PI-PZ

Bioactive Small Molecules

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SML1343 3PO ≥98% (HPLC) 3PO is a potent and selective inhibitor of PFKFB3 (6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase) that reduces glycolytic flux and suppresses glucose uptake. 3PO is selectively cytostatic to transformed cells and suppresses the growth of established tumor in mice.
 
PZ0255 CP-101606 mesylate ≥98% (HPLC) CP-101606 mesylate (Traxoprodil mesylate) is a potent noncompetitive antagonist of N-methyl-D-aspartate (NMDA) receptors, selective for the NR2B subunit. CP-101606 mesylate has been shown to be neuroprotective in animal models of brain injury and stroke.
 
SML1189   4-P-PDOT ≥98% (HPLC) 4-P-PDOT is a slelctive MT2 melatonin receptor antagonist 300 fold selective for MT2 (MEL-1B-R) vs MT1 (MEL-1A-R) melatonin receptor subtype.
 
PZ0269 PF-03049423 ≥98% (HPLC) PF-03049423 is an orally active, brain penetrant phosphodiesterase 5 (PDE5) inihbitor.
 
PZ0349 PF-04449613 ≥98% (HPLC) PF-04449613 is a potent and selective cGMP-competitive PDE9A inhibitor (IC50 = 24 nM; IC50 >800 nM against other PDE members), displaying more than 1000-fold selectivity over the majority of 79 non-PDE targets investigated with the exception of cytochrome P450 2C19 (IC50 = 1600 nM), dopamine transporter (Ki = 110 nM), μ-opioid receptor (Ki = 3500 nM), and sodium channel binding site 2 (Ki = 470 nM). PF-4449613 is shown to effectively increase cGMP levels in brain (1-10 mg/kg s.c.; mice) and CSF (1-32 mg/kg s.c.; rats and cynomolgus macaques) in vivo with good brain penetration (brain/plasma ratio of 0.8 in mice). PF-04449613 is effective against D-amphetamine-induced auditory gating deficit (by 43% with 1 mg/kg PF-04449613 s.c.; 1 mg/kg AMP i.v.) and transverse aortic constriction-caused cardiac dysfunction (30 mg/kg/12 h p.o.) in mice in a NOS-independent manner.
 
PZ0235 PF-04691502 ≥98% (HPLC) PF-04691502 is a potent dual mTOR/PI3K inhibitor with Ki values of 1.6, 1.8, 1.9, 2.1 and 16 nM for human PI 3-K δ, α, β, γ, and mTOR, respectively, with no significant inhibitory activity at more than 80 other protein kinases, including PI 3-K downstream kinases, and MAPK family members. PF-04691502 showed antitumor activity in several non-small cell lung carcer (NSCLC) xenografts and ovarian cancer cell lines. PF-04691502 is currently in clinical trials.
 
PZ0278 PF-05020182 ≥98% (HPLC) PF-05020182 is a Kv7.2/4 potassium channel opener.
 
PZ0281   PF-05212384 ≥98% (HPLC) PF-05212384, also known as PKI-587 and Gedatolisib, is a dual phosphatidylinositol-3-kinase (PI3K) / mammalian target of rapamycin (mTOR) inhibitor. PKI-587 potently inhibited class I PI3Ks (IC50 vs PI3K-α = 0.4 nM), PI3K-α mutants, and mTOR. PF-05212384 inhibited growth of 50 diverse human tumor cell lines at IC50s <100 nM and has been in clinical trials in patients with advanced solid tumors. PF-05212384 has also been found to sensitize cells to radiation.
 
PZ0254 PF-06273340 ≥98% (HPLC) PF-06273340 is a brain penetrant, orally available and potent tropomyosin-related kinase (Trk) inhibitor. PF-06273340 is under development as a remedy acute and chronic pain.
 
SML1735 PFM01 ≥98% (HPLC) PFM01 is a cell-permeable N-alkylated Mirin (Sigma Cat. No. 475954) derivative that selectively inhibits against MRE11 endo-, but not exo-, nuclease activity. PFM01 targets MRE11 at a site near the dimer interface, distinct from that occupied by Mirin and PFM39 to allow disruption of the ssDNA-binding groove and selective inhibition against MRE11 endo-, but not exo-, nuclease activity. While both endonuclease and exonuclease activities are required for MRE11-mediated homologous recombination (HR) repair, only FM01 (100 μM), but not the exonuclease inhibitors Mirin (500 μM) and PFM39 (100 μM), rescues G2-phase double-strand break (DSB) repair defect in HR protein BRCA2-deficient HSC62-hTERT fibroblasts following ionizing irradiation (IR) by blocking HR initiation and thereby allowing non-homologous end joining (NHEJ) to proceed.
 
B7688 PiB ≥98% (HPLC) PiB is an inhibitor of the peptidylprolyl isomerase Pin-1. Inhibition of Pin-1 leads to destabilization of the transcription factor Nanog, which is required for maintenance of embryonic stem cell cultures.
 
P0453 Piceatannol powder A plant metabolite possessing anti-leukemic activity; inhibits the non-receptor kinases, Syk and Lck.
human ... CDK2(1017)
SML0585   Piclamilast ≥98% (HPLC) Piclamilast is a potent and selective cyclic AMP phosphodiesterase-4 inhibitor that exhibits equal, high affinity for both the PDE4 high- and low-affinity rolipram binding states (HARBS and LARBS). Recent studies shown that piclamilast inhibits Trypanosoma brucei PDEB1 (TbrPDEB1) and TbrPDEB2.
 
T9576 Picropodophyllotoxin ≥96% (HPLC), powder Picropodophyllotoxin (PPP), an epimer of podophyllotoxin (PPT), has been reported to target insulin-like growth factor-I receptor (IGF-IR) and mediate anticancer functions. However, a study in 2007, has reported that PPP can induce G2-M cell cycle arrest even in IGF-IR deficient cells. Hence, the role of PPP in IGF-IR-mediated anticancer functions is debatable.
Picropodophyllotoxin is an insulin-like growth factor-I (IGF-I) receptor kinase inhibitor.
 
P1675 Picrotoxin powder GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562)
P8390 Picrotoxinin GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
 
SML1335 Pidotimod ≥98% (HPLC) Pidotimod is a dipeptide immunostimulant with biological activity on both the adaptive and the innate immune responses. Pidotimod has been reported to modulate airway epithelial cells functions involved in host-virus interaction possibly through NF-kB activation, promote functional maturation of dendritic cells, and facilitate M2 macrophage polarization and function. Pidotimod has been investigated for use to increase response to recurrent respiratory infections primarily in children.
 
P4368 Piericidin A from microbial source >95% (HPLC), DMSO solution Piericidin A is a potent inhibitor of the mitochondrial and bacterial type I NADH-ubiquinone oxireductase (Complex I). It is considered to bind to the ubiquinone binding sites of the enzyme. Peiricidin A inactivation of complex I completely prevents NADH-induced proton translocation in the NADH-endogenous ubiquinone reductase reaction.
 
P4359 Pifithrin-α ≥95% (HPLC), powder Pifithrin-α is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. Pifithrin-α enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin, etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. Pifithrin-α protects mice from lethal whole body γ-irradiation without an increase in cancer incidence. The protective effect is not seen in p53-null mice or cells expressing a dominant negative mutant of the p53 gene. Protection is conferred by the transient expression of p53 in p53-deficient cell lines.
 
P0122 Pifithrin-μ ≥97% (HPLC), solid Pifithrin-μ is an inhibitor of p53 binding and anti-apoptotic, which directly inhibits p53 binding to mitochondria as well as to Bcl-xL and Bcl-2 proteins. PFTμ rescues cells from lethal γ-irradiation-induced cell death. Because pifithrin-μ shuts down only the p53-mitochondrial pathway without affecting the transcriptional functions of p53, it is superior to pifithrin-α.
 
SML1381 PIK-294 ≥98% (HPLC) PIK-294 is a highly selective inihibitor of the phosphoinositide 3-kinase (PI3K) p110δ with an IC50 value of 10 nM compared to IC50 values of 10 μM, 490 nM and 160 nM for PI3Kα/β/γ, respectively. PIK-294 has been used to help distinguish the unique roles of the various PI3-K isoforms. For example, in a study of CXCL8-induced neutrophil migration, PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration whereas PI3Kγ inhibitor AS-605240 markedly reduced CXCL8 induced chemokinetic migration but had no effect on CXCL8 induced chemotactic migration.
 
SML0546   PIK93 ≥98% (HPLC) PIK-93 inhibits of replication of enterovirus including polio and hepatitis C. PIK93 is a potent, selective, ATP competitive and reversible inhibitor of PI3Kγ and PI4KIIIβ (IC50 = 16 nM and 19 nM, respectively). Also PIK93 moderately inhibits other members of the family including p110δ, PI 3-KC2β, hsVPS34, ATM, p110β and PI 4-KIIIα (IC50 = 0.120, 0.140, 0.320, 0.490, 0.590 and 1.1 μM, respectively). PIK93 blocks ceramide transfer protein-mediated ceramide traffic between endoplasmic reticulum and Golgi.
 
P6503 Pilocarpine hydrochloride ≥98% (titration), powder Nonselective muscarinic acetylcholine receptor agonist; used to produce an experimental model of epilepsy.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
P6628 Pilocarpine nitrate salt ≥98% (TLC), powder Nonselective muscarinic acetylcholine receptor agonist; used to produce an experimental model of epilepsy.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
P0026 Pilsicainide hydrochloride ≥98% (HPLC) Pilsicainide hydrochloride is a pure sodium channel blocker and an open channel blocker of Na+1 channels. Pilsicainide was defined as a pure sodium channel blocker. The compound is classified as a class Ic antiarrhythmic drug, and was originally developed in Japan. Similar to Lidocaine, Pilsicainide binds to open channels, but slowly. Pilsicainide is capable of selectively blocking the late currents in the mutant Na(+) channels that show dominant abnormal burst openings such as in δKPQ mutants. The compound is used to induce Brugada syndrome (BS) in animal models.
 
SML0313 Pimelic Diphenylamide 106 ≥98% (HPLC) 106 is a Class I HDAC inhibitor, demonstrating no activity against class II HDACs. It is a slow, tight-binding inhibitor of HDACs 1, 2, and 3, with a preference toward HDAC3 with Ki of 14 nM, 15 times lower than the Ki for HDAC1.
 
SML1333 Pimobendan ≥98% (HPLC) Pimobendan is an inotropic agent with a dual mechanism of action: it increases myocardial contractility by increasing calcium sensitization to troponin C and it promotes vasodilation by inhibiting phosphodiesterase III (PDE3). Pimobendan has been studied for treating heart failure and cardiomyopathy, primarily for veterinary uses.
 
N1165 Pimonidazole ≥98% (HPLC) Pimonidazole is an effective and nontoxic exogenous 2-nitroimidazole hypoxia marker. Pimonidazole forms adducts with thiol groups in proteins, peptides and amino acids.
 
P1793   Pimozide D2 dopamine receptor antagonist; binds with high affinity to the cloned 5-HT7 receptor; Ca2+ channel antagonist; antipsychotic
human ... ABCB1(5243), CACNA1G(8913), CYP3A4(1576), DRD2(1813), HTR7(3363), KCNH1(3756), KCNH2(3757), OPRD1(4985)
mouse ... Abcb1a(18671), Abcb1b(18669)
rat ... Scnn1g(24768)
SML1592   Pimprinine ≥98% (HPLC) Pimprinine is an indole alkaloid extracted from Streptomyces species that exhibits anticonvulsant activity. Pimprinine is a potent MAO inhibitor. Also, Pimprinine effectively inhibits replication of enterovirus 71 (EV71) and adenovirus 7 (ADV-7).
 
P154 Pinacidil monohydrate powder K+ channel activator; antihypertensive.
mouse ... Kcnj11(16514)
rat ... Kcna1(24520), Kcnj1(24521), Kcnj11(83535), Kcnj5(29713), Kcnj8(25472)
P0778 Pindolol ≥98% (TLC), powder β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator.
human ... ADRB1(153), HTR1A(3350)
P152 S(–)-Pindolol solid β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Active enantiomer of pindolol.
human ... ADRB1(153), HTR1A(3350), HTR1B(3351)
SML0073 Pinoresinol ≥95% (HPLC) Pinoresinol is present in a number of plants including medical plants like Sambucus williamsii, Eucommia ulmoides (duzhong), Styrax sp, Forsythia suspensa, and in extra virgin olive oil. The genus Sambucus is widely distributed in Europe, Asia, and North Africa, and has been used in traditional medicine as an analgesic, antivirus, antiinflammatory, homoeostatic, and diuretic drugs which act on bruises, fractures, and edema. Pinoresinol displays potent antifungal properties by causing damage to the fungal plasma membrane. It exerts anti-oxidative and anti-inflammatory activities by inhibition of TNF- α production (presumably through inhibition of NF- κB and AP-1).
 
SML0098 Pinostilbene hydrate ≥95% (HPLC) Pinostilbene is a resveratrol derivative that induced apoptosis in several cancer cell lines.
 
E6910 Pioglitazone hydrochloride ≥98% (HPLC) Pioglitazone hydrochloride is a PPARγ agonist and thiazolidinedione (TZD) anti-diabetic. Pioglitazone is a selective agonist of the nuclear receptor peroxisome proliferator-activated receptor γ (PPAR-γ) and to a lesser extent PPAR-α.
 
P3246 Pipamperone dihydrochloride ~99% (HPLC), powder D2 dopamine receptor antagonist; 5-HT2 serotonin receptor antagonist; antipsychotic.
 
P0872 8-PIP-cAMP ≥98% (HPLC), solid Selective cAMP-dependent protein kinase (PKA) activator. Site selective cyclic AMP analog with high selectivity for site A of protein kinase A type I and for site B of type II. Acts synergistically together with analogs having opposite site-selectivity.
 
P5865 Rp-8-PIP-cAMPS ≥98% (HPLC), solid Site-selective, lipophilic analogue of the phosphodiesterase-stable protein kinase A inhibitor Rp-cAMPS (Prod. No. A-165).
 
SML1636   Pipecuronium bromide ≥98% (HPLC) Pipecuronium is a bisquaternary aminosteroid muscle relaxant which acts at the nicotinic acetylcholine receptor of the neuromuscular junction. Pipecuronium is a non-depolarizing neuromuscular blocking agent.
 
C7874 Piperaquine tetraphosphate tetrahydrate ≥98% (HPLC) Piperaquine tetraphosphate tetrahydrate is an antimalarial agent highly active against chloroquine-resistant Plasmodium falciparum and Plasmodium vivax.
 
P9159 Piperidine-4-sulfonic acid GABAA receptor agonist.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562)
SML0221 Piperlongumine ≥97% (HPLC) Piperlongumine selectively kills cancer cells regardless of p53 status without harming normal cells. It binds to and inihbits proteins known to regulate oxidative stress, in particular, Glutathione S-transferase pi 1 (GSTP1). It increases the level of reactive oxygen species (ROS) and apoptotic cell death in cancer cells with little effect on either rapidly or slowly dividing primary normal cells. Piperlongumine showed significant antitumour effects in a variety of mouse tumour models and inhibited growth of spontaneously formed malignant breast tumours and their associated metastases.
 
P5295 Piracetam Prototypical nootropic with mechanism of action similar to that of aniracetam and oxiracetam; modulates Na+-flux at AMPA receptors.
human ... GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
rat ... Gria1(50592)
P126 Pirenperone >97%, solid 5-HT2 serotonin receptor antagonist.
human ... HTR2A(3356), HTR2B(3357), HTR2C(3358)
P7412 Pirenzepine dihydrochloride ≥98% (TLC), powder Selective M1 muscarinic acetylcholine receptor antagonist.
human ... CHRM1(1128)
P2116 Pirfenidone ≥97% (HPLC) Pirfenidone inhibits collagen production and fibroblast proliferation. It has shown antifibrotic and anti-inflammatory properties in variety of animal models of pulmonary fibrosis, and in clinical trials.
 
P9233 Piribedil maleate salt A direct dopamine agonist; may be selective for the D3 subtype; no significant affinity for D1 receptors.
human ... DRD3(1814)
SML1818 Pirodavir ≥98% (HPLC) Pirodavir is a broad-spectrum antipicornavirus agent that targets viral capsid protein VP1. Pirodavir is a broad spectrum inhibitor of human rhinovirus (HRV).
 
P5654 Piroxicam ≥98% (TLC) Cyclooxygenase inhibitor.
Non-steroidal anti-inflamatory agent (NSAID) shown to be effective in the prevention of colon cancer.
human ... PTGS1(5742), PTGS2(5743)
rat ... Alox5(25290)
SML0122   Pit-1 ≥98% (HPLC) PIT-1 represents a new class of molecules referred to as PITenins, or PITs. PITs inhibit the binding of PIP3 to the PH domains of several target proteins, including Akt and PDK1, without affecting interactions against PIP2-selective PH domains. PIT-1 inhibits PI3K-PKD-1-Akt dependent phosphorylation in cell based assays, including the phosphorylation of Akt-1, 2 and 3.
PIT-1 is a PIP3-PH domain antagonist
Pit-1 is a small-molecule phosphatidylinositol-3,4,5-trisphosphate (PIP3) antagonist that binds and blocks the pleckstrin domain. It shows inhibitory effects on tumor angiogenesis and metastasis by interfering with the activation of Akt.
 
SML1169   Pitstop 2 ≥98% (HPLC) Pitstop 2 is a selective inhibitor of clathrin-mediated endocytosis that acts via blocking ligand access to the clathrin terminal domain. Pitstop 2 selectively inhibits clathrin-mediated HIV entry and stalls clathrin-coated pit (CCP) dynamics.
 
SML0817 Pivmecillinam ≥98% (HPLC) Pivmecillinam is a gram negative antibiotic, and inhibitor of penicillin-binding protein 2 (PBP2). Pivmecillinam has been shown to have synergistic effects with several antibiotics including novobiocin and rifampin in gram negative bacteria.
 
B9688 Pizotifen ≥98% (HPLC) Pizotifen is a serotonin antagonist acting mainly at the 5-HT1, 5-HT2A and 5HT2C receptors with some antihistamine activity. It is used for the prevention of vascular headache including migraine and cluster headache.
 
P4365 PJ-34 hydrochloride hydrate ≥98% (HPLC), powder PJ-34 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor.
 
C0424 PK 11195 Peripheral benzodiazepine antagonist.
human ... BZRAP1(9256), TSPO(706)
rat ... Gabra2(29706), Tspo(24230)
P0102 PKCβII Peptide Inhibitor I trifluoroacetate salt ≥95% (HPLC), lyophilized powder PKCβII Peptide Inhibitor I is a cell-permeable protein kinase C inhibitor.
 
K4394 PKF118-310 ≥98% (HPLC) PKF118-310 is an antagonist of the Tcf4/b-catenin signaling. The compound disrupts the Tcf4/b-catenin complex and inhibits expression of Tcf4 responsive genes. PKF118-310 inhibits expression of survivin and induces apoptosis in HCC, colon tumor and lymphocytic leukemia cell lines.
 
SML1095 PKI-166 ≥98% (HPLC) PKI-166 is a potent, selective and orally available EGF-R tyrosine kinase inhibitor. PKI-166 potently inhibits the growth and metastasis of many human cancers including human pancreatic cancer.
 
SML1326 PK-THPP ≥98% (HPLC) PK-THPP is a potent antagonist of tandem pore potassium channel subunit TASK-3 (KCNK9, K2P9.1) with an IC50 value of 35 nM for TASK-3 compared to 303 nM for TASK-1 and with >140 fold selectivity over a wider range of potassium channels. PK-THPP was found to act as a respiratory stimulant, stimulating breathing in isoflurane-anesthetized rats.
 
L7670 PL405 trifluoroacetate salt ≥98% (HPLC) PL405 is a specific and high affinity endothelin converting enzyme-2 (ECE-2) fluorigenic substrate. PL405 is cleaved by ECE-2 at the Pya-F amide bond to yield the highly fluorigenic Ac-SKG-Pya.
 
SML0090 PL415 trifluoroacetate salt hydrate ≥98% (HPLC) PL415 is fluorescent cleavage product of PL405, an endothelin converting enzyme-2 (ECE-2) fluorigenic substrate. PL415 UV maximum absorption (λ max) is 342 nm (ε= 24 940L. mol-1.cm-1). PL415 is used to obtain calibration curve for kinetic studies utilizing PL405.
 
SML0307 Pleconaril ≥98% (HPLC) Pleconaril is an orally bioavailable, broad-spectrum antipicorna-viral agent that binds to hydrophobic pocket in VP1 major capsid protein. Also, pleconaril delays the onset of diabetes in experimental animals infected with Ljungan virus (LV).
 
SML0285 Pleuromutilin ≥95% Pleuromutilin is an antibiotic natural product that inhibits bacterial protein synthesis by binding to bacterial ribosomes in the peptidyl transferase center and inhibiting peptide bond formation.
 
SML0444 Pluripotin ≥98% (HPLC) Pluripotin is an activator of murine embryonic stem (ES) cell self-renewal. It appears that pluripotin mediates the activity by dual RasGAP and ERK1 inhibition.
 
SML0682   PluriSIn #1 ≥95% (HPLC) PluriSIn #1 is a pluripotent cell specific inhibitor that induces ER stress and apoptosis in hPSC (human pluripotent stem cells). PluriSIn #1 selectively purges hPSCs while saving progenitor and differentiated cells. PluriSIn #1 is an inhibitor of stearoyl-coA desaturase (SCD1).
 
SML0966   PLX647 ≥98% (HPLC) PLX647 is a potent and specific dual inhibitor of the receptor tyrosine kinases FMS and KIT. PLX647 blocks activation of macrophages, osteoclasts and mast cells in both cell based and in vivo inflammation models.
 
SML1203 2-PMAP ≥98% (HPLC) 2-PMAP is a brain penetrant inhibitor of amyloid precursor protein (APP) production. 2-PMAP lowers levels of the amyloid precursor protein (APP) in CHO APP751SW cells. Also it reduces brain level of APP in mice model. 2-PMAP exhibits no cellular toxicity up to 100 μM.
 
M2199 PMEG hydrate ≥98% (HPLC) The acyclic nucleotide 9-(2-phosphonylmethoxyethyl)guanine (PMEG) forms an active phosphorylated metabolite, PMEG diphosphate (PMEGpp), in cells and causes cytotoxicity in dividing cells due to potent inhibition of the nuclear DNA polymerases resulting in inhibition of DNA synthesis and/or DNA repair.
 
S0826 S-PMH ≥98% (HPLC) S-PMH augments cell-cell adhesion by enhancing tight and adherens junctions (TJ and AJ) and by abolishing the destabilizing actions of Calcitonin (CT) on these complexes. Calcitonin and its receptor are expressed in prostate cell cancers and plays a pivotal role in metastasis and tumorgenesis. It appears that CT promotes prostate cancer metastasis by reducing cell-cell adhesion through the disassembly of tight and adherens junctions and activation of B-catenin signaling. S-PMH apparently blocks CT-stimulated alphavbeta3 activity (a key factor in bone metastasis). In a nude mice model I.p. administered S-PMH and its S-ethyl derivative decreased orthotopic tumor growth and inhibited the formation of tumor micrometastases in distant organs. S-PMH is relatively nontoxic in a cell proliferation assay.
 
SML1612 2-PMPA ≥98% (HPLC) 2-PMPA is a potent (IC50 ~ 1 nM) and selective inhibitor of Glutamate carboxypeptidase II (GCPII), also known as N-acetyl-L-aspartyl-L-glutamate peptidase I (NAALADase I), NAAG peptidase, or prostate-specific membrane antigen (PSMA). 2-PMPA has neuroprotective activity activity. 2-PMPA has been shown to prevent and treat cognitive impairment in the EAE model of multiple sclerosis and to protect against soman-induced neuropathology.
 
SML0498 PNU112455A ≥98% (HPLC) PNU112455A is an ATP site competetive inhibitor of CDK2 and CDK5. The Km for binding to the ATP site of CDK2 and CDK5 is 3.6 and 3.3 mM, respectively.
 
P0043 PNU-120596 ≥98% (HPLC) An allosteric modulator of α7 nicotinic receptors, N-(5-chloro-2,4-dimethoxyphenyl)-N′-(5-methyl-3-isoxazolyl)-urea (PNU-120596), causes conformational changes in the extracellular ligand binding domain similar to those caused by acetylcholinePNU-120596 is a positive allosteric modulator selective for the α7 nicotinic acetylcholine receptor. PNU-120596 produces no detectable change in currents mediated by α4β2, α3β4, α9α10 nAChRs. It increases channel mean open time, but does not affect ion selectivity. It does not bind at the agonist binding site, but induces conformational changes similar to the natural effector.
 
P6499 PNU-282987 hydrate solid, ≥98% (HPLC) Decreased expression of a homomeric alpha7 nicotinic acetylcholine receptor (nAChR) is connected with inability to process sensory information in schizophrenia. PNU-282987 is a novel selective agonist of the alpha7 nAChR that evoked whole-cell currents from cultured rat hippocampal neurons that were sensitive to the selective alpha7 nAChR antagonist methyllycaconitine (MLA) and enhanced GABAergic synaptic activity. The alpha7 nAChR agonist PNU-282987 improves auditory gating and enhances hippocampal oscillatory activity. These results provide further support for the concept that drugs that selectively activate alpha7 nAChRs may offer a novel, potential pharmacotherapy in treatment of schizophrenia.
 
P0052 PNU-74654 ≥98% (HPLC), solid PNU-74654 inhibits the Wnt-β catenin pathway by blocking the interaction between β-catenin and TCF (T cell factor). PNU-74654 is also an anti-tumor agent. Aberrant activation of the Wnt/β-catenin pathway (canonical pathway) is implicated in driving development/progression of different tumors, such as colon cancer, through interaction between β-catenin and T cell factor (TCF), which regulates the expression of target genes in cell proliferation and differentiation. Inhibition of this pathway activity in cancer cell lines efficiently blocks their growth. PNU-74654 inhibits this pathway by blocking the interaction between β-catenin and TCF.
 
SML0688   PO1 ≥98% (HPLC) PO-1 is a cell-permeable fluorescent sensor that is highly selective for detecting the presence of H2O2 in living cells.
 
P4405 Podophyllotoxin Inhibits microtubule assembly; antineoplastic.
 
SML0469 Poloxin ≥98% (HPLC) Poloxin is a non-ATP competitive Polo-like Kinase 1 (Plk1) inhibitor that targets the polo-box domain. Poloxin inductees Plk1 mislocalization, chromosome congression defects, mitotic arrest, and apoptosis in HeLa cells.
 
P2008 Polyanetholesulfonic acid sodium salt powder Polyanetholesufonic acid has effect on antithrombin III activity.
 
P8824 Polyanetholesulfonic acid sodium salt BioUltra    
SML0049   Polygodial ≥97% (HPLC) Polygodial is a selective activator of Transient Receptor Potential Anykrin 1 (TRPA1) channels. Initially painful, polygodial acts as an analgesic by desensitizing sensory neuron. Polygodial also has broad antifungal properties, and is cytotoxic against bacteria and algae.
 
P0018 Pomalidomide ≥98% (HPLC) Pomalidomide is a second generation immunomodulator, TNF-α inhibitor, and thalidomide analog.
 
P6237   α-Pompilidotoxin >98% Voltage-gated sodium channel activator
 
P3490 Ponasterone A ≥65% Ponasterone A is an insect hormone, involved in regulating metamorphosis.
 
P0040 PP1 ≥98% (HPLC) PP1 is a potent and selective Src family protein tyrosine kinase inhibitor.
 
P0042 PP2 ≥98% (HPLC) PP2 is a selective inhibitor of Src-family tyrosine kinases with >10,000-fold selectivity over ZAP-70 and JAK2.
 
P0036 PP121 ≥98% (HPLC) PP121 is a dual inhibitor of tyrosine and phosphoinositide kinases. PP121 is the first inhibitor active on both Tyrosine kinases and the phosphatidylinositol-3-OH kinase (PI(3)K) family. The inhibitor is not effecting other serine-threonine protein kinases.
 
P0037 PP242 hydrate ≥98% (HPLC), powder PP242 is a potent and selective mTOR inhibitor. PP242 is a first selective inhibitor that targets ATP domain of mTOR.
 
P0057 PPBP maleate ≥98% (HPLC), powder PPBP maleate is a potent σ1 receptor ligand. PPBP is a very potent agonist of σ1 receptor (Ki = 0.8 nM).
 
G6298   (RS)-PPG ≥98% (HPLC) (RS)-PPG is a potent selective group III mGluR agonist; anticonvulsant and neuroprotectant in vivo.
 
SML1596   PPZ2 ≥98% (HPLC) PPZ2 selectively activates DAG-activated TRPC3/TRPC6/TRPC7 channels. PPZ2 activates native TRPC6-like channels in smooth muscle cells isolated from the rabbit portal vein. PPZ2 induces BDNF-like neurite growth and neuroprotection in cultured neurons.
TRPCs are cation channels, mainly permeable to Ca2+ ions. TRPC6 plays a crucial role in tumor development. TRPC3 controls fibronectin expression, thereby regulating wound healing process. TRPC7 is involved in the proliferation of osteoblasts.
 
SML1116 PQ-10 ≥98% (HPLC) PQ-10 is a potent and selective inhibitor of phosphodiesterase 10A (PDE10). Apparently, PQ-10 enhances basic auditory information processing in rats. PQ-10 as other PED10 inhibitors suppresses a growth of human non-small cell lung cancer (NSCLC) cell lines.
 
SML0431 PQ1 succinate ≥98% (HPLC) PQ1 binds tightly to connexin 43 and activates intracellular gap junctions. Treatment of the breast cancer cell line T47D with 200 nM PQ1 induces a 30% increase in gap junctional intercellularcommunication (GJIC) and a 90% decrease in cell growth, with no effect on normal breast epithelial cells.
 
P0113 PQ401 ≥98% (HPLC), powder PQ401 is an insulin growth factor-1 receptor (IGF-1R) inhibitor.
 
SML0430 PR-619 ≥95% (HPLC) PR-619 is a cell permeable broad spectrum deubiquitylating enzymes (DBUs) inhibitor. PR-619 induces the accumulation of polyubiquitylated proteins in cells without directly affecting proteasome activity.
 
SML1462 Practolol ≥95% (HPLC) Practolol is a potent and selective β-adrenoceptor antagonist. Practolol is a beta blocker that was discontinued to due to adverse reactions (keratoconjunctivitis sicca, conjunctival scarring, fibrosis, metaplasia, and shrinkage).
 
P0240 PRAK Substrate Peptide 1 mg/mL in H2O, ≥98% (HPLC), aqueous solution Peptide substrate for the enzyme PRAK (P38 regulated/activated protein kinase)
 
A1237 Pramipexole dihydrochloride >98% (HPLC), powder Pramipexole is a dopamine agonist active at D3 and D2 receptor subtypes. Pramipexole has been found to have neuroprotective effects independent of its dopamine receptor agonism. It reduces mitochondrial reactive oxygen species (ROS) production and inhibits the activation of apoptotic pathways.
Pramipexole is a therapeutic agent for Parkinson’s disease and restless leg syndrome. It also exhibits antidepressant responses in patients suffering from MDD (major depressive disorder) and bipolar depression.
 
SML0816   Pramiracetam ≥98% (HPLC) Pramiracetam is a potent nootropic agent that is a member of the racetam drug family. Pramiracetam improves cognitive deficits associated with traumatic brain injuries. Also, pramiracetam is a specific inhibitor of prolyl endopeptidase.
 
P0080 Pranlukast hemihydrate ≥98% (HPLC), white solid Pranlukast is a subtype specific CysLT1 receptor antagonist. Leukotrienes are involved in the inflammation response and are divided into two main classes; leukotriene B4 and cysteinyl-substituted leukotrienes.
 
SML1423 Pranoprofen ≥98% (HPLC) Pranoprofen is a non-steroidal anti-inflammatory drug (NSAID) used primarily in ophthalmology. Pranoprofen is a cyclooxygenase (COX) inhibitor.
 
SML0331 Prasugrel ≥98% (HPLC) Prasugrel is a platelet inhibitor that reduces the aggregation of platelets by irreversible binding to P2Y12 receptors. Prasugrel interacts in an irreversible manner with the residues Cys97 and Cys175 of the human P2Y12-receptor.
 
P4498 Pravastatin sodium salt hydrate ≥98% (HPLC), powder Competitive, water-soluble 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor. Inhibits cholesterol synthesis in vivo (Ki ~1 nM).
Pravastatin sodium is a competitive, water-soluble 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.
 
P3654 Prazepam Anxiolytic
 
P7791 Prazosin hydrochloride ≥99% (TLC) Peripheral α1-adrenoceptor antagonist; vasodilator.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
P2607 PRE-084 solid Potent and highly selective σ1 opioid receptor agonist.
human ... OPRS1(10280)
rat ... Oprs1(29336), Slc6a3(24898)
P6004 Prednisolone ≥99% Prednisolone is a glucocorticoid with anti-inflammatory and immunosuppressive activity.
human ... AR(367), ESR1(2099), NR3C1(2908), NR3C2(4306), PGR(5241), SERPINA6(866)
mouse ... Nr3c1(14815)
rat ... Ar(24208)
P8650 Prednisolone 21-acetate ≥97%    
P4153 Prednisolone 21-hemisuccinate sodium salt ≥90%, powder    
P6254 Prednisone ≥98% Prednisone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activity.
 
PZ0010 Pregabalin ≥97% (NMR) Pregabalin is a lipophilic GABA analog/ligand at α2δ subunit of voltage-dependent Ca2+ channels. Pregabalin is an anticonvulsant, anxiolytic analgesic used to treat peripheral neuropathic pain and fibromyalgia.
 
P3635 5β-Pregnane-3α,20α-diol glucuronide    
P8629 5β-Pregnane-3α,17α,20α-triol    
P8754 5β-Pregnane-3α,17α,21-triol-20-one    
P5052 5α-Pregnan-3α-ol-11,20-dione powder, ≥98% (TLC) Synthetic steroid compound alphaxalone (AFX) - 5α-Pregnan-3α-ol-11,20-dione- is a neurosteroid that directly activates and potentiates GABAA receptor-activated membrane current (IGABA). It acts as a positive allosteric modulator of the GABAA receptor; anesthetic. The alpha subunit subtype of GABAA determines the efficacy, but not the potency, of AFX neuroactive steroid to potentiate IGABA.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRG2(2566)
P8887 5α-Pregnan-3α-ol-20-one solid Positive allosteric modulator of GABAA chloride channel.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562)
mouse ... Gabrg2(14406)
rat ... Gabra1(29705), Gabra2(29706), Gabrg2(29709)
P8129 5β-Pregnan-3α-ol-20-one   rat ... Gabra2(29706)
P8004 5α-Pregnan-3β-ol-20-one 3β-acetate ≥98%    
P0543 5-Pregnen-3β-ol-20-one-16α-carbonitrile ≥97% Pregnenolone-16α-carbonitrile (PCN) is a glucocorticoid receptor antagonist and a PXR (pregnane X receptor) activator.
 
P162 Pregnenolone sulfate sodium salt Neurosteroid that antagonizes the GABAA receptor chloride channel.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562)
SML0807   PreQ1 dihydrochloride ≥98% (HPLC) PreQ1 (pre-queuosine1) is an intermediate of the queuosine pathway. Also, PreQ1 binds with high affinity to the aptamer of PreQ1 riboswitch, which attenuates protein expression.
 
P9547 Prilocaine hydrochloride ≥98% (TLC) Used for local nerve block and for spinal anesthesia; pharmacological properties are similar to those of lidocaine.
 
P0069 PRIMA-1 ≥98% (HPLC), solid PRIMA-1 is a selective re-activator of mutant p53 activity in tumor cells, and an inducer of apoptosis and inhibitor of growth of human tumors with mutant p53. Mutations in the tumor suppressor p53 take place in >50% tumor cells. PRIMA-1 selectively restores sequence-specific DNA binding and transactivational activity to mutant p53 proteins at μM concentrations. PRIMA-1 works as a re-activator of the apoptotic function of mutant p53 via conformational modulation of function-specific epitopes.
 
PZ0198 Prinomastat hydrochloride ≥95% (HPLC) Prinomastat is a matrix metalloprotease (MMP) inhibitor with selectivity for MMPs 2, 3, 9, 13, and 14. Inhibition of these MMPs has been postulated to block tumor invasion and metastasis. It is extremely potent at MMP-3 and MMP-2 with IC50s, 30 pM & 50 pM, respectively.
 
P6617 Pristanic acid solution mixture of isomers, ethanol solution, ≥97% (GC) Oxidation product of fatty acids in the diet, particularly phytanic acid. Phytanic acid is oxidized by alpha oxidation yielding pristanic acid, which is subsequently degraded by peroxisomal beta oxidation. Several inborn errors of metabolism with one or more deficiencies in the phytanic acid and pristanic acid breakdown have been described.
 
P0020 Pristimerin More active than euphol against MGL, better activity with rat neurons, but less selective relative to similar enzymes. First MGL inhibitor to act reversibly, several others covalently bind to cysteine residues. Other studies involve multiply mylome, pristimerin inhibits NF-κB activation via inhibition of IKK-α or IKK-β. It is the methyl ester of celastrol (C0869).
 
P0108 PRL-3 Inhibitor I ≥98% (HPLC), solid PRL-3 Inhibitor I is a rhodanine derivative with an IC50 value of 0.9 μM against phosphatase of regenerating liver-3 (PRL-3), a nonclassical protein tyrosine phosphatase that has recently been shown to be involved in cancer metastasis. PRL-3 Inhibitor I reduced the invasiveness of B16F10 melanoma cells in a cell based assay.
 
P8761 Probenecid    
P9391 Procainamide hydrochloride Inhibits DNA methyltransferase and modulates epigenetic regulation of gene expression. Na+ channel blocker and Class IA anti-arrhythmic.
 
P9879 Procaine hydrochloride ≥97% Na+ channel blocker
 
SML0036 Procarbazine hydrochloride ≥98% (HPLC) Procarbazine is an antineoplastic alkylating agent widely used in cancer chemotherapy in combination with other compounds. It has multiple mechanisms of action. Procarbazine inhibits protein, RNA and DNA synthesis in addition to being an alkylating agent.
 
P9180 Procaterol hydrochloride β2-adrenoceptor agonist; bronchodilator.
 
P0350   Procathepsin B Fragment 26-50, rat ≥95% (HPLC) Cathepsin B inhibitor.
rat ... Ctsb(64529)
P9178 Prochlorperazine dimaleate salt Phenothiazine antipsychotic; D2 dopamine receptor antagonist; antispasmodic
human ... DRD2(1813)
P3794 Procyclidine hydrochloride Atropine-like antispasmodic
 
P0130 Progesterone ≥99% Induces maturation and secretory activity of the uterine endothelium; suppresses ovulation. Progesterone is implicated in the etiology of breast cancer.
human ... ABCB1(5243), AR(367), CYP2C9(1559), EBP(10682), ESR1(2099), ESR2(2100), NR3C1(2908), NR3C2(4306), PGR(5241), SERPINA6(866)
mouse ... Esr1(13982)
rat ... Ar(24208), Nr3c1(24413), Pgr(25154)
P8779   Progesterone 3-(O-carboxymethyl)oxime:BSA–fluorescein isothiocyanate conjugate    
UC184   Progesterone 11α-glucuronide Phase II metabolite of progesterone
 
G7048 Proguanil hydrochloride ≥95% (HPLC) Chlorguanide (proguanil) is combined with atovaquone for malaria prophylaxis. The two compounds act synergistically to inhibit the plasmodial dihydrofolate reductase (DHFR) and interrupt the electron transport chain. Mutations in DHFR account for the development of resistant strains.
 
P6656 Promazine hydrochloride D2 dopamine receptor antagonist; phenothiazine antipsychotic.
human ... DRD2(1813)
P4651 Promethazine hydrochloride H1 histamine receptor antagonist; CNS depressant; anticholinergic.
human ... HRH1(3269)
SML1777 Propacetamol hydrochloride ≥98% (HPLC) Propacetamol is a prodrug of paracetamol (acetaminophen) with improved water solubility. Propacetamol is an analgesic drug delivered by IV when oral application of NSAID is not appropriate or contradicted.
 
P4670 Propafenone hydrochloride Blocks hKv1.5 and ATP-sensitive K+ channels; class 1C antiarrhythmic agent that is also an antagonist at β adrenergic receptors.
human ... ABCB1(5243), ADRB1(153), ADRB2(154), ADRB3(155), CYP1A2(1544)
P8891 Propantheline bromide ≥97% (TLC), powder Inhibits action of acetylcholine at post-ganglionic synapses; muscarinic acetylcholine receptor antagonist; antispasmodic; reduces gastric acid secretion.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
P9114 6-(2-Propargyloxyphenyl)hexanoic acid ≥98%, solid Selective inhibitor of epoxygenation catalyzed by CYP450 isozymes.
 
P9689 Propentofylline solid c-AMP phosphodiesterase inhibitor; nerve growth factor stimulator; adenosine transport inhibitor; non-selective adenosine receptor antagonist.
human ... ADORA1(134), PRKAR1A(5573), PRKAR1AP(5574), PRKAR1B(5575), PRKAR2A(5576), PRKAR2B(5577)
P4170 Propidium iodide ≥94.0% (HPLC)    
81845 Propidium iodide ≥94% (HPLC)    
P5648 β-Propiolactone Grade II, ≥90%    
P7780 Propionylpromazine hydrochloride Phenothiazine antipsychotic; D2 dopamine receptor antagonist.
human ... DRD2(1813)
SML0602   Propiverine hydrochloride ≥98% (HPLC) Propiverine is an antimuscarinic drug used for the treatment of overactive blaqdder and urinary incontinence. Propiverine and/or its metabolites also have calcium channel blocking properties in addition to antimuscarinic activity, which may contribute to the clinical activity.
 
P0689 (R)-(+)-Propranolol hydrochloride ≥98% (TLC) Less active enantiomer of propranolol.
 
P8688 (S)-(−)-Propranolol hydrochloride ≥98% (TLC), powder Active β-adrenoceptor blocking enantiomer, as measured by inhibition of isoprenaline-induced tachycardia; Propranolol is also non-specific 5-HT1A, 5-HT1B and 5-HT1C serotonin receptor antagonist. The stereoselective association of mianserin and propranolol with the 5HT1A, 5HT1B and 5HT1C sites may prove useful in the characterization of these sites
human ... ADRB1(153), ADRB2(154), ADRB3(155), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355)
P0884 (±)-Propranolol hydrochloride ≥99% (TLC), powder β-adrenoceptor antagonist; 5-HT1/5-HT2 serotonin receptor antagonist; cardiac depressant (anti-arrhythmic).
human ... ADRB1(153), ADRB2(154), ADRB3(155), HTR1A(3350), HTR1B(3351), HTR1D(3352), HTR1E(3354), HTR1F(3355), HTR2A(3356), HTR2B(3357), HTR2C(3358)
P5489 Propybicyphat 95% (NMR), solid GABA-gated chloride channel blocker, non-competitive GABA antagonist in mammals.
 
P3130 Propyl gallate powder An antioxidant that exhibits antimicrobial activity. Propyl gallate has been reported to be an effective antioxidant-based hepatoprotector, both in vitro and in vivo. It has also been shown to prevent neuronal apoptosis and block the death of neurons exposed to FeSO4/GA as well as partially protect endothelial cells against TNF-induced apoptosis. However, propyl gallate induced single strand breaks in DNA at concentrations higher than 0.25 μM when it was combined with copper concentrations at 5 μM and above. Another report, however, found that incubation of isolated rat hepatocytes with propyl gallate at concentrations of >1 mM induced cell killing, whereas, a lower concentration of propyl gallate > 0.5 mM resulted in a ladder formation of soluble low-molecular weight DNA fragments, characteristic of apoptosis.
An antioxidant that exhibits antimicrobial activity. Propyl gallate has been reported to be an effective antioxidant-based hepatoprotector, both in vitro and in vivo. It has also been shown to prevent neuronal apoptosis and block the death of neurons exposed to FeSO4/GA as well as partially protect endothelial cells against TNF-induced apoptosis.
 
48710 Propyl gallate antioxidant, ≥98.0% (HPLC) An antioxidant that exhibits antimicrobial activity. Propyl gallate has been reported to be an effective antioxidant-based hepatoprotector, both in vitro and in vivo. It has also been shown to prevent neuronal apoptosis and block the death of neurons exposed to FeSO4/GA as well as partially protect endothelial cells against TNF-induced apoptosis. However, propyl gallate induced single strand breaks in DNA at concentrations higher than 0.25 μM when it was combined with copper concentrations at 5 μM and above. Another report, however, found that incubation of isolated rat hepatocytes with propyl gallate at concentrations of >1 mM induced cell killing, whereas, a lower concentration of propyl gallate > 0.5 mM resulted in a ladder formation of soluble low-molecular weight DNA fragments, characteristic of apoptosis.
An antioxidant that exhibits antimicrobial activity. Propyl gallate has been reported to be an effective antioxidant-based hepatoprotector, both in vitro and in vivo. It has also been shown to prevent neuronal apoptosis and block the death of neurons exposed to FeSO4/GA as well as partially protect endothelial cells against TNF-induced apoptosis.
 
D027 R(−)-Propylnorapomorphine hydrochloride solid Highly potent and selective D2 dopamine receptor agonist.
human ... DRD2(1813)
D041 S(+)-Propylnorapomorphine hydrochloride solid Limbic-selective dopamine antagonist.
 
SML1417   Prosaptide Tx 14(A) trifluoroacetate salt ≥95% (HPLC) Prosaptide Tx 14(A) is a potent agonist of G protein-coupled receptors GPR37 (also known as Parkin-associated endothelin receptor-like receptor Pael-R) and GPR37L1. Prosaptide Tx 14(A) is the active fragment of prosaposin, a secreted neuroprotective and glioprotective factor. Prosaptide Tx 14(A) has EC50 values of 5 nM for GPR37L1 and 7 nM for GPR37, and has also been shown to have some GSK3 inhibitory properties. Prosaptide has been shown to improve nerve regeneration in diabetic rats, to reduce neuropathic pain, and to protect dopaminergic neurons in animal models of Parkinson disease.
 
P7265 Prostaglandin A1 synthetic Cyclopentenone prostaglandin that stimulates the expression of stress genes.
 
P5515 Prostaglandin E1 ≥98% (HPLC), synthetic Vasodilator; activates adenylate cyclase.
human ... PTGIR(5739)
mouse ... Ptger1(19216), Ptger2(19217), Ptger3(19218), Ptger4(19219)
P5390 Prostaglandin B2 ≥98%, synthetic Primary prostaglandin of osteoblasts; induces pulmonary hypertension.
 
P5172 Prostaglandin D2 ≥95%, synthetic Primary prostaglandin in brain; induces inflammation; stimulates adenylyl cyclase.
 
P7742 Prostaglandin G2 ≥95% (HPLC), acetone solution Aryl hydrocarbon receptor (AhR) ligand and activator of the AhR signal transduction pathway. Also shown to activate nitric oxide synthase (NOS) in rat brain synaptosomal membrane fractions.
 
P7867 Prostaglandin H2 ≥95% (HPLC), acetonitrile solution Aryl hydrocarbon receptor (AhR) ligand and activator of the AhR signal transduction pathway. Also acts as a modest ligand of the peroxisome proliferator-activated receptor (PPAR-γ).
 
P0077 Prostratin ≥98% (HPLC) Prostratin, an unusual non-tumorigenic phorbol ester, is an activator of protein kinase C (PKC) and also an activator of nuclear factor KB (NF-KB) mediated through activation of the IKKs (IKB kinases). Prostratin exhibits potent in vitro activity by inducing HIV expression in latently infected cell lines and primary cells, thus antagonizing HIV latency. Activation of PKC and NF-kB has been proposed as the mechanism of action. Prostratin also inhibits HIV entry into target cells by down-regulating CD4 and CXCR4 receptors.
 
F4051   Proteasome Fraction II from rabbit 5 mg/mL, Reticulocyte cell extract, solution Essentially ubiquitin and ATP free. Contains E1, most E2s, UCHs, and the proteasome 20S and 26S isoforms.
Protein fraction of a cell extract that binds to anion-exchange resin.
 
19459   Protein G recombinant from Escherichia coli, ≥90%    
P6062 Protein Kinase A Inhibitor Fragment 6-22 amide ≥97% (HPLC) Potent inhibitor of cAMP-dependent protein kinase (PKA) (Ki = 2.5 nM); derived from the active portion of the heat-stable PKA inhibitor protein PKI.
 
P3115   Protein Kinase C Inhibitor, Myristoylated ≥7.5 mg/mL (peptide and counter ion), ≥95% (Minimum peptide content 70%, HPLC), aqueous solution (neutral pH) Protein Kinase C Inhibitor, Myristoylated is a cell permeable, specific inhibitor of calcium and phospholipid-dependent Protein Kinase C.
 
P1614   Protein kinase Cζ pseudosubstrate, myristoyl trifluoroacetate salt ≥90% (HPLC) Cell permeable protein kinase C (PKC) ζ inhibitor.
 
P0300 Protein Kinase Inhibitor from rabbit ≥85% (HPLC) Inhibitor of c-AMP-dependent protein kinase
These proteins bind to the catalytic subunit of cyclic-AMP dependent protein kinase, displacing the regulatory subunit and inhibiting phosphorylating activity. The cyclic-AMP binding capacity of the regulatory subunit is enhanced.
 
P8489 Protopine hydrochloride ≥98%, solid Protopine hydrochloride is a Ca2+ channel blocker and antiplatelet agent.
 
P8813 Protriptyline hydrochloride ≥99% (TLC), powder Norepinephrine uptake blocker.
 
SML1013 PRT4165 ≥98% (HPLC) PRT4165 is a potent inhibitor of PRC1 (polycomb-repressive complex 1)-mediated histone H2A ubiquitylation in vivo and in vitro. PRT4165 inhibits the in vitro histone H2A E3 ubiquitin ligase activity of PRC1 components RING1, RNF2, and a BMI1/RNF2 complex. PRT4165 also inhibits DNA double-strand breaks induced ubiquitylation of histone H2AX.
 
SML1371 Prucalopride ≥98% (HPLC) Prucalopride is a selective 5-HT4 serotonin receptor agonist with enterokinetic activity. 5-HT4 receptors are GPCRs that are expressed in the CNS and peripheral tissues. The receptor has a role in GI motility disorders such as irritable bowel syndrome and idiopathic constipation. Agonists are prokinetic and of potential use for disoroders of reduced motility. Prucalopride is a selective 5-HT4 serotonin receptor agonist with enterokinetic activities. Prucalopride has pK(i) values of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively, and at least 290-fold selectivity for 5-HT4 over other serotonin and dopamine receptors.
 
P6624 PS-1145 dihydrochloride ≥98% (HPLC), solid PS-1145 is an IKB kinase (IKK) inhibitor.
 
SML0850 PS372424 hydrochloride ≥97% (HPLC) PS372424 is a highly specific agonist of human CXCR3 that potently inhibits the migration of activated T cells toward the chemokine mixture in synovial fluid from patients with active rheumatoid arthritis. PS372424 activated ERK in T cells with a similar potency and kinetic to the natural ligand CXCL11.
 
P0022 PS48 ≥98% (HPLC) PS48 is a PDK1 (phosphoinositide-dependent protein kinase 1) activator which binds to the HM/PIF binding pocket rather than the ATP-binding site. PS48 is one of only a few truly allosteric compounds targeting a regulatory binding site on a protein kinase catalytic domain that is not adjacent to or overlapping with the ATP-binding site.
 
P0373 PSB 1115 potassium salt hydrate ≥95% (HPLC) PSB 1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist.
 
SML0753   PSB-12062 ≥98% (HPLC) PSB-12062 is a P2X4 receptor antagonist. P2X4 receptors are highly expressed in the CNS, and have been studied as a therapeutic target for neutopathic pain, and treatment of traumatic brain injury, cerebral ischemia, and spinal cord injury. PBS-12062 is a new P2X4-specific antagonist with equal potency against human, rat and mouse receptors (IC50s 1.38, 0.92 and 1.76 μM, respecitively). The compound does not display significant inhibition of human P2X1, P2X2, P2X3 or P2X7 at 10 μM.
 
SML0212 PSB36 ≥98% (HPLC) Inhibition of A1 adenosine receptor by PSB36 modulates the spinal antinociception in animal models.
PSB36 is a very potent, selective antagonist of the adenosine A1 receptor. The compound selectivity (Ki) for human A1, A2A, A2B and A3 receptors is 0.7, 980, 187 and 2300 respectively. PSB36 is considerably more potent that DPCPX (EC50 0.012 nM vs 2.9 nM)
 
SML0226   Pseudocantharidin C ≥98% (HPLC) Pseudocantharidin C stimulates PP2A activity up to two-fold without influencing PP1. PP2A activation by pseudocantharidin C changes phosphorylation of tra2-beta1 at position T33 and promotes the SMN2 pre-mRNA exon 7 inclusion.
 
E2750 (+)-Pseudoephedrine hydrochloride ≥98% Non-selective adrenergic agonist; decongestant
 
P0184   Pseudomonas exotoxin A from Pseudomonas aeruginosa lyophilized powder Shown to be toxic to animals and to cell lines, and to inhibit protein synthesis via ADP ribosylation of elongation factor 2.
 
P0028 PSN-375963 ≥98% (HPLC) PSN-375963 is a GPR119 partial agonist. GPR119 is an orphan GPCR, expressed predominantly in pancreas and GI tract, that has been characterized. Its endogenous ligands are oleoylethanolamide (OEA) and oleoyl-lysophosphatidylcholine, lipid signaling molecules that regulate food intake and body weight. OEA decreases food intake, so GPR119 agonists are potential therapies for obesity. Initial studies showed that PSN-375963 has similar potency and partial efficacy compared to OEA. Further studies revealed that although OEA and PSN-375963 are GPR119 agonists, they have divergent effects on insulin secretion, calcium signaling, and cAMP production.
 
SML0298 PSNCBAM-1 ≥98% (HPLC) PSNCBAM-1 is an allosteric, non-competitive antagonist of CB-1. The compound blocks the effects of WIN 55212-2 and CP55940, and reduces food intake and weight gain in rats.
 
P9872 Psora-4 ≥98% (HPLC) The lymphocyte potassium channel Kv1.3 is regarded as a new target for immunosuppression. Psora-4 is the most potent small-molecule Kv1.3 blocker known. It blocked Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 value of 3 nM, by preferentially binding to the C-type inactivated state of the channel. It exhibited 17- to 70-fold selectivity for Kv1.3 over closely related Kv1-family channels (Kv1.1, Kv1.2, Kv1.4, and Kv1.7) with the exception of Kv1.5 (EC50, 7.7 nM) and showed no effect on human ether-a-go-go-related channel, Kv3.1, the calcium-activated K+ channels (IKCa1, SK1-SK3, and BKCa), or the neuronal NaV1.2 channel. In a test of in vivo toxicity in rats, Psora-4 did not display any signs of acute toxicity after five daily subcutaneous injections at 33 mg/kg body weight. Psora-4 selectively suppressed the proliferation of human and rat myelin-specific effector memory T cells with EC50 values of 25 and 60 nM, respectively, without persistently suppressing peripheral blood naive and central memory T cells. Because autoantigen-specific effector memory T cells contribute to the pathogenesis of T cell-mediated autoimmune diseases such as multiple sclerosis, Psora-4 and other Kv1.3 blockers may be useful as immunomodulators for the therapy of autoimmune disord.
 
P8399 Psoralen ≥99% (HPLC) Phototoxic phytoalexin; when activated by UV light, psoralen induces interstrand cross-links in DNA.
 
SML0932   Psoralidin ≥98% (HPLC) Psoralidin is a furanocoumarin natural product used in Chinese medicine. Psoralidin, a PTP1B inhibitor, has been shown to have anticancer activity with a variety of mechanisms proposed. Psoralidin induces ROS generation in androgen-independent prostate cancer cells, leading to inhibition of cell proliferation. Psoralidin has been found to downregulate NOTCH1 signaling, causing growth arrest in both breast cancer stem cells and breast cancer cells.
 
P9256 Psychosine from bovine brain lyophilized powder, ≥98% (TLC) Glycolipid precursor of cerebrosides
 
SML1194 PT1 ≥98% (HPLC) PT1 is a direct activator of the α-subunit of AMP-activated protein kinase (AMPK), thought to act via antagonizing the autoinhibition in the α subunits.
 
P5874 PTACH ≥98% (HPLC), solid HDAC inhibitor; more potent than the majority of HDAC inhibitors except for SAHA (gold standard).
 
SML1143 PTC-209 ≥98% (HPLC) PTC-209 inhibits the expression of the oncogene BMI-1 (B lymphoma Mo-MLV insertion region 1 homolog), which encodes a polycomb group RING finger protein involved in cell cycle. PTC-209 lowers the self-renewal properties of colorectal cancer-initiating cells (CICs) The compound inhibits tumor growth, and reduces the levels of CICs present in colon cancer tumor xenografts in mice.
 
P1499 Pterostilbene ≥97% (HPLC), solid Antioxidant, antiproliferative, apoptosis inducer, antihyperglycemic, antidiabetic.
 
SML0410 PT-S58 ≥98% (HPLC) PT-S58 is a PPAR β/δ full antagonist, and a derivative of GSK0660. PT-S58 has a three-fold higher affinity for the receptor than GSK0660 and is a potent inhibitor of agonist-induced target gene expression. Unlike GSK0660, PT-S58 blocks the recruitment co-repressor molecules such as SMRT.
 
SML0868   Purmorphamine ≥98% (HPLC) Purmorphamine activates the Hedgehog (Hh) signaling pathway, directly binding to the Smoothened (Smo) receptor. In various studies, purmorphamine has been shown to induce osteoblast differentiation, generate cardiomyocytes from human embryonic stem cells, increase the neuronal differentiation of a human striatal neural stem cell line, and to differentiate human umbilical cord mesenchymal stem cells (hUCMSCs) into motoneurons.
 
P7255 Puromycin dihydrochloride from Streptomyces alboniger ≥98% (HPLC), powder Mode of Action: Puromycin inhibits protein synthesis by causing premature chain termination acting as an analog of the 3′-terminal end of the aminoacyl-tRNA.

Mode of Resistance: Puromycin acetyltransferase is an effective resistance gene.

Antimicrobial Spectrum: This product is active against gram-positive microorganisms, less active against acid-fast bacilli and more weakly active against gram-negative microorganisms. Puromycin can prevent growth of bacteria, protozoa, algae and mammalian cells and acts quickly, killing 99% of cells within 2 days.
 
P5234 Purvalanol B ≥97% (HPLC), solid Purvalanol B is a cyclin-dependent; 2,6,9-substituted kinase inhibitor.
 
P4484 Purvalanol A ≥98% (HPLC), powder Purvalanol A is a potent, cell-permeable cyclin-dependent protein kinase (cdk) inhibitor.
 
P7505 Putrescine dihydrochloride ≥98% (TLC) Binds to the polyamine modulatory site of the NMDA receptor and potentiates NMDA-induced currents; precursor of spermidine.
 
M5324 PX 12 ≥98% (HPLC), powder PX-12 inhibits the thioredoxin redox system and HIF-1a activity. PX 12 inhibits hypoxia-induced HIF-1a transcriptional activity (IC50 11 nM) and proliferation of HT29 and MCF-7 tumor cells (IC50 1.9 and 0.9 uM, respectively).
 
SML0676   PY1 ≥98% (HPLC) PY1 is a cell-permeable fluorescent sensor that is highly selective for detecting the presence of H2O2 in living cells.
 
P0046 Pyocyanin from Pseudomonas aeruginosa, ≥98% (HPLC) Pyocyanin, a blue-green pigment belonging to phenazine pigments, is a redox-active phenazine. Pyocyanin is an electron receptor, which stimulates redox cycling in bacteria, liver cells, and human epithlial cell lines. Pyocyanin enhances the oxidative metabolism, which in turn increases the formation of intracellular reactive oxygen species (ROS) via reduction of NADPH. Pyocyanin also increases the release of IL-8 by airway epithelial cells both in vitro and in vivo. This involves signal transduction pathways that include oxidants, protein tyrosine kinases, and MAP kinases. IL-8 secretion by these cells is in synergy with inflammatory cytokines. Pyocyanin has been shown to accelerate neutrophil apoptosis in vitro, resulting in resolution of acute inflammation, which is beneficial for bacteria survival.
 
R9532 Pyocyanin, Ready Made Solution from Pseudomonas aeruginosa 5 mg/mL in DMSO, sterile; 0.2 μm filtered Pyocyanin, a redox-active phenazine, is an electron receptor, which stimulates redox cycling in bacteria, liver cells, and human epithlial cell lines. It enhances oxidative metabolism, which increases the formation of intracellular reactive oxygen species (ROS) via reduction of NADPH. Pyocyanin also increases the release of the neutrophil chemoattractant IL-8 by airway epithelial cells both in vitro and in vivo. This involves signal transduction pathways that include oxidants, protein tyrosin kinases and MAP-kinases. IL-8 secretion by these cells is in synergy with inflammatory cytokines. Pyocyanin accelerates neutrophil apoptosis in vitro. Mice infected with a pyocyanin-deficient strain of P. aeruginosa showed elevated levels of neutrophils and neutrophil chemokines and cytokines, as well as compromised bacterial clearance from the lungs compared with mice infected with a wild type strain. This suggests that pyocyanin production by P. aeruginosa suppresses the acute inflammatory response by pathogen-driven acceleration of neutrophil apoptosis and by reducing local inflammation, and that this is advantageous for bacterial survival.
 
P8249   Pyoverdines−Gallium (III) complex from Pseudomonas fluorescens, >90% (HPLC) Gallium-pyoverdines act as growth inhibitors of both P. fluorescens and P. aeruginosa possibly due to gallium interference with bacterial iron metabolism.
Pyoverdines, also called pseuobactins and pyoverdins, are fluorescent siderophores that have high affinity for iron (1032 M-1), and are synthesized by fluorescent pseudomonads under iron-deficient growth conditions. Pyoverdines were shown to prevent iron toxicity produced by iron overload in hepatocyte cultures and effectively scavenges the hydroxyl and peroxyl radicals. Pyoverdines are effective in acquiring iron from transferrin and lactoferrin. Pyoverdines are also involved in the suppression of pythium-induced damping-off of tomato and promotion of growth in some higher plants.
 
N2915 PYR-41 ≥98% (HPLC), powder PYR-41 is a cell permeable inhibitor of Ubiquitin activating enzyme (E1) with little or no activity against E3, E2, or caspase enzymatic activity.
 
SML1243   Pyr10 ≥98% (HPLC) Pyr10 is a novel, selective inhibitor of the transient receptor potential channel TRPC3. Pyr10 blocks carbachol-induced calcium entry into TRPC3-transfected HEK293 cells (IC50 = 0.72 μM), with significantly lower activity against STIM1/Orai1 mediated release of calcium from endoplasmic reticulum (store operated calcium entry) in BRL-2H3 cells (IC50 = 13.08 μM).
 
P0032 Pyr3 ≥98% (HPLC) Pyr3 is a pyrazole compound that potently and selectively antagonizes TRPC3. Pyr3 inhibits TRPC3 by binding to the extracellular side of the receptor, resulting in suppression of B cell activation and cardiac hypertrophy.

Members of the canonical transient receptor potential (TRPC) channel family are ion channels which conduct Ca+2 and are activated by membrane receptor-mediated stimulation of phospholipase C (PLC) activity. However, TRPC3 and other family members are also activated by membrane-independent diacylglycerol (DAG). BTP1 and BTP2 are pyrazoles that block TRPC channels, but they are not specific for TRPC subtypes. This channel is implicated in various processes, including B cell receptor (BCR)-mediated Ca+2 oscillations, activation of nuclear factor of activated T cells (NFAT), and promotion of cardiac hypertrophy.
 
SML1241 Pyr6 ≥98% (HPLC) Pyr6 is a selective inhibitor of calcium release from the endoplasmic reticulum via STIM1/Orai1 mediated, store operated calcium entry (SOCE). Pyr6 blocks SOCE in thapsigargin treated, calcium depleted BRL-2H3 cells (IC50 = 0.49 μM), but has poor activity against carbachol-induced, TRPC3-mediated calcium entry in TRPC3-transfected HEK293 cells (IC50 = 18.46 μM).
 
B3438 Pyrabactin ≥98% (HPLC) Pyrabactin is a synthetic plant growth inhibitor that acts as a seed-selective abscisic acid (ABA) agonist. Pyrabactin acts through Pyrabactin Resistance 1 (PYR1), the founding member of a family of START proteins called PYR/PYLs, which are necessary for both pyrabactin and ABA signaling in vivo. Eventually, it is hoped to lead to a compound that could be sprayed on crops to protect them from drought.
 
SML1502 Pyrazofurin ≥98% (HPLC) Pyrazofurin is an orotidine-5’-monophosphate decarboxylase (ODCase, OMP decarboxylase) inhibitor that exhibit potent antiviral, anti-malarial and anti-trypanosomes activities.
 
SML0678 Pyridostatin trifluoroacetate salt ≥98% (HPLC) Pyridostatin stabilizes G-quadruplexes, targeting the proto-oncogene SRC and telomeric G-quadruplexes, inducing DNA damage and cell-cycle arrest.
 
P9797 Pyridostigmine bromide Acetylcholinesterase inhibitor.
human ... ACHE(43)
P178 Pyridoxal phosphate-6-azo(benzene-2,4-disulfonic acid) tetrasodium salt hydrate solid, ≥98% (HPLC) Non-selective P2 purinoceptor antagonist which blocks responses at both pre- and post-junctional sites.
human ... LPAR4(2846), LTB4R(1241), P2RX1(5023), P2RY1(5028), P2RY10(27334), P2RY11(5032), P2RY12(64805), P2RY13(53829), P2RY14(9934), P2RY2(5029), P2RY4(5030), P2RY5(10161), P2RY6(5031), P2RY8(286530)
P0865 N-(3-Pyridyl)indomethacinamide ≥98% Potent and selective reversible cyclooxygenase-2 (COX-2) inhibitor (IC50 = 0.1 μM, human recombinant); about 300-fold less potent as an inhibitor of human recombinant COX-1. Not as selective with natural ovine COX (IC50 = 75 μM for COX-1 and 50 μM for COX-2).
 
P5514 Pyrilamine maleate salt H1 histamine receptor antagonist.
human ... HRH1(3269)
SML0175   Pyrovalerone hydrochloride ≥98% (HPLC) Pyrovalerone hydrochloride is a rapidly-absorbed psychostimulant. It belongs to the class of synthetic cathinones often used as performance-enhancing agent by athletes before being banned.
Pyrovalerone is a norepinephrine-dopamine reuptake inhibitor (NDRI) that acts as a CNS stimulant.
 
SML0296 Pyroxamide ≥97% (HPLC) Pyroxamide is an inhibitor of HDAC1 (IC50 = 100 nM). Pyroxamide induces apoptosis and cell cycle arrest in leukemia, bladder and prostate cancer cell lines.
 
P7575 L-trans-Pyrrolidine-2,4-dicarboxylic acid ≥98% Selective inhibitor of glutamate uptake
rat ... Gria1(50592), Grik1(29559), Grin2a(24409), Slc1a2(29482), Slc1a3(29483)
P8861 Pyrrolnitrin from Pseudomonas cepacia ≥98% (HPLC), solid Pyrrolnitrin blocks the terminal electron transport between succinate or reduced NADH and coenzyme Q. In mitochondria preparations of S. cerevisiae, the antibiotic inhibited succinate oxidase, NADH oxidase, succinate cythochrome C reductase, and NADH-cytochrome C reductase. Pyrrolnitrin is involved in many cellular processes such as oxidative stress, electron transport, DNA and RNA synthesis.
 
V9763 V-Pyrro/NO Liver-selective nitric oxide donor that blocks TNF-α-induced apoptosis and toxicity
 
P0027 Pyrvinium pamoate salt hydrate ≥98% (HPLC) Pyrvinium pamoate is a potent androgen receptor inhibitor. Androgen receptors (ARs) are nuclear hormone receptors/transcription factors that reside in the cytoplasm and activated by testosterone and dihydrotestosterone. AR inhibitors have potential therapeutic benefit in prostate cancer; competitive inhibitors and chemical castration methods have been discovered, but both therapies have undesirable side effects and/or resistance potential. A screen for non-competitive inhibitors was performed, resulting in the discovery of pyrvinium as an AR inhibitor. In comparison to competitive inhibitors, this compound does not bind to the ligand-binding domain of AR or block DNA occupancy by AR, but it inhibits AR-dependent gene expression via a distinct signaling mechanism. It is more potent than classical competitive AR antagonists and exhibits synergy with other AR inhibitors.
 
SML1693 Pz-1 ≥98% (HPLC) Pz-1 is a cell-permeable, non-cytotoxic (up to 0.1 μM and 6 days; NIH/3T3 cells), and highly potent type II kinase inhibitor that potently inhibits RET and VEGFR2 tyrosine kinase activity (IC50 <1 nM; [ATP] = 190 μM) by targeting the kinases in their inactive DFG-out conformation, displaying significant affinity (Kd <50 nM) toward only TRKB, TRKC, GKA, FYN, SRC, TAK1, MUSK from a panel of 96 other kinases. Pz-1 inhibits cellular RET mutants (C634R, C634Y, V804L, V804M, M918T) and VEGFR2 phosphorylations, and selectively inhibits the growth of RET C634Y- than HRas G12V-transformed NIH/3T3 cultures (IC50 = 0.5 vs. 34.4 nM). Likewise, Pz-1 completely abrogated tumor formation from RET C634Y-transformed NIH/3T3 cells in mice in vivo (1 mg/kg/d, p.o.), while only up to 70% tumor suppression of HRas G12V-transformed cells was achieved with 10 mg/kg daily oral dosage.
 
SML0775   PZ-II-029 ≥98% (HPLC) PZ-II-029 is the first compound to be identified as a specific postitive modulator of GABAA channels composed of α6β3γ2 subunits.