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Product Description
– PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride 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-13007A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C25H31ClN8OS
References
– [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.
CAS Number
– 1279034-84-2
Molecular Weight
– 527.08
SMILES
– O=C(N1C(C)(C)C2=NNC(NC3=C4C(C=CS4)=NC(C)=N3)=C2C1)N[C@@H](C5=CC=CC=C5)CN(C)C.[H]Cl
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Apoptosis;PAK
Isoform
– PAK1;PAK2;PAK3;PAK4;PAK5;PAK6
Pathway
– Apoptosis;Cell Cycle/DNA Damage;Cytoskeleton
Product type
– Reference compound
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