PF-3758309

PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM) . PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation[1][2][3].

Product Specifications

CAS Number

[898044-15-0]

Product Name Alternative

PF-03758309

UNSPSC

12352005

Hazard Statement

H302, H317

Target

Apoptosis; PAK

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Cytoskeleton

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PF-3758309.html

Concentration

10mM

Purity

99.79

Solubility

DMSO : ≥ 100 mg/mL

Smiles

CC1=NC2=C(SC=C2)C(NC3=NNC4=C3CN(C(N[C@@H](C5=CC=CC=C5)CN(C)C)=O)C4(C)C)=N1

Molecular Formula

C25H30N8OS

Molecular Weight

490.62

Precautions

H302, H317

References & Citations

[1]Murray, Brion W., et al. Small-molecule p21-activated kinase inhibitor PF3758309 is a potent inhibitor of oncogenic signaling and tumor growth. Proceedings of the National Academy of Sciences of the United States of America (2010), 107 (20), 9446-9451, S94|[2]Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70.|[3]Ryu BJ, et al. PF-3758309, p21-activated kinase 4 inhibitor, suppresses migration and invasion of A549 human lung cancer cells via regulation of CREB, NF-κB, and β-catenin signalings. Mol Cell Biochem. 2014 Apr;389 (1-2) :69-77.|[4]Pitts TM, et al. Association of the epithelial-to-mesenchymal transition phenotype with responsiveness to the p21-activated kinase inhibitor, PF-3758309, in colon cancer models. Front Pharmacol. 2013 Mar 28;4:35.