P-PH

Bioactive Small Molecules

O | P-PH | PI-PZ | Q

Product #

Image

Product Name

Biochem/physiol Actions

Gene Symbol (ID)

Add to Cart

SML0543   p38 MAP Kinase Inhibitor IV ≥98% (HPLC) p38 MAP Kinase Inhibitor IV is an ATP-competitive inhibitor of p38α/β MAPK with IC50 values of 130 nM for p38α and 550 nM for p38β. It is much less active with ≤23% inhibition at 1 μM against p38γ/σ, ERK1/2, and JNK1/2/3. Shown to be more effective than SB 203580 in inhibiting LPS-induced IL-1β release from hPBMC (100% vs. 50% inhibition with 100 μM inhibitor). A recent study showed that p38 MAP Kinase Inhibitor IV could consistently and significantly enhance reprogramming and iPS cell generation from somatic cells.
 
SML0770   P5091 ≥98% (HPLC) P5091 is a cell permeable, potent and specific inhibitor of deubiquitylating enzyme USP7 (Ubiquitin-Specific Protease-7) that induces HDM2 polyubiquitylation and accelerates degradation of HDM2. P5091 induces apoptosis in MM cells resistant to conventional and bortezomib therapies. P5091 inhibits tumor growth and prolongs survival in animal models of cancer.
 
D8446 P7C3 ≥98% (HPLC) P7C3 is neurogenic and protects new neurons against apoptosis. These activities may be related to its capacity to protect mitochondrial integrity.

Degeneration of the hippocampus is an early manifestation of Alzheimer′s disease. P7C3 promotes neurogenesis in the subgranular zone of the hippocampal dentate gyrus, the site of normal neurogenesis in adult mammals, making it an important lead compound in development of new Alzheimer′s treatments.
 
SML1290   PA-824 ≥98% (HPLC) PA-824 is an anti-tuberculosis drug that exhibits multiple mechanism of action including both cell wall inhibition and respiratory poisoning.
PA-824 is an anti-tuberculosis drug that exhibits multiple mechanism of action, including both cell wall inhibition and respiratory poisoning.
 
P0115 PAC-1 ≥98% (HPLC) PAC-1 is a caspase 3 activator. Caspase activation is a key strategy in cancer therapy. Caspase 3 is a key executioner caspase and direct effector of apoptosis. Hallmark of many cancers is the circumvention of signal in the activation of executioner caspases and loss of apoptotic response. EC50 for caspase 3 activation = 0.33 μM and caspase 7= 4.5 μM. The IC50 for apoptosis induction = 0.92 μM. Elevated caspase 3 level in cancerous cell lines and tissues allows PAC-1 to selectively induce apoptosis in tissues.
 
SML1470 PACA ≥98% (HPLC) PACA is a potentiator of NGF-induced neurite outgrowth that attenuates 6-hydroxydopamine (6-OHDA) neurotoxicity in dopaminergic PC12 cells. PACA induced the nuclear translocation of transcription factor Nrf2 and the expression of antioxidant heme oxygenase-1 (HO-1).
 
T7402 Paclitaxel from Taxus brevifolia, ≥95% (HPLC), powder Paclitaxel is a potent anti-neoplastic and anti-mitotic taxane drug, which binds to the N-terminus of β-tubulin and and stabilizes microtubules arresting the cell cycle at the G2/M phase. The microtubule damage induces apoptosis through a JNK-dependent pathway followed by a JNK-independent pathway, perhaps related to the activation of protein kinase A (PKA) or of Raf-1 kinase, resulting in phosphorylation of Bcl-2. A major metabolite via CYP2CB is 6α-hydroxypaclitaxel (6α-OHP).
human ... BCL2(596)
T1912 Paclitaxel from Taxus yannanensis, powder Paclitaxel is a potent anti-neoplastic and anti-mitotic taxane drug, which binds to the N-terminus of β-tubulin and and stabilizes microtubules arresting the cell cycle at the G2/M phase. The microtubule damage induces apoptosis through a JNK-dependent pathway followed by a JNK-independent pathway, perhaps related to the activation of protein kinase A (PKA) or of Raf-1 kinase, resulting in phosphorylation of Bcl-2. A major metabolite via CYP2CB is 6α-hydroxypaclitaxel (6α-OHP).
human ... BCL2(596)
T7191 Paclitaxel from semisynthetic (from Taxus sp.), ≥97% Paclitaxel is a potent anti-neoplastic and anti-mitotic taxane drug, which binds to the N-terminus of β-tubulin and and stabilizes microtubules arresting the cell cycle at the G2/M phase. The microtubule damage induces apoptosis through a JNK-dependent pathway followed by a JNK-independent pathway, perhaps related to the activation of protein kinase A (PKA) or of Raf-1 kinase, resulting in phosphorylation of Bcl-2. A major metabolite via CYP2CB is 6α-hydroxypaclitaxel (6α-OHP).
human ... BCL2(596)
SML0838 PACMA 31 ≥98% (HPLC) PACMA 31 is an orally bioavailable, selective inhibitor (IC50 = 10 μM) of protein disulfide isomerase (PDI), an endoplasmic reticulum protein that regulates oxidative protein folding by catalyzing the breakage and reformation of disulfide bonds. PDI is upregulated in ovarian, and several other cancers. PACMA 31 dose dependently inhibits proliferation of OVCAR-8 in culture and in a tumor xenograft model.
 
PZ0182 Pactamycin ≥95% (HPLC) Pactamycin is a potent protein synthesis inhibitor, inhibiting protein synthesis at the translocation step on the 70S ribosome. It has activity against Gram-positive and Gram-negative bacteria, and broad antitumor, antiviral, and antiplasmodial activity. Cytotoxicity limits it clinical use.
 
P0064 PalGly ≥98% (HPLC), solid PalGly is an endogenous signaling lipid that modulates calcium influx and nitric oxide production. PalGly inhibits heat-evoked firing of wide dynamic range (WDR) neurons, activates calcium influx in DRG cells and stimulates NO production. Preliminary studies suggest its signaling mechanism involves GPCR-mediated cation channel activation and a Gαi/o-coupled signaling pathway, which is being further investigated.
 
P0099 Paliperidone ≥98% (HPLC) Paliperidone is an atypical antipsychotic; active metabolite of risperidone.
 
H4648 1-O-Palmitol-2-(N-methylcarbamyl)-sn-glycero-3-phosphocholine ≥98% (TLC), white powder Nonhydrolyzable form of PAF[C16]. Activates platelets and exhibits potent inflammatory activity, mediator of cellular damage due to cerebral ischemia.
 
P4509 Palmitoyl-DL-carnitine chloride powder Long-chain acylcarnitine and well-known intermediate in mitochondrial fatty acid oxidation. Modifies myocardial levels of high-energy phosphates and free fatty acids in the heart. Increases erythroid colony formation in culture. Reduces surface negative charge of erythrocytes and myocytes. Reported to affect currents and inhibit endothelium-dependent relaxation induced by acetylcholine and substance P in a dose dependent manner by suppressing the intracellular calcium signal transduction in endothelial cells.
 
P9716 Palmitoyl coenzyme A lithium salt ≥90% Long chain fatty acid (C16) covalently linked to Coenzyme A. Covalent attachment of palmitate is a common occurrence on a wide variety of viral and cellular proteins and plays a role in promoting membrane binding. Palmitoylation may also be a general mechanism for prolonging or potentiating G-protein signaling.
 
P0359 Palmitoylethanolamide Endogenous CB2 cannabinoid receptor agonist.
human ... CNR1(1268), CNR2(1269)
rat ... Faah(29347)
L5016 1-O-Palmityl-sn-glycero-3-phosphocholine ≥99%, synthetic Intermediate in the synthesis of platelet activating factor (PAF). Inactive form that can be used as a control in studies of PAF activity.
 
SML0801   Palomid 529 ≥98% (HPLC) Palomid 529 (P529) is a PI3K/Akt/mTOR inhibitor, which is unique in that it causes the dissociation of both the TORC1 and TORC2 complexes and inhibits both Akt and mTOR signaling. Palomid 529 has been shown to inhibit tumor growth, angiogenesis, and vascular permeability. Palomid 529 (P529) inhibited glioblastoma growth, penetrating the blood brain barrier with little affinity for ATP-binding cassette (ABC) drug efflux transporters ABCB1 and ABCG2. Palomid 529 has also shown promise as a possible treatment for macular degeneration and keloid disease.
 
SML1195 Palonosetron hydrochloride ≥98% (HPLC) Palonosetron is a potent and selective 5-HT3 receptor antagonist (Aloxi) used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
 
P2371 Pamidronate disodium salt hydrate ≥95% (NMR), solid Bone resorption inhibitor; inhibitor of farnesyl diphosphate synthase (IC50 = 200 nM).
 
P1918 Pancuronium bromide Aminosteroidal neuromuscular blocking agent; skeletal muscle relaxant
 
SML0726   Panepoxydone from Lentinus conatus, ≥95% (HPLC) Panepoxydone is a fungal metabolite that inhibits NF-κB transcription factor by preventing IκB phosphorylation, thus inhibiting the release of NF-κB from the IκB : NF-κB complex and its translocation into the nucleus. Panepoxydone also has antimalarial, cytotoxic activities and anti-parasitic activity against Trypanosoma cruzi.
 
P0021 Pantoprazole sodium hydrate ≥98% (HPLC) Pantoprazole is a gastric proton pump inhibitor.
 
P3510 Papaverine hydrochloride powder Smooth muscle relaxant and cerebral vasodilator; phosphodiesterase inhibitor.
human ... PDE4B(5142)
SML1876 PaPE-1 ≥98% (HPLC) PaPE-1 is a "Pathway Preferential Estrogen" that activates the extranuclear signaling pathway without activating the nuclear signaling pathway. PaPE-1 bound 50,000-fold less well to ERα and Erβ estrogen receptors. PaPE-1 activated extranuclear-initiated ER-regulated genes, but showed essentially no activation of nuclear-initiated estrogen receptor (ER) gene targets such as the progesterone receptor. Unlike estradiol (E2), PaPE-1 did not stimulate proliferation of MCF-7 breast cancer cells. Like estradiol, PaPE-1 strongly activated MAPK and mTOR pathway. Instead, it showed preferential estrogen-like activity in non-reproductive (metabolic and vascular) tissues, reducing body weight gain and fat accumulation in ovariectomized mice and accelerating repair of endothelial damage in the vascualture.
 
UC448 Paracetamol sulfate potassium salt solid, ≥97% (HPLC) Phase II metabolite of paracetamol.
 
P8013 Pargyline hydrochloride Selective MAO-B inhibitor.
human ... MAOB(4129)
P9623 Paroxetine hydrochloride hemihydrate ≥98% (HPLC), powder Paroxetine hydrochloride hemihydrate is one of the most potent and selective of the selective serotonin reuptake inhibitors (SSRI); antidepressant
 
P1372 Paroxetine maleate salt ≥98% (HPLC), solid Paroxetine maleate is a selective serotonin reuptake inhibitor; antidepressant.
 
P0667 Parthenolide ≥98% (HPLC) Anti-inflammatory agent that inhibits NF-κB activation.
human ... ELA2(1991), IKBKG(8517), NFKB1(4790), NKAP(79576), NKRF(55922)
P5806   Pasteurella multocida toxin lyophilized powder    
P2928 Paxilline powder, ≥98% (HPLC) Selective blocker of high-conductance Ca2+-activated (Maxi-K) potassium channels
 
P9246 PB28 dihydrochloride ≥98% (HPLC), solid Selective σ2 opioid receptor ligand; putative σ2 agonist
 
SML1058   PBIT ≥98% (HPLC) PBIT is a potent inhibitor of JARID1B (KDM5B) histone lysine demethylase that inhibits removal of H3K4me3 in UACC-812 cells. PBIT inhibits proliferation of cells overexpressing JARID1B. PBIT is selective for JARID1 enzymes and does not inhibit demethylases UTX or JMJD3.
 
B4688 PBPE hydrochloride ≥98% (HPLC) PBPE is a selective ligand of anti-estrogen binding site (AEBS) (Ki=1.2 nM).
 
SML0730   PCNA-I1 ≥98% (HPLC) PCNA-I1 is a small molecule PCNA inhibitor that selectively binds to PCNA trimers and reduces the association of PCNA with chromatin. PCNA-I1 induces S and G2/M phase cell cycle arrest in tumor cells with greater efficacy than non-transformed cells.
 
SML1848 PCS1055 dihydrochloride ≥98% (HPLC) PCS1055 is a potent and selective muscarinic M4 acetylcholine receptor competitive antagonist that exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 was originally described as a potent electric eel AChE inhibitor (IC50 = 22 nM) and less potent at human AChE (IC50 = 120 nM).
 
PZ0162 PD 0325901 ≥98% (HPLC) PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. The Ki is 1.1 and 0.79 nM for MEK1 and MEK2, respectively. PD 0325901 was inactive against a panel of 27 other kinases. PD 0325901 inhibited C26 tumor pERK by 75% when dosed at 25 mg/kg in mice.
 
PZ0199 PD 0332991 isethionate ≥98% (HPLC) PD 0332991 is a potent selective inhibitor of cyclin dependent kinases CDK4 and CDK6 with in vitro IC50 = 11 nM (CDK4) and 16 nM (CDK6). PD 0332991 induces G1 arrest in retinoblastoma (Rb)-positive tumor cells.
 
P215 PD 98,059 solid Specific inhibitor of the activation of mitogen-activated protein kinase kinase (MAPKK).
human ... MAP2K1(5604), MAP2K2(5605), MAP2K3(5606), MAP2K4(6416), MAP2K5(5607), MAP2K6(5608), MAP2K7(5609), MAP3K1(4214), RAF1(5894)
P5624 PD-118057 ≥98% (HPLC), solid PD-118057 is an activator of ether-a-go-go-related (hERG) potassium channel. PD-118057 is a second identified hERG channel activator, a representative in the series of structural analogs; PD-118057 at 10 μM leads to a 111% current increase in rabbit ventricular wedge (in comparison RPR260243 leads to only a 15% increase at the same concentration);PD-118057, unlike RPR260243, does not have a major effect on gating or kinetic properties of this channel. PD-118057prevents and reverses QT interval prolongation; Compounds such as PD-118057 may offer new approach in the treatment of delayed repolarization conditions, which occur in inherited or acquired long QT syndrome and congestive heart failure
 
P5749 S-(+)-PD 123177 trifluoroacetate salt hydrate ≥98% (HPLC), solid S-(+)-PD 123177 is selective AT2 angiotensin receptor antagonist. The angiotensin AT2 receptor is an atypical seven transmembrane domain receptor that is coupled to activation of tyrosine phosphatase and inhibition of MAP kinase, and does not undergo agonist-induced internalization. An investigation of the occurrence and nature of AT2 receptor phosphorylation revealed that phorbol ester-induced activation of protein kinase C (PKC) in HA-AT2 receptor-expressing COS-7 cells caused rapid and specific phosphorylation of a single residue (Ser354) located in the cytoplasmic tail of the receptor. Agonist activation of AT2 receptors by angiotensin II (Ang II) also caused rapid PKC-dependent phosphorylation of Ser354 that was prevented by the AT2 antagonist, S-(+)-PD 123177, and by inhibitors of PKC. In cells coexpressing AT1 and AT2 receptors, Ang II-induced phosphorylation of the AT2 receptor was reduced by S-(+)-PD 123177 and abolished by treatment with both antagonists or with PKC inhibitors. These findings indicate that the AT2 receptor is rapidly phosphorylated via PKC during homologous activation by Ang II, and also undergoes heterologous PKC-dependent phosphorylation during activation of the AT1 receptor.
 
P183 (+)-PD 128,907 hydrochloride >97%, solid Selective D3 dopamine receptor agonist.
human ... DRD3(1814)
P216 (±)-PD 128,907 hydrochloride solid, ≥98% (HPLC) Selective D3 dopamine receptor agonist.
human ... DRD3(1814)
P4620 PD 146176 ≥98% (HPLC), solid 15-Lipoxygenase inhibitor
human ... ALOX15(246)
mouse ... ALOX15(11687)
rat ... ALOX15(81639)
PZ0175 PD 149163 tetrahydrochloride hydrate ≥95% (HPLC) PD 149163 is a Neurotensin NTR1 receptor agonist; a Neurotensin (8-13) analog. PD149163 is a selective, brain penetrating NT1 receptor agonist with pro-cognitive, antipsychotic and anxiolytic effects.
 
D5946 PD 150606 ≥97% (HPLC) PD 150606 is a selective; cell-permeable; non-peptide; uncompetitive calpain inhibitor.
 
SML0402 PD 151746 ≥98% (HPLC) PD 151746 is a potent inhibitor of calpains 1 and 2.
 
SML0564 PD153035 hydrochloride ≥98% (HPLC) PD153035 is apotent and selective ATP competitive inhibitor of the epidermal growth factor receptor tyrosine kinase EGFR.
 
PZ0141 PD-156707 ≥98% (HPLC) PD-156707 is a selective endothelin receptor (ETA) antagonist.
 
B7063 PD158780 ≥98% (HPLC) PD158780 is a potent, cell-permeable, reversible ATP-competitive inhibitor of EGFR tyrosine kinase activity with IC50 values of 0.008, 49 and 52 nM for EGFR, ErbB2 (HER2) and Erb4 (HER4).
 
PZ0109 PD-161570 ≥98% (HPLC) PD-161570 is an inhibitor of human FGF-1 receptor tyrosine kinase.
 
PZ0144 PD-161989 2-Hydroxyethanesulfonate ≥98% (HPLC) PD-161989 is an AMPA receptor antagonist.
 
PZ0116 PD-166285 hydrate ≥98% (HPLC) PD-166285 hydrate is a broad spectrum protein tyrosine kinase inhibitor; Src and FGFR kinase inhibitor.
 
P0047 PD166793 hydrate ≥98% (HPLC) PD166793 is a broad spectrum, but class-selective, MMP inhibitor (low nM at MMP-2 & 3 and low μM at MMP-1, 7 & 9). Adding PD166793 to the high-fat diet substantially reduced the rise in blood glucose. The improvement of glucose homeostasis in PD166793-treated ZDF rats was a result of the enhancement of β-cell function. It prevents β-cell dysfunction and diabetes in female ZDF rats on a high-fat diet. It has been shown to block left ventricular remodeling and dysfunction in a rat model of heart failure. Preservation of normoglycemia and normal glucose tolerance in compound PD166793-treated animals is accompanied by preservation of the high serum insulin levels that are a consequence of the insulin resistance present in these animals. It is not reversing insulin resistance these animals. The most striking effect of the compound is on pancreatic insulin content and β-cell volume.
 
PZ0114 PD-166866 ≥98% (HPLC) PD-166866 is a selective inhibitor of the FGF-1 receptor tyrosine kinase (FGFR1) with IC50 = 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
 
P233 PD 168,077 maleate salt powder Selective D4 dopamine receptor agonist.
human ... DRD4(1815)
PZ0285 PD168393 ≥98% (HPLC) PD168393 is potent, cell-permeable, irreversible and selective inhibitor of EGF receptor (EGFR) tyrosine kinase and ErbB2. PD168393 has an IC50 value of 0.70 nM for EGFR, and is inactive against insulin, PDGFR, FGFR and PKC.
 
P9248 PD 169316 ≥98% (HPLC), solid Potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).
human ... MAPK14(1432)
P2499 PD 173074 ≥96% (HPLC), powder PD 173074 is a fibroblast growth factor receptor 3 (FGFR3) inhibitor: IC50 = 5 nM inhibition of FGFR3 autophosphorylation. PD 173074 arrests the G0/G1 phase of FGFR3-expressing cells. It is 100-fold more selective for FGFR3 than for VEGF receptors, IGF-1 receptors, and MAPKs.
human ... FGFR1(2260), KDR(3791)
mouse ... Pdgfrb(18596)
PZ0113 PD173952 ≥98% (HPLC) PD173952 is a Src family kinase inhibitor.
 
PZ0142 PD-180970 ≥98% (HPLC) PD-180970 is a potent inhibitor of the p210 Bcr-Abl tyrosine kinase.
 
PZ0112 PD-184161 ≥98% (HPLC) PD-184161 is a MEK inhibitor.
 
PZ0181 PD184352 ≥98% (HPLC) PD184352 (CI-1040) is a highly selective non-competitive inhibitor of MEK (MKK1; MAPK kinase) and the closely related MKK2. It has anti-cancer activity, suppresses the ERK pathway, and has been used along with other classes of inhibitors to establish embryonic stem cell lines.
 
P2742 PD 404,182 ≥98% (HPLC) Potential antibiotic of gram negative bacteria. KDO-8-P synthase inhibitor.
 
PZ0111 PD-407824 ≥98% (HPLC) PD-407824 is a Wee1/Chk1 inhibitor.
 
SML1781 PDD00017273 ≥98% (HPLC) PDD00017273 is a potent and selective inhibitor of Poly(ADP-ribose) glycohydrolase (PARG), which catalyses hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, reversing the effects of poly(ADP-ribose) polymerases (PARPs). PARG has been shown to be involved in the repair of single strand DNA breaks. PDD00017273 is selective for PARG, with EC50 = 26 nM, compared to values of 30 μM for PARP1 and ARH3.
 
SML0021 PDI inhibitor 16F16 ≥98% (HPLC) 16F16 is a protein disulfide isomerase (PDI) inhibitor, first identified in a screen for compounds that prevent apoptosis induced by mutant huntingtin protein. 16F16 not only suppressed apoptosis induced by the misfolded protein mutant hungtingtin, it also protected rat neurons from cell death triggered by Aβ peptide. The actions of this inhibitor helped to identify a new mechanism in which a cell death pathway is regulated by protein misfolding via PDI upregulation.
 
SML1126 PDP-EA ≥98% (HPLC) 3-N-Pentadecylphenolethanolamide (PDP-EA) is an activator of fatty acid amide hydrolase (FAAH) from plant and mammalian species. PDP-EA appears to enhance FAAH activity by reduction of negative feedback from free ethanoloamine.
 
SML0624   PE 154 ≥97% (HPLC) Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are known to associate with β-amyloid plaques, and histological co-localization of AChE and Ab peptides is well established in Alzheimer’s disease. PE-154 is a fluorescent inhibitor of both AChE and BChE with IC50 values of 280 pM and 16 nM. PE-154 stains Aβ plaques in both rodent and human tissue samples, and does not cross react with phospho-tau.
 
P1999 PEAQX tetrasodium hydrate ≥98% (HPLC) NMDA receptor antagonist.
 
PZ0197   Pelitinib ≥98% (HPLC) Pelitinib (EKB-569) is an orally active, potent, second generation irreversible epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Pelitinib is selective for EGFR (ErbB-1) with an IC50 about 80 nM, but also covalently binds to ErbB-2 (HER2/c-neu) and ErbB-4 (Her 4) with much lower potency. Pelitinib has been shown to inhibit the growth of EGFR-overexpressing tumor cell lines.
 
SML1490   Pemetrexed disodium heptahydrate ≥98% (HPLC) Pemetrexed is antifolate cancer drug approved for treatment of variety of cancer including pleural mesothelioma and non-small cell lung cancer. Pemetrexed is a folate antimetabolite that inhibits thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase, three enzymes used in purine and pyrimidine synthesis.
 
SML0107 Pemirolast potassium ≥98% (HPLC) Pemirolast potassium is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent. It Inhibits chemical mediator release from tissue mast cells and has recently also been shown to inhibit the release of peptides including substance P, neurokinin (NK) A, and calcitonin gene-related peptide (CGRP) from sensory nerves. It has been used for the treatment of allergic conjunctivitis prophylaxis of for pulmonary hypersensitivity reactions to drugs such as paclitaxel
 
P0048 Pemoline ≥98% (HPLC) Pemoline is a CNS stimulant. Pemoline is used to treat attention-deficit hyperactivity disorder (ADHD). Pemoline is a Schedule IV drug and offers some advantages over other stimulants in that it does not reduce the appetite or cause dry mouth.
 
P3371 Penfluridol ≥97% (HPLC), powder T-type Ca2+ channel blocker; antipsychotic
 
P3053 Penitrem A ≥95% (HPLC and TLC) Tremorgenic fungal toxin; blocks high-conductance Ca2+-activated K+ channels.
 
G7548 Penta-O-galloyl-β-D-glucose hydrate ≥96% (HPLC) PGG induces predominantly (caspase dependent) apoptosis in DU145 and LNCaP cells, while inducing autophagy in more resistant PC3 and TRAMP-C2 cells. It appears that PGG targeted signaling downstream of rather than the mTOR itself. Polyphenolic pyranoses were reported (J Biol Chem. 2010, 285 (11), 7892-902) to inhibit the plasminogen activator inhibitor type 1 (PAI-1).
 
P0547 Pentamidine isethionate salt powder Neuroprotective; inhibits constitutive nitric oxide synthase in the brain; NMDA glutamate receptor antagonist.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRINA(2907), NOS1(4842), NOS2(4843), NOS2B(201288), NOS2C(645740), NOS3(4846)
P134 (−)-Pentazocine ≥98% (HPLC)    
P127 (+)-Pentazocine solid σ receptor agonist; active enantiomer of pentazocine.
human ... EBP(10682)
rat ... Chrm1(25229), Chrm2(81645), Drd2(24318), Oprm1(25601)
SML0508 Pentostatin ≥95% (HPLC) Pentostatin is a ring-expanded nucleoside (REN) that potently inhibits adenosine deaminase, which leads to lymphocyte toxicity. Pentostatin is used as anticancer agent to treat leukemia (hairy cell leukemia and chronic lymphocytic leukemia) and is investigated as an agent to treat graft-versus-host disease (GVHD).
 
P1784 Pentoxifylline solid Phosphodiesterase inhibitor; inhibits synthesis of tumor necrosis factor α (TNF-α).
human ... ADORA2B(136), LITAF(9516), PDE4B(5142), TNF(7124)
rat ... Tnf(24835)
P6500 Pentylenetetrazole Non-specific CNS stimulant; convulsant.
 
SML1132   Pep2-8 trifluoroacetate salt ≥95% (HPLC), contains 58μL of solution at 10mM in DMSO Pep2-8 is a potent PCSK9 (proprotein convertase subtilisin/kexin type 9) inhibitor that selectively binds to PCSK9 and interferes with LDL receptor binding to PCSK9. Pep2-8 restores LDL receptor function and LDL uptake of PCSK9-treated HepG2 cells.
 
P8828 Pergolide mesylate salt ≥98%, solid Dopaminergic agonist; suppresses pituitary secretion of prolactin; anti-Parkinsonian agent.
human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
SML0120 Perhexiline maleate salt ≥98% (HPLC) Perhexiline maleate is an anti-anginal metabolic modulator. It inhibits the mitochondrial enzyme carnitine palmitoyltransferase CPT-1 and to a lesser extent CPT-2. This causes a shift in myocardial substrate utilisation from long chain fatty acids to carbohydrates, resulting in increased glucose and lactate utilization and increased ATP production for the same O2 consumption as before and consequently increases myocardial efficiency. Perhexiline maleate was also recently found to inhibit the activity of mTORC1.
 
SML0612   Perifosine ≥98% (HPLC) Perifosine (KRX-0401) is a selective bioavailable alkylphospholipid inhibitor of protein kinase B/Akt (PKB/Akt) with anti-proliferative activity. Perifosine acts on cell membranes, selectively targeting proliferating cells, inducing growth arrest and apoptosis.
 
P0094 Perindopril erbumine Perindopril erbumine is an angiotensin converting enzyme (ACE) inhibitor; antihypertensive; becomes hydrolyzed in vivo to the active diacid metabolite; unlike the other ACE inhibitors, inhibits tumor growth in hepatocellular carcinoma cells due to suppression of VEGF levels; also suppresses angiotensin II production in vitro. Long-term therapy with this agent has a beneficial effect on the cerebral circulation by improving cerebral perfusion reserve in patients with previous minor stroke.
 
SML1587 Perlapine ≥98% (HPLC) Perlapine is a potent and selective agonist of hM3Dq DREADD (Designer Receptors Exclusively Activated by Designer Drugs), which does not activate the native human M3 receptor. Perlapine is a neuroleptic agent that exhibits sedative and sleep-promoting properties.
 
P6402 Perphenazine D2 dopamine receptor antagonist; α-adrenergic receptor antagonist and σ-receptor agonist; phenothiazine antipsychotic. Inhibits glutamate dehydrogenase in vitro.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), DRD2(1813), OPRS1(10280)
P7208   Pertussis toxin from Bordetella pertussis lyophilized powder Pertussis toxin catalyzes the ADP-ribosylation of the α subunits of the heterotrimeric guanine nucleotide regulatory proteins Gi, Go, and Gt. This prevents the G protein heterotrimers from interacting with receptors, thus blocking their coupling and activation. Since the Gα subunits remain in their GDP-bound, inactive state, they are unable to inactivate adenylyl cyclase or open K+ channels.
Bordetella pertussis Tohama I ... ptxA(2665068), ptxB(2665069), ptxC(2665408)
P2980   Pertussis toxin from Bordetella pertussis buffered aqueous glycerol solution Pertussis toxin catalyzes the ADP-ribosylation of the α subunits of the heterotrimeric guanine nucleotide regulatory proteins Gi, Go, and Gt. This prevents the G protein heterotrimers from interacting with receptors, thus blocking their coupling and activation. Since the Gα subunits remain in their GDP-bound, inactive state, they are unable to inactivate adenylyl cyclase or open K+ channels.
Bordetella pertussis Tohama I ... ptxA(2665068), ptxB(2665069), ptxC(2665408)
P159   Pertussis toxin B oligomer solid Subunit of pertussis toxin responsible for binding to cell surfaces; stimulates both platelet aggregation and cytosolic Ca2+ level elevation, may also activate phospholipase C; isolated from B pertussis strain 165.
 
P0622 PET-cGMP ≥98% (HPLC), solid cGMP-dependent protein kinase (PKG I and PKG II) activator. Potent membrane permeant activator of both isozymes I α and I β of cGMP-dependent protein kinase. Common stimulators such as 8-Br-cGMP or 8-pCPT-cGMP mainly activate kinase subtype Iα.
 
PZ0274   PF-01247324 ≥98% (HPLC) PF-01247324 is an orally bioavailable, selective and potent NaV1.8 channel blocker that inhibits that exhibits analgesic efficacy in rodent behavioral models of pain.
 
PZ0298 PF-03084014 hydrobromide ≥98% (HPLC) PF-03084014 is a highly potent γ-secretase inhibitor that reduces Aβ production in vitro. PF-03084014 does not show a paradoxical increase in plasma Aβ at low concentrations in both preclinical species and humans.
 
PZ0229 PF-03246799 hydrochloride ≥98% (HPLC) PF-3246799 is a potent serotonin 5-HT2C receptor agonist with an EC50 of 4.5 nM and minimal activity at 5-HT2A and 5-HT2B receptors. PF-3246799 had good efficacy in a preclinical canine model of stress urinary incontinence.
 
PZ0326   PF-03549184 ≥98% (HPLC) PF-03549184 (PF-9184) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 value of 16.5 nM in recombinant human mPGES-1. mPEGS-1 is the terminal enzyme that synthesizes prostaglandin E2 (PGE2) from PGH2 to PGE2 downstream of cyclooxygenase-2 (COX-2). Its expression is induced in response to pro-inflammatory mediators, similar to COX-2. Unlike the effects of COX inhibition, PF-9184 does not inhibit the production of other PGH2-derived products such as 6-keto-PGFα or PGF2α. PF-9184 inhibits PGE2 production in cell based assays with IC50 ranges from 0.5 to 5 μM. IC50 concentrations for rhCOX1 and rHCOX2 are 118 μM and 236 μM, respectively.
PGE2 is involved in inflammation and is one of the most abundant prostanoid.
 
PZ0155 PF-03716556 ≥98% (HPLC) potent, selective and reversible acid pump antagonist (H, K-ATPase)
 
PZ0218   PF-03814735 ≥98% (HPLC) PF-03814735 is a potent inhibitor of Aurora kinase A and B (IC50 = 5 and 0.8 nM, respectively). PF-03814735 inhibits proliferation of tumor cells in culture and in xenograft tumor models. The compound PF-03814735 blocks phosphorylation of Aurora B and Histone H3, and leads to the formation of polyploid cells in culture (HCT116 and MDA-MB-231).
 
PZ0031 PF-03882845 ≥98% (HPLC) PF-03882845 is a potent non-steroidal mineralocorticoid antagonist with and IC50 of 0.755 nM, compared to eplerenone with an IC50 of 109 nM. PF-03882845 was tested in a rat model for renal protection against aldosterone-mediated renal disease, and found to be more potent than eplerenone in suppressing the urinary albumin to creatinine ratio (UACR), a measure of renal fibrosis. The therapeutic index, calculated as the ratio of the EC50 for increasing serum K+ to the EC50 for UACR lowering, was 83.8 for PF-03882845 and 1.47 for eplerenone.
 
SML0263 PF-04217903 ≥98% (HPLC) PF-04217903 is a highly selective, potent inhibitor of the hepatocyte growth factor receptor c-Met. PF-04217903 inhibits endogenous, wild type c-Met in A549 human lung carcinoma cells with an IC50 of 4.8 nM. The compund displays 1000-fold selectivity against a panel of 208 other kinases.
 
PZ0224   PF-04279405 ≥98% (HPLC) PF-04279405 is a potent and selective glucokinase activator.
 
PZ0354 PF-04363467 hydrochloride ≥98% (HPLC) PF-4363467 hydrochloride is a Dopamine D3/D2 receptor antagonist. PF-4363467 has 100-fold selectivity for D3 with a Ki value of 3.1 nM for D3R compared to a Ki value of 692 nM for D2R and high selectivity for D3R compared to other biogenic amine receptors. PF-4363467 attenuated opioid drug-seeking behavior in a rat model of addiction without causing the extrapyramidal symptoms often associated with D2R antagonism.
 
PZ0213   PF-04418948 ≥98% (HPLC) PF-04418948 is a PGE2 Receptor (EP2) specific antagonist (IC50 = 16 nM) with greater than 2000-fold selectivity over other EP subtypes. PF-04418948 inhibits EP2 activity in smooth muscle preps from human, dog and mouse.
 
PZ0222   PF-04445597 ≥98% (HPLC) PF-04445597 is a potent, orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP).
 
PZ0303 PF-04449913 maleate salt ≥98% (HPLC) PF-04449913 (Glasdegib) is an orally bioavailable Hedgehog pathway inhibitor. PF-04449913 acts by binidng Smoothened (Smo) and blocking signal transduction. PF-04449913 has an IC50 of 5 nM in the Gli-Luciferase assay. In a Phase I clinical trial in patients with advanced solid tumors, PF-04449913 caused disease stabilization in 34% of patients.
 
PZ0206 PF-04455242 hydrochloride ≥98% (HPLC) PF-4455242 is a selective k opioid receptor (KOR) antagonist with 20-fold selectivity for kappa over mu receptors (k Ki = 3 nM, μ Ki =64 nM). PF-4455242 is orally active, has good brain penetration in rats and was able to block the effects of the kappa agonist U50488. Studies indicate that k blockade has afforded antidepressant activity in several animal models. PF-4455242 has been in phase I clinical trials for trial for bipolar depression.
 
PZ0184 PF-04457845 ≥98% (HPLC) PF-04457845 is a potent, orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. PF-04457845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It was shown to be both potent and selective against other serine hydrolases. It has an IC50 value of 7.2 nM for human FAAH. The endocannabinoid system is a target for therapeutic pain relief. In a rat model of inflammatory pain, PF-04457845 produced significant reduction of inflammatory pain with efficacy comparable to that of naproxen at 10 mg/kg.
 
PZ0232 PF-04471141 hydrochloride ≥98% (HPLC) PF-04471141 is a potent, selective inhibitor of the calcium-activated phosphodiesterase PDE1. (PDE1B IC50 = 35 nM).
 
PZ0032 PF-04479745 ≥98% (HPLC) PF-04479745 (PF-4479745) is a selective serotonin 5HT2C agonist.
 
PZ0273   PF-04531083 ≥98% (HPLC) PF-04531083 is an orally available, potent and selective sodium channel Nav1.8 blocker. PF-04531083 was designated as a potential treatment of pain.
 
PZ0207 PF-04620110 ≥98% (HPLC) PF-04620110 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that inhibits triacylglycerol synthesis in cells and in rodents.
 
PZ0228   PF-04628935 ≥98% (HPLC) PF-04628935 is a potent antagonist/inverse agonist of the ghrelin receptor, growth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. Ghrelin and GSHR are involved in regulation of food intake and long-term energy homeostasis; GSHR ligands are of interest for obesity and other metabolic disorders. PF-04628935 is orally bioavailable and brain penetrant.
 
PZ0309 PF-04634817 succinate ≥98% (HPLC) PF-04634817 is a potent and selective antagonist of CC chemokine receptor 2 and 5 (CCR2/5).
 
PZ0314   PF-04671536 ≥98% (HPLC) PF-04671536 is a highly potent and selective inhibitor of phosphodiesterase 8B (PDE8B) phosphodiesterase 8A (PDE8A). In primary human pancreatic islets, PF-04671536 increases insulin secretion in a glucose-dependent manner.
 
PZ0215   PF-04701475 ≥98% (HPLC) PF-04701475 is a potent and selective α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) positive allosteric potentiator.
 
PZ0216   PF-04725379 ≥98% (HPLC) PF-04725379 is a potent and selective α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) positive allosteric potentiator.
 
PZ0284 PF-04753299 ≥98% PF-04753299 is a potent and selective inhibitor of LpxC (UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase) that is effective in a murine of gram-negative bacteria infection model.
 
PZ0313 PF-04802367 ≥98% (HPLC) PF-04802367 (PF-367) is a potent and specific ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK-3α/β) with an IC50 value of 2.3 nM and >450-fold selectivity for GSK-3 in a panel of >400 neuroreceptors, enzymes and kinases. GSK-3 dysregulation has been implicated in the pathogenesis of neurological diseases including Alzheimer′s disease.
 
SML1061 PF-04856264 ≥98% (HPLC) PF-04856264 is a potent, selective inhibitor of the human Nav1.7 voltage gated sodium channel (IC50 = 28 nM). PF-04856264 blocks mouse Nav1.7 (IC50 = 131 nM) but has low potency against the rat Nav1.7 channel (IC50 = 4.2 mM).
 
PZ0250 PF-04859989 hydrochloride ≥98% (HPLC) PF-04859989 is a brain-penetrable irreversible inhibitor of kynurenine amino transferase II (KAT II), the enzyme responsible for most of the brain synthesis of kynurenic acid, which has been implicated in several psychiatric and neurological disorders, including schizophrenia and bipolar disorder, and thought to impair cognitive function. PF-04859989 has IC50 values of 23 nM for hKAT II and 263 nM for rKAT II. PF-04859989 is ~1000-fold selective for KAT II over human KAT I, KAT III, and KAT IV. PF-04859989 prevented ketamine-induced disruption of performance in memory tasks in both rodents and nonhuman primates.
 
PZ0294 PF-04880594 ≥98% (HPLC) PF-04880594 is a potent and selective RAF inhibitor that inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 potently inhibits tumor growth in BRAF-mutant melanoma xenograft models.
 
PZ0210   PF-04885614 ≥98% (HPLC) PF-04885614 is a potent and selective Nav1.8 inhibitor.
 
PZ0320 PF-04937319 ≥98% (HPLC) PF-04937319 is a glucokinase activator with an EC50 value of 174 nM. PF-04937319 was found to improve glycemic control in adults with type 2 diabetes when used in conjunction with metformin.
PF-04937319, unlike other glucokinase activators, is capable of maintaining lower-glucose levels without it resulting in hypoglycemia. In type II diabetic patients where metformin treatment is inadequate, PF-04937319 is capable of maintaining glycemic control within the acceptable risk-benefit profile.
 
PZ0304 PF-04965842 ≥98% (HPLC) PF-04965842 is a Janus Kinase (JAK) inhibitor selective for JAK1 with an IC50 value of 29 nM for JAK1 compared to 803 nM for JAK2, >10000 nM for JAK3 and 1250 nM for Tyk2. JAKs mediate cytokine signaling, and are involved in cell proliferation and differentiation. PF-04965842 has been investigated as a possible treatment for psoriasis.
 
PZ0247 PF-04979064 ≥98% (HPLC) PF-04979064 is an orally available, potent and selective PI3K/mTOR dual kinase inhibitor that potently inhibits tumor growth in mouse xenografts.
 
PZ0223   PF-04991532 ≥98% (HPLC) PF-04991532 is a potent and hepatoselective glucokinase activator that reduces mean daily glucose (MDG), fasting plasma glucose (FPG) and glucose excursion in humans.
 
PZ0310 PF-04995274 ≥98% (HPLC) PF-04995274 is a potent partial agonist of serotonin 5HT4 receptor with Ki = 0.15 - 0.46 nM for 5-HT4 isoforms a, b, d and e. 5-HT4 agonists modulate cholinergic function are being studied as possible treatment for cognitive disorders associated with Alzheimer′s Disease. PF-04995274 is brain penetrant and was shown to increase brain acetylcholine levels and reversed scopolamine-induced learning deficits in the rat Morris water maze test.
 
PZ0311 PF-05089771 ≥98% (HPLC) PF-05089771 is a selective and potent inhibitor of the human voltage-gated sodium ion channel Nav1.7 with an IC50 value of 11 nM. PF-05089771 targets the voltage-sensing domain, preferentially interacting with, and stabilizing, inactivated channel conformations by interaction with the voltage-sensor domain (VSD) of Domain 4. Nav1.7 is expressed in sensory neurons and is critical for pain processing. PF-05089771 is being investigated for the treatment of chronic neuropathic pain.
 
PZ0299 PF-05175157 ≥98% (HPLC) PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively. Acetyl CoA carboxylase (ACC) generates malonyl CoA, which is a substrate for de novo lipogenesis and is also an inhibitor of mitochondrial fatty acid β-oxidation through inihbition of carnitine-palmitoyl transferase I (CPT-1), responsible for the transport of long-chain fatty acyl-CoAs across the mitochondrial membrane. ACC inihibitors are hoped to inhibit de novo lipogenesis and increase β-oxidation of long-chain fatty acids with potential for treatment of type 2 diabetes, hepatic steatosis, and cancer. In Phase I clinical studies for diabetes treatment, PF-05175157 inhibited de novo lipogenesis and increased net whole-body fatty acid utilization.
 
PZ0251   PF-05180999 ≥98% (HPLC) PF-05180999 is an inhibitor of cyclic nucleotide phosphodiesterase-2 (PDE2).
 
PZ0286 PF-05883083-00 ≥98% (HPLC) PF-05883083-00 is an analog of orally available dual Src/Abl kinase inhibitor Bosutinib.
 
PZ0220   PF-06250112 ≥98% (HPLC) PF-06250112 is a potent inhibitor of Bruton′s tyrosine kinase (BTK). PF-06250112 blocks both B-cell receptor and FcR-mediated signaling, and prevents FcR-dependent, Antibody-mediated proteinuria in a mouse glomerulonephritis model.
 
PZ0343 PF-06260414 ≥98% (HPLC) PF-06260414 is a nonsteriodal selective androgen receptor modulator (SARM). PF-06260414 is being investigated as a treatment for muscle weakening such as that associated with muscular dystrophy and the sarcopenia associated with natural aging. PF-06260414 has anabolic activity without unwanted androgenic activity on reproductive organs, liver or kidneys.
 
PZ0272 PF-06260933 dihydrochloride ≥98% (HPLC) PF-06260933 dihydrochloride is a MAP4K4 inhibitor.
 
PZ0324 PF-06263276 ≥98% (HPLC) PF-06263276 is an inhibitor of the Janus kinase (JAK) enzymes 1, 2, 3 and tyrosine kinase 2 (TYK2). PF-06263276 has been investigated for the treatment of psoriasis.
 
PZ0277   PF-06281355 ≥98% (HPLC) PF-06281355 (PF-1355) is an orally available, selective and potent mechanism based inhibitor of the myeloperoxidase (MPO) that reduces plasma MPO activity, vascular edema, neutrophil recruitment, and elevated circulating cytokines. PF-06281355 suppresses albuminuria and chronic renal dysfunction in model of anti-Glomerular Basement Membrane (GBM) disease.
 
PZ0301 PF-06284674 ≥98% (HPLC) PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator.
 
PZ0356 PF-06291874 ≥98% (HPLC) PF-06291874 is an orally active, potent and selective glucagon receptor antagonist. PF-06291874 exhibits a robust glucose reductions in subjects with type 2 diabetes mellitus.
 
PZ0219 PF-06297470 ≥98% (HPLC) PF-06297470 is a potent negative allosteric modulator of the Metabotropic Glutamate Receptor 5 (mGluR5). PF-06297470 binds to mGluR5 with a Ki of 0.9 nM. The compound PF-06297470 displays slight antagonism of mGluR1 (IC50 = 30.5 mM), with no agonist or antagonist activities against any other mGlu receptor subtype at concentrations up to 50 mM. PF-06297470 reduces dyskinesia in a rodent (MPTP)-rendered Parkinsonian model of L-DOPA-induced dyskinesia (PD-LID).
 
PZ0297 PF-06305591 dihydrate ≥98% (HPLC) PF-06305591 is a potent and highly selective sodium channel Nav1.8 inhibitor.
 
PZ0319 PF-06409577 ≥98% (HPLC) PF-06409577 is a potent and selective activator of 5′ adenosine monophosphate-activated protein kinase (AMPK).
PF-06409577 potently activates a1β1γ1 AMPK (5′ adenosine monophosphate-activated protein kinase) isoform, and prevents its dephosphorylation. It is similarly potent for β1 containing isoforms, but shows significantly lower potency for β2-containing isoforms of AMPK. Patch-clamp assays show that this compound does not inhibit hERG (human ether-a-go-go gene). It interacts with the allosteric drug and metabolite site (ADaM) of AMPK.
 
PZ0333 PF-06412154 hydrochloride ≥98% (HPLC) PF-06412154 hydrochloride is a glucagon receptor antagonist.
 
PZ0334 PF-06422913 ≥98% (HPLC) PF-06422913 is an orally active, potent and selective metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
 
PZ0233 PF-06424439 ≥98% (HPLC) PF-06424439 is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).
 
PZ0221 PF-06439015 methanesulfonate salt ≥98% (HPLC) PF-06439015 is a potent and selective inihibitor that overcomes clinical ALK (receptor tyrosine kinase anaplastic lymphoma kinase) mutations resistant to Crizotinib. PF-06439015 is potent across a broad panel of ALK mutant cell lines with an IC50 of 6.6 nM for tumor growth inhibition in a crizotinib-resistant cell line (H3122-L1196M).
 
PZ0258   PF-06442609 ≥98% (HPLC) PF-06442609 is a potent γ secretase inhibitor that produces a robust reduction of brain Aβ42 and Aβ40 in in a guinea pig model. Apparently, PF-06442609 is suitable for rodent model of AD.
 
PZ0248 PF-06447475 ≥98% (HPLC) PF-06447475 is a potent and selective LRRK2 inhibitor.
 
PZ0249 PF-06454589 ≥98% (HPLC) PF-06454589 is a potent and selective LRRK2 inhibitor.
 
PZ0296 PF-06459988 ≥98% (HPLC) PF-06459988 is an orally available irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant (EGFRm) forms including the secondary acquired resistance mutation T790M. PF-06459988 has minimal activity against wild-type EGFR (WT EGFR).
 
PZ0231 PF-06462894 ≥98% (HPLC) PF-06462894 is a muscarinic metabotropic receptor mGluR5 ligand.
 
PZ0271 PF-06463922 acetate ≥98% (HPLC) PF-06463922 is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).
 
PZ0209   PF-06465469 ≥97% (HPLC) PF-06465469 is a potent, covalent inhibitor of the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase), which is expressed primarily in immune cells, and is strongly upregulated following activation of T-cells. PF-06465469 inhibits Itk enzymatic activity with an IC50 of 2 nM. The compound blocks anti-CD3 induced phosphorylation of PLCg in Jurkat cells (IC50 = 31 nM) and IL-2 production in anti-CD3 stimulated human whole blood (IC50 = 48 nM).
 
PZ0261 PF-06649283 ≥98% (HPLC) PF-06649283 is a new β-Secretase (BACE) inhibitor.
 
PZ0327 PF06650833 ≥98% (HPLC) PF06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4). IRAK4 kinase is important in innate immunity, involved in initiating signaling from Toll-like receptors and members of th einterleukin-1 receptor family. IRAK4 kinase is an attractive target for the treatment of various diseases associated with deregulated inflammation, such as rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, and systemic lupus erythematosus. PF06650833 has been investigated for treatment of lupus.
 
PZ0289 PF-06651481-00 ≥98% (HPLC) PF-06651481-00 is an isomer of orally available dual Src/Abl kinase inhibitor Bosutinib.
 
PZ0316 PF-06651600 ≥98% (HPLC) PF-06651600 is a potent and selective JAK3 inhibitor.
 
PZ0292   PF-06658959-00 ≥98% (HPLC) PF-05883083-00 is an analog of orally available dual Src/Abl kinase inhibitor Bosutinib.
 
PZ0290 PF-06663181-00 ≥98% (HPLC) PF-06663181-00 is an isomer of orally available dual Src/Abl kinase inhibitor Bosutinib.
 
PZ0262 PF-06663195 ≥98% (HPLC) PF-06663195 is a potent inhibitor of β-site amyloid precursor protein (APP) Cleaving Enzyme 1 (BACE1, β-Secretase 1).
 
PZ0291   PF-06663827-00 ≥98% (HPLC) PF-06663827-00 is an isomer of orally available dual Src/Abl kinase inhibitor Bosutinib.
 
PZ0288 PF-06663829-00 ≥98% (HPLC) PF-06663829-00 is an analog of orally available dual Src/Abl kinase inhibitor Bosutinib.
 
PZ0287   PF-06665105-00 ≥97% (HPLC) PF-06665105-00 is an analog of orally available dual Src/Abl kinase inhibitor Bosutinib.
 
PZ0339 PF-06683324 ≥98% (HPLC) PF-0668324 is pan tropomyosin-related kinase (Trk) inhibitor.
 
PZ0260 PF06691283 ≥98% (HPLC) PF06691283 is a new β-Secretase (BACE) inhibitor.
 
PZ0345 PF-06700841 tosylate salt ≥98% (HPLC) PF-06700841 is an inhibitor of JAK1 and TYK2 kinases. PF-06700841 has been investigated for the treatment of psoriasis and lupus.
 
PZ0346 PF-06726304 acetate ≥98% (HPLC) PF-06726304 is a selective inhibitor of Histone-lysine N-methyltransferase EZH2 (enhancer of Zeste homolog 2), which catalyzes trimethylation of histone H3 lysine 27 (H3K27) and is amplified and/or overexpressed in several human cancers including breast, prostate and lymphoma. PF-06726304 is a novel structural class of EZH2 inhibitor.
 
PZ0341 PF-06733804 ≥98% (HPLC) PF-06733804 is pan tropomyosin-related kinase (Trk) inhibitor.
 
PZ0340 PF-06737007 ≥98% (HPLC) PF-06737007 is pan tropomyosin-related kinase (Trk) inhibitor.
 
PZ0283 PF-06745013 ≥98% (HPLC) PF-06745013 is a potent and selective inhibitor of MAP4K4.
 
PZ0302 PF-06747775 ≥98% (HPLC) PF-06747775 is an orally available, potent and selective inhibitor of the epidermal growth factor receptor) mutant form T790M (EGFR T790M inhibitor). PF-06747775 exhibits minimal activity against wild type EGFR.
 
PZ0350 PF-06748962 ≥98% (HPLC) PF-06748962 is a potent and selective lactam-based prostaglandin EP3 receptor antagonist.
 
PZ0282 PF-06758955 hydrochloride ≥98% (HPLC) PF-06758955 is a potent and selective inhibitor of MAP4K4.
 
PZ0318 PF-06761281 ≥97% (HPLC) PF-06761281 is an inhibitor of the sodium-coupled citrate transporter (NaCT or SLC13A5), which may be a target for tretment and prevention of metabolic disorders. The SLC13 transporters SLC13A2 (NaDC1), SLC13A3 (NaDC3), and SLC13A5 (NaCT) co-transport di- and tricarboxylates with multiple sodium ions into cells. PF-06761281 inhibits citrate uptake with an IC50 of 740 nM for NaCT in human hepatocytes. PF-06761281 has >25-fold in vitro selectivity for NaCT over NaDC1 and NaDC3 and was inactive in a selectivity panel of 65 targets.
 
PZ0300 PF-06764427 ≥98% (HPLC) PF-06764427 is a selective azaindole muscarinic receptor M1 positive allosteric modulator.
 
PZ0323 PF-06767832 ≥98% (HPLC) PF-06767832 is a cell permeable, potent and selective M1 muscarinic acetylcholine receptor Positive Allosteric Modulator (PAM). Studies have shown that PF-06767832 potentiates the activity of acetylcholine (Ach) in vitro.
 
PZ0359 PF-06827443 ≥98% (HPLC) PF-06827443 is a otent, low clearance, orally bioavailable, and CNS penetrant muscarinic M1-selectivepositive allosteric modulator (PAM) with minimal agonist activity.
 
PZ0351 PF-2545920 hydrochloride ≥97% (HPLC) PF-2545920 hydrochloride (MP-10) is a potent and selective cyclic nucleotide phosphodiesterase (PDE) 10A competitive inhibitor with a reported IC50 value of 1.26 nM. PDE10A hydrolyzes both cAMP and cGMP, and is highly expressed in medium spiny neurons of the mammalian striatum and in basal ganglia areas where D1 and D2 dopamine receptors are expressed. PF-2545920 has been studied for treatment of schizophrenia and Huntington′s disease.
 
PZ0188 PF-3644022 hydrate ≥98% (HPLC) PF-3644022 is a potent inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK2; Ki = 3 nM). PF-3644022 inhibits TNFa and IL-6 production in LPS-stimulated human whole blood (IC50 = 1.6 and 10.3 μM, respectively) and blocks TNFα production and paw swelling in a streptococcal cell wall-induced arthritis in rats.
 
PZ0263 PF-3774076 ≥98% (HPLC) PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors.
 
PZ0158 PF 3845 hydrate ≥98% (HPLC) PF 3845 is a potent, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. The endocannabinoid system is a target for therapeutic pain relief. PF-3845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It high selectivity over other enzymes including FAAH-2. In mouse studies, PF-3845 has been shown to raise brain anandamide levels for up to 24 hr; and in a rat model it produced significant reduction of inflammatory pain..
 
SML0667   PF-429242 dihydrochloride ≥98% (HPLC) PF-429242 is a potent inhibitor of S1P (cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease) that reduces expression levels of hepatic SREBP target genes and lower rates of cholesterol and fatty acid synthesis in mice. PF-429242 is a potent antiviral agent against prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV in cultured cells. PF-429242 efficiently prevented the processing of GPC from the LCMV and LASV. PF-429242 is expected to be active against CCHFV.
 
PZ0185 PF-431396 hydrate ≥98% (HPLC) PF-431396 is a potent inhibitor of PYK2 and FAK kinases (IC50 = 11 and 1.5 nM, respectively). PF-431396 increases bone formation and protects against bone loss in ovariectomized rats.
 
PZ0143 PF-4708671 ≥98% (HPLC) PF-4708671 is a selective p70 ribosomal S6 kinase (S6K1) inhibitor. PF-4708671 inhibits S6K1 with a Ki of 20 nM and IC50 of 160 nM, while having no effect on the closely related RSK and MSK kinases.
human ... RPS6KB1(6198)
mouse ... Rps6kb1(72508)
rat ... Rps6kb1(83840)
PZ0186 PF-477736 ≥98% (HPLC) PF-00477736 is a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49 nM. The compound abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin.
 
PZ0211   PF-4778574 ≥98% (HPLC) PF-4778574 is a potent AMPA receptor positive allosteric modulator (PAM) that has been shown to enhance cognition in animal models.
 
PZ0328   PF-4800567 hydrochloride ≥98% (HPLC) PF-4800567 is a casein kinase 1e (CK1e) selective inhibitor (IC50 = 32 nM) that is 20 fold selective for the CK1e isoform over CK1d. PF-4800567 blockes CK1e-mediated PER3 nuclear translocation, but does not effect the circadian clock in animal studies.
 
PZ0246 PF-5006739 ≥98% (HPLC) PF-5006739 is a potent inhibitor of casein kinases 1 delta (CK1δ) and 1 epsilon (CK1ε), key regulators of the suprachiasmatic nucleus (SCN) central clock and also linked to the development of drug addiction through PERIOD proteins (PER1–3) and dopamine- and cAMP-regulated neuronal phosphoprotein (DARPP-32) modulation. PF-5006739 has low nM in vitro potency for CK1δ/ε (IC50 values of 3.9 nM for CK1δ and 17.0 nM for CK1ε) and high kinome selectivity. PF-5006739 induced profound phase delays in circadian periodicity in both nocturnal and diurnal animal models and attenuated opioid drug-seeking behavior in a rodent operant reinstatement model.
 
PZ0194 PF-5081090 ≥98% (HPLC) PF-5081090 is a potent inhibitor of LpxC, a metalloenzyme required for the synthesis of lipid A, an essential component of the outer membrane of Gram-negative bacteria. The IC50 for enzyme inhibition is 1.1 nM and the minimal inhibitory concentration (MIC) for inhibiting growth of Pseudomonas aeruginosa growth is 0.008 mg/mL.
 
SML0389 PF-514273 ≥98% (HPLC) PF-514273 is a highly selective CB1 antagonist. The Ki for binding to CB1 and CB2 receptors is 1 nM and 10 mM, respectively. PF-514273 inhibits food intake and weight gain in rodents.
 
PZ0217 PF-5274857 hydrochloride ≥98% (HPLC) PF-5274857 is a hedgehog (Hh) signaling pathway inhibitor acting as a potent and selective Smoothened (Smo) antagonist with an IC50 of 5.8 nM and a Ki of 4.6 nM. PF-5274857 completely blocked downstream gene Gli1 transcriptional activity in Gli-Luc mouse embryonic fibroblast (MEF) cells with an IC50 of 2.7 nM. PF-5274857 is brain penetrant. The compound PF-5274857 showed anti-tumor activity in a mouse medulloblastoma model with an in vivo IC50 of 8.9 nM.
 
PZ0234 PF-543 hydrochloride ≥98% (HPLC) PF-543 hydrochloride is a novel, cell-permeable, potent and selective inhibitor of sphingosine kinase-1 (SphK1). PF-543 inhibits SphK1 with a Ki of 3.6 nM, is sphingosine competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 decreased the level of endogenous S1P by 10-fold with proportional increase of the level of sphingosine.
 
PZ0117 PF-573228 ≥95% (HPLC) PF-573228 is a focal adhesion kinase (FAK) inhibitor; Non-receptor tyrosine kinase inhibitor.
 
PZ0342 PF-6274484 ≥98% (HPLC) PF-6274484 is an irreversible EGFR kinase inhibitor that covalently reacts with active-site cysteine residues in the ATP binding pocket. PF-6274484 inhibits autophosphorylation of both wild type and mutant EGFR in tumor cells with IC50 values of 5.8 nM and 6.6 nM, respectively.
 
PZ0241 PF-6422899 ≥98% (HPLC) PF-6422899 is an alkynylated derivative of PF-6274484; irreversible inhibitor of EGFR kinase activity. PF-6422899 binds covalently to active-site cysteine residues in the ATP binding pocket of EGFR.
 
SML0795   PF-670462 ≥98% (HPLC) PF-670462 is a selective inhibitor of the δ- and ε-isoforms of casein kinase I, with IC50 values of 7.7 and 14 nM respectively, and >30 selectivity relative to 42 other kinases tested. Casein kinase Iε phosphorylates PER proteins, which are involved in setting the period of the circadian pacemaker or clock. PF-670462 is potent (IC50 7.7 nM) and effective in vivo (i.e. it induces profound phase delays in circadian periodicity).
 
PZ0306 PF-6808472 ≥98% (HPLC) PF-6808472 is a cell permeable covalent probe suitable for click chemistry designated to measure kinase selectivity in intact cells. PF-6808472 contains sulfonyl fluoride group, which react with conserved lysine residue within kinase ATP binding site.
 
SML0835   PF74 ≥98% (HPLC) PF74 (PF-3450074) is a HIV-1 inhibitor that targets HIV capsid protein. PF74 binds specifically to HIV-1 particles and triggers premature HIV-1 uncoating in target cells.
 
P0041 PF-750 ≥98% (HPLC) PF-750 is a potent, time-dependent, irreversible FAAH inhibitor with IC50 values 0.6 and 0.016 μM when preincubated with recombinant human FAAH for 5 and 60 minutes, respectively. Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. Activity-based profiling of various human and murine tissue proteome samples revealed that PF-750 is highly selective for FAAH relative to other serine hydrolases, showing no discernable off-site activity up to 500 μM. PF-750 shows 10-fold better potency than URB597 (Sigma# U4133) after 30 min preincubation. PF-750 is highly selective on FAAH. Even at as high as 500 μM, it had no interactions with many tested enzymes, but URB597 and other known FAAH inhibitors did not perform well at low concentraction (100 μM).
 
SML0715   PF-8380 ≥98% (HPLC) PF-8380 is a potent orally bioavailable inhibitor of autotaxin (ATX), the enzyme that synthesize lysophosphatidic acid (LPA) from lysophosphatidyl choline, and is an emerging target for treatment of inflammatory conditions, including cancer, arthritis and multiple sclerosis. 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.
 
PZ0151 PF-956980 hydrate ≥98% (HPLC) PF-956980 is a FGF1 receptor antagonist; PDGF receptor modulator; Flt3 tyrosine kinase modulator; and VEGF antagonist.
 
SML0587   PF9601N ≥98% (HPLC) PF9601N is a selective and potent monoamine oxidase B inhibitor that exhibit anti-Parkinsonian effects in several models of PD.
 
PZ0131 PF-998425 ≥98% (HPLC) PF-998425 is a novel, nonsteroidal androgen receptor antagonist.
 
PZ0325   PF-CBP1 ≥98% (HPLC) CBP is a transcriptional coactivator. The protein is a link between the DNA-associated transcription factors and the RNA polymerase 2 complex. It also exhibits histone acetyltransferase activity.
PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons. Also, PF-CBP1 significantly reduces levels of RGS4 mRNA levels in neurons.
 
SML0352 PFI-1 ≥98% (HPLC) The human BET family, which includes BRD2, BRD3, BRD4 and BRDT, play a role in regulation of gene transcription. PFI-1 is a selective BET bromodomain inhibitor with activity at BRD2 (IC50 = 98 nM) and BRD4 (IC50 = 220 nM). For full characterization details, please visit the PFI-1 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML1408 (R)-PFI-2 ≥97% (HPLC) (R)-PFI-2 is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (also known as SET9). (R)-PFI-2 has an IC50 value of 2 nM and 1000-fold selectivity over other methyltransferases and other non-epigenetic targets. For full characterization details, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
PZ0312 (S)-PFI-2 (S)-PFI-2 is the negative control probe for (R)-PFI-2 hydrochloride (catalog no. SML1408), which is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (SET9). (R)-PFI-2 has 1000-fold selectivity for SETD7 (SET9) over other methyltransferases and other non-epigenetic targets and an IC50 value of 2 nM. (S)-PFI-2 is 500-fold less active. For characterization details of (R)-PFI-2 and (S)-PFI-2, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML0939 PFI-3 ≥98% (HPLC) SMARCA4 (SWI/SNF related, Matrix associated, Actin dependent Regulator of Chromatin, subfamily A, member 4) is a transcriptional activator and is a component of the large ATP-dependent chromatin remodeling complex SWI/SNF, which is required for transcriptional activation of genes normally repressed by chromatin. SMARC4 (also known as BRG1) and the related protein SMARCA2 (also known as BRM) contain a bromodomain that is structurally similar to the PolyBromo1 (PB1) 5 bromodomain. PFI-3 is a selective chemical probe for SMARCA bromodomains that inhibits SMARCA2, SMARCA4 and PB1(5) bromodomains. For full characterization details, please visit the PFI-3 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
PZ0307 PFI-4 ≥98% (HPLC) PFI-4 is an SGC chemical probe for the bromodomains of the BRPF (BRomodomain and PHD Finger containing) scaffolding protein BRPF1B. The BRPF proteins (BRPF1/2/3) assemble histone acetyltransferase (HAT) complexes of the MYST transcriptional coactivator family members MOZ and MORF. The BRPF1 protein is the scaffold subunit of the MYST acetyltransferase complex, which plays a crucial roles in DNA repair, recombination and replication as well as transcription activation. Mutations in MOZ, MORF, and BRPF1 have all been associated with cancer. BRPF1 exists in 2 different isoforms: BRPF1A and BRPF1B. PFI-4 specifically binds to BRPF1B with a Kd =13 nM as determined by ITC. It reduces recovery time in triple BRD cell construct in FRAP and is potent in cells with IC50 250nM, while showing no effect on BRPF1A. For full characterization details, please visit the PFI-4 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
 
SML1009   PFK15 ≥98% (HPLC) PFK15 is potent and selective antagonist of PFKB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3) that causes a rapid induction of apoptosis in cancer and transformed cells. PFK15 inhibits the growth of LLC xenografts.
 
SML1839 PFM39 ≥98% (HPLC) PFM39 is a potent cell-permeable Mirin analog that selectively inhibits MRE11 exo-, but not endo-, nuclease activity. PFM39 targets MRE11 in a fashion similar to Mirin, but distinct from that of PFM01 to allow a blockage of dsDNA phosphate backbone rotation and selective inhibition against MRE11 exo-, but not endo-, nuclease activity. FM39 potently impairs G2-phase double-strand break (DSB) repair in 1BR3-hTERT fibrolasts following ionizing irradiation (IR).
 
P0024 PG-01 ≥98% (HPLC) CFTR mutations are responsible for cystic fibrosis. The most common mutation is ΔF508, but many others exist. Drugs which can correct channel function of a broad range of CFTR mutants are most desirable for clinical development. PG-01 is a potentiator of ΔF508 (Ka 70 nM) as well as mutants G551D and G1349D (Ka 1100 and 40 nM, respectively). Its broad spectrum may make it more desirable than more mutant-specific CFTR correctors.
 
SML0018 PG01037 dihydrochloride hydrate ≥98% (HPLC) PG01037 dihydrochloride is a selective dopamine D3 receptor antagonist. It is more selective for D3 receptors than other D3 antagonists that are currently available with a D2/D3 selectivity ratio of 867and a D4/D3 selectivity ratio of 13,000.
Selective dopamine D3 receptor antagonist
 
P3998 PGL-135 hydrochloride monohydrate ≥98% (HPLC), solid Cell-permeable polyglutamine aggregation inhibitor
 
P6490 PGP-4008    
SML0461 PH-002 ≥98% (HPLC) PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that restores mitochondrial cytochrome c oxidase subunit 1 levels, rescues impairments of mitochondrial motility and neurite outgrowth. PH-002 is an apoE4 structure corrector that reverses the apoE4 detrimental effects.
 
PZ0259 PH-797804 ≥98% (HPLC) PH-797804 is an orally active, potent and readily reversible ATP competitive inhibitor of the alpha isoform of human p38 MAP kinase. PH-797804 blocks inflammation-induced production of cytokines and proinflammatory mediators.
 
PZ0266   PHA-408 ≥98% (HPLC) PHA-408 is a potent, selective I kappa B-kinase 2 (IKK-2) inhibitor. PHA-408 is a tight binding, ATP competitive IKK-2 inhibitor with greater than 350-fold selectivity for IKK-2 vs IKK-1 (IC50 values of 10-40 nM at IKK-2 vs 14 μM at IKK-1). PHA-408 was shown to suppress inflammatory cellular events, and to reduce inflammation in animal models of arthritis.
 
PZ0135 PHA-543613 ≥98% (HPLC) PHA-543613 is a potent selective α7 nAChR agonist. Nicotinic acetylcholine receptors are ligand-gated ion channels activated by nicotine, expressed in multiple tissues, with high functional expression in brain. The homomeric subtype α7 is a potential therapeutic target for cognitive deficits in schizophrenia and Alzheimer′s disease. PHA-543613 is active in both in vitro (binding, calcium flux, patch-clamp) and in vivo (auditory gating, novel object recognition) assays.
 
PZ0147 PHA-665752 hydrate ≥98% (HPLC) PHA-665752 ia a c-Met kinase inhibitor. PHA-665752 is ATP-competitive, an active-site inhibitor with greater than 50-fold selectivity for c-Met vs a panel of tyrosine and serine-threonine kinases.
 
PZ0178 PHA 767491 hydrochloride ≥98% (HPLC) PHA-767491 is a potent and selective ATP-competitive dual inhibitor cdc7/cdk9. PHA-767491 blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites.
 
P8716   Phalloidin, Biotin Labeled ≥90% Shown to bind actin filaments and streptavidin simultaneously, due to the longer space between the two active components.
Toxin that binds polymeric F actin, stabilizing it and interfering with the function of actin-rich structures.
 
P0243   Phalloidin, poly-L-Lysine bound ≥90% It is predicted that poly-L-lysine bound phalloidin is approximately 100 fold more potent than the unbound form.
Toxin that binds polymeric F actin, stabilizing it and interfering with the function of actin-rich structures.
 
SML1432 PHCCC ≥97% (HPLC) PHCCC is a positive allosteric modulator (PAM) at the mGluR4 subtype that exhibits anxiolytic and anti-Parkinsonian effects in animal models. PHCCC is a potent group I metabotropic glutamate receptor antagonist.
 
P203 Phenamil methanesulfonate salt solid Irreversible inhibitor of amiloride-sensitive Na+ channels; derivative of amiloride.
human ... SCNN1A(6337), SCNN1B(6338), SCNN1D(6339), SCNN1G(6340)
mouse ... Scnn1a(20276), Scnn1b(20277), Scnn1d(140501), Scnn1g(20278)
rat ... Scnn1a(25122), Scnn1b(24767), Scnn1g(24768)
SML0647   Phenazepam ≥97% (HPLC) Phenazepam is the benzodiazepine that exhibit anticonvulsive, anxiolytic, sedative and hypnotic effects in humans and experimental animals. Phenazepam is an agonist of the γ-Aminobutyric acid A (GABAA)-benzodiazepine receptor chloride channel complex.
 
P9625 Phenazine methosulfate ≥90% (UV)    
P3029 Phencyclidine hydrochloride σ opioid receptor agonist and psychostimulant; inhibits NMDA glutamate receptor activation by binding to an allosteric site within the ion channel.
 
P6777 Phenelzine sulfate salt Non-selective MAO-A/B inhibitor.
human ... MAOA(4128), MAOB(4129)
P6902   Pheniramine maleate salt H1 histamine receptor antagonist.
human ... HRH1(3269)
P1636 Phenobarbital Anesthetic; sedative; hypnotic; anticonvulsant
 
P5178 Phenobarbital sodium salt Sedative; hypnotic; anticonvulsant; enhances GABAergic activity.
 
D7446 Phenoxodiol ≥98% (HPLC) Phenoxodiol is a Pan-cancer drug; causes apoptosis via both intrinsic and extrinsic pathways; targets plasma membrane electron transport (PMET).
 
B019 Phenoxybenzamine hydrochloride ≥97%, powder Calmodulin antagonist; α-adrenoceptor antagonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
P6124 5-(4-Phenoxybutoxy)psoralen ≥98% (HPLC), solid Selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. Effective orally or intraperitoneally. 5-(4-Phenoxybutoxy)psoralen has 23-fold selectivity for Kv1.3 over Kv1.5, and 33-125-fold selectivity over other Kv1 family channels.
 
P0111 Phenserine ≥98% (HPLC), solid (-)-Phenserine, a phenylcarbamate derivative, is a selective, non-competitive inhibitor of acetylcholinesterase (AChE). (-)-Phenserine produces rapid, potent, and long-lasting AChE inhibition, in vivo. It is significantly less toxic than (-)-physostigmine. (-)-Phenserine improves cognitive performance in both young learning-impaired and elderly rats. Reduced secretion of β-amyloid (Abeta) has been observed in cell lines exposed to (-)-phenserine, occurring through translational regulation of β-amyloid precursor protein (beta-APP) mRNA via a non-cholinergic mechanism. These in vitro findings appear to translate in vivo into animal models and humans.
 
P7547 Phentolamine hydrochloride ≥98% (TLC), powder α-adrenoceptor antagonist; peripheral vasodilator.
 
P7561 Phentolamine methanesulfonate salt ≥98% (TLC), powder α-Adrenergic receptor antagonist; peripheral vasodilator.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
P101 2-Phenylaminoadenosine >97%, solid Selective A2 adenosine receptor agonist; potent coronary vasodilator; weak inhibitor of adenosine uptake by rat cerebral cortical synaptosomes.
human ... ADORA2A(135), ADORA2B(136)
rat ... Adora1(29290), Adora2a(25369)
P3075 Phenylarsine oxide ≥97%, powder Phenylarsine oxide inhibits internalization of cell surface receptors; inhibits tyrosine phosphatases, with no effect on tyrosine kinase. Metabolic poison.
 
P8386 Phenylbutazone   human ... CYP2C9(1559), PTGIS(5740), PTGS2(5743)
SML0026 4-Phenylbutyryl hydroxamic acid ≥98% (HPLC) 4-Phenylbutyryl hydroxamic acid is a cell permeable HDAC inhibitor which is about 100 times more potent than parent carboxylic acid among nine HDAC enzymes.
 
P1761 trans-2-Phenylcyclopropylamine hemisulfate salt Non-selective MAO-A/B inhibitor.
 
P8511 trans-2-Phenylcyclopropylamine hydrochloride Non-selective MAO-A/B inhibitor.
human ... MAOA(4128), MAOB(4129)
P7340 (±)-threo-1-Phenyl-2-decanoylamino-3-morpholino-1-propanol hydrochloride Glucosylceramide synthase inhibitor; blocks formation of glucosylceramide from ceramide.
 
P6126 (R)-(−)-Phenylephrine hydrochloride powder α1-adrenoceptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
P8155