The p21-activated kinases (PAKs 1-6; EC are serine/threonine protein kinases whose activity is stimulated by the binding of active Rac and Cdc42 GTPases, both members of the Rho GTPase family of proteins, which are well established key regulators of cell migration and invasion processes involved in cancer metastasis, and control the formation of lamellipodia  and filopodia respectively. The GTPase-activated PAKs function as effectors through their kinase activity, and mediate downstream signalling events that bring about the physiological effects of GTPase signalling[1]. PAK1 acts as an key mediator to control cell proliferation, survival, death and motility. The PAK family members are categorized into two groups (PAK1-3, group I; PAK4-6, group II) based on their structural and biochemical discrepancies. In general, group I PAKs are comprised of two Src homology 3 (SH-3)-binding motifs and a distinctive p21/GTPase binding domain (PBD) overlapped with an auto-inhibitory domain (AID) at the N-terminal region and a conserved non-classical SH3-binding site for the binding of guanine-nucleotide-exchange factor PAK-interacting exchange factor (PIX). The kinase domain can be found at the C-terminal. In contrast, group II PAKs only have a PBD and a kinase domain[2].

[1] R. Kumar et al. p21-activated kinases in cancer. Nat Rev Cancer. 2006 Jun;6(6):459-71.
[2] E.Y. Tse et al. The role of p21-activated kinases in hepatocellular carcinoma metastasis. J Mol Signal. 2014 Aug 1;9:7.

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2669 AZ13705339 Potent and selective PAK1 inhibitor €125.00
2351 EHop 016 Rac GTPase inhibitor specific for Rac1 and Rac3 €85.00
1485 Fingolimod S1PR1 agonist; Immunosuppressant €60.00
2331 FRAX 486 Bioavailable, brain penetrating inhibitor of p21-activated kinases (PAKs) €90.00
3557 KPT-9274 Orally bioavailable dual PAK4/NAMPT inhibitor €130.00
3961 PF-03758309 Potent and ATP-competitive inhibitor of p21-activated kinase (PAK4) Inquire

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