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.
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.
human ... MTOR(2475), PIK3CA(5290), PIK3CB(5291), PIK3CD(5293), PIK3CG(5294), PIK3R1(5295), PIK3R2(5296), PIK3R3(8503), PIK3R5(23533)
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.
SML2564 PIAA ≥98% (HPLC) PIAA is an inhibitor of TANK binding kinase 1 (TBK1) and IKB kinase epsilon (IKKε) that has been shown to promote regeneration of pancreatic β-cells. PIAA improved function and replication of mammalian β-cells including primary human β-cells and induced β-cell proliferation in streptozotocin-induced diabetic mice resulting in increased pancreas insulin content and improved glycemic control. PIAA exhibited an IC50 value of 400 nM for TBK1 and 1.07 μM for IKKε with minimum toxicity
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 Piceatannol is an analog of resveratrol that possess potential anti-oxidant, anti-cancer and anti-inflammatory properties. Picetannol has been shown to interfere with the cytokine signaling pathway, notably in the inhibition of the spleen tyrosine kinase (Syk) and PI3K. It also inhibits the activation of NFκB in human cultured cells, after treatment with several inflammatory agents, through inhibition of IκBα kinase and p65 phosphorylation.
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.
Piclamilast is also known as N-(3,5-dichloropyrid-4-yl)-3-cyclopentyloxy-4-methoxybenzamide. Piclamilast regulates the cAMP (cyclic adenosine monophosphate) signaling pathway. It increases the retinoid-dependent transactivation and the degradation of retinoic acid receptor α (RARα).
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.
human ... IGF1R(3480)
P1675 Picrotoxin powder GABAA receptor antagonist; binds to the GABA receptor-linked Cl channel.
Picrotoxin is a competitive inhibitor of glycine receptors (GlyRs). It is a non-competitive antagonist, which binds to ligand bounded γ-aminobutyric acid (GABAA) receptor.
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.
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.
Pifithrin-μ(PFT-μ) has neuroprotective capabilities against cell death in a preclinical model of hypoxia-ischemia (HI)-induced neonatal encephalopathy. It inhibits nuclear factor-ΙB (NF-ΙB) pathway by inhibiting the interaction of molecular chaperone heat shock protein (HSP)-70 with its substrates.
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.
PIK93 is also known as N-(5-(4-Chloro-3-(((2-hydroxyethyl)amino)sulfonyl)phenyl)-4-methyl-2-thiazolyl)-acetamide. It inhibits poliovirus (PV) and coxsackievirus B3 (CVB3) viral RNA production and virus replication. PIK93 also prevents translation mediated by internal ribosome entry site (IRES).
P6503 Pilocarpine hydrochloride ≥99% (titration), powder Nonselective muscarinic acetylcholine receptor agonist; used to produce an experimental model of epilepsy.
Pilocarpine is alkaloid isolated from the shrub Pilocarpus species. It comprises imidazole ring and γ- lactone rings in its structure. It has cholinergic potential and it stimulates the parasympathetic system. Pilocarpine is also effective for treating glaucoma. It stimulates ciliary muscle contraction by binding to muscarinic M3 receptors. It is effective in treating corneal dryness in Sjogren′s syndrome. It is a secretagogue, which improves salivary secretions in Xerostomia or a dry mouth condition in Sjogren′s syndrome patients and in radiotherapy patients with head and neck carcinoma.
human ... CHRM1(1128), CHRM2(1129), CHRM3(1131), CHRM4(1132), CHRM5(1133)
P6628 Pilocarpine nitrate salt ≥98% (HPLC) Nonselective muscarinic acetylcholine receptor agonist; used to produce an experimental model of epilepsy.
Pilocarpine is a cholinergic muscarinic agonist, useful in inducing epilepsy in animal models. It is specially used to study the pathogenesis of epileptogenesis and pharmacoresistant epilepsy. Pilocarpine application is more popular among the rat and mice models.
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.
Pimelic diphenylamides has the ability to enhance the expression of the frataxin gene in lymphocytes from Friedreich ataxia patients.
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.
Pimonidazole possesses a nitro group at position 2 and an imidazole ring. Pimonidazole undergoes reduction and is activated in hypoxic cells.
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), DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816), HTR2A(3356), 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.
Pinacidil is a KATP channel agonist. It protects cardiomyocytes by preventing loss of mitochondrial membrane potential. It prevents the caspase 3 activation in hypoxia/reoxygenation injury.
human ... ABCC9(10060), KCNJ11(3767)
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.
β1-adrenoceptor antagonist; putative 5-HT1A serotonin receptor agonist; vasodilator. Pindolol is a non-cardioselective beta-adrenergic blocking agent. It possesses intrinsic sympathomimetic activity.
human ... ADRB1(153), ADRB2(154), 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)
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.
Pioglitazone hydrochloride is usually used to treat type-II diabetes. It has the ability to block hepatic gluconeogenesis.
human ... PPARG(5468)
P3246 Pipamperone dihydrochloride ~99% (HPLC), powder D2 dopamine receptor antagonist; 5-HT2 serotonin receptor antagonist; antipsychotic.
Pipamperone, a butyrophenone derivative is a pharmacological chaperone and is a membrane-permeable dopamine receptor D4 (DRD4) antagonist. The affinity of pipamperone is higher for DRD4 and 5-hydroxytryptamine 2A receptor (5-HT2A) in comparison with DRD2. It may be useful therapeutic in treating behavioral disorders and psychomotor agitation symptoms.
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.
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 Piracetam (2-oxo-1-pyrrolidinyl-acetamide) is a nootropic drug, which enhances memory and facilitates learning. Piracetam also acts as a vasodilator and improves blood flow. It has a potential to treat cognitive impairment in aging, brain injury, memory and balance problems. In addition, piracetam is also used to treat peripheral vascular disease.
human ... GRIA1(2890), GRIA2(2891), GRIA3(2892), GRIA4(2893)
rat ... Gria1(50592)
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.
Pirfenidone is used to treat idiopathic pulmonary fibrosis (IPF). It helps to decrease the weakening of lung function decline and ameliorate progression-free survival. Pirfenidone can repress the multiplication and contraction of collagen of human tenon′s fibroblasts.
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.
SML2473 Pitavastatin calcium ≥98% (HPLC) Pitavastatin calcium is a water-soluble inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonic acid, the rate-limiting step in cholesterol biosynthesis. Pitavastatin calcium is antilipemic and is used to reduce plasma cholesterol levels and prevent cardiovascular disease.
SML2764 Pitofenone hydrochloride ≥98% (HPLC) Pitofenone is a potent muscarinic receptor antagonist. Pitofenone in combination with diclofenac exhibits potent antispasmodic effect in cholinergic spasm.
SML2716 Pitolisant hydrochloride ≥98% (HPLC) Potent and selective competitive antagonist/inverse agonist of histamine H3 receptor
SML1169   Pitstop 2 ≥98% (HPLC) Pitstop 2 also has an ability to breakdown the nuclear pore complex (NPC) permeability barrier and decrease importin β binding along with alteration of the NPC ultrastructure. Pitstop 2 is also involved in the inhibition of platelet activation, platelet aggregation and secretion.
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.
Pitstop 2 is a selective inhibitor of clathrin-mediated endocytosis.
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.
SML2577 Pixantrone dimaleate ≥98% (HPLC) Pixantrone (BBR 2778) is an aza-anthracenedione with enhanced antitumor activity due to its DNA-intercalating and topoisomerase II-poisoning activity. Pixantrone shows no signs of acute or delayed cardiotoxicity seen with anthracyclines mitoxantrone and doxorubicin (DOX), while exhibiting comparable in vivo efficacy against solid tumors in mice. Tests conducted on human myocardial strips ex vivo shows that not only pixantrone does not form superoxide anion and hydrogen peroxide (O2•− and H2O2) seen with DOX due to redox activation, pixantrone and its metabolites, especially N-dealkylated, show competitive inhibition against DOX reduction. While mitoxantrone does not form O2•− and H2O2 on its own, it synergizes with DOX to form more O2•− and H2O2, whose formation and subsequent production of the long-lived metabolite doxorubicinol contribute to DOX cardiotoxicity.
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.
SML1891 PK11007 ≥98% (HPLC) PK11007 is a thiol-reactive anticancer agent that stabilizes wild type and mutant p53 through selective alkylation of two surface cysteines without interfering with its DNA binding. Additionally independently from p53, PK11007 impairs reactive oxygen species (ROS) detoxification in a number of mutant p53 cancer cells. PK11007 exhibits anticancer activity in number of cancer cell lines while shoving low cytotoxicity toward normal cells.
C0424 PK 11195 PK 11195 is a peripheral benzodiazepine antagonist. It is also an antagonist for human constitutive androstane receptor (hCAR) and human pregnane X receptor (PXR). In human primary hepatocytes, PK 11195 upon demethylation elicits agonist functionality towards the receptor hCAR. PK 11195 also antagonise B-cell lymphoma 2 (Bcl-2) and may serve as a potential compound for mitochondrial targeting therapies and in the treatment of cholangiocarcinoma.
human ... BZRAP1(9256), TSPO(706)
rat ... Gabra2(29706), Tspo(24230)
SML2448 PK4C9 ≥98% (HPLC) PK4C9 is a splice modulator of survival of motor neuron gene SMN2 that increases production of full-length SMN protein. Spinal muscular atrophy (SMA) is a motor neuron disease caused by deficiency in SMN protein resulting from loss of expression of the SMN1 gene. The related SMN2 gene can compensate, but polymorphism in SMN2 often results in altered splicing and exclusion of exon 7, which is required for a full-length SMN transcript. PK4C9 binds to pentaloop conformations of the stem-loop RNA structure TSL2, a cis-regulatory element for E7 inclusion, and promotes a shift to triloop conformations that display enhanced E7 splicing. In SMA cells, PK4C9 increased E7 inclusion by 40% accompanied by a 1.5-fold increase in SMN protein, a level shown to reverse SMA phenotypes in mice models.
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.
human ... EGFR(1956)
SML2445 PKS21004 ≥98% (HPLC) PKS21004 is highly selective, potent and reversible inhibitor of the Plasmodium falciparum proteasome (Pf20S) β5 subunit. It is not active against mammalian c-20S and i-20S proteasome subunits. PKS21004 is effective against erythrocytic, sexual, and liver-stage parasites. Also it is active against parasites resistant to current antimalarials, and strains from patients in Africa.
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.
SML1970   PKUMDL-WQ-2101 ≥98% (HPLC) PKUMDL-WQ-2101 is a potent and selective non-NAD+-competing allosteric inhibitor of phosphoglycerate dehydrogenase (PHGDH) that selectively inhibits serine synthesis in cancer cells. PKUMDL-WQ-2101 binds to allosteric site I, which is located close to active site. PKUMDL-WQ-2101 inhibits tumor growth of MDA-MB-468 xenografts in mice.
SML1965 PKUMDL-WQ-2201 ≥98% (HPLC) PKUMDL-WQ-2201 is a potent and selective non-NAD+-competing allosteric inhibitor of phosphoglycerate dehydrogenase (PHGDH) that selectively inhibits serine synthesis in cancer cells. PKUMDL-WQ-2201 binds to allosteric site II, which is located in the substrate-binding domain. PKUMDL-WQ-2201 inhibits tumor growth of MDA-MB-468 xenografts in mice.
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 effective drug against enteroviral infections. It can be used to treat chronic meningoencephalitis caused by echo virus 6.This can block viral replication by blocking the viral uncoating process and viral attachment to host cell receptors.
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 a diterpene that acts against gram positive bacteria and mycoplasm. It is present in Pleurotus mutilus and Pleurotus passecherianus. Pleuromutilin exhibits its antibacterial action by interfering with the prokaryotic 70S ribosomal subunit and inactivates initiation complex. Pleuromutilin is useful in treating mycoplasma infections in animals.
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.
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-(phosphonomethyl)pentanedioic acid (2-PMPA) blocks intravenous cocaine self-administration maintained by low unit doses of cocaine. In addition, it also inhibits cocaine-induced reinstatement of drug-seeking behavior. 2-PMPA reduces blood oxygen-level dependent (BOLD) signals in brain of anesthetized mice.
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.
2-PMPA is a potent and selective inhibitor of Glutamate carboxypeptidase II (GCPII).
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.
PNU-282987 is an agonist of nicotinic α-7 acetylcholine receptor (nAChRα7). It helps to decrease acute lung injury (ALI), stimulated by lipopolysaccharide (LPS). PNU-282987 can increase GABAergic synaptic activity in brain slices and helps to bring back auditory gating deficits in anesthetized rats.
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.
SML2854 Polmacoxib ≥98% (HPLC) Polmacoxib is a nonsteroidal anti-inflammatory drug (NSAID) that acts as an inhibitor of cyclooxygenase 2 (COX-2) and the carbonic anhydrases CAI and CAII. It has also been found to inhibit colorectal adenoma and tumor growth in mouse models.
SML2186 Poloppin ≥98% (HPLC) Poloppin is a cell penetrant and potent inhibitor of mitotic Polo-like kinases (PLKs) that binds to the Polo-box domain (PBD) and prevents PLKs interaction with pSer/pThr phosphopeptide substrates. Poloppin induces mitotic arrest and apoptosis in cancer cells expressing mutant KRAS in 2D and organoid cultures. It also sensitizes mutant KRAS-expressing cancer cells to Crizotinib.
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.
Polygodial is a sesquiterpene dialdehyde. It is obtained from the plants Polygonum hydropiper, Warburgia ugandensis, Pseudowintera colorata and Warburgia stuhlmannii. It exhibits antifeedant activity and antimicrobial activity against insects and microbes, respectively. It is responsible for the “hot taste” in peppery spices of traditional Japanese cuisine.
P0018 Pomalidomide ≥98% (HPLC) Pomalidomide is a second generation immunomodulator, TNF-α inhibitor, and thalidomide analog.
human ... CRBN(51185), CUL4A(8451), DDB1(1642), RBX1(9978)
P6237   α-Pompilidotoxin >98% Voltage-gated sodium channel activator
P3490 Ponasterone A ≥65% Ponasterone A is an analogue of ecdysone.
Ponasterone A is an insect hormone, involved in regulating metamorphosis.
SML2287 Posaconazole ≥98% (HPLC) inhibitor of the lanosterol 14α-demethylase (CYP51); highly potent broadspectrum antifungal drug
P0040 PP1 ≥98% (HPLC) PP1 is a potent and selective Src family protein tyrosine kinase inhibitor.
P0042 PP2 ≥98% (HPLC)    
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 (6,7-dimethoxy-4-[3-(quinoxalin-2-yloxy)pyrrolidin-1-yl]quinazoline), is capable of suppressing tumor cell growth. It can also reverse the RO-4-1284-induced sedation and catalepsy.
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)
SML2494 Pralatrexate ≥98% (HPLC) Pralatrexate is an antifolate that selectively enters cancer cells expressing reduced folate carrier type 1 (RFC-1). Pralatrexate potently inhibits DHFR (dihydrofolate reductase).
SML2056 Pralmorelin trifluoroacetate salt ≥97% (HPLC) Pralmorelin, also known as Growth hormone-releasing peptide 2 or GHRP-2, is an orally-active, synthetic peptide analogue of met-enkephalin that acts as a ghrelin/growth hormone secretagogue receptor (GHSR) agonist to selectively stimulate the ghrelin receptor and cause growth hormone release. Pralmorelin (GHRP-2) has been used clinically for the assessment of growth hormone deficiency (GHD), It has also been shown to have anti-inflammatory activity.
A1237 Pramipexole dihydrochloride >98% (HPLC), powder Pramipexole elicits neuroprotective role and may help in treating depression. It also has a potential to modulate limb movement and may be effective in treating restless legs syndrome.
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.
human ... DRD2(1813), DRD3(1814), DRD4(1815)
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.
Pramiracetam plays an important role in spatial learning and memory in rats. It is considered as a memory enhancing agent and is stronger than piracetam.
SML2523   Pramlintide acetate salt ≥95% (HPLC) Pramlintide (AC0137, AC137, triPro-amylin) is a synthetic antidiabetic peptide that corresponds to human amylin (aa34-70) with proline substitutions at N25, S28 and S29 to limit the self-aggregation seen with native amylin. Pramlintide augments endogenous amylin-mediated glycemic control (blood glucose regulation) in vivo by delaying gastric emptying and inhibiting the secretion of glucagon, a catabolic hormone that opposes the effects of insulin and amylin.
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.
Pranoprofen is used in eyes to treat chronic allergic conjunctivitis. It is also used as an anti-inflammatory and analgesic drug after strabismus surgery.
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.
Prasugrel is a thienopyridine prodrug and is considered to be more potent than clopidogrel. It shows a faster generation and also reduces thrombotic events. Prasugrel is less dependent on the CYP (cytochrome P450) enzymes for its conversion to active metabolite.
human ... P2RY12(64805)
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.
human ... HMGCR(3156)
P3654 Prazepam Anxiolytic
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
P7791 Prazosin hydrochloride ≥99.0% (HPLC) Peripheral α1-adrenoceptor antagonist; vasodilator. Prazosin can be used to treat chronic posttraumatic stress disorder (PTSD). It plays a role in reducing blood pressure by relaxing blood vessels, hence used in the treatment of high blood pressure.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
P2607 PRE-084 solid PRE-084 is a potent and highly selective σ1 opioid receptor agonist. It offers neuroprotection upon embolic stroke.
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%   human ... NR3C1(2908)
P4153 Prednisolone 21-hemisuccinate sodium salt ≥90%, powder    
P6254 Prednisone ≥98% Prednisone is a synthetic glucocorticoid with anti-inflammatory and immunosuppressive activity. It is useful in treating many disease states and has a half-life of 3.4 to 3.8 hours in plasma. Prednisone is metabolized to prednisolone, which is physiologically active.
human ... NR3C1(2908)
P3635 5β-Pregnane-3α,20α-diol glucuronide    
P8629 5β-Pregnane-3α,17α,20α-triol    
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 5α-Pregnan-3α-ol-20-one is a positive allosteric modulator of γ-aminobutyric acid (GABA) A receptor (GABAA). It is also called pregnan and during pregnancy it modulates the atrial volume receptors transducer properties. During estrus cycle, 5α-Pregnan-3α-ol-20-one or allopregnanolone levels changes in hypothalamus. It is present in high levels post adrenalectomy and gonadectomy.
human ... GABRA1(2554), GABRA2(2555), GABRA3(2556), GABRA4(2557), GABRA5(2558), GABRA6(2559), GABRB1(2560), GABRB2(2561), GABRB3(2562), GABRD(2563), GABRE(2564), GABRG1(2565), GABRG2(2566), GABRG3(2567), GABRP(2568), GABRQ(55879)
mouse ... Gabrg2(14406)
rat ... Gabra1(29705), Gabra2(29706), Gabrg2(29709)
P8129 5β-Pregnan-3α-ol-20-one 5β-Pregnan-3α-ol-20-one or pregnanolone is a neurosteroid that acts as a positive allosteric modulator (PAMs) of γ-aminobutyric acid A receptors (GABAARs). It mediates anti-convulsive, anxiolytic and sedative effects. Pregnanolone inhibits γ-aminobutyric acid C receptor (GABAC) receptor-based response and favors GABAA receptor-mediated currents.
rat ... Gabra2(29706)
P8004 5α-Pregnan-3β-ol-20-one 3β-acetate ≥98%    
P0543 5-Pregnen-3β-ol-20-one-16α-carbonitrile ≥97% Pregnenolone-16a-carbonitrile (PCN) is a glucocorticoid receptor antagonist and a PXR (pregnane X receptor) activator.
P162 Pregnenolone sulfate sodium salt Pregnenolone sulfate is a neurosteroid and a neuromodulator. It is involved in the stimulation of N-methyl-D-aspartate receptor (NMDA), γ-Aminobutyric acid type A (GABAA ) and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA-kainate). It activates transient receptor potential melastatin (TRPM3) which is a calcium-permeable ion channel. It improves schizophrenia and behavioral anomalies by modulating NMDA mediated Ser/Thr kinase - glycogen synthase kinase 3 β (AKT/GSK3β) signaling pathway.
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.
PreQ1 is a nucleobase derived from guanine and a precursor of the modified base queuosine that is present in four tRNAs. Prequeuosine (preQ1) riboswitches are RNA regulatory elements present in the 5′ UTR of genes that participates in the biosynthesis and transport of preQ1.
P9547 Prilocaine hydrochloride ≥98% (TLC) Used for local nerve block and for spinal anesthesia; pharmacological properties are similar to those of lidocaine.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
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 Probenecid is a uricosuric agent, which increases uric acid removal in the urine and reduces urate reuptake. It also reduces the renal tubular excretion of many other drugs and increases their plasma concentration. The inhibitory action of probenecid is mediated by organic anion transporters. It is found useful for the treatment of gout. Probenecid is responsible for the rise in the levels of neurochemicals in the brain by preventing its movement from choroid plexus and parenchyma cells into plasma.
human ... SLC22A11(55867), SLC22A6(9356), SLC22A8(9376)
SML2088 Procainamide hydrochloride ≥98% (HPLC) Procainamide hydrochloride is a sodium channel blocker and Class IA anti-arrhythmic. It has also been shown to Inhibit DNA methyltransferase and modulate epigenetic regulation of gene expression.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
P9879 Procaine hydrochloride ≥97% Procaine is a Na+ channel blocker, commonly used as an anesthetic agent and is considered safer than cocaine. It is also useful as a painkiller to treat pain, associated with joints and tendons.
human ... SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
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.
Procarbazine is metabolized to azoprocarbazine either by cytochrome P450 enzyme and monoamine oxidase in an NADPH (nicotinamide adenine diphosphate) dependent or independent manner. It is considered neurotoxic. Procarbazine is used in combination with therapy for treating Hodgkin′s disease.
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
Prochlorperazine is an anti-nausea and neuroleptic agent. It is known to cause neuropsychiatric side effects. Prochlorperazine inhibits the action of dopamine in the central nervous system. It acts as an antiemetic drug and prevents vomiting and stimulates sleep. Prochlorperazine is useful as a tranquilizer in the treatment of schizophrenia and nonpsychotic anxiety.
human ... DRD2(1813)
P3794 Procyclidine hydrochloride Procyclidine is a synthetic anti-cholinergic agent and atropine-like antispasmodic. It exhibits therapeutic effects against Parkinson′s disease and schizophrenia. Procyclidine acts as a muscarinic receptor antagonist. It also affects N-methyl-D-aspartate (NMDA) glutamine and nicotinic acetylcholine receptors to a lower extent.
human ... CHRM1(1128)
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)
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), DRD3(1814), DRD4(1815), HTR2A(3356)
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), SCN10A(6336), SCN11A(11280), SCN1A(6323), SCN2A(6326), SCN3A(6328), SCN4A(6329), SCN5A(6331), SCN7A(6332), SCN8A(6334), SCN9A(6335)
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 (S)-(−)-Propranolol hydrochloride is biologically active enantiomer. It acts as β1 receptor antagonist in thalamocortical neurons. (S)-(−)-Propranolol hydrochloride elicits its inhibitory function on the β1 adrenoceptor in trigeminovascular pain pathway and serves as a preventive medicine in migraine.
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 Propranolol hydrochloride is a β-adrenoceptor antagonist. Its action at β2 receptor results in bronchoconstriction. Due to its lipophilic nature, propranolol can penetrate to the central nervous system and has a negative effect. It serves as a 5-HT1/5-HT2 serotonin receptor antagonist. Propranolol hydrochloride is useful as an antihypertensive drug, cardiac depressant and also in the treatment of angina pectoris. It decreases the effect of stress and exercise on heart by reducing the rate of contraction and conduction of impulse. It is known to competitively block the action of catecholamines.
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.
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.
SML2800 Proscillaridin A ≥90% (HPLC) New Proscillaridin A, a cardiac glycoside, is an antiarrhythmic drug that enhances DNMT inhibitors and HDAC inhibitors activity. Combination of decitabine with proscillaridin A produced profound gene expression reprogramming associated with down-regulation of 153 epigenetic regulators including SYMD3 and KDM8. Proscillaridin A was recently identified as a potent anti-HBV agent (IC50 = 7.2?nM).
P7265 Prostaglandin A1 synthetic Cyclopentenone prostaglandin that stimulates the expression of stress genes.
P5515 Prostaglandin E1 ≥98% (HPLC), synthetic Prostaglandin E1 (PGE1) is a hormone synthesized from dihomo-γ-linolenic acid (DGLA) by the action of enzyme prostaglandin synthase. It is a vasodilator and activates adenylate cyclase. It is majorly present in human semen and is a potent platelet aggregation inhibitor. PGE1 infusions is effective in treating limb ischemia and peripheral vascular disease. It is unstable and is hydrolyzed to PGA1 in the lungs. Nanoparticle encapsulation of PGE1 is essential for its delivery at the vascular injury site. It elicits vasodilator effects on the retinal artery and vein in central retinal artery occlusion (CRAO). PGE1 and its synthetic analog misoprostol interact with E-prostanoid receptor 4 (EP4) and elicits protection in chronic myelogenous leukemia (CML).
human ... PTGER1(5731), PTGER2(5732), 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.
SML2810 Prostetin Trifluoroacetic acid salt ≥98% (HPLC) Prostetin is an orally available, blood-brain barrier-penetrant, potent and metabolically stable inhibitor of the mitogen-activated protein kinase kinase kinase kinase (MAP4K, or HGK) that exhibits neuroprotective and anti-inflammatory properties. Prostetin is more potent than URMC-099 in motor neuron survival assay. Prostetin rescues CPA-induced neurodegeneration in motor neurons.
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.
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.
Protopine possesses anti-parasitic, antimicrobial and anti-inflammatory property. It mediates mitotic arrest by favoring tubulin polymerization. Protopine elicits anti-invasive effects in breast cancer tumor progression.. It also provides protection against oxidative stress-induced cell death.
P8813 Protriptyline hydrochloride ≥99% (TLC), powder Norepinephrine uptake blocker.
human ... SLC6A2(6530), SLC6A4(6532)
SML2505 PRT-060318 ≥95% (HPLC) PRT-060318 (PRT318; P142-76) is a highly potent and selective Syk inhibitor (IC50 = 4 nM; much reduced potency against 138 other kinases) that blocks BCR-dependent signaling in chronic lymphocytic leukemia (CCL) cultures (2-3 μM) and specifically inhibits platelets activation via ITAM receptor complex GPVI/FcRγ, but not P2Y1/12 or PAR1, stimulation (IC50 = 2.5 μM; aggregation by 8 ng/mL convulxin). PRT318 demonstrates in vivo efficacy in animal models of thrombosis (30 mg/kg mouse bis p.o.; 5.1675 mg/3.1 mL/kg/rabbit/15 min then 7.33 mg/4.4 mL/kg/h i.v.; 8.90 mg/mL/kg pig/h i.v.) and B-cell acute lymphoblastic leukemia (30 mg /kg bis p.o.; human B-ALL xenograft mice).
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) In healthy male individuals, prucalopride decreases the display of esophageal acid and promotes gastric emptying. It is effective, safe and shows good tolerance for the treatment of men with chronic constipation.
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.
SML2418 PS10 ≥98% (HPLC) 2-[(2,4-dihydroxyphenyl) sulfonyl]isoindoline-4,6-diol (PS10) can be considered as a therapeutic method to preserve glucose and lipid homeostasis in obesity and type 2 diabetes (T2D). It can induce pyruvate dehydrogenase complex (PDC) activity in liver and kidney. It is also considered as an effective PDK inhibitor to treat diabetic cardiomyopathy. In the normal myocardium, PS10 helps to enhance fractional carbohydrate oxidation.
PS10 is a potent and selective PDK (Pyruvate dehydrogenase kinase) inhibitor that improves glucose tolerance and lessens hepatic steatosis in diet-induced obese mice. PS10 binds to the ATP-binding pocket of PDKs.
P6624 PS-1145 dihydrochloride ≥98% (HPLC), solid PS-1145 is an IKB kinase (IKK) inhibitor.
PS-1145, a β-carboline derivative, blocks the phosphorylation and degradation of the inhibitor of nuclear factor kappa-β (NF-κB;). It also inhibits the subsequent activation of nuclear factor kappa-β (NF-κB) and thereby prevents the release of tumor necrosis factor-α (TNF-α) in lipopolysaccharide treated mice. PS-1145 hinders pro-inflammatory cytokine production and cell proliferation. It plays a potential therapeutic role in carcinogenesis in multiple myeloma. PS-1145 exhibits anti-tumor activity on nasopharyngeal carcinoma (NPC) cell lines.
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.
SML1991 PS432 ≥98% (HPLC) PS432 is an allosteric inhibitor of Protein Kinase C (PKC) that targets regulatory site (PIF-pocket) present in the kinase domain. PS432 potently inhibits non-small cell lung cancer cells proliferation and tumor growth without side effects in a mouse xenograft model.
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)
SML1983 PSB-603 ≥98% (HPLC) PSB-603 is an adenosine receptor A2b antagonist (IC50 = 1.13 nM against 10 μM A2bR agonist NECA-induced calcium response in Jurkat T cells in the presence of 200 nM A2aR antagonist MSX-2) that targets A2bR with high affinity (KD = 0.403 nM/human, 0.457 nM/rat, 4.09 nM/mouse A2bR; Ki against 0.3 nM [3H]PSB-603 = 0.553 nM/human, 0.355 nM/rat, 0.265 nM/mouse A2bR) and selectivity, exhibiting little affinity toward A1, A2a, or A3 adenosine receptors by competition binding assay (Ki >10 μM against 0.4 nM [3H]DPCPX for human/rat A1R, 1 nM [3H]MSX-2 for human/mouse/rat A2aR, 10 nM [3H]NECA for human/mouse/rat A3R) with the exception of mouse A1R (Ki = 42.2 nM against 0.4 nM [3H]DPCPX).
PSB-603 is known to modify cellular metabolism and enhance cellular sensitivity for chemotherapy. Thus, PSB-603 is recognized to possess anticancer action, which has been studied in colorectal cancer.
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 Pseudomonas exotoxin A functions as an anticancer agent.
It catalyses the transfer of ADP-ribose moiety of NAD+ to the histidine imidazole ring of diphthamide.
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) Psoralen belongs to the linear type furanocoumarins. It intercalates and induces interstrand cross-links in DNA. On UV exposure psoralen is excited leading to irreversible intercalation with DNA by covalent bond formation. This property of psoralen ultraviolet A light (PUVA) is exploited in treating skin diseases and cutaneous T-cell lymphoma. However, usage psoralen also leads to hepatotoxicity and cytotoxicity by the generation of psoralen photoproducts (POPs). It may be useful in treating osteoporosis
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) Psychosine is a neurotoxic lysosphingolipid and a glycolipid precursor for the synthesis of cerebrosides. It is synthesized from galactosylceramide, phrenosin. Elevated psychosine levels are implicated in Krabbe disease. It mediates demyelination and consequently oligodendrocytes degeneration. Psychosine is also correlated to neurological disease, Globoid cell leukodystrophy (GLD), where in galactosylceramidase (GALC) enzyme deficiency leads to its accumulation.
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.
Pterostilbene exhibits antineoplastic properties in some of the malignancies, hence it is considered as an active anticancer agent. It has the ability to stimulate apoptosis and block the viability of cell in estrogen-receptor positive and negative breast cancer cell lines.
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.
SML2556 Pt-ttpy >97% (NMR) Pt-ttpy, a metallo-organic complex, is a G-quadruplex ligand that potently induces significant telomere-associated DNA damage in cancer cells. It inhibits telomerase and/or telomere functions. Pt-ttpy induces number of chromatin defects in mitosis including chromatin bridges, ultrafine bridges (UFBs), and double-stranded breaks (DSBs).
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 Green Alternative 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.
Puromycin dihydrochloride is a part of the amino-nucleoside family of antibiotics and is derived from Streptomyces alboniger. It is a broad spectrum antibiotic with antitumor activity, as an inhibitor of protein synthesis and has been used to study transcription regulatory mechanisms that control the sequential and coordinate expression of genes during cell differentiation. The recommended working concentration in eukaryotic cell culture is 1-10 μg/mL.
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.
Purvalanol A is found to inhibit ABCG2 (ATP-binding cassette G2) transporter in vitro. It is also known to attenuate cellular Src kinase action and induce cell cycle arrest at the G2 to M phase transition.
P7505 Putrescine dihydrochloride ≥98% (TLC) Binds to the polyamine modulatory site of the NMDA receptor and potentiates NMDA-induced currents; precursor of spermidine.
SML2796 PVHD121 ≥98% (HPLC) PVHD121 is potent antimitotic agent that binds to the colchicine site of tubulin. PVHD121 selectively inhibits microtubule formation at centrosomes during mitosis. It delays entry into mitosis causing long lasting mitotic arrest by activation of spindle checkpoint.
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) DPP-Py1 is a ratiometric sensor. It is accurate and reactive with a relatively lower detection limit (1.8 × 10-7 M) than DPP-Py2. It is also stable in various pH buffers than DPP-Py2.
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 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.
N2915 PYR-41 ≥98% (HPLC), powder PYR-41 inhibits E1 ubiquitin ligases like mouse double minute 2 homolog (MDM2), Itchy (ITCH) and HOIL-1L interacting protein (HOIP). It has anticancer potential.
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.
Pyrazofurin serves as an effective drug against HIV (human immuno virus), vaccinia virus, West Nile viral infection.
SML2690 Pyridostatin hydrochloride ≥98% (HPLC) Pyridostatin is a highly selective G-quadruplex (G4) interacting molecule. It retards the growth of human cancer cells by inducing replication/transcription dependent on DNA damage. Pyridostatin stabilizes G-quadruplexes, targeting the proto-oncogene SRC and telomeric G4, inducing DNA damage and cell-cycle arrest.
P9797 Pyridostigmine bromide Acetylcholinesterase inhibitor.
Pyridostigmine bromide inhibits acetylcholine esterase and is membrane impermeable. It is used as a preventive medicine in chemical warfare. Pyridostigmine bromide is a carbamate compound comprising quaternary amine structure. It displays low absorption at the gastrointestinal tract. Sustained release of pyridostigmine is recommended for improving its bioavailability in treating myasthenia gravis.
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 Pyrilamine maleate is a H1 histamine receptor antagonist. Pyrilamine maleate induces sleep in vertebrates. In Cassiopea, it induces concentration dependent dormancy.
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)