Pimonidazole, also known as Ro 03-8799 and PD 126675, is a nitroimidazole drug with hypoxic selectivity and radiosensitizing property. Pimonidazole is reduced in hypoxic environments as in tumor cells, thereby it can be used as an hypoxia marker. In hypoxic cells, reduced pimonidazole binds to -SH-containing molecules such as glutathione and proteins, and the resulting complexes accumulated in tissues, thereby sensitizing cells to be more susceptible for radiation treatment.
Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist. It has been used as an atypical antipsychotic in the treatment of psychosis associated with Parkinson's disease.
Pilaralisib, also known as XL147, is a methylbenzenesulfonamide derivative that reversibly inhibits class I PI3Ks (IC50s = 39, 36, 23, and 383 nM for p110α, δ, γ, and β, respectively), with potential antineoplastic activity.
PIK-75 is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM.
Picoplatin is a new generation organic platinum analog with an extended spectrum of antineoplastic activity. Designed to overcome platinum drug resistance, picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis.
Picfeltarraenin X is a triterpenoid compound isolated from the herbs of Picria felterrae Lour. Picfeltarraenin X exhibits inhibitory effect against AChE.
Picaridin,also known as Icaridin, KBR 3023, under the INCI name hydroxyethyl isobutyl piperidine carboxylate, and the trade names Bayrepel and Saltidin, is an insect repellent that is effective against a range of arthropods, including mosquitoes and ticks.
Physostigmine salicylate is a cholinesterase inhibitor that can cross blood-brain barrier. It forms slowly degrading carbamylated enzyme complex with acetylcholinesterase (AChE). It has been used to improve cognitive ability and treat glaucoma.
Physcion-1-O-β-D-glucoside is a diterpenoid compound. It is a by-product during the synthesis of Physcion 8-β-D-glucoside. Physcion 8-β-D-glucoside has been studied in research relating to the treatment of the glomerulonephritis. It is the glucoside of Physcion that is a natural anthraquinone derivative, on the infection process of Blumeria graminis on wheat. Physcion is one of the important active ingredients of ethanol extract from the roots of Chinese rhubarb (Rheum officinale) for controlling powdery mildew.
PHTPP, a pyrazolo[1,5-α]pyrimidine-based ligand, is a selective estrogen ERβ receptor antagonist that displays 36-fold selectivity over ERα. This compound has been used to selectively target ERβ in the study of the opposing effects of hormone therapy on tumors expressing either ER subtype.
Phosphoric acid 6,6'-di(9-anthryl)-1,1'-spirobiindan-7,7'-diyl ester is a chiral phosphoric acid catalyst for a variety of enantioselective transformations, especially for carbon-carbon and carbon-heteroatom bond-forming reactions.
Phosphoramidochloridic acid, N,N-dimethyl-, [(2S,6R)-6-[6-(benzoylamino)-9H-purin-9-yl]-4-(triphenylmethyl)-2-morpholinyl]methyl ester is a novel biomedical compound. With its unique molecular structure, it exhibits potential as a targeted therapeutic agent for treating various diseases.
Dimethyl ester of [(1S)-1-hydroxyethyl]-phosphonic acid is an intriguing derivative of phosphonic acid that has been analyzed extensively due to its potential as an anti-osteoporotic drug as well as its application as a chelating agent for heavy metal ions and a flame retardant for polymers. Its multifaceted usage makes it an attractive compound for further research and development.
(2-Ethylhexyl) diphenyl phosphate, an esteemed biomedical commodity, boasts of its versatility in the medical industry as a plasticizing agent employed in medical apparatuses, notably PVC tubing and blood bags, while also exhibiting efficacy in ameliorating a myriad of neurological illnesses, particularly Alzheimer's disease, thanks to its calcium modulating properties within the brain.
The chemical compound, Phospho(enol)pyruvic acid tri(cyclohexylammonium) salt, is a complex and multifaceted substance extensively utilized in the biomedical field for investigating ailments related to glycolysis, such as cancer and diabetes. Additionally, this compound acts as a pivotal substrate for enzymes, enabling the detection and diagnosis of these conditions.
Phenyl(1H-pyrrol-2-yl)methanone, a chemical entity utilized in the biomedicine domain as an intermediary in the preparation of drugs, exhibits promising anti-tumor properties and is being studied intensively for its potential in tackling diverse types of cancers. Its multifaceted therapeutic capabilities entail a comprehensive investigation aimed at establishing its clinical effectiveness.
Phenyl 4-O-acetyl-2,6-Di-O-benzoyl-1-thio-beta-thio-beta-D-galactopyranoside is a compound, exhibiting its paramount significance in delving deep into the enigmatic realms of glycosylation processes and the enthralling world of carbohydrate chemistry. It effortlessly assumes the dual roles of an eminent substrate in an immense array of biochemical assays, particularly those centered around the captivating realms of glycosyltransferases, glycosidases and various other riveting carbohydrate enzymes.
Phenyl 3,4,6-Tri-O-acetyl-2-deoxy-1-thio-2-(2,2,2-trichloroethoxyformamido)-b-D-glucopyranoside, an intricate chemical entity, is extensively employed in the realm of biomedical research. Its utilization spans diverse applications embracing the examination of pharmaceutical interplays and the formulation of remedies for numerous ailments. The compound possesses distinctive characteristics and exhibits intricate phenomena, thereby enabling comprehensive inquiries into drug metabolism, protein binding, and receptor interactions.
Phenyl 2-hydroxy-4,5-dimethoxybenzoate is an impurity of Acotiamide, a drug for the treatment of postprandial fullness, upper abdominal bloating, and early satiation due to functional dyspepsia.
Phenyl 2,3,4,6-tetra-O-acetyl-a-D-glucopyranoside is an essential biochemical reagent involved in the synthesis of glycosides and glycosidase inhibitors with potential anti-cancer properties. Leveraging it as a substrate for enzyme assays makes it a valuable addition to research experiments. Caution must be exercised as it is not intended for human consumption and requires careful handling. The multifaceted nature of this product showcases a complex interplay of chemical functionalities, which in turn further reinforces its importance as a key biochemical reagent.
Phensuximide is an anticonvulsant drug. It can be used for the treatment of neurological disorders stemming from the brain. Phensuximide can suppress the paroxysmal three cycle per second spike and wave EEG pattern associated with lapses of consciousness in petit mal seizures.
Phellodendrine chloride can be found in the peel of Phellodendron amurense Rupr. Phellodendrine was effective in crescentic-type anti-GBM nephritis and the antinephritic mechanisms of this agent may be due to its ability to inhibit the proliferation or the migration of macrophages and cytotoxic T lymphocytes in the glomeruli.
PFK15 is a potent and selective inhibitor of 6-phosphofructo-2-kinase (PFKFB3) with IC50 of 207 nM. Overexpression of the PFKFB3 enzyme leads to high glycolytic metabolism, which is required for cancer cells to survive in the harsh tumor microenvironment.
PFI-3, a potent and selective SMARCA2/4 bromodomain inhibitor, is a cell-permeable probe that binds avidly to the structurally-similar SMARCA4 bromodomain (Kd= 89 nM) and PB1(bromodomain 5) (Kd= 48 nM).
PF-8380 blocks inflammation-induced LPA synthesis. PF-8380 works both in vitro and in vivo through direct inhibition of autotaxin. In human whole blood PF-8380 inhibited autotaxin with an IC50 of 101 nM. Inhibition of ATX by PF-8380 led to decreased invasion and enhanced radiosensitization of GBM cells. Radiation-induced activation of Akt was abrogated by inhibition of ATX. Furthermore, inhibition of ATX led to diminished tumor vascularity and delayed tumor growth. PF-8380 can serve as a tool compound for elucidating LPA's role in inflammation.
PF-670462 is a potent and selective inhibitor of CK1ε in isolated enzyme preparations. It inhibits PER protein nuclear translocation causing phase shifts in circadian rhythms and attenuates methamphetamine-stimulated locomotion in vivo. It less effectively inhibits a wide variety of related or common kinases. It disrupts circadian rhythms in cells and animals and blocks the locomotor response to amphetamines in mice. It remains unclear whether one of the kinases has a predominant role in regulating the circadian clock.
PF-562271 is a potent, ATP-competitive, reversible inhibitor of FAK with IC50 of 1.5 nM, ~10-fold less potent for Pyk2 than FAK and >100-fold selectivity against other protein kinases, except for some CDKs.
PF-5190457 is a selective Growth hormone secretagogue receptor inverse agonist and it can increase insulin secretion in glucose-stimulated human islets. No recent reports of development were reported for phase-I development in Type-2-diabetes-mellitus.
PF-4136309 is a potent, selective, and orally bioavailable antagonist of CCR2, a chemokine receptor of the super family of seven-transmembrane G-protein-coupled receptors (GPCRs).
PF-3084014 is a selective γ-secretase inhibitor (IC50 = 6.2 nM in a cell-free assay). It has been shown to inhibit self-renewal and proliferation of cancer stem cells.
PF-1355 is a selective, mechanism-based inhibitor of myeloperoxidase (MPO) (IC50 = 1.5 μM in LPS-stimulated human whole blood) with excellent selectivity for MPO without disrupting a panel of 50 receptors, enzymes, ion channels and transporters, including thyroid peroxidase. PF-1355 was used to test the hypothesis that MPO activity is a critical mediator of disease activity in immune complex vasculitis mouse models, and to support the confidence in rationale for this mechanism as a therapeutic approach to treat related human condition such as alleviating tissue injury caused by Goodpasture syndrome and pulmonary vasculitis induced by immune complexes.
PF-07321332 is an orally available SARS-CoV 3C-like protease (3CLPRO) inhibitor. 3C-like protease (3CLPRO) is the main protease found in coronaviruses, which cleaves the coronavirus polyprotein at eleven conserved sites. PF-07321332 has demonstrated oral activity in a mouse-adapted SARS-CoV-2 model and has achieved oral plasma concentrations exceeding the in vitro antiviral cell potency in a phase I clinical trial in healthy human participants.
PF-06651600 is a selective JAK3 inhibitor with IC50 value of 0.346 nM. It was shown to inhibit Th1 and Th17 cell differentiation and function in vitro.
PF-06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), which is an omnipresently expressed serine/threonine kinase involved in the regulation of innate immunity. PF-06650833 is useful for the treatment of autoimmune and inflammatory diseases associated with lnterleukin-1 Receptor Associated Kinase (IRAK) and more particularly modulates the function of IRAK. It is undergoing testing in a Phase II clinical study.