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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V21361 | FRAX1036 | 1432908-05-8 | FRAX1036 (FRAX-1036; FRAX 1036) is a selective p21-activated kinase 1 (PAK1) inhibitor with potential anticancer activity. |
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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). |
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V76993 | G-5555 hydrochloride | G-5555 HCl is a potent and specific PAK1 inhibitor (antagonist) with Ki of 3.7 nM. | |
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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. |
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V2252 | LCH-7749944 | 796888-12-5 | LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor (antagonist) with IC50 of 14.93 μM. |
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V2849 | NVS-PAK1-1 | 1783816-74-9 | NVS-PAK1-1 is a specific allosteric PAK1 inhibitor discovered in a fragment-based screen. |
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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. |
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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). | |
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V35252 | st-Ht31 | 188425-80-1 | st-Ht31 is a protein kinase A (PKA)-anchored, membrane-permeable (penetrable) peptide inhibitor. |
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V81533 | TAT-PAK18 inhibitory peptide | TAT-PAK18 inhibitory peptide is a membrane-permeable (penetrable) PAK inhibitory peptide. |
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