PAK
p21 activated kinases
PAKs (p21-activated kinases) are a family of six serine/threonine kinases that act as key effectors of RHO family GTPases in mammalian cells. PAKs are subdivided into two groups: group I (PAK1, PAK2, and PAK3) and group II (PAK4, PAK5, and PAK6), based on their domain architecture and regulation. Group I PAKs are activated by GTPases such as Cdc42, Rac, TC10, CHP, and Wrch-1, as well as in a GTPase-independent manner. Group II PAKs are generally not activated by Cdc42/Rac binding. PAK plays important roles in cytoskeletal organization, cellular morphogenesis, and survival, and members of this family have been implicated in many diseases including cancer, infectious diseases, and neurological disorders.
PAKs participate in various signaling networks. PAKs activate the MAPK pathway by phosphorylating Raf1 in addition to NF-κB. PAKs also phosphorylate a number of regulators of the cytoskeleton such as MLCK, LIMK, filamin A, ILK, merlin, and Arpc1b. In addition, PAKs regulate survival and apoptotic pathways through phosphorylation of its effectors such as DLC1 and BimL. On translocation to the nucleus, PAKs directly affect gene transcription. Several transcription factors and transcriptional co-regulators such as FKHR, SHARP, CTBP1 and SNAI1 are substrates to PAK1. PAKs also regulate cell cycle progression through phosphorylation of histone H3, Aurora A and PlK1.
PAK Isoform Specific Products
All Product Categories
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PAK Related Products (107)
Related Products (107)
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Recombinant Proteins (4)
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Antibodies (22)
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PAK Isoform Comparison
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Y-27632
0 ImagesY-27632 is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
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5-Aminosalicylic Acid
0 Images5-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).
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WX2-43
0 ImagesWX2-43 is a PRMT5-KLF4 inhibitor (Kd of 11.0 nM). WX2-43 binds to the region between amino acids L400-M500 on PRMT5. WX2-43 efficiently intercepts the interaction between KLF4 and PRMT5, and blocks KLF4 methylation. WX2-43 decreases p21 levels and increases Bax levels. WX2-43 suppresses triple negative breast tumor progression. WX2-43 can be used in the research of triple-negative breast cancer and colorectal cancer.
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LDN-0028574
0 ImagesCat. No.: HY-123739CAS No.: 337500-87-5LDN-0028574 is a PAK3 inhibitor. LDN-0028574 can be used in the research of p53-deficient cancers.
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SIK2/3-IN-2
0 ImagesCat. No.: HY-164534CAS No.: 1648864-21-4SIK2/3-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 Ki 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.
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PF-3758309
0 ImagesSynonyms: PF-03758309PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=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.
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Padnarsertib
0 ImagesSynonyms: KPT-9274
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G-5555
0 ImagesG-5555 is a potent p21-activated kinase 1 (PAK1) inhibitor with Kis of 3.7 nM and 11 nM for PAK1 and PAK2, respectively.
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PRT062607 Hydrochloride
0 ImagesSynonyms: P505-15 Hydrochloride
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G-5555 hydrochloride
0 ImagesG-5555 hydrochloride is a potent and selective p21-activated kinase 1 (PAK1) inhibitor with a Ki of 3.7 nM.
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PQA-18
0 ImagesPQA-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.
