An ATP-competitive inhibitor of PAK4

PF-3758309 – 5 mg

Brand:
Cayman
CAS:
898044-15-0
Storage:
-20
UN-No:
Non-Hazardous - /

p21-Activated kinases (PAKs) are STE20 serine/threonine kinases that are vital to normal cell function. Binding of various upstream partners to PAKs results in release of an autoinhibitory domain that blocks activity of the kinase domain.{23498} PAKs are upregulated in several human cancers and are potential therapeutic targets for cancer intervention.{23498} PF-3758309 is an ATP-competitive inhibitor of PAK4, preventing the phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and blocking anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM).{30920} It also inhibits the ability of kinase domains from other PAKs to phosphorylate peptide substrates (Kis = 18.1, 17.1, 13.7, 190, and 99 nM for PAKs 5, 6, 1, 2, and 3, respectively).{30920} PF-3758309 blocks the growth of multiple human tumor xenografts.{30920}  

 

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Description

An ATP-competitive inhibitor of PAK4, preventing the phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and blocking anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM); blocks the growth of multiple human tumor xenografts

Formal name: N-[(1S)-2-(dimethylamino)-1-phenylethyl]-4,6-dihydro-6,6-dimethyl-3-[(2-methylthieno[3,2-d]pyrimidin-4-yl)amino]-pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide

Synonyms:  PF-309

Molecular weight: 490.6

CAS: 898044-15-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling||Research Area|Cell Biology|ECM & Adhesion Molecules

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