydrastine (beta-Hydrastine; l-Hydrastine) is a natural alkaloid present in Hydrastis canadensis and other plants of the ranunculaceae family.
LCH-7749944 V2252 LCH-7749944 796888-12-5 LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor (antagonist) with IC50 of 14.93 μM.
NVS-PAK1-1 V2849 NVS-PAK1-1 1783816-74-9 NVS-PAK1-1 is a specific allosteric PAK1 inhibitor discovered in a fragment-based screen.
NVS-PAK1-C V41085 NVS-PAK1-C 2250019-95-3 NVS-PAK1-C is a potent, ATP-competitive and specific allosteric PAK1 inhibitor probe with IC50s of 5 nM and 6 nM for dephosphorylated PAK1 and phosphorylated PAK1, respectively.
PF-3758309 dihydrochloride (PF-03758309 dihydrochloride) V78827 PF-3758309 dihydrochloride (PF-03758309 dihydrochloride) PF-3758309 (PF-03758309) di-HCl is a potent, orally bioavailable, reversible ATP-competitive PAK4 inhibitor (Kd= 2.7 nM; Ki=18.7 nM).
st-Ht31 V35252 st-Ht31 188425-80-1 st-Ht31 is a protein kinase A (PKA)-anchored, membrane-permeable (penetrable) peptide inhibitor.
TAT-PAK18 inhibitory peptide V81533 TAT-PAK18 inhibitory peptide TAT-PAK18 inhibitory peptide is a membrane-permeable (penetrable) PAK inhibitory peptide.
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