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
-
PAK Related Products (113)
Related Products (113)
-
Recombinant Proteins (4)
-
Antibodies (22)
-
PAK Isoform Comparison
-
WRN-IN-26
0 ImagesCat. No.: HY-183610CAS No.: 3059172-54-9WRN-IN-26 is an orally active Werner syndrome helicase (WRN) inhibitor with a human Ki value of 58.7 μM and an IC50 value of 0.026 μM. WRN-IN-26 selectively targets the cysteine residues of WRN. WRN-IN-26 induces the expression of p21 protein in MSI-H tumor cells. WRN-IN-26 inhibits the growth of MSI-H tumor cells and exhibits potent in vivo efficacy in MSI-H xenograft tumor models. WRN-IN-26 can be used for the research of microsatellite instability-high (MSI-H) cancers.
-
PS21M
0 ImagesCat. No.: HY-174248PS21M is a negative control PROTAC degrader derived from CPS-021, as well as an inhibitor of ternary complex formation. PS21M attenuates the interaction with Cereblon ligase, restricting the formation of the PAK4-PROTAC-Cereblon ternary complex and the subsequent degradation of PAK4. PS21M serves as a negative control molecule to verify the degradation mechanism of CPS-021.
-
AKT1-IN-13
0 ImagesCat. No.: HY-184145AKT1-IN-13 is an orally active AKT1 inhibitor with an IC50 of 5.17 μM. AKT1-IN-13 also exhibits high inhibitory activity against PAK1, PKA, MAP2K1 (MEK1 / MAPKK1) and MAPK1 (ERK2). AKT1-IN-13 induces cell apoptosis, activates the pro-apoptotic protein BAX, inhibits the anti-apoptotic protein Bcl-2, and activates caspase 3 simultaneously. As a cytotoxic agent, AKT1-IN-13 exerts a killing effect on orthotopically transplanted liver cancer in an AKT1-dependent manner. AKT1-IN-13 can be used in studies related to hepatocellular carcinoma.
-
PROTAC BRD4 Degrader-27
0 ImagesCat. No.: HY-162875CAS No.: 2407163-44-2PROTAC BRD4 Degrader-27 is a selective cereblon-mediated BRD4 PROTAC degrader. PROTAC BRD4 Degrader-27 exhibits anticancer activity, induces G1 phase arrest, and inhibits DNA synthesis and colony formation. PROTAC BRD4 Degrader-27 suppresses HCC1806 tumor growth in xenograft mouse models. PROTAC BRD4 Degrader-27 can be used in breast cancer-related research.
-
WC-2
0 ImagesCat. No.: HY-189009CAS No.: 3112500-81-6WC-2 is an ATP-competitive covalent WRN helicase inhibitor with IC50 values of 252 nM and 250 nM. WC-2 binds covalently to Cys727 of WRN helicase and maintains conformational complementarity with this protein. WC-2 induces p21 transcription as part of the DNA damage response, and selectively reduces the viability of MSI-H cancer cells. WC-2 can be used in the research of MSI-H tumors.
-
PF-3758309 hydrochloride
0 ImagesCat. No.: HY-13007ACAS No.: 1279034-84-2Synonyms: PF-03758309 hydrochloridePF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation.
-
GR2-128
0 ImagesCat. No.: HY-184396GR2-128 is a dual inhibitor targeting MLK3 and NAMPT with IC50 values of 84 nM and 14 nM, respectively. GR2-128 inhibits downstream JNK/c‑Jun signaling and reduces NAD+ levels. GR2-128 exhibits antiproliferative and pro-apoptotic activities in triple-negative breast cancer cells without significant toxicity to normal cells. GR2-128 suppresses tumor growth, reduces macrophage and neutrophil infiltration, and increases tumor T-cell markers in a syngeneic mouse model, and can be used for triple-negative breast cancer research.
-
Rac/Cdc42-IN-1
0 ImagesCat. No.: HY-183246CAS No.: 2143950-05-2Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr423/Thr402/Thr436 and Ser141/Ser144/Ser154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer.
-
RN193
0 ImagesCat. No.: HY-184447CAS No.: 3091508-49-2RN193 is a type II kinase inhibitor with a human PAK1 IC50 of 4.28 μM. RN193 functionally inhibits kinase activity of PAK1, PAK2, and PAK3, and engages with their kinase domains in live cells. RN193 induces thermal shifts in CLK1, GSK3B, ULK1, MELK, MAPK13, BRAF, and STK10, indicating binding and stabilization of these proteins. RN193 induces formation of PAK3:PAK2 heterodimers and displaces PAK2 homodimers in live cells. RN193 acts as a tool compound for studying group I PAK conformational states.
-
PAK4-IN-5
0 ImagesCat. No.: HY-159897PAK4-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.).
-
PF-3758309 dihydrochloride
0 ImagesCat. No.: HY-13007BSynonyms: PF-03758309 dihydrochloridePF-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.
-
CPS-021
0 ImagesCat. No.: HY-174247CPS-021 is a selective PAK4 PROTAC degrader with a DC50 of 50 nM. CPS-021 degrades PAK4 via the ubiquitin-proteasome system. CPS-021 inhibits the migration and invasion of tumor cells, suppresses TGFβ-induced epithelial-mesenchymal transition (EMT) in tumor cells, and can be used in studies related to lung cancer metastasis.
-
G-9791
0 ImagesCat. No.: HY-116917CAS No.: 1926204-95-6G-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.
-
PI3Kα-IN-27
0 ImagesCat. No.: HY-178812CAS No.: 2098649-83-1PI3Kα-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.
-
Anti-aging agent 2
0 ImagesCat. No.: HY-187429Anti-aging agent 2 is an anti-aging agent. Anti-aging agent 2 attenuates senescence-associated secretory phenotype (SASP), alleviates cell cycle arrest, reduces the levels of senescence markers in renal tissues, and downregulates the expression of p21, p16 and p53 in the kidney. Anti-aging agent 2 improves renal function and alleviates renal fibrosis. Anti-aging agent 2 extends the lifespan of Caenorhabditis elegans. Anti-aging agent 2 can be used in the research of chronic kidney disease.
