PF-06282999 is a selective myeloperoxidase Inhibitor originate by Pfizer. It showed good oral pharmacokinetics in preclinical species and robust irreversible inhibition of plasma MPO activity. In Mar 2015, Pfizer terminated phase I trial for the treatment of Acute coronary syndromes in Healthy volunteers in USA.
PF-04691502 is an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. It inhibits both PI3K and mTOR kinases, which may result in apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy. mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K.
PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen.
PF-04418948 is a potent and selective prostaglandin EP₂ receptor antagonist with IC50 of 16 nM. Phase 1. PF-04418948 antagonizes the effects of butaprost and PGE2 on an EFS-induced contraction of the human myometrium, and antagonizes PGE2-induced relaxation of carbachol pre-contracted rings of mouse trachea.
PF 429242 is a reversible and competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM), a transcriptional regulators of cholesterol, fatty acid, and glucose metabolism. It reduces hepatic synthesis of cholesterol and fatty acid in mice.
PF 06409577 is a potent and selective allosteric activator of AMPK (EC50 values are 7 and >40000 nM for AMPKα1β1γ1 and AMPKα1β2γ1, respectively) for the potential treatment of diabetic nephropathy. PF-06409577 showed efficacy in a preclinical model of diabetic nephropathy.
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. It has potential antineoplastic, anti-inflammatory, and antiangiogenic activities. It inhibits other kinases including vascular endothelial growth factor receptor (VEGFR2) and Src tyrosine kinases.
Pexidartinib is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R with IC50 of 20 nM, Kit with IC50 of 10 nM, and Flt3 with IC50 160 nM.
Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R with IC50 of 20 nM, Kit with IC50 of 10 nM, and Flt3 with IC50 160 nM. Phase 3, respectively.
Pevonedistat, also known as MLN-4924 and TAK-924, is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with potential antineoplastic activity.
Petunidin-3-arabinoside chloride is a remarkable natural compound, renowned for its illustrious anti-inflammatory and antioxidant attributes. This prodigious compound aids in studying cardiovascular afflictions and select malignancies.
Permethrin is a synthetic pyrethroid insectide, affecting neuron membranes by prolonging sodium channel activation. It is used for the treatment of infestation with Sarcoptes scabiei (scabies).
Perindopril Erbumine displays a higher binding affinity for the bradykinin binding sites than the angiotensin I binding sites of the angiotensin-converting enzyme (ACE) with bradykinin/angiotensin I selectivity ratio of 1.44.
Perifosine is an orally active alkyl-phosphocholine compound with potential antineoplastic activity. Targeting cellular membranes, perifosine modulates membrane permeability, membrane lipid composition, phospholipid metabolism, and mitogenic signal transduction, resulting in cell differentiation and inhibition of cell growth. This agent also inhibits the anti-apoptotic mitogen-activated protein kinase (MAPK) pathway and modulates the balance between the MAPK and pro-apoptotic stress-activated protein kinase (SAPK/JNK) pathways, thereby inducing apoptosis. Perifosine has a lower gastrointestinal toxicity profile than the related agent miltefosine.
Perfluoro(4-methylpent-2-ene) is an exceptional compound with diverse applications, particularly in the fabrication of various fluorinated polymers and resins like the ubiquitous Teflon. Furthermore, this specialty chemical is indispensable in the pharmaceutical and electronics industries. It holds immense potential in the synthesis of surfactants as well. Nonetheless, there is limited knowledge on its therapeutic benefits against drugs or pathologies.
Peretinoin, also known as NIK-333, orally available, acyclic retinoid with potential antineoplastic and chemopreventive activities. Peretinoin binds to and activates nuclear retinoic acid receptors (RAR), which in turn recruit coactivator proteins and promote, with other transcriptional complexes, the transcription of target genes. As a result, this agent may modulate the expression of genes involved in the regulation of cell proliferation, cell differentiation, and apoptosis of both normal and tumor cells.
2,6-Difluoro-4-[2-(phenylsul-fonyl-amino)-ethyl-thio]-phenoxy-acet-amide is a structurally novel, selective, high affinity AMPA ionotropic glutamate receptor agonist that reduces ischemia-induced performance deficits in rats.
Pentylamine-6-carboxyltetramethylrhodamine TFA salt, also called Xanthylium, 9-[5-[[(5-aminopentyl)amino]carbonyl]-2-carboxyphenyl]-3,6-bis(dimethylamino)-, inner salt, is a novel molecular rhodamine-type fluorescent probe.
An impurity of Sulbactam. Sulbactam is an irreversible inhibitor of β-lactamase; it binds to the enzyme and does not allow it to degrade the antibiotic.
Pemigatinib is an inhibitor of fibroblast growth factor receptor types 1, 2, and 3 (FGFR1/2/3). Under the brand name Pemazyre, it is used as a medication for the treatment of adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma.
An impurity of Pemetrexed, which has been approved by FDA in 2004 for the treatment of malignant pleural mesothelioma (MPM) in combination with cisplatin, a platinum-containing chemotherapeutic drug.
Peimisine is an alkaloid FR 5 from Fritillaria thunbergii, and an angiotensin converting enzyme inhibitory steroidal alkaloid. It is a commonly used antitussive and expectorant herb in traditional Chinese medicine.
Peficitinib is a potent JAK inhibitor with IC50 values of 3.9, 5.0, 0.71 and 4.8 nM for JAK1, JAK2, JAK3 and TYK2 enzyme activities, respectively. It inhibits the IL-2-induced proliferation of human T cells with IC50 value of 18 nM. Moreover, peficitinib is 14-fold more potent against JAK1/3 than JAK2/2 on the basis of EPO-induced proliferation of human leukemia cells. Peficitinib has been used for the treatment of psoriasis and rheumatoid arthritis.
PD-1-IN-17 is a programmed cell death-1 (PD-1) inhibitor. PD-1-IN-17 was first reported in patent WO2015033301A1, (Compound 12), inhibits 92% splenocyte proliferation at 100 nM.
PD-173955 is a src tyrosine kinase inhibitor. PD173955 inhibited Bcr-Abl-dependent cell growth. PD173955 showed cell cycle arrest in G(1). PD173955 has an IC(50) of 1-2 nM in kinase inhibition assays of Bcr-Abl, and in cellular growth assays it inhibits Bcr-Abl-dependent substrate tyrosine phosphorylation. PD173955 inhibited kit ligand-dependent c-kit autophosphorylation (IC(50) = approximately 25 nM) and kit ligand-dependent proliferation of M07e cells (IC(50) = 40 nM) but had a lesser effect on interleukin 3-dependent (IC(50) = 250 nM) or granulocyte macrophage colony-stimulating factor (IC(50) = 1 microM)-dependent cell growth.
PD173074 is a small-molecule FGFR3-selective tyrosine kinase inhibitor (TKI), as a therapeutic modality using eight UC cell lines. PD173074 suppressed cell proliferation remarkably in two cell lines, namely, UM-UC-14 and MGHU3, which expressed mutated FGFR3 protein. Cell cycle analysis revealed the growth inhibitory effect of PD173074 was associated with arrest at G(1)-S transition in a dose-depending manner. In the mouse xenograft models using subcutaneously transplanted UM-UC-14 and MGHU3, orally administered PD173074 suppressed tumor growth and induced apoptotic changes comparable with the results of our in vitro assay. These findings elucidated the effectiveness of molecular targeted approach for bladder UC harboring FGFR3 mutations and the potential utility to decrease the intravesical recurrence of nonmuscle invasive bladder UC after transurethral surgical resection.
PD-0325901 is a potent bioavailable and selective MEK inhibitor, which targets mitogen-activated protein kinase kinase (MAPK/ERK kinase or MEK) with potential antineoplastic activity. MEK inhibitor PD325901, a derivative of MEK inhibitor CI-1040, selectively binds to and inhibits MEK, which may result in the inhibition of the phosphorylation and activation of MAPK/ERK and the inhibition of tumor cell proliferation. The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors.
PC Spacer phosphoramidite can be used as an intermediate to link any modification reagent (which can be used as phosphoramidite) to the end of the oligonucleotide. After light cleavage, 5'-phosphate is generated on the DNA, making it suitable for further biotransformation, such as gene construction and cloning after ligation.
Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM, respectively.
Patisiran sodium is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran sodium specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran sodium can be used for the research of hereditary TTR amyloidosis.
