2. Signaling Pathways
  3. Cell Cycle/DNA Damage
    Cytoskeleton
  4. PAK

PAK

p21 activated kinases

PAK

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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:

PAK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-159897
    PAK4-IN-5
    		Inhibitor
    PAK4-IN-5 (Compound 12i) is a PAK4 inhibitor (IC50: 7.68 nM for PAK4, 1872.01 nM for PAK1). PAK4-IN-5 binds to PAK4 stably via multiple interactions. PAK4-IN-5 inhibits the proliferation and the migratory potential of MDA-MB-231 cells by inhibiting the phosphorylation of PAK4 and LIMK1. PAK4-IN-5 arrests cell cycle in the G0/G1 phase, induces apoptosis and ROS production. LD50: >500 mg/kg for mice (p.o.).
    PAK4-IN-5
  • HY-RS09993
    PAK4 Human Pre-designed siRNA Set A
    		Inhibitor

    PAK4 Human Pre-designed siRNA Set A contains three designed siRNAs for PAK4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    PAK4 Human Pre-designed siRNA Set A
  • HY-RS09988
    Pak2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Pak2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pak2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Pak2 Mouse Pre-designed siRNA Set A
  • HY-13007B
    PF-3758309 dihydrochloride
    		Inhibitor
    PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
    PF-3758309 dihydrochloride
  • HY-174247
    CPS-021
    		Degrader
    CPS-021 is a selective PAK4 PROTAC degrader with a DC50 of 50 nM. CPS-021 has potent antimigratory and invasive activity and significantly suppresses the invasion and metastasis of tumor cells in A549-luc lung metastasis mice model. Pink: PAK4 ligand (HY-174822); Blue: CRBN ligase ligand (HY-10984); Black: linker
    CPS-021
  • HY-116917
    G-9791
    		Inhibitor
    G-9791, a poyridone side chain analogue, is a potent PAK inhibitor with Ki values of 0.95 nM and 2.0 nM for PAK1 and PAK2, respectively.
    G-9791
  • HY-110085
    2,2′-Dihydroxy-6,6′-dinaphthyl disulfide
    		Inhibitor 98.49%
    2,2′-Dihydroxy-6,6′-dinaphthyl disulfide (PIR-3.5) is a PAK1 inhibitor.
    2,2′-Dihydroxy-6,6′-dinaphthyl disulfide
  • HY-178812
    PI3Kα-IN-27
    		Inhibitor
    PI3Kα-IN-27 (Compound 50b) is an orally active PI3K-α inhibitor, with an IC50 of 40 nM. PI3Kα-IN-27 effectively inhibits PAK3, p110α, phospho-mTOR and phospho-ERK1/2. PI3Kα-IN-27 induces early Apoptosis. PI3Kα-IN-27 shows anticancer activity against pancreatic cancer, lung cancer, breast cancer.
    PI3Kα-IN-27
  • HY-P10106
    TAT-PAK18 inhibitory peptide
    		Inhibitor
    TAT-PAK18 inhibitory peptide is a membrane-permeable PAK inhibitory peptide. TAT-PAK18 inhibitory peptide reduces F-actin clusters and occludes the effect of Shank3 knockdown.
    TAT-PAK18 inhibitory peptide
  • HY-182357
    PAK1-IN-3
    		Inhibitor
    PAK1-IN-3 is a PAK1 inhibitor with an IC50 of 10 nM, an IC50 of 20 nM against PAK2, and an IC50 of 1079 nM against hERG potassium channels. PAK1-IN-3 forms a salt bridge with Asp106 in PAK1 via a properly positioned tertiary amine. PAK1-IN-3 inhibits PAK2 and hERG potassium channels.
    PAK1-IN-3
  • HY-10071A
    Y-27632 hydrochloride hydrate
    		Activator 99.65%
    Y-27632 hydrochloride hydrate is a ROCK inhibitor with Ki values of 220 nM and 300 nM for ROCK1 and ROCK2, respectively. Y-27632 hydrochloride hydrate exerts anti-inflammatory and immunomodulatory effects in systemic lupus erythematosus models by inhibiting the ROCK/NF-κB pathway. Y-27632 hydrochloride hydrate enhances autophagy by inhibiting the AKT/mTOR pathway, thereby inducing apoptosis apoptosis in oral squamous cell carcinoma. Y-27632 hydrochloride hydrate induces the formation of tunneling nanotubes in ARPE-19 cells and significantly enhances mitochondrial transfer through these channels. Y-27632 hydrochloride hydrate promotes neurite outgrowth in PC12 cells by activating the Rac1/NOX1/ROS/AKT/PAK1 signaling cascade.
    Y-27632 hydrochloride hydrate
  • HY-RS09996
    PAK5 Human Pre-designed siRNA Set A
    		Inhibitor

    PAK5 Human Pre-designed siRNA Set A contains three designed siRNAs for PAK5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    PAK5 Human Pre-designed siRNA Set A
  • HY-111103A
    CZh226 hydrochloride
    		Inhibitor
    CZh226 hydrochloride is a potent and selective PAK4 inhibitor with an IC50 of 18 nM, and its selectivity for PAK1 is 346 times. The oral bioavailability of CZh226 hydrochloride is poor, and it requires the use of the prodrug PAK4-IN-1 (HY-130628) to improve absorption and metabolic stability. CZh226 hydrochloride can be used for research on colorectal cancer and melanoma.
    CZh226 hydrochloride
  • HY-174822
    PAK4-IN-6
    		Degrader
    PAK4-IN-6 is a selective degrader of PAK4. PAK4-IN-6 can be used to synthesize PROTACs such as CPS-021 (HY-174247).
    PAK4-IN-6
  • HY-RS09994
    Pak4 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Pak4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pak4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Pak4 Mouse Pre-designed siRNA Set A
  • HY-119216
    AZ13711265
    		Inhibitor
    AZ13711265 is an orally active PAK1 inhibitor with high selectivity. AZ13711265 has IC50 values of 0.58 nM and 0.11 µM for PAK1 and pPAK1, respectively. AZ13711265 has low lipophilicity and low clearance, and can be used as an in vivo probe compound for PAK1. AZ13711265 can be used in the study of cancer.
    AZ13711265
  • HY-181769
    Anticancer agent 306
    		Activator
    Anticancer agent 306 is a spiro tetramic acid derivative and a inhibitor of MMP1, MMP7 and PLK1. Anticancer agent 306 exerts antiproliferative activity against H1299, RKO and MCF-7 cells with IC50 values of 19.25 μM, 3.29 μM and 102.36 μM, respectively. Anticancer agent 306 can up-regulate p21 protein and down-regulate CCND1 and CCNB1 proteins to induce cell cycle arrest, regulate the expression of Bcl-2 and Bax to induce cell apoptosis. Anticancer agent 306 can down-regulate MMP1 and MMP7 proteins to inhibit tumor invasion and metastasis. Anticancer agent 306 can be used for the research of lung cancer, colorectal cancer, breast cancer.
    Anticancer agent 306
  • HY-131265
    Mesalamine impurity P
    		Inhibitor
    Mesalamine impurity P is an impurity of Mesalamine (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
    Mesalamine impurity P
  • HY-181505
    BRD4-IN-12
    		Activator
    BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC50 of 7.9 nM. BRD4-IN-12 downregulates the expression of c-MYC, BCL-2, CDK4 and upregulates p21. BRD4-IN-12 inhibits tumor cell proliferation and promotes apoptosis. BRD4-IN-12 exhibits excellent antitumor effects in the HCT-116 colorectal cancer xenograft model. BRD4-IN-12 can be used for the study of colorectal cancer (CRC).
    BRD4-IN-12
  • HY-156453
    PAK4-IN-3
    		Inhibitor
    PAK4-IN-3(compound 27e) is aPAK4inhibitor, with theIC50of 10 nM.PAK4-IN-3shows antiproliferative activity against A549 cells with anIC50value of 0.61μM, and inducesapoptosisof A549 cells in a concentration-dependent manner and blocked the cell cycle at phase G0/G1.
    PAK4-IN-3
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
PAK Isoform Comparison

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