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PAK

PAK

PAKs (p21-activated kinases) are a family of six serine/threonine kinases that act as key effectors of RHO family GTPases in mammalian cells. Based on their domain architecture and regulation, PAKs are divided into two groups: group I (PAK1, PAK2, and PAK3) and group II (PAK4, PAK5, and PAK6). GTPases like Cdc42, Rac, TC10, CHP, and Wrch-1, as well as other GTPases independently of GTPases, activate Group I PAKs. Cdc42/Rac binding typically does not activate Group II PAKs. Members of the PAK family have been linked to a variety of diseases, including cancer, infectious diseases, and neurological disorders. PAK plays critical roles in cytoskeletal organization, cellular morphogenesis, and survival.

PAKs take part in a number of signaling networks. Along with NF-B, phosphorylating Raf1 by PAKs activates the MAPK pathway. Other cytoskeleton regulators phosphorylated by PAKs include MLCK, LIMK, filamin A, ILK, merlin, and Arpc1b. Additionally, PAKs control apoptotic and survival pathways by phosphorylating their effectors, like DLC1 and BimL. Gene transcription is directly impacted by PAKs after they move to the nucleus. PAK1 is a substrate for a number of transcription factors and transcriptional co-regulators, including FKHR, SHARP, CTBP1, and SNAI1. Through the phosphorylation of histone H3, Aurora A, and PlK1, PAKs also control the progression of the cell cycle.

PAK related products

Structure Cat No. Product Name CAS No. Product Description
FRAX597 V1595 FRAX597 1286739-19-2 FRAX597 (FRAX-597;FRAX 597) is a novel, potent and ATP-competitive inhibitor of group I PAKs (p21-activated Kinases) with potential anticancer activity.
IPA-3 V1593 IPA-3 42521-82-4 IPA-3 (IPA3; IPA 3) is a novel, potent, selective and non-ATP competitive PAK1 (p21-activated protein kinase 1) inhibitor with potential antitumor activity.
LCH-7749944 V23834 LCH-7749944 796888-12-5 LCH-7749944, formerly known as GNF-Pf-2356, is a novel and highly potent PAK4 inhibitor with an IC50 of 14.93 μM.
PF-3758309 V1594 PF-3758309 898044-15-0 PF-03758309 (PF03758309;PF-3758309;PF 03758309;PF3758309), apyrrolopyrazole analog, is a novel, potent, orally bioavailable, and ATP-competitive small molecule inhibitor of PAK4 (p21-activated kinase 4) with potential antineoplastic activity.
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