p21-activated Kinase (PAK)|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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PAKs (p21-activated kinases) are key regulators of actin dynamics, cell proliferation and cell survival. PAKs are Ser/Thr kinases that are classified into two groups on the basis of their structural and functional features: group I (PAK1–3) and group II (PAK4–6). Group I PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain, CD) and are activated by the binding of the active (that is, GTP-bound) forms of Rho GTPases, such as Cdc42 and Rac1. Group II PAKs have no auto-inhibitory domains and are not activated by active Rho GTPases. Because the deregulation of PAKs is closely associated with various human diseases,small-molecule inhibitors of these kinases have great potential as therapeutic agents. In addition, these compounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway.

PAKs are considered prime regulators of the actin cytoskeleton and motility. Due to their central role in actin remodelling and their ability to activate Matrix metalloproteinases (MMPs), Rho GTPases play an important role in tumor cell invasion and metastasis. The current evidence suggests the involvement of PAKs in motility, cell survival, anchorage-independent growth, angiogenesis, invasion, migration and regulation of cell cycle and mitosis. Consequently, PAKs have also been implicated in a number of pathological conditions including cancer.

Cat. No.	Product Name	CAS No.	Information
H2183	PF-3758309	898044-15-0	PF-3758309 (PF03758309) is a potent, ATP-competitive p21-activated kinase (PAK) inhibitor with Ki of 18.7 nM, shows similar enzymatic potency against other group B PAKs (PAK5 Ki=18.1 nM, PAK6 Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), less active against PAK2 and PAK3 (IC50=190 nM and 99 nM); inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM); PF-3758309 inhibits PAK4-dependent pathways in proteomic studies and regulates functional activities related to cell proliferation and survival; blocks the growth of multiple human tumor xenografts.
H2182	LCH 7749944	796888-12-5	LCH 7749944 (GNF-PF-2356) is a novel and potent PAK4 with IC50 of 14.93 uM, shows weak activity against other PAK family members; effectively suppresses the proliferation, migration and invasion of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway; also inhibits the formation of filopodia and induces cell elongation in SGC7901 cells, causes successful inhibition of EGFR activity.
H2181	KY-04045	1223284-75-0	KY-04045 is a novel PAK4 inhibitor with IC50 of 8.7 uM, a basic building block in designing novel imidazo[4,5-b]pyridine-based PAK4 inhibitors.
H2180	KY-04031	468056-29-3	KY-04031 is a PAK4 inhibitor with IC50 of 0.79 uM, a basic building block in designing novel imidazo[4,5-b]pyridine-based PAK4 inhibitors.
H2179	KPT-9274	1643913-93-2	KPT-9274(Padnarsertib) is a potent, specific, dual NAMPT and PAK4 inhibitor with IC50 of 120 nM (NAMPT), also is an orally bioavailable PAK4 allosteric modulator with IC50 of 30 nM in MS-751 cell MTT assay; attenuates the PAK4/β-catenin pathway, results in NAD depletion, and attenuates viability, invasion, and migration in several RCC cell lines (IC50=600 nM for Caki-1 cells); attenuates G2/M transit and induces apoptosis, shows specificity for attenuation of NAD biosynthesis targets preferentially in RCC cells; decreases tumor growth in xenograft model of RCC.
H2178	IPP-14		IPP-14 is a novel PAK1 inhibitor that selectively blocks the PAK1-PUMA binding and suppresses cell proliferation via PUMA-dependent manner; suppresses cancer cell viability and migration, induces p21 expression and induces M-phase arrest by inhibition of PAK1; also induces p21/WAF1/CIP1 (Cyclin-dependent kinase inhibitor 1A) expression by releasing from Bcl-2 and by inhibition of AKT-mediated p21 suppression.
H2177	Hydrastine	118-08-1	An alkaloid of Hydrastis canadensis used in many dietary supplements intended to enhance the immune system; inhibits PAK4 kinase activity, suppresses the proliferation and invasion of human lung adenocarcinoma cells, inhibits expression of cyclin D1/D3 and CDK2/4/6, leading to cell cycle arrest at the G1 phase; also promotes the early apoptosis of lung adenocarcinoma cells through the mitochondrial apoptosis pathway.
H2176	GNE-2861	1394121-05-1	GNE-2861 is a potent, selective group II PAK (PAK4/5/6) inhibitor with IC50 of 7.5/126/36 nM, respectively, shows selectivity over group I PAKs (IC50=5.42/0.97/>10 uM for PAK1/2/3); decreases tumor cell migration and invasion in triple-negative breast cancer cell lines, perturbs estrogen receptor alpha signaling and restores tamoxifen-sensitivity in breast cancer cells.
H2175	GL-1196	591242-70-5	GL-1196 is a PAK4 inhibitor that effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclinD1 pathway and CDK4/6 expression; prominently inhibits the invasion of human gastric cancer cells in parallel with blockage of the PAK4/LIMK1/cofilin pathway; also inhibits the formation of filopodia and induced cell elongation in SGC7901 and BGC823 cells.
H2174	G-9791	1926204-95-6	A potent and selective group I PAK (pan-PAK1/2/3) inhibitor with Ki of 0.95/2 nM for PAK1/2, respectively; displays 57-fold selectivity over Lck kinase; inhibits the phosphorylation of residue S298 of MEK1 in EBC1 cells with IC50 of 33 nM.

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