PF-3758309 dihydrochloride_product_DataBase

Bioactivity	PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride 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].
Invitro	PF-3758309 dihydrochloride has similar enzymatic potency against the kinase domains of the other group B PAKs (PAK5, Ki=18.1 nM; PAK6, Ki=17.1 nM) and group A PAK1 (Ki=13.7 nM), but is less active against the other two group A PAKs (PAK2, IC50=190 nM; PAK3, IC50=99 nM)[1].In cells, PF-3758309 dihydrochloride inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50=1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50=4.7 nM)[1].PF-3758309 dihydrochloride also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50=20 nM) and anchorage-independent growth (IC50=27 nM) of A549 cells[1].
Name	PF-3758309 dihydrochloride
Formula	C25H32Cl2N8OS
Molar Mass	563.55
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.

PeptideDB