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PF-3758309
$66 – $480
Products Details
Product Description
– 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].
Web ID
– HY-13007
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C25H30N8OS
References
– [1]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.|[2]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.|[3]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|[4]Zhao ZS, et al. Do PAKs make good drug targets? F1000 Biol Rep. 2010 Sep 23;2:70.
CAS Number
– 898044-15-0
Molecular Weight
– 490.62
Compound Purity
– 99.84
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
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– DMSO : ≥ 100 mg/mL
Target
– Apoptosis;PAK
Isoform
– PAK1;PAK2;PAK3;PAK4;PAK5;PAK6
Pathway
– Apoptosis;Cell Cycle/DNA Damage;Cytoskeleton
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
