pf-04554878 hydrochloride

PF-3758309 hydrochloride (PF-03758309 hydrochloride) , is a PAK4 inhibitor, is also a n orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity. PF-3758309 hydrochloride binds to PAK4, inhibiting PAK4 activity and cancer cell growth. PAK4, a serine/threonine kinase belonging to the p21-activated kinase (PAK) family, is often upregulated in a variety of cancer cell types and plays an important role in cancer cell motility, proliferation, and survival.

PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.

PF-562271 hydrochloride (PF-562271 HCl) is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM in cell-free assays, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.

Defactinib hydrochloride (PF 04554878 hydrochloride) is a novel inhibitor of FAK. Which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner.

PF-06815345 hydrochloride, an orally active potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9), has an IC50 value of 13.4 μM. It significantly decreases in vivo PCSK9 levels in mice.

PF-05236216 hydrochloride is a brain penetrant, potent and selective inhibitor of casein kinase 1 delta/epsilon (CK1δ/ε) that modulates circadian rhythms in mice.

PF-CBP1 hydrochloride (PF-CBP1 HCl) is a highly selective inhibitor of the bromodomain of CREB-binding protein(CREBBP).It inhibits CREBBP and p300 bromodomains with IC50 of 125 and 363 nM respectively.

PF-00356231 hydrochloride is an inhibitor of matrix metalloproteinase MMP-12 with IC50 of 1.4 μM.

Potent and selective PDE8B/8A inhibitor ( IC50 values are 1.3 and 1.9 nM, respectively). Exhibits selectivity for PDE8A/B over other PDEs (IC50 values are >10 μM) and a range of other targets. Increases glucose-dependent insulin secretion from human pacreatic islet cells. Orally bioavailable. DeNinno et al (2012) Discovery of triazolopyrimidine-based PDE8B inhibitors: exceptionally ligand-efficient and lipophilic ligand-efficient compounds for the treatment of diabetes. Bioorg.Med.Chem.Lett. 22 5721 PMID:22858141

PF-03246799 hydrochloride is a potent serotonin 5-HT2C receptor agonist.

PF-5274857 hydrochloride is a potent, orally active, selective, blood-brain barrier permeable Smo antagonist with IC50=5.8 nM and Ki=4.6 nM. It has research potential in a variety of tumors including brain tumors and brain metastases driven by activated Hh pathways.

PF-8380 hydrochloride is a powerful inhibitor of autotaxin, exhibiting an IC(50) of 2.8 nM in isolated enzyme assays and 101 nM in human whole blood.

casein kinase 1ε inhibitor

PF-06446846 hydrochloride, an orally active and highly selective inhibitor, targets Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) translation by inducing ribosomal stalling at approximately codon 34, effectively suppressing PCSK9 expression.