Bioactive Small Molecules

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

Degeneration of the hippocampus is an early manifestation of Alzheimer′s disease. P7C3 promotes neurogenesis in the subgranular zone of the hippocampal dentate gyrus, the site of normal neurogenesis in adult mammals, making it an important lead compound in development of new Alzheimer′s treatments.
SML2185 PA-6 ≥98% (HPLC) PA-6 (Pentamidine-Analogue 6) is a selective and potent IK1 (inward rectifier potassium current) inhibitor that terminates atrial fibrillation and does not cause ventricular arrhythmias in goat and dog models. PA-6 interacts with the cytoplasmic pore region of the KIR2.1 (KCNJ2) ion channel.
SML1290   PA-824 ≥98% (HPLC) PA-824 is a pro-drug that has an effect on both replicating and non-replicating Mycobacterium tuberculosis. It is activated by deazaflavin (cofactor F420)-dependent nitroreducase.
PA-824 is an anti-tuberculosis drug that exhibits multiple mechanism of action, including both cell wall inhibition and respiratory poisoning.
PA-824 is an anti-tuberculosis drug.
P0115 PAC-1 ≥98% (HPLC) PAC-1 is a caspase 3 activator. Caspase activation is a key strategy in cancer therapy. Caspase 3 is a key executioner caspase and direct effector of apoptosis. Hallmark of many cancers is the circumvention of signal in the activation of executioner caspases and loss of apoptotic response. EC50 for caspase 3 activation = 0.33 μM and caspase 7= 4.5 μM. The IC50 for apoptosis induction = 0.92 μM. Elevated caspase 3 level in cancerous cell lines and tissues allows PAC-1 to selectively induce apoptosis in tissues.
T7402 Paclitaxel from Taxus brevifolia, ≥95% (HPLC), powder Paclitaxel is a potent anti-neoplastic and anti-mitotic taxane drug, which binds to the N-terminus of β-tubulin and and stabilizes microtubules arresting the cell cycle at the G2/M phase. The microtubule damage induces apoptosis through a JNK-dependent pathway followed by a JNK-independent pathway, perhaps related to the activation of protein kinase A (PKA) or of Raf-1 kinase, resulting in phosphorylation of Bcl-2. A major metabolite via CYP2CB is 6α-hydroxypaclitaxel (6α-OHP).
human ... BCL2(596), TUBA1A(7846), TUBA1B(10376), TUBA1C(84790), TUBA3C(7278), TUBA3E(112714), TUBA4A(7277), TUBB(203068), TUBB1(81027), TUBB2A(7280), TUBB2B(347733), TUBB3(10381), TUBB4A(10382), TUBB4B(10383), TUBB6(84617), TUBB8(347688)
T7191 Paclitaxel from semisynthetic, ≥97% Paclitaxel is a potent anti-neoplastic and anti-mitotic taxane drug, which binds to the N-terminus of β-tubulin and and stabilizes microtubules arresting the cell cycle at the G2/M phase. The microtubule damage induces apoptosis through a JNK-dependent pathway followed by a JNK-independent pathway, perhaps related to the activation of protein kinase A (PKA) or of Raf-1 kinase, resulting in phosphorylation of Bcl-2. A major metabolite via CYP2CB is 6α-hydroxypaclitaxel (6α-OHP).
Paclitaxel is highly lipophilic. It serves as a substrate for p-glycoprotein, a multi-drug resistance protein. Paclitaxel is thus, less localized to the brain. Apart from its cytocidal action, paclitaxel is known to stimulate tumor invasion process.
human ... BCL2(596), TUBA1A(7846), TUBA1B(10376), TUBA1C(84790), TUBA3C(7278), TUBA3E(112714), TUBA4A(7277), TUBB(203068), TUBB1(81027), TUBB2A(7280), TUBB2B(347733), TUBB3(10381), TUBB4A(10382), TUBB4B(10383), TUBB6(84617), TUBB8(347688)
T1912 Paclitaxel from Taxus yannanensis, powder Paclitaxel is a potent anti-neoplastic and anti-mitotic taxane drug, which binds to the N-terminus of β-tubulin and and stabilizes microtubules arresting the cell cycle at the G2/M phase. The microtubule damage induces apoptosis through a JNK-dependent pathway followed by a JNK-independent pathway, perhaps related to the activation of protein kinase A (PKA) or of Raf-1 kinase, resulting in phosphorylation of Bcl-2. A major metabolite via CYP2CB is 6α-hydroxypaclitaxel (6α-OHP).
human ... BCL2(596), TUBA1A(7846), TUBA1B(10376), TUBA1C(84790), TUBA3C(7278), TUBA3E(112714), TUBA4A(7277), TUBB(203068), TUBB1(81027), TUBB2A(7280), TUBB2B(347733), TUBB3(10381), TUBB4A(10382), TUBB4B(10383), TUBB6(84617), TUBB8(347688)
SML0838 PACMA 31 ≥98% (HPLC) Both in vivo and in vitro studies reveal that PACMA 31 possesses anti-tumor function, especially observed in ovarian cancer.
PACMA 31 is an orally bioavailable, selective inhibitor (IC50 = 10 μM) of protein disulfide isomerase (PDI), an endoplasmic reticulum protein that regulates oxidative protein folding by catalyzing the breakage and reformation of disulfide bonds. PDI is upregulated in ovarian, and several other cancers. PACMA 31 dose dependently inhibits proliferation of OVCAR-8 in culture and in a tumor xenograft model.
PZ0383 Palbociclib ≥98% (HPLC) PF-00080665 (Palbociclib; PD 0332991) is an orally active and highly specific inhibitor against cyclin-dependent kinase 4 & 6 (IC50 = 9, 11, 15 nM, respectively, using CDK4/cycD3, CDK4/cycD1, CDK6/cycD2; IC50 >10 μM against 36 other kinases) that potently suppresses Cdk4/6-dependent cellular Rb phosphorylation (IC50 = 66 nM/pSer780 & 63 nM/pSer795; MDA-MB-435). PF-00080665 exhibits selective antiproliferation activity against Rb-positive human breast/colon/lung/leukemia cancer cultures (IC50 = 40-400 nM; IC50 >3 μM/Rb-negative MDA-MB-468 & H2009) and displays in vivo efficacy against various advanced stage human tumor xenografts in mice (12.5-150 mg/kg/day p.o.).
P0064 PalGly ≥98% (HPLC), solid PalGly is an endogenous signaling lipid that modulates calcium influx and nitric oxide production. PalGly inhibits heat-evoked firing of wide dynamic range (WDR) neurons, activates calcium influx in DRG cells and stimulates NO production. Preliminary studies suggest its signaling mechanism involves GPCR-mediated cation channel activation and a Gαi/o-coupled signaling pathway, which is being further investigated.
P0099 Paliperidone ≥98% (HPLC) Paliperidone is an atypical antipsychotic; active metabolite of risperidone.
human ... DRD2(1813), HTR2A(3356)
P4509 Palmitoyl-DL-carnitine chloride powder Palmitoyl-DL-carnitine chloride is known to inhibit biofilm formation mediated by Pseudomonas aeruginosa and Escherichia coli. It is a phosphokinase C inhibitor.
P9716 Palmitoyl coenzyme A lithium salt ≥90% Long chain fatty acid (C16) covalently linked to Coenzyme A. Covalent attachment of palmitate is a common occurrence on a wide variety of viral and cellular proteins and plays a role in promoting membrane binding. Palmitoylation may also be a general mechanism for prolonging or potentiating G-protein signaling.
Palmitoyl coenzyme A is useful in the biosynthesis of sphingosine, a component of sphingolipids and phospholipids.
P0359 Palmitoylethanolamide Endogenous CB2 cannabinoid receptor agonist.
human ... CNR1(1268), CNR2(1269)
rat ... Faah(29347)
L5016 1-O-Palmityl-sn-glycero-3-phosphocholine ≥99%, synthetic Intermediate in the synthesis of platelet activating factor (PAF). Inactive form that can be used as a control in studies of PAF activity.
SML0801   Palomid 529 ≥98% (HPLC) Palomid 529 (P529) is a PI3K/Akt/mTOR inhibitor, which is unique in that it causes the dissociation of both the TORC1 and TORC2 complexes and inhibits both Akt and mTOR signaling. Palomid 529 has been shown to inhibit tumor growth, angiogenesis, and vascular permeability. Palomid 529 (P529) inhibited glioblastoma growth, penetrating the blood brain barrier with little affinity for ATP-binding cassette (ABC) drug efflux transporters ABCB1 and ABCG2. Palomid 529 has also shown promise as a possible treatment for macular degeneration and keloid disease.
SML1195 Palonosetron hydrochloride ≥98% (HPLC) Palonosetron is a potent and selective 5-HT3 receptor antagonist (Aloxi) used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).
human ... HTR3A(3359)
P2371 Pamidronate disodium salt hydrate ≥95% (NMR), solid Bone resorption inhibitor; inhibitor of farnesyl diphosphate synthase (IC50 = 200 nM).
Pamidronate disodium has the ability to block Wnt and β-catenin signaling, which modulates the osteogenic differentiation in bone marrow mesenchymal stem cells (BMMSCs). It can also reduce bilirubin-impaired apoptosis and helps to develop dentinogenic dysfunction of stem cells from human deciduous teeth.
P1918 Pancuronium bromide Aminosteroidal neuromuscular blocking agent; skeletal muscle relaxant
human ... CHRNA1(1134), CHRNB1(1140), CHRND(1144), CHRNE(1145), CHRNG(1146)
SML0726   Panepoxydone from Lentinus conatus, ≥95% (HPLC) Panepoxydone is a fungal metabolite that inhibits NF-κB transcription factor by preventing IκB phosphorylation, thus inhibiting the release of NF-κB from the IκB : NF-κB complex and its translocation into the nucleus. Panepoxydone also has antimalarial, cytotoxic activities and anti-parasitic activity against Trypanosoma cruzi.
P0021 Pantoprazole sodium hydrate ≥98% (HPLC) Pantoprazole is a benzimidazole derivative,activated in acidic environment. It is useful in treating long term prophylaxis and acid-related disorders.
Pantoprazole is a gastric proton pump inhibitor.
human ... ATP4A(495), ATP4B(496)
P3510 Papaverine hydrochloride powder Papaverine is originally used to resolve male impotence.
Smooth muscle relaxant and cerebral vasodilator; phosphodiesterase inhibitor.
human ... PDE4B(5142)
SML1876 PaPE-1 ≥98% (HPLC) PaPE-1 is a "Pathway Preferential Estrogen" that activates the extranuclear signaling pathway without activating the nuclear signaling pathway. PaPE-1 bound 50,000-fold less well to ERα and Erβ estrogen receptors. PaPE-1 activated extranuclear-initiated ER-regulated genes, but showed essentially no activation of nuclear-initiated estrogen receptor (ER) gene targets such as the progesterone receptor. Unlike estradiol (E2), PaPE-1 did not stimulate proliferation of MCF-7 breast cancer cells. Like estradiol, PaPE-1 strongly activated MAPK and mTOR pathway. Instead, it showed preferential estrogen-like activity in non-reproductive (metabolic and vascular) tissues, reducing body weight gain and fat accumulation in ovariectomized mice and accelerating repair of endothelial damage in the vascualture.
SML2883 Paquinimod ≥98% (HPLC) New Paquinimod (ABR-215757) is an orally active quinoline-3-carboxamide (Q substance) class immunomodulator that targets S100A9 (Calgranulin B; MRP14) via direct binding and blocks its interaction with receptor for advanced glycation end products (RAGE) and Toll-like receptor 4 (IC50 = 26 μM & 23 μM against 100 nM hS100A9 from binding immobilized hRAGE & hTLR4/MD2, respectively). Paquinimod in vivo efficacy is demonstrated in murine models of autoimmune/inflammatory diseases, including liver fibrosis, collagen-induced osteoarthritis, peritonitis, EAE, type 1 diabetes, lupus (0.04-25 mg/kg/day p.o.), and atherosclerosis (10 mg/kg i.p.).
UC448 Paracetamol sulfate potassium salt solid, ≥97% (HPLC) Phase II metabolite of paracetamol.
SML2217 Parecoxib sodium ≥98% (HPLC) Parecoxib sodium is a non-steroidal anti-inflammatory drug (NSAID), a cyclooxygenase-2 (COX-2) selective inhibitor. It is a water-soluble and injectable prodrug of valdecoxib.
P8013 Pargyline hydrochloride Pargyline hydrochloride acts as a histone demethylase inhibitor. It has antihypertensive action.
Selective MAO-B inhibitor.
human ... MAOA(4128), MAOB(4129)
P9623 Paroxetine hydrochloride hemihydrate ≥98% (HPLC), powder Paroxetine hydrochloride hemihydrate is one of the most potent and selective of the selective serotonin reuptake inhibitors (SSRI); antidepressant
Paroxetine is a phenylpiperidine derivative. It has the ability to cross placenta. Paroxetine is known to increase the risk of congenital cardiac malformations. It might be useful in hormone replacement therapy for treating vasomotor symptoms during menopause. It is known to ameliorate the effects of panic disorder, obsessive‐compulsive disorder and social phobia.
human ... SLC6A4(6532)
P1372 Paroxetine maleate salt ≥98% (HPLC), solid Paroxetine is a strong cytochrome P450 2D6 isotype (CYP2D6) inhibitor, which reduces the effectiveness of tamoxifen. This phenylpiperidine derivative inhibits clozapine metabolism. Paroxetine is used to treat social phobia, obsessive-compulsive disorder and panic disorder. It is also used to treat the premenstrual dysphoric disorder, post-traumatic stress disorder and chronic headache.
Paroxetine maleate is a selective serotonin reuptake inhibitor; antidepressant.
human ... SLC6A4(6532)
P0667 Parthenolide ≥98% (HPLC) Anti-inflammatory agent that inhibits NF-κB activation.
human ... ELA2(1991), IKBKG(8517), NFKB1(4790), NKAP(79576), NKRF(55922)
P5806   Pasteurella multocida toxin lyophilized powder Pasteurella multocida toxin (PMT) is a bacterial protein toxin produced by few P. multocida serotype A and D strains. It acts as an effective mitogen in numerous cell types in vitro. PMT inhibits osteoblast differentiation by activating the Rho/Rho-associated coiled-coil containing protein kinase (Rho/ROCK) pathway. Infections of PMT cause atrophic rhinitis in pigs and by local dermatonecrosis, respiratory disease in cattle and rabbits. PMT is also a pathogenic agent of dermatonecrosis and bacteremia in humans.
P2928 Paxilline powder, ≥98% (HPLC) Paxilline is a selective blocker of high-conductance Ca2+-activated (Maxi-K) potassium channels. It also blocks big potassium (BK) channels.
P9246 PB28 dihydrochloride ≥98% (HPLC), solid Selective σ2 opioid receptor ligand; putative σ2 agonist
SML1058   PBIT ≥98% (HPLC) S,S′-1,4-phenylenebis(1,2-ethanediyl)bis-isothiourea (PBIT) is an iNOS (inducible nitric oxide synthase) inhibito. It is capable of inhibiting the multiplication of breast cancer cell lines expressing high levels of JARIDB1.
PBIT is a potent inhibitor of JARID1B (KDM5B) histone lysine demethylase that inhibits removal of H3K4me3 in UACC-812 cells. PBIT inhibits proliferation of cells overexpressing JARID1B. PBIT is selective for JARID1 enzymes and does not inhibit demethylases UTX or JMJD3.
SML1881 PBOX-6 ≥98% (HPLC) PBOX-6 belongs to a group of tubulin-targeting pyrrolo-1,5-benzoxazepine (PBOX) compounds that potently induce apoptosis in a wide spectrum of cancer cells, including those originating from the four main types of leukemia and those exhibiting multi-drug resistance (IC50 = 2.28 μM/HL60-MDR1, 2.86 μM/HL60-ABCG2, 1.91 μM/HL60; IC50 = 4.71 μM/A2780-ADR, 4.10 μM/A2780). PBOX-6 inhibits the assembly of purified tubulin in cell-free assays and causes microtubule depolymerization in MCF-7 cells by binding a tubulin site distinct from those targeted by vinblastine and colchicine. When administered via intratumoral injection (7.5 mg/kg/day) in vivo, PBOX-6 is reported to significantly inhibit tumour growth in a murine model of neuroblastoma and a CML model of the imatinib-resistant T315I mutants.
SML1895 PBOX-15 ≥98% (HPLC) PBOX-15 belongs to a group of tubulin-targeting pyrrolo-1,5-benzoxazepine (PBOX) compounds that potently induce apoptosis in a wide spectrum of cancer cells, including those originating from the four main types of leukemia and those exhibiting multi-drug resistance (IC50 = 155 nM/HL60-MDR1, 252 nM/HL60-ABCG2, 210 nM/HL60). PBOX-15 inhibits the assembly of purified tubulin in cell-free assays and causes microtubule depolymerization in MCF-7 cells.
B4688 PBPE hydrochloride ≥98% (HPLC) PBPE is a selective ligand of anti-estrogen binding site (AEBS) (Ki=1.2 nM).
SML0730   PCNA-I1 ≥98% (HPLC) PCNA-I1 is a small molecule PCNA inhibitor that selectively binds to PCNA trimers and reduces the association of PCNA with chromatin. PCNA-I1 induces S and G2/M phase cell cycle arrest in tumor cells with greater efficacy than non-transformed cells.
Proliferating cell nuclear antigen-l1 (PCNA) is a member of the scaffold B class. It acts as a linker at the monomer-monomer interface. PCNA-I1 has the ability to block the development of primary cultures of bone marrow mesenchymal stem cells, endothelial cells, lymphocytes, mammary epithelial cells and prostate epithelial cells.
SML1848 PCS1055 dihydrochloride ≥98% (HPLC) PCS1055 is a potent and selective muscarinic M4 acetylcholine receptor competitive antagonist that exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 was originally described as a potent electric eel AChE inhibitor (IC50 = 22 nM) and less potent at human AChE (IC50 = 120 nM).
PZ0162 PD 0325901 ≥98% (HPLC) PD 0325901 by inhibiting mitogen-activated protein kinases (MAPKs) elicits growth-inhibitory and antiangiogenic effects on glioblastoma and melanoma tumor progression.
PD 0325901 is a potent MKK1 (MEK1) and MKK2 (MEK2) inhibitor. The Ki is 1.1 and 0.79 nM for MEK1 and MEK2, respectively. PD 0325901 was inactive against a panel of 27 other kinases. PD 0325901 inhibited C26 tumor pERK by 75% when dosed at 25 mg/kg in mice.
human ... MAP2K1(5604), MAP2K2(5605)
PZ0199 PD 0332991 isethionate ≥98% (HPLC) PD 0332991 is a potent selective inhibitor of cyclin dependent kinases CDK4 and CDK6 with in vitro IC50 = 11 nM (CDK4) and 16 nM (CDK6). PD 0332991 induces G1 arrest in retinoblastoma (Rb)-positive tumor cells.
PD 0332991 might act as a chemsensitizer. It is useful in the treatment of breast cancer along with antioestrogens. PD 0332991 is also known to possess antitumor action.
human ... CCND1(595), CDK4(1019), CDK6(1021)
P215 PD 98,059 solid PD 98,059 is a flavonoid and specific inhibitor of mitogen-activated protein kinase kinase (MAPKK). In mice, PD 98,059 helps to block zymosan stimulated organ dysfunction syndrome and non-septic shock. It is known to inhibit in vitro hypertrophy. PD 98,059 also induces cartilage formation in mesenchymal stromal cells.
human ... MAP2K1(5604), MAP2K2(5605), MAP2K3(5606), MAP2K4(6416), MAP2K5(5607), MAP2K6(5608), MAP2K7(5609), MAP3K1(4214), RAF1(5894)
P5624 PD-118057 ≥98% (HPLC), solid PD-118057 is an activator of ether-a-go-go-related (hERG) potassium channel. PD-118057 is a second identified hERG channel activator, a representative in the series of structural analogs; PD-118057 at 10 μM leads to a 111% current increase in rabbit ventricular wedge (in comparison RPR260243 leads to only a 15% increase at the same concentration);PD-118057, unlike RPR260243, does not have a major effect on gating or kinetic properties of this channel. PD-118057prevents and reverses QT interval prolongation; Compounds such as PD-118057 may offer new approach in the treatment of delayed repolarization conditions, which occur in inherited or acquired long QT syndrome and congestive heart failure
P5749 S-(+)-PD 123177 trifluoroacetate salt hydrate ≥98% (HPLC), solid S-(+)-PD 123177 is selective AT2 angiotensin receptor antagonist. The angiotensin AT2 receptor is an atypical seven transmembrane domain receptor that is coupled to activation of tyrosine phosphatase and inhibition of MAP kinase, and does not undergo agonist-induced internalization. An investigation of the occurrence and nature of AT2 receptor phosphorylation revealed that phorbol ester-induced activation of protein kinase C (PKC) in HA-AT2 receptor-expressing COS-7 cells caused rapid and specific phosphorylation of a single residue (Ser354) located in the cytoplasmic tail of the receptor. Agonist activation of AT2 receptors by angiotensin II (Ang II) also caused rapid PKC-dependent phosphorylation of Ser354 that was prevented by the AT2 antagonist, S-(+)-PD 123177, and by inhibitors of PKC. In cells coexpressing AT1 and AT2 receptors, Ang II-induced phosphorylation of the AT2 receptor was reduced by S-(+)-PD 123177 and abolished by treatment with both antagonists or with PKC inhibitors. These findings indicate that the AT2 receptor is rapidly phosphorylated via PKC during homologous activation by Ang II, and also undergoes heterologous PKC-dependent phosphorylation during activation of the AT1 receptor.
P183 (+)-PD 128,907 hydrochloride >97%, solid Selective D3 dopamine receptor agonist.
human ... DRD3(1814)
P216 (±)-PD 128,907 hydrochloride solid, ≥98% (HPLC) Selective D3 dopamine receptor agonist.
human ... DRD3(1814)
P4620 PD 146176 ≥98% (HPLC), solid 15-Lipoxygenase inhibitor
PD 146176 blocks neuroprotectin D1 (NPD1) and eicosanoid synthesis by inhibiting the 5-lipoxygenase-1 (15-LOX-1) enzyme.
human ... ALOX15(246)
mouse ... ALOX15(11687)
rat ... ALOX15(81639)
PZ0175 PD 149163 tetrahydrochloride hydrate ≥90% (HPLC) PD 149163 is a Neurotensin NTR1 receptor agonist; a Neurotensin (8-13) analog. PD149163 is a selective, brain penetrating NT1 receptor agonist with pro-cognitive, antipsychotic and anxiolytic effects.
D5946 PD 150606 ≥97% (HPLC) PD 150606 is a selective; cell-permeable; non-peptide; uncompetitive calpain inhibitor.
SML0402 PD 151746 ≥98% (HPLC) PD 151746 is a potent inhibitor of calpains 1 and 2.
SML0564 PD153035 hydrochloride ≥98% (HPLC) PD153035 is apotent and selective ATP competitive inhibitor of the epidermal growth factor receptor tyrosine kinase EGFR.
PZ0141 PD-156707 ≥98% (HPLC) PD-156707 is a selective endothelin receptor (ETA) antagonist.
PZ0109 PD-161570 ≥98% (HPLC) PD-161570 is an inhibitor of human FGF-1 receptor tyrosine kinase.
PZ0144 PD-161989 2-Hydroxyethanesulfonate ≥98% (HPLC) PD-161989 is an AMPA receptor antagonist.
PZ0116 PD-166285 hydrate ≥98% (HPLC) PD-166285 hydrate is a broad spectrum protein tyrosine kinase inhibitor; Src and FGFR kinase inhibitor.
PZ0366 PD166326 ≥98% (HPLC) ATP-competitive dual BCR-ABL and Src kinase inhibitor
PD166326 is an ATP-competitive dual BCR-ABL and Src kinase inhibitor. In some studies it has been found to be more potent than imatinib with inhibition of cancer growth in the low nanomolar range or even picomolar range in various biological systems.
P0047 PD166793 hydrate ≥98% (HPLC) PD166793 is a broad spectrum, but class-selective, MMP inhibitor (low nM at MMP-2 & 3 and low μM at MMP-1, 7 & 9). Adding PD166793 to the high-fat diet substantially reduced the rise in blood glucose. The improvement of glucose homeostasis in PD166793-treated ZDF rats was a result of the enhancement of β-cell function. It prevents β-cell dysfunction and diabetes in female ZDF rats on a high-fat diet. It has been shown to block left ventricular remodeling and dysfunction in a rat model of heart failure. Preservation of normoglycemia and normal glucose tolerance in compound PD166793-treated animals is accompanied by preservation of the high serum insulin levels that are a consequence of the insulin resistance present in these animals. It is not reversing insulin resistance these animals. The most striking effect of the compound is on pancreatic insulin content and β-cell volume.
PZ0114 PD-166866 ≥98% (HPLC) PD-166866 is a selective inhibitor of the FGF-1 receptor tyrosine kinase (FGFR1) with IC50 = 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4.
P233 PD 168,077 maleate salt powder Selective D4 dopamine receptor agonist.
human ... DRD4(1815)
PZ0285 PD168393 ≥98% (HPLC) PD168393 is a 6-acrylamido-4-anilinoquinazoline compound. It increases apoptosis in malignant peripheral nerve sheath tumor cells, stimulated by lysosomal dysfunction.
PD168393 is potent, cell-permeable, irreversible and selective inhibitor of EGF receptor (EGFR) tyrosine kinase and ErbB2. PD168393 has an IC50 value of 0.70 nM for EGFR, and is inactive against insulin, PDGFR, FGFR and PKC.
P9248 PD 169316 ≥98% (HPLC), solid Potent, cell-permeable and selective p38 MAP kinase inhibitor (IC50 = 89 nM).
human ... MAPK14(1432)
P2499 PD 173074 ≥96% (HPLC), powder PD 173074 inhibitor is specific for receptor tyrosine kinases. It competes with adenosine triphosphate (ATP) for its inhibition. PD 173074 prevents the FGF/ vascular endothelial growth factor (VEGF) induced angiogenesis.
PD 173074 is a fibroblast growth factor receptor 3 (FGFR3) inhibitor: IC50 = 5 nM inhibition of FGFR3 autophosphorylation. PD 173074 arrests the G0/G1 phase of FGFR3-expressing cells. It is 100-fold more selective for FGFR3 than for VEGF receptors, IGF-1 receptors, and MAPKs.
human ... FGFR1(2260), KDR(3791)
mouse ... Pdgfrb(18596)
PZ0113 PD173952 ≥98% (HPLC) PD173952 is a Src family kinase inhibitor.
PZ0142 PD-180970 ≥98% (HPLC) PD-180970 is a potent inhibitor of the p210 Bcr-Abl tyrosine kinase.
PZ0112 PD-184161 ≥98% (HPLC) PD-184161 is a MEK inhibitor.
PZ0181 PD184352 ≥98% (HPLC) PD184352 (CI-1040) is a highly selective non-competitive inhibitor of MEK (MKK1; MAPK kinase) and the closely related MKK2. It has anti-cancer activity, suppresses the ERK pathway, and has been used along with other classes of inhibitors to establish embryonic stem cell lines.
human ... MAP2K1(5604), MAP2K2(5605)
PZ0111 PD-407824 ≥98% (HPLC) PD-407824 is a Wee1/Chk1 inhibitor.
PZ0370 PD-85639 PD-85639 (PD85,639) is a voltage-gated sodium (Na+) channel blocker (75% in 10 min & >95% in 25 min blockage of Na+ current by 25 μM PD85,639; whole-cell patch clamp using primary rat brain neurons) that is shown to target rat brain Nav1.2 with simultaneous high- and low-affinity modes of binding (EC50 = 56 nM/40% & 20 μM/60% at pH 9.0, 5 nM/28% & 3 μM/72% at pH 7.4, against 2 nM [3H]-PD85,639 for binding rat brain synaptosomes; EC50 = 17 nM/39% & 10 μM/61% using at pH 9.0 using rat brain synaptosome membranes) and a fast kinetic (t1/2 = 1.2 at 4°C, <0.5 min at 25°C), competitive against the local anesthetic Na+ channel blockers tetracaine, bupivacaine, and mepivacaine, as well as Na+ channel activators veratridine and batrachotoxin (K1 = 0.26 μM against 5 nM [3H]-BTX for binding rat neocrotical membranes).
SML1781 PDD00017273 ≥98% (HPLC) PDD00017273 is a potent and selective inhibitor of Poly(ADP-ribose) glycohydrolase (PARG), which catalyses hydrolysis of the O-glycosidic linkages of ADP-ribose polymers, reversing the effects of poly(ADP-ribose) polymerases (PARPs). PARG has been shown to be involved in the repair of single strand DNA breaks. PDD00017273 is selective for PARG, with EC50 = 26 nM, compared to values of 30 μM for PARP1 and ARH3.
PDD00017273 is cell permeable in nature. It is used for specific killing of cells defective in certain homologous recombination (HR) proteins such as breast cancer gene 1/2 (BRCA1/2).
SML0021 PDI inhibitor 16F16 ≥98% (HPLC) 16F16 is a protein disulfide isomerase (PDI) inhibitor, first identified in a screen for compounds that prevent apoptosis induced by mutant huntingtin protein. 16F16 not only suppressed apoptosis induced by the misfolded protein mutant hungtingtin, it also protected rat neurons from cell death triggered by Aβ peptide. The actions of this inhibitor helped to identify a new mechanism in which a cell death pathway is regulated by protein misfolding via PDI upregulation.
SML1126 PDP-EA ≥98% (HPLC) 3-N-Pentadecylphenolethanolamide (PDP-EA) is an activator of fatty acid amide hydrolase (FAAH) from plant and mammalian species. PDP-EA appears to enhance FAAH activity by reduction of negative feedback from free ethanoloamine.
P1999 PEAQX tetrasodium hydrate ≥98% (HPLC) NMDA receptor antagonist.
PEAQX is more specific for N-methyl-D-aspartate (NMDA) receptor 2A (NR2A) than N-methyl-D-aspartate (NMDA) receptor 2B (NR2B) and induces striatal apoptosis. It is less potent in activating caspase-3 than its stereomer NVP-AAM007.
PZ0197   Pelitinib ≥98% (HPLC) Pelitinib (EKB-569) is an orally active, potent, second generation irreversible epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Pelitinib is selective for EGFR (ErbB-1) with an IC50 about 80 nM, but also covalently binds to ErbB-2 (HER2/c-neu) and ErbB-4 (Her 4) with much lower potency. Pelitinib has been shown to inhibit the growth of EGFR-overexpressing tumor cell lines.
SML2503 Pellitorine ≥97% (HPLC) Pellitorine is an α-Glucosidase inhibitor isolated from the roots of Piper Nigrum that exhibit anti-diabetic, anti-cancer, anti-bacterial and anti-inflammatory properties. Pellitorine is an ACAT (Acyl-CoA cholesteryl acyl transferase) inhibitor that inhibits cholesterol esterification in HepG2 cells. Also pellitorine exhibit potent larvicide activity in mosquito by Inhibition of gene expression encoding V-type H+-ATPase and aquaporine 4. Some new research suggests that anti-adipogenic activity of pellitorine depends on TRPV1.
SML1490   Pemetrexed disodium heptahydrate ≥98% (HPLC) Pemetrexed is antifolate cancer drug approved for treatment of variety of cancer including pleural mesothelioma and non-small cell lung cancer. Pemetrexed is a folate antimetabolite that inhibits thymidylate synthase, dihydrofolate reductase and glycinamide ribonucleotide formyltransferase, three enzymes used in purine and pyrimidine synthesis.
SML0107 Pemirolast potassium ≥98% (HPLC) Pemirolast potassium is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent. It Inhibits chemical mediator release from tissue mast cells and has recently also been shown to inhibit the release of peptides including substance P, neurokinin (NK) A, and calcitonin gene-related peptide (CGRP) from sensory nerves. It has been used for the treatment of allergic conjunctivitis prophylaxis of for pulmonary hypersensitivity reactions to drugs such as paclitaxel
P0048 Pemoline ≥98% (HPLC) Pemoline is a CNS stimulant. Pemoline is used to treat attention-deficit hyperactivity disorder (ADHD). Pemoline is a Schedule IV drug and offers some advantages over other stimulants in that it does not reduce the appetite or cause dry mouth.
P3371 Penfluridol ≥97% (HPLC), powder T-type Ca2+ channel blocker; antipsychotic
P3053 Penitrem A ≥95% (HPLC and TLC) Penitrem A intoxication causes ataxia, polypnea, and sustained tremors and may lead to seizures and death. Penitrem A affects the central and peripheral nervous system. It impairs the GABAergic neurotransmission in the cerebellum.
G7548 Penta-O-galloyl-β-D-glucose hydrate ≥96% (HPLC) PGG induces predominantly (caspase dependent) apoptosis in DU145 and LNCaP cells, while inducing autophagy in more resistant PC3 and TRAMP-C2 cells. It appears that PGG targeted signaling downstream of rather than the mTOR itself. Polyphenolic pyranoses were reported (J Biol Chem. 2010, 285 (11), 7892-902) to inhibit the plasminogen activator inhibitor type 1 (PAI-1).
Penta-O-galloyl-β-D-glucose hydrate (PCG) is a polyphenolic gallotannin compound produced by plants. It has an ability to inhibit matrix metalloproteinase (MMP) related metastatic activity. Thus, PCG can be used for treating metastatic activity in squamous cell carcinoma. In addition, it also acts as a potential drug for stabilizing small abdominal aneurysms.
P0547 Pentamidine isethionate salt powder Neuroprotective; inhibits constitutive nitric oxide synthase in the brain; NMDA glutamate receptor antagonist.
Pentamidine isethionate is used as a second line drug for leishmaniasis.
human ... GRIN1(2902), GRIN2A(2903), GRIN2B(2904), GRIN2C(2905), GRIN2D(2906), GRINA(2907), NOS1(4842), NOS2(4843), NOS2B(201288), NOS2C(645740), NOS3(4846)
P134 (−)-Pentazocine ≥98% (HPLC)    
P127 (+)-Pentazocine solid σ receptor agonist; active enantiomer of pentazocine.
human ... EBP(10682)
rat ... Chrm1(25229), Chrm2(81645), Drd2(24318), Oprm1(25601)
SML0508 Pentostatin ≥95% (HPLC) Pentostatin is a ring-expanded nucleoside (REN) that potently inhibits adenosine deaminase, which leads to lymphocyte toxicity. Pentostatin is used as anticancer agent to treat leukemia (hairy cell leukemia and chronic lymphocytic leukemia) and is investigated as an agent to treat graft-versus-host disease (GVHD).
Pentostatin/2′-deoxycoformycin is used to treat patients with Waldenström′s macroglobulinemia.
human ... ADA(100)
P1784 Pentoxifylline solid Pentoxifylline (PTX) is considered as a nonspecific phosphodiesterase inhibitor. It possesses rheologic properties. Pentoxifylline is used to treat peripheral vascular disease. It has the ability to block the phosphorylation of I kappa B-alpha (IĸBα) in serines 32 and 36.
Phosphodiesterase inhibitor; inhibits synthesis of tumor necrosis factor α (TNF-α).
human ... ADORA2B(136), LITAF(9516), PDE4B(5142), TNF(7124)
rat ... Tnf(24835)
P6500 Pentylenetetrazole Pentylenetetrazole is a non-specific central nervous system (CNS) stimulant and convulsant. PTZ induces oxidative stress and increases cortical malondialdehyde content and affects hippocampus, resulting in seizures.
SML1132   Pep2-8 trifluoroacetate salt ≥95% (HPLC), contains 58μL of solution at 10mM in DMSO Pep2-8 is a potent PCSK9 (proprotein convertase subtilisin/kexin type 9) inhibitor that selectively binds to PCSK9 and interferes with LDL receptor binding to PCSK9. Pep2-8 restores LDL receptor function and LDL uptake of PCSK9-treated HepG2 cells.
SML2626   PEP87 trifluoroacetate salt ≥95% (HPLC) PEP87, a highly conserved helical fragment of hemagglutinin HA2 subunit, is an inhibitor of H7 and H5 hemagglutinin (HA) mediated influenza virus entry. PEP87 binds to the hemagglutinin trimer where it disrupts native tertiary structure and prevents HA function.
SML2486 Peramivir trihydrate ≥98% (HPLC) Peramivir is an Influenza viral neuraminidase inhibitor.
SML2652 Peretinoin ≥97% (HPLC) Peretinoin is an orally active synthetic acyclic retinoid (ACR) whose in vivo anti-hepatocellular carcinoma (HCC) efficacy is attributed to its upregulatory activity toward retinoid nuclear receptors (RARbeta & RXRalpha), as well as negative regulation against sphingosine kinase 1 (SPHK1) expression and, thereby, sphingosine metabolic pathway. Peretinoin inhibits the replication of hepatitis B & C viruses in cultures (HBV & HCV EC50 = 9-25 μM) and shows in vivo efficacy in rodent models of hepatocarcinogenesis among rats (10, 40, or 80 mg/kg/day p.o.) and mice (0.03% or 0.06% in diet) subjected to chronic inflammation induction by diethylnitrosamine (DEN).
SML0120 Perhexiline maleate salt ≥98% (HPLC) Perhexiline maleate is an anti-anginal metabolic modulator. It inhibits the mitochondrial enzyme carnitine palmitoyltransferase CPT-1 and to a lesser extent CPT-2. This causes a shift in myocardial substrate utilisation from long chain fatty acids to carbohydrates, resulting in increased glucose and lactate utilization and increased ATP production for the same O2 consumption as before and consequently increases myocardial efficiency. Perhexiline maleate was also recently found to inhibit the activity of mTORC1.
human ... CPT1B(1375), CPT2(1376), MTOR(2475)
SML0612   Perifosine ≥98% (HPLC) Perifosine (KRX-0401) is a selective bioavailable alkylphospholipid inhibitor of protein kinase B/Akt (PKB/Akt) with anti-proliferative activity. Perifosine acts on cell membranes, selectively targeting proliferating cells, inducing growth arrest and apoptosis.
Perifosine (octadecyl-(1,1-dimethyl-4-piperidylio)) is an antitumor compound. It acts at lipid rafts and stops lysosomal accumulation and mTORC1 (mammalian target of rapamycin complex 1) signaling. This drug exhibits significant antiproliferative activity in vitro and in vivo in various human cancer model systems.
P0094 Perindopril erbumine Perindopril erbumine is an angiotensin converting enzyme (ACE) inhibitor; antihypertensive; becomes hydrolyzed in vivo to the active diacid metabolite; unlike the other ACE inhibitors, inhibits tumor growth in hepatocellular carcinoma cells due to suppression of VEGF levels; also suppresses angiotensin II production in vitro. Long-term therapy with this agent has a beneficial effect on the cerebral circulation by improving cerebral perfusion reserve in patients with previous minor stroke.
human ... ACE(1636)
SML1587 Perlapine ≥98% (HPLC) Perlapine is a potent and selective agonist of hM3Dq DREADD (Designer Receptors Exclusively Activated by Designer Drugs), which does not activate the native human M3 receptor. Perlapine is a neuroleptic agent that exhibits sedative and sleep-promoting properties.
human ... HRH1(3269)
SML2331 Perospirone hydrochloride ≥98% (HPLC) Perospirone (SM-9018) is a typical neuroleptic (antipsychotic) agent that displays high affinity for 5-HT2, D2 and 5-HT1A receptors (Ki = 0.61, 1.4 and 2.9-1.8 nM, respectively), moderate affinity for alpha 1 and D1 receptors (Ki = 17 and 41 nM, respectively), while exhibiting much reduced affinity for alpha 2 (Ki = 408 nM) and little affinity toward muscarinic, opiate, glutamate, phencyclidine, benzodiazepine or GABAA receptors (Ki >1 μM). SM-9018 antagonizes both D2-dependent (e.g. methamphetamine-induced hyperactivity, apomorphine-induced stereotypy) and 5-HT2-mediated (e.g. tryptamine-induced clonic seizure) activities in vivo, while exhibiting very low cataleptogenic and central depressant activities commonly observed with two other neuroleptics, haloperidol and chlorpromazine.
P6402 Perphenazine D2 dopamine receptor antagonist; α-adrenergic receptor antagonist and σ-receptor agonist; phenothiazine antipsychotic. Inhibits glutamate dehydrogenase in vitro.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), DRD2(1813), OPRS1(10280)
P7208   Pertussis toxin from Bordetella pertussis lyophilized powder Pertussis toxin catalyzes the ADP-ribosylation of the α subunits of the heterotrimeric guanine nucleotide regulatory proteins Gi, Go, and Gt. This prevents the G protein heterotrimers from interacting with receptors, thus blocking their coupling and activation. Since the Gα subunits remain in their GDP-bound, inactive state, they are unable to inactivate adenylyl cyclase or open K+ channels.
Bordetella pertussis Tohama I ... ptxA(2665068), ptxB(2665069), ptxC(2665408)
P2980   Pertussis toxin from Bordetella pertussis buffered aqueous glycerol solution Pertussis toxin catalyzes the ADP-ribosylation of the α subunits of the heterotrimeric guanine nucleotide regulatory proteins Gi, Go, and Gt. This prevents the G protein heterotrimers from interacting with receptors, thus blocking their coupling and activation. Since the Gα subunits remain in their GDP-bound, inactive state, they are unable to inactivate adenylyl cyclase or open K+ channels.
Bordetella pertussis Tohama I ... ptxA(2665068), ptxB(2665069), ptxC(2665408)
P0622 PET-cGMP ≥98% (HPLC), solid cGMP-dependent protein kinase (PKG I and PKG II) activator. Potent membrane permeant activator of both isozymes I α and I β of cGMP-dependent protein kinase. Common stimulators such as 8-Br-cGMP or 8-pCPT-cGMP mainly activate kinase subtype Iα.
PZ0274   PF-01247324 ≥98% (HPLC) In humans, PF-01247324 [6-amino-5-(2, 3, 5-trichloro-phenyl)-pyridine-2-carboxylic acid methylamide] prevents native tetrodotoxin-resistant (TTX-R) currents in dorsal root ganglion (DRG) neurons.
PF-01247324 is an orally bioavailable, selective and potent NaV1.8 channel blocker that inhibits that exhibits analgesic efficacy in rodent behavioral models of pain.
PZ0367 PF-02413873 ≥98% (HPLC) PF-02413873 is a potent, selective and fully competitive non-steroidal progesterone receptor (PR) antagonist that blocks progesterone binding and PR nuclear translocation. PF-02413873 suppresses endometrial growth in the macaque and human.
PZ0298 PF-03084014 hydrobromide ≥98% (HPLC) PF-03084014 inhibits the Notch signalling pathway. It contributes totumor suppression in breast, pancreatic carcinoma, hepatocellular carcinoma and progressive desmoid tumors. PF-03084014 in combination with dexamethasone elicits antileukemic effects in T-cell acute lymphoblastic leukemias (T-ALL).
PF-03084014 is a highly potent γ-secretase inhibitor that reduces Aβ production in vitro. PF-03084014 does not show a paradoxical increase in plasma Aβ at low concentrations in both preclinical species and humans.
PZ0229 PF-03246799 hydrochloride ≥98% (HPLC) PF-3246799 is a potent serotonin 5-HT2C receptor agonist with an EC50 of 4.5 nM and minimal activity at 5-HT2A and 5-HT2B receptors. PF-3246799 had good efficacy in a preclinical canine model of stress urinary incontinence.
PZ0326   PF-03549184 ≥98% (HPLC) PF-03549184 (PF-9184) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1) with an IC50 value of 16.5 nM in recombinant human mPGES-1. mPEGS-1 is the terminal enzyme that synthesizes prostaglandin E2 (PGE2) from PGH2 to PGE2 downstream of cyclooxygenase-2 (COX-2). Its expression is induced in response to pro-inflammatory mediators, similar to COX-2. Unlike the effects of COX inhibition, PF-9184 does not inhibit the production of other PGH2-derived products such as 6-keto-PGFα or PGF2α. PF-9184 inhibits PGE2 production in cell based assays with IC50 ranges from 0.5 to 5 μM. IC50 concentrations for rhCOX1 and rHCOX2 are 118 μM and 236 μM, respectively.
PGE2 is involved in inflammation and is one of the most abundant prostanoid.
PZ0155 PF-03716556 ≥98% (HPLC) potent, selective and reversible acid pump antagonist (H, K-ATPase)
PZ0218   PF-03814735 ≥98% (HPLC) PF-03814735 is a potent inhibitor of Aurora kinase A and B (IC50 = 5 and 0.8 nM, respectively). PF-03814735 inhibits proliferation of tumor cells in culture and in xenograft tumor models. The compound PF-03814735 blocks phosphorylation of Aurora B and Histone H3, and leads to the formation of polyploid cells in culture (HCT116 and MDA-MB-231).
PZ0031 PF-03882845 ≥98% (HPLC) PF-03882845 is a potent non-steroidal mineralocorticoid antagonist with and IC50 of 0.755 nM, compared to eplerenone with an IC50 of 109 nM. PF-03882845 was tested in a rat model for renal protection against aldosterone-mediated renal disease, and found to be more potent than eplerenone in suppressing the urinary albumin to creatinine ratio (UACR), a measure of renal fibrosis. The therapeutic index, calculated as the ratio of the EC50 for increasing serum K+ to the EC50 for UACR lowering, was 83.8 for PF-03882845 and 1.47 for eplerenone.
PZ0369 PF-04217329 ≥98% (HPLC) PF-04217329 is a selective and potent prostaglandin EP2 receptor agonist. PF-04217329 is an ocular bioavailable isopropyl ester prodrug of CP-544326 (active acid metabolite).
SML0263 PF-04217903 ≥98% (HPLC) PF-04217903 is a highly selective, potent inhibitor of the hepatocyte growth factor receptor c-Met. PF-04217903 inhibits endogenous, wild type c-Met in A549 human lung carcinoma cells with an IC50 of 4.8 nM. The compund displays 1000-fold selectivity against a panel of 208 other kinases.
PF-04217903 is an ATP-competitive inhibitor. It elicits antiangiogenic functionality. PF-04217903 inhibits c-Met phosphorylation in xenograft models leading to partial tumor growth suppression.
human ... MET(4233)
PZ0224   PF-04279405 ≥98% (HPLC) PF-04279405 is a potent and selective glucokinase activator.
PZ0354 PF-04363467 hydrochloride ≥98% (HPLC) PF-4363467 hydrochloride is a Dopamine D3/D2 receptor antagonist. PF-4363467 has 100-fold selectivity for D3 with a Ki value of 3.1 nM for D3R compared to a Ki value of 692 nM for D2R and high selectivity for D3R compared to other biogenic amine receptors. PF-4363467 attenuated opioid drug-seeking behavior in a rat model of addiction without causing the extrapyramidal symptoms often associated with D2R antagonism.
PZ0213   PF-04418948 ≥98% (HPLC) PF-04418948 is a PGE2 Receptor (EP2) specific antagonist (IC50 = 16 nM) with greater than 2000-fold selectivity over other EP subtypes. PF-04418948 inhibits EP2 activity in smooth muscle preps from human, dog and mouse.
PF-04418948 represses the formation of colorectal tumor.
PZ0222   PF-04445597 ≥98% (HPLC) PF-04445597 is a potent, orally bioavailable inhibitor of cholesteryl ester transfer protein (CETP).
PZ0380 PF-04447943 ≥98% (HPLC) PF-04447943 is a potent selective brain penetrant phosphodiesterase PDE9A inhibitor both potency (8 nM) and selectivity (>10 μM versus all the PDEs except PDE1C at >1 μM). It has been investigated for the treatment of cognitive disorders including Alzheimer′s Disease. PF-04447943 increased neurite outgrowth and synapse formation in hippocampal neurons in culture, exhibited synaptic stabilization in an amyloid precursor protein (APP) transgenic mouse model, and improved memory and enhanced attention in several animal models.
PZ0303 PF-04449913 maleate salt ≥98% (HPLC) PF-04449913 (Glasdegib) is an orally bioavailable Hedgehog pathway inhibitor. PF-04449913 acts by binidng Smoothened (Smo) and blocking signal transduction. PF-04449913 has an IC50 of 5 nM in the Gli-Luciferase assay. In a Phase I clinical trial in patients with advanced solid tumors, PF-04449913 caused disease stabilization in 34% of patients.
PF-04449913 maleate salt is also known as 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea. It increases the differentiation of blood cells from hematopoietic precursors of the lymph gland medullary zone. This human Smo inhibitor protein is now under clinical trials to treat myeloid malignancies.
human ... SMO(6608)
PZ0206 PF-04455242 hydrochloride ≥98% (HPLC) PF-4455242 is a selective k opioid receptor (KOR) antagonist with 20-fold selectivity for kappa over mu receptors (k Ki = 3 nM, μ Ki =64 nM). PF-4455242 is orally active, has good brain penetration in rats and was able to block the effects of the kappa agonist U50488. Studies indicate that k blockade has afforded antidepressant activity in several animal models. PF-4455242 has been in phase I clinical trials for trial for bipolar depression.
PZ0184 PF-04457845 ≥98% (HPLC) PF-04457845 is a potent, orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. PF-04457845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It was shown to be both potent and selective against other serine hydrolases. It has an IC50 value of 7.2 nM for human FAAH. The endocannabinoid system is a target for therapeutic pain relief. In a rat model of inflammatory pain, PF-04457845 produced significant reduction of inflammatory pain with efficacy comparable to that of naproxen at 10 mg/kg.
PZ0232 PF-04471141 hydrochloride ≥98% (HPLC) PF-04471141 is a potent, selective inhibitor of the calcium-activated phosphodiesterase PDE1. (PDE1B IC50 = 35 nM).
PZ0032 PF-04479745 ≥98% (HPLC) PF-04479745 (PF-4479745) is a selective serotonin 5HT2C agonist.
PZ0273   PF-04531083 ≥98% (HPLC) PF-04531083 is an orally available, potent and selective sodium channel Nav1.8 blocker. PF-04531083 was designated as a potential treatment of pain.
PZ0207 PF-04620110 ≥98% (HPLC) PF-04620110 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that inhibits triacylglycerol synthesis in cells and in rodents.
PF-04620110 is known to regulate gut hormones. Inhibition of DGAT1 might serve as a good approach for the treatment of obesity and type 2 diabetes. DGAT1 inhibition might increase the oxidation of fatty acids, thus it is found to be protective against hepatic steatosis.
PZ0228   PF-04628935 ≥98% (HPLC) PF-04628935 is a potent antagonist/inverse agonist of the ghrelin receptor, growth hormone secretagogue receptor 1a (GHS-R1a) with an IC50 of 4.6 nM. Ghrelin and GSHR are involved in regulation of food intake and long-term energy homeostasis; GSHR ligands are of interest for obesity and other metabolic disorders. PF-04628935 is orally bioavailable and brain penetrant.
PZ0309 PF-04634817 succinate ≥98% (HPLC) PF-04634817 is a potent and selective antagonist of CC chemokine receptor 2 and 5 (CCR2/5).
PZ0314   PF-04671536 ≥98% (HPLC) PF-04671536 is a highly potent and selective inhibitor of phosphodiesterase 8B (PDE8B) phosphodiesterase 8A (PDE8A). In primary human pancreatic islets, PF-04671536 increases insulin secretion in a glucose-dependent manner.
PZ0215   PF-04701475 ≥98% (HPLC) PF-04701475 is a potent and selective α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) positive allosteric potentiator.
PZ0216   PF-04725379 ≥98% (HPLC) PF-04725379 is a potent and selective α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR) positive allosteric potentiator.
PZ0284 PF-04753299 ≥98% PF-04753299 is a potent and selective inhibitor of LpxC (UDP-3-O-(R-3-hydroxymyristol)-N-acetylglucosamine deacetylase) that is effective in a murine of gram-negative bacteria infection model.
PZ0313 PF-04802367 ≥98% (HPLC) PF-04802367 (PF-367) is a potent and specific ATP-competitive inhibitor of glycogen synthase kinase 3 (GSK-3α/β) with an IC50 value of 2.3 nM and >450-fold selectivity for GSK-3 in a panel of >400 neuroreceptors, enzymes and kinases. GSK-3 dysregulation has been implicated in the pathogenesis of neurological diseases including Alzheimer′s disease.
PF-04802367 is also known as [N-(3-(1H-1,2,4-triazol-1-yl)propyl)-5-(3-chloro-4-methoxyphenyl)oxazole-4-carboxamide) or PF-367. It regulates tau phosphorylation in the brain.
PZ0379 PF-04827736 ≥98% (HPLC) PF-04827736 is a non-brain penetrant potent and selective inhibitor of phosphodiesterase PDE1, thought to be involved in regulation of vascular smooth muscle.
SML1061 PF-04856264 ≥98% (HPLC) PF-04856264 is a potent, selective inhibitor of the human Nav1.7 voltage gated sodium channel (IC50 = 28 nM). PF-04856264 blocks mouse Nav1.7 (IC50 = 131 nM) but has low potency against the rat Nav1.7 channel (IC50 = 4.2 mM).
PZ0250 PF-04859989 hydrochloride ≥98% (HPLC) PF-04859989 is a brain-penetrable irreversible inhibitor of kynurenine amino transferase II (KAT II), the enzyme responsible for most of the brain synthesis of kynurenic acid, which has been implicated in several psychiatric and neurological disorders, including schizophrenia and bipolar disorder, and thought to impair cognitive function. PF-04859989 has IC50 values of 23 nM for hKAT II and 263 nM for rKAT II. PF-04859989 is ~1000-fold selective for KAT II over human KAT I, KAT III, and KAT IV. PF-04859989 prevented ketamine-induced disruption of performance in memory tasks in both rodents and nonhuman primates.
PZ0294 PF-04880594 ≥98% (HPLC) PF-04880594 is a potent and selective RAF inhibitor that inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 potently inhibits tumor growth in BRAF-mutant melanoma xenograft models.
PZ0210   PF-04885614 ≥98% (HPLC) PF-04885614 is a potent and selective Nav1.8 inhibitor.
PZ0320 PF-04937319 ≥98% (HPLC) PF-04937319 is a glucokinase activator with an EC50 value of 174 nM. PF-04937319 was found to improve glycemic control in adults with type 2 diabetes when used in conjunction with metformin.
PF-04937319, unlike other glucokinase activators, is capable of maintaining lower-glucose levels without it resulting in hypoglycemia. In type II diabetic patients where metformin treatment is inadequate, PF-04937319 is capable of maintaining glycemic control within the acceptable risk-benefit profile.
PZ0247 PF-04979064 ≥98% (HPLC) PF-04979064 is an orally available, potent and selective PI3K/mTOR dual kinase inhibitor that potently inhibits tumor growth in mouse xenografts.
PZ0223   PF-04991532 ≥98% (HPLC) PF-04991532 is a potent and hepatoselective glucokinase activator that reduces mean daily glucose (MDG), fasting plasma glucose (FPG) and glucose excursion in humans.
PZ0310 PF-04995274 ≥98% (HPLC) PF-04995274 is a potent partial agonist of serotonin 5HT4 receptor with Ki = 0.15 - 0.46 nM for 5-HT4 isoforms a, b, d and e. 5-HT4 agonists modulate cholinergic function are being studied as possible treatment for cognitive disorders associated with Alzheimer′s Disease. PF-04995274 is brain penetrant and was shown to increase brain acetylcholine levels and reversed scopolamine-induced learning deficits in the rat Morris water maze test.
PZ0355 PF-05085727 ≥98% (HPLC) PF-05085727 is a potent inhibitor against cGMP-dependent phosphodiesterase PDE2 (PDE2A; IC50 = 2.3 nM) with >500-fold selectivity over other PDEs. Its 3-[(18)F]fluoroazetidinyl derivative ([(18)F]PF-05270430) has been successfully applied via i.v. injection as a brain-permeant probe for imaging brain PDE2 in live cynomolgus monkeys by positron emission tomography (PET).
PZ0311 PF-05089771 ≥98% (HPLC) PF-05089771 is a selective and potent inhibitor of the human voltage-gated sodium ion channel Nav1.7 with an IC50 value of 11 nM. PF-05089771 targets the voltage-sensing domain, preferentially interacting with, and stabilizing, inactivated channel conformations by interaction with the voltage-sensor domain (VSD) of Domain 4. Nav1.7 is expressed in sensory neurons and is critical for pain processing. PF-05089771 is being investigated for the treatment of chronic neuropathic pain.
PZ0299 PF-05175157 ≥98% (HPLC) PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively. Acetyl CoA carboxylase (ACC) generates malonyl CoA, which is a substrate for de novo lipogenesis and is also an inhibitor of mitochondrial fatty acid β-oxidation through inihbition of carnitine-palmitoyl transferase I (CPT-1), responsible for the transport of long-chain fatty acyl-CoAs across the mitochondrial membrane. ACC inihibitors are hoped to inhibit de novo lipogenesis and increase β-oxidation of long-chain fatty acids with potential for treatment of type 2 diabetes, hepatic steatosis, and cancer. In Phase I clinical studies for diabetes treatment, PF-05175157 inhibited de novo lipogenesis and increased net whole-body fatty acid utilization.
PZ0251   PF-05180999 ≥98% (HPLC) PF-05180999 is an inhibitor of cyclic nucleotide phosphodiesterase-2 (PDE2).
PZ0394 PF-05212377 succinate ≥98% (HPLC) PF-05212377 (SAM-760; WYE-103760) is an orally available, high-affinity, selective 5-hydroxytryptamine (5-HT; serotonin) receptor 5-HT6 antagonist (Ki/IC50 = 0.53/1.06 nM against 3 nM [3H]-LSD for binding human 5-HT6). PF-05212377 modulates glutamate and acetylcholine release in the cerebral cortex and hippocampus in rodents with in vivo pro-cognitive efficacy.
PZ0377 PF-05236216 hydrochloride ≥98% (HPLC) PF-05236216 is a brain penetrant, potent and selective inhibitor of casein kinase 1 delta/epsilon (CK1δ/ε) that modulates circadian rhythms in mice.
PZ0286 PF-05883083-00 ≥98% (HPLC) PF-05883083-00 is an analog of orally available dual Src/Abl kinase inhibitor Bosutinib.
PZ0220   PF-06250112 ≥98% (HPLC) PF-06250112 is a potent inhibitor of Bruton′s tyrosine kinase (BTK). PF-06250112 blocks both B-cell receptor and FcR-mediated signaling, and prevents FcR-dependent, Antibody-mediated proteinuria in a mouse glomerulonephritis model.
PZ0343 PF-06260414 ≥98% (HPLC) PF-06260414 is a nonsteriodal selective androgen receptor modulator (SARM). PF-06260414 is being investigated as a treatment for muscle weakening such as that associated with muscular dystrophy and the sarcopenia associated with natural aging. PF-06260414 has anabolic activity without unwanted androgenic activity on reproductive organs, liver or kidneys.
PZ0272 PF-06260933 dihydrochloride ≥98% (HPLC) PF-06260933 dihydrochloride is a MAP4K4 inhibitor.
PZ0324 PF-06263276 ≥98% (HPLC) PF-06263276 is an inhibitor of the Janus kinase (JAK) enzymes 1, 2, 3 and tyrosine kinase 2 (TYK2). PF-06263276 has been investigated for the treatment of psoriasis.
PZ0277   PF-06281355 ≥98% (HPLC) PF-06281355 (PF-1355) is an orally available, selective and potent mechanism based inhibitor of the myeloperoxidase (MPO) that reduces plasma MPO activity, vascular edema, neutrophil recruitment, and elevated circulating cytokines. PF-06281355 suppresses albuminuria and chronic renal dysfunction in model of anti-Glomerular Basement Membrane (GBM) disease.
PZ0375 PF-06282999 ≥98% (HPLC) PF-06282999 is an orally active thiouracil class myeloperoxidase (MPO) suicide substrate (kinact/KI = 11600 M-1s-1) that targets MPO heme group for mechanism-based irreversible inactivation wtih high selectivity over thyroid peroxidase (TPO kinact/KI <3 M-1s-1) and heme-containing cytochrome P450 (CYP) isoforms (IC50 >100 μM). PF-06282999 effectively inhibits MPO activity in human blood stimulated by LPS ex vivo (IC50 = 1.9 μM) and in blood of LPS-treated cynomolgus monkeys in vivo (5-80 mg/kg p.o. 1hr post LPS i.v.) with good pharmacokinetics and oral availability (100%/86%/75%/76% in mice/rats/dogs/monkeys). PF-06282999 also exhibits weak PXR activating activity (EC50/Emax = 279 μM/9.36-fold vs.0.8 μM/19.6-fold with rifampin).
PZ0301 PF-06284674 ≥98% (HPLC) PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator.
PZ0356 PF-06291874 ≥98% (HPLC) PF-06291874 is an orally active, potent and selective glucagon receptor antagonist. PF-06291874 exhibits a robust glucose reductions in subjects with type 2 diabetes mellitus.
PZ0219 PF-06297470 ≥98% (HPLC) PF-06297470 is a potent negative allosteric modulator of the Metabotropic Glutamate Receptor 5 (mGluR5). PF-06297470 binds to mGluR5 with a Ki of 0.9 nM. The compound PF-06297470 displays slight antagonism of mGluR1 (IC50 = 30.5 mM), with no agonist or antagonist activities against any other mGlu receptor subtype at concentrations up to 50 mM. PF-06297470 reduces dyskinesia in a rodent (MPTP)-rendered Parkinsonian model of L-DOPA-induced dyskinesia (PD-LID).
PZ0297 PF-06305591 dihydrate ≥98% (HPLC) PF-06305591 is a potent and highly selective sodium channel Nav1.8 inhibitor.
PZ0319 PF-06409577 ≥98% (HPLC) PF-06409577 is a potent and selective activator of 5′ adenosine monophosphate-activated protein kinase (AMPK).
PF-06409577 potently activates a1β1γ1 AMPK (5′ adenosine monophosphate-activated protein kinase) isoform, and prevents its dephosphorylation. It is similarly potent for β1 containing isoforms, but shows significantly lower potency for β2-containing isoforms of AMPK. Patch-clamp assays show that this compound does not inhibit hERG (human ether-a-go-go gene). It interacts with the allosteric drug and metabolite site (ADaM) of AMPK.
PF-06409577 preserves retinal pigment epithelium cells from UV radiation by activating AMPK (AMP-activated protein kinase) signaling. This orally bioavailable and possesses pharmacokinetic properties. PF-06409577 blocks de novo lipid and cholesterol synthesis pathways that shows a decrease in hepatic lipids and mRNA expression of markers of hepatic fibrosis.
PZ0333 PF-06412154 hydrochloride ≥98% (HPLC) PF-06412154 hydrochloride is a glucagon receptor antagonist.
PZ0357 PF-06412562 ≥98% (HPLC) PF-06412562 is a dopamine receptor D1 (DRD1) agonist ligand.
PZ0334 PF-06422913 ≥98% (HPLC) PF-06422913 is an orally active, potent and selective metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator.
PZ0233 PF-06424439 ≥98% (HPLC) PF-06424439 is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).
PZ0412 PF-06427878 ≥98% (HPLC) New PF-06427878 is an orally active, potent and selective diacylglycerol acyltransferase 2 inhibitor (human/rat DGAT2 IC50 = 99/202 nM; >470-fold selectivity over DGAT1, MGAT1/2/3) that inhibits DGAT2-dependent triglyceride (TG) synthesis in primary human hepatocytes (IC50 = 11.6 nM in the presence of DGAT1 inhibitor PF-04620110). PF-06427878 reduces hepatic and circulating plasma TG levels as well as lipogenic gene expression in rats maintained on a Western-type diet (0.3-30 mg/kg bid. po.). Likewise, PF-06427878 significantly improves steatosis and hepatocellular ballooning with a decrease in lobular inflammation in a murine nonalcoholic steatohepatitis (NASH) model (2 or 20 mg/kg bid. po.).
PZ0221 PF-06439015 methanesulfonate salt ≥98% (HPLC) PF-06439015 is a potent and selective inihibitor that overcomes clinical ALK (receptor tyrosine kinase anaplastic lymphoma kinase) mutations resistant to Crizotinib. PF-06439015 is potent across a broad panel of ALK mutant cell lines with an IC50 of 6.6 nM for tumor growth inhibition in a crizotinib-resistant cell line (H3122-L1196M).
PZ0258   PF-06442609 ≥98% (HPLC) PF-06442609 is a potent γ secretase inhibitor that produces a robust reduction of brain Aβ42 and Aβ40 in in a guinea pig model. Apparently, PF-06442609 is suitable for rodent model of AD.
PZ0374 PF-06446846 hydrochloride ≥98% (HPLC) PF-06446846 is a selective orally active PCSK9 inhibitor that appears to act by causing the ribosome to stall when synthesizing PCSK9. PCSK9 binds to the LDL receptor, preventing it from removing LDL cholesterol from the blood. PF-06446846 was found to reduce plasma PCSK9 and total cholesterol levels in rats.
PZ0386 PF-06456384 trihydrochloride ≥98% (HPLC) PF-06456384 is a highly potent and selective inhibitor against voltage-gated sodium channel NaV1.7 (SCN9A; IC50 = 0.01, <0.1, 75 nM against human, mouse, rat Nav1.7, respectively, by conventional patch clamp; human Nav1.7 IC50 = 0.58 nM by PatchExpress electrophysiology) with >300-fold selectivity over other human NaVs (IC50 = 3 nM/NaV1.2, 5.8 nM/NaV1.6, 75 nM/NaV1.7, 314 nM/NaV1.1, 1.45 μM/NaV1.4, 2.59 μM/NaV1.5, 6.44 μM/NaV1.3, 26 μM/NaV1.8).
PZ0296 PF-06459988 ≥98% (HPLC) PF-06459988 is an orally available irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant (EGFRm) forms including the secondary acquired resistance mutation T790M. PF-06459988 has minimal activity against wild-type EGFR (WT EGFR).
PZ0231 PF-06462894 ≥98% (HPLC) PF-06462894 is a muscarinic metabotropic receptor mGluR5 ligand.
PZ0271 PF-06463922 acetate ≥98% (HPLC) PF-06463922 is a potent, selective brain-penetrable inhibitor of both anaplastic lymphoma kinase (ALK) and c-ros Oncogene 1 (ROS1) with strong activity against all known ALK and ROS1 mutants identified in patients with crizotinib-resistant disease. PF-06463922 is in clinical trials for the treatment of non–small cell lung cancer (NSCLC).
PZ0209   PF-06465469 ≥97% (HPLC) PF-06465469 is a potent, covalent inhibitor of the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase), which is expressed primarily in immune cells, and is strongly upregulated following activation of T-cells. PF-06465469 inhibits Itk enzymatic activity with an IC50 of 2 nM. The compound blocks anti-CD3 induced phosphorylation of PLCg in Jurkat cells (IC50 = 31 nM) and IL-2 production in anti-CD3 stimulated human whole blood (IC50 = 48 nM).
PZ0261 PF-06649283 ≥98% (HPLC) PF-06649283 is a new β-Secretase (BACE) inhibitor.
PZ0327 PF06650833 ≥98% (HPLC) PF06650833 has been studied for its use in the treatment of Waldenstrom macroglobulinemia, indicated by overproduction of IgM (immunoglobulin M)-producing lymphoplasmacytic cells.
PF06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4). IRAK4 kinase is important in innate immunity, involved in initiating signaling from Toll-like receptors and members of th einterleukin-1 receptor family. IRAK4 kinase is an attractive target for the treatment of various diseases associated with deregulated inflammation, such as rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, and systemic lupus erythematosus. PF06650833 has been investigated for treatment of lupus.
PZ0381 PF-06651385 ≥98% (HPLC) PF-06651385 is an Nav1.3 voltage-gated sodium channel modulator.
PZ0289 PF-06651481-00 ≥98% (HPLC) PF-06651481-00 is an isomer of orally available dual Src/Abl kinase inhibitor Bosutinib.
PZ0316 PF-06651600 ≥98% (HPLC) PF-06651600 is a potent and selective JAK3 inhibitor.
PF-06651600 specifically targets the ATP (adenosine triphosphate)-binding domain of JAK3 (Janus kinase 3). Loss of function of JAK3 is associated with severe combined immunodeficiency syndrome.
PZ0290 PF-06663181-00 ≥98% (HPLC) PF-06663181-00 is an isomer of orally available dual Src/Abl kinase inhibitor Bosutinib.
PZ0262 PF-06663195 ≥98% (HPLC) PF-06663195 is a potent inhibitor of β-site amyloid precursor protein (APP) Cleaving Enzyme 1 (BACE1, β-Secretase 1).
PZ0288 PF-06663829-00 ≥98% (HPLC) PF-06663829-00 is an analog of orally available dual Src/Abl kinase inhibitor Bosutinib.
PZ0339 PF-06683324 ≥98% (HPLC) PF-0668324 is pan tropomyosin-related kinase (Trk) inhibitor.
PZ0260 PF06691283 ≥98% (HPLC) PF06691283 is a new β-Secretase (BACE) inhibitor.
PZ0345 PF-06700841 tosylate salt ≥98% (HPLC) PF-06700841 is an inhibitor of JAK1 and TYK2 kinases. PF-06700841 has been investigated for the treatment of psoriasis and lupus.
PF-06700841 prevents IL-23 (interleukin 23) signaling through TYK2 (Tyrosine-protein kinase 2)/JAK1 (Janus kinase 1) inhibition.
PZ0346 PF-06726304 acetate ≥98% (HPLC) PF-06726304 is a selective inhibitor of Histone-lysine N-methyltransferase EZH2 (enhancer of Zeste homolog 2), which catalyzes trimethylation of histone H3 lysine 27 (H3K27) and is amplified and/or overexpressed in several human cancers including breast, prostate and lymphoma. PF-06726304 is a novel structural class of EZH2 inhibitor.
PZ0341 PF-06733804 ≥98% (HPLC) PF-06733804 is pan tropomyosin-related kinase (Trk) inhibitor.
PZ0340 PF-06737007 ≥98% (HPLC) PF-06737007 is pan tropomyosin-related kinase (Trk) inhibitor.
PZ0283 PF-06745013 ≥98% (HPLC) PF-06745013 is a potent and selective inhibitor of MAP4K4.
PZ0391 PF-06745268 ≥98% (HPLC) PF-06745268 is an orally available, brain penetrant, potent and selective γ-secretase modulator. PF-06745268 induces robust and sustained reduction of brain amyloid-β42 (Aβ42) in rats.
PZ0390 PF-06747711 ≥98% (HPLC) PF-06747711 is a potent and selective RORC2 modulator.
PZ0302 PF-06747775 ≥98% (HPLC) PF-06747775 is an orally available, potent and selective inhibitor of the epidermal growth factor receptor) mutant form T790M (EGFR T790M inhibitor). PF-06747775 exhibits minimal activity against wild type EGFR.
PZ0350 PF-06748962 ≥98% (HPLC) PF-06748962 is a potent and selective lactam-based prostaglandin EP3 receptor antagonist.
PZ0282 PF-06758955 hydrochloride ≥98% (HPLC) PF-06758955 is a potent and selective inhibitor of MAP4K4.
PZ0318 PF-06761281 ≥97% (HPLC) PF-06761281 is an inhibitor of the sodium-coupled citrate transporter (NaCT or SLC13A5), which may be a target for tretment and prevention of metabolic disorders. The SLC13 transporters SLC13A2 (NaDC1), SLC13A3 (NaDC3), and SLC13A5 (NaCT) co-transport di- and tricarboxylates with multiple sodium ions into cells. PF-06761281 inhibits citrate uptake with an IC50 of 740 nM for NaCT in human hepatocytes. PF-06761281 has >25-fold in vitro selectivity for NaCT over NaDC1 and NaDC3 and was inactive in a selectivity panel of 65 targets.
PZ0300 PF-06764427 ≥98% (HPLC) PF-06764427 is a selective azaindole muscarinic receptor M1 positive allosteric modulator.
PZ0323 PF-06767832 ≥98% (HPLC) PF-06767832 is a cell permeable, potent and selective M1 muscarinic acetylcholine receptor Positive Allosteric Modulator (PAM). Studies have shown that PF-06767832 potentiates the activity of acetylcholine (Ach) in vitro.
PZ0402 PF-06807656 ≥98% (HPLC) PF-06807656 is a 3-sulfamoylbenzamide-based renal outer medullary potassium channel (ROMK, CCNJ1, Kir1.1) inhibitor (IC50 = 61 nM by whole cell patch clamp) that is insensitive to K80M or N171D pore mutation and exhibits high selectivity for human over rat species (IC50 against thallium sulfate/TlSO4-stimulated influx = 391 nM vs. >30 μM using human or rat ROMK1-expressing HEK293 cells; 82% vs. 0% inhibition by patch clamp using human or rat ROMK2-expressing HEK293 cells).
PZ0406 PF-06815345 ≥98% (HPLC) New PF-06815345 is a liver-targeted, orally available prodrug, which is converted by liver carboxyesterase (CES1) to its zwitterionic active drug (liver active drug = 33.9 μg/mL in mice 0.5 hr post 300 mg/kg p.o. and 9.0 μg/mL in monkeys 0.5 hr post 30 mg/kg p.o.) that selectively inhibits PCSK9 protein synthesis (IC50 = 3.7 μM by in vitro hPCSK9 translation; 4.95/3.81/21/24/>27-fold selective over CDH1/HSD17B11/PCBP2/RPL27/BCAP31). PF-06815345 effectively lowers plasma PCSK9 in humanized PCSK9 mice (by 26/42/53% 5 hrs post 100/300/500 mg/kg p.o.) and is well tolerated in rats and monkeys in vivo. Note: PF-06815345 is not active in non-humanized mice.
PZ0359 PF-06827443 ≥98% (HPLC) PF-06827443 is a otent, low clearance, orally bioavailable, and CNS penetrant muscarinic M1-selectivepositive allosteric modulator (PAM) with minimal agonist activity.
PZ0401 PF-06855800 variable hydrate ≥98% (HPLC) PF-06855800 is a cell penetrant, potent and selective S-adenosylmethionine (SAM) competitive inhibitor of the protein arginine methyltransferase 5 (PRMT5) that exhibits anticancer activity in both in vitro and in vivo models.
PZ0389 PF-06869206 ≥98% (HPLC) PF-06869206 is a selective inhibitor against sodium-phosphate cotransporter 2A (NaPi-2a, NaPi-Iia, Na+/Pi cotransporter 2A, Na+-dependent phosphate cotransporter 2A).
PF-06869206 may be used to treat patients with mineral and hormonal derangements linked with increased cardiovascular risk in chronic kidney disease. This drug might also improve urinary phosphate excretion. PF-06869206 has an ability to decrease phosphate uptake in human embryonic kidney (HEK) cells transfected with mouse or rat renal sodium-dependent phosphate transporter genes (Npt2a).
PZ038   PF-06928215 ≥98% (HPLC) PF-06928215 is a high affinity (KD = 200 nM) active site-targeting, substrate-competitive cyclic GMP-AMP synthase (cGAS) inhibitor (IC50 = 4.9 μM; in the presence of 1 mM ATP, 0.3 mM GTP, 100 nM 45-bp interferon-stimulatory dsDNA (ISD)). PF-06928215 displays no inhibitory potency against dsDNA-induced IFN-β expression in cellular cGAS assays, most likely due to limited cell-permeability and/or high levels of cellular ATP and GTP in the reporter cells employed.
PZ0351 PF-2545920 hydrochloride ≥97% (HPLC) PF-2545920 hydrochloride (MP-10) is a potent and selective cyclic nucleotide phosphodiesterase (PDE) 10A competitive inhibitor with a reported IC50 value of 1.26 nM. PDE10A hydrolyzes both cAMP and cGMP, and is highly expressed in medium spiny neurons of the mammalian striatum and in basal ganglia areas where D1 and D2 dopamine receptors are expressed. PF-2545920 has been studied for treatment of schizophrenia and Huntington′s disease.
PZ0188 PF-3644022 hydrate ≥98% (HPLC) PF-3644022 is a potent inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK2; Ki = 3 nM). PF-3644022 inhibits TNFa and IL-6 production in LPS-stimulated human whole blood (IC50 = 1.6 and 10.3 μM, respectively) and blocks TNFα production and paw swelling in a streptococcal cell wall-induced arthritis in rats.
PZ0263 PF-3774076 ≥98% (HPLC) PF-3774076 is a CNS penetrant, potent, selective, partial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors.
PZ0158 PF 3845 hydrate ≥98% (HPLC) PF 3845 is a potent, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. The endocannabinoid system is a target for therapeutic pain relief. PF-3845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It high selectivity over other enzymes including FAAH-2. In mouse studies, PF-3845 has been shown to raise brain anandamide levels for up to 24 hr; and in a rat model it produced significant reduction of inflammatory pain..
PZ0360 PF-4191834 ≥98% (HPLC) PF-4191834 a selective, non-redox, non-iron chelating competitive inhibitor of 5-lipoxygenase effective in inflammation and pain.
SML0667   PF-429242 dihydrochloride ≥98% (HPLC) PF-429242 is a potent inhibitor of S1P (cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease) that reduces expression levels of hepatic SREBP target genes and lower rates of cholesterol and fatty acid synthesis in mice. PF-429242 is a potent antiviral agent against prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV in cultured cells. PF-429242 efficiently prevented the processing of GPC from the LCMV and LASV. PF-429242 is expected to be active against CCHFV.
PZ0185 PF-431396 hydrate ≥98% (HPLC) PF-431396 is a potent inhibitor of PYK2 and FAK kinases (IC50 = 11 and 1.5 nM, respectively). PF-431396 increases bone formation and protects against bone loss in ovariectomized rats.
PZ0143 PF-4708671 ≥98% (HPLC) PF-4708671 is a selective p70 ribosomal S6 kinase (S6K1) inhibitor. PF-4708671 inhibits S6K1 with a Ki of 20 nM and IC50 of 160 nM, while having no effect on the closely related RSK and MSK kinases.
human ... RPS6KB1(6198)
mouse ... Rps6kb1(72508)
rat ... Rps6kb1(83840)
PZ0186 PF-477736 ≥98% (HPLC) PF-00477736 is a potent, selective ATP-competitive small-molecule inhibitor that inhibits Chk1 with a Ki of 0.49 nM. The compound abrogates cell cycle arrest induced by DNA damage and enhances cytotoxicity of clinically important chemotherapeutic agents, including gemcitabine and carboplatin.
PF-477736 may be effectively used to resensitize platinum resistant ovarian cancer cells. PF-477736 alone or in combination with other chemotherapeutic agents may be used to treat triple-negative breast cancer.
PZ0211   PF-4778574 ≥98% (HPLC) PF-4778574 is a potent AMPA receptor positive allosteric modulator (PAM) that has been shown to enhance cognition in animal models.
PZ0328   PF-4800567 hydrochloride ≥98% (HPLC) PF-4800567 is a casein kinase 1e (CK1e) selective inhibitor (IC50 = 32 nM) that is 20 fold selective for the CK1e isoform over CK1d. PF-4800567 blockes CK1e-mediated PER3 nuclear translocation, but does not effect the circadian clock in animal studies.
PF-4800567 is also known as (3-[(3-Chlorophenoxy)methyl]-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine hydrochloride). It can block the epidermal growth factor receptor (EGFR) at micromolar concentrations. PF-4800567 helps to improve the locomotor stimulant reaction to methamphetamine (MA) and fentanyl.
PZ0246 PF-5006739 ≥98% (HPLC) PF-5006739 is a potent inhibitor of casein kinases 1 delta (CK1δ) and 1 epsilon (CK1ε), key regulators of the suprachiasmatic nucleus (SCN) central clock and also linked to the development of drug addiction through PERIOD proteins (PER1–3) and dopamine- and cAMP-regulated neuronal phosphoprotein (DARPP-32) modulation. PF-5006739 has low nM in vitro potency for CK1δ/ε (IC50 values of 3.9 nM for CK1δ and 17.0 nM for CK1ε) and high kinome selectivity. PF-5006739 induced profound phase delays in circadian periodicity in both nocturnal and diurnal animal models and attenuated opioid drug-seeking behavior in a rodent operant reinstatement model.
SML0389 PF-514273 ≥98% (HPLC) PF-514273 is a highly selective CB1 antagonist. The Ki for binding to CB1 and CB2 receptors is 1 nM and 10 mM, respectively. PF-514273 inhibits food intake and weight gain in rodents.
PZ0217 PF-5274857 hydrochloride ≥98% (HPLC) PF-5274857 is a hedgehog (Hh) signaling pathway inhibitor acting as a potent and selective Smoothened (Smo) antagonist with an IC50 of 5.8 nM and a Ki of 4.6 nM. PF-5274857 completely blocked downstream gene Gli1 transcriptional activity in Gli-Luc mouse embryonic fibroblast (MEF) cells with an IC50 of 2.7 nM. PF-5274857 is brain penetrant. The compound PF-5274857 showed anti-tumor activity in a mouse medulloblastoma model with an in vivo IC50 of 8.9 nM.
PZ0234 PF-543 hydrochloride ≥98% (HPLC) PF-543 hydrochloride is a novel, cell-permeable, potent and selective inhibitor of sphingosine kinase-1 (SphK1). PF-543 inhibits SphK1 with a Ki of 3.6 nM, is sphingosine competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 decreased the level of endogenous S1P by 10-fold with proportional increase of the level of sphingosine.
PF-543 stimulates granular accumulation of microtubule-associated protein light chain 3 (LC3). It also induces LC3-I to LC3-II conversion, inhibited by autophagy inhibitors, wortmannin, 3-methyladenine (3-MA) and bafilomycin A1. In human head and neck squamous cell carcinoma (SCC) cells, PF-543 hydrochloride promotes necrosis,apoptosis and autophagy.
PZ0387 PF-562,271 ≥98% (HPLC) PF-562,271 is a potent, ATP-competitive, reversible and selective inhibitor of FAK and Pyk2. PF-562,271 inhibits FAK phosphorylation in vivo.
PZ0117 PF-573228 ≥95% (HPLC) PF-573228 is a focal adhesion kinase (FAK) inhibitor; Non-receptor tyrosine kinase inhibitor.
PZ0342 PF-6274484 ≥98% (HPLC) PF-6274484 is an irreversible EGFR kinase inhibitor that covalently reacts with active-site cysteine residues in the ATP binding pocket. PF-6274484 inhibits autophosphorylation of both wild type and mutant EGFR in tumor cells with IC50 values of 5.8 nM and 6.6 nM, respectively.
PZ0241 PF-6422899 ≥98% (HPLC) PF-6422899 is an alkynylated derivative of PF-6274484; irreversible inhibitor of EGFR kinase activity. PF-6422899 binds covalently to active-site cysteine residues in the ATP binding pocket of EGFR.
SML0795   PF-670462 ≥98% (HPLC) PF-670462 is a selective inhibitor of the δ- and ε-isoforms of casein kinase I, with IC50 values of 7.7 and 14 nM respectively, and >30 selectivity relative to 42 other kinases tested. Casein kinase Iε phosphorylates PER proteins, which are involved in setting the period of the circadian pacemaker or clock. PF-670462 is potent (IC50 7.7 nM) and effective in vivo (i.e. it induces profound phase delays in circadian periodicity).
PF-670462 is also termed as 4-[1-cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine dihydrochloride). It participates in ceramide transfer between Golgi and ER (endoplasmic reticulum) compartments. PF-670462 affects actin filament consolidation. It also hinders the stability at the front edge of cells treated with N-formyl Met-Leu-Phe.
PZ0306 PF-6808472 ≥98% (HPLC) PF-6808472 is a cell permeable covalent probe suitable for click chemistry designated to measure kinase selectivity in intact cells. PF-6808472 contains sulfonyl fluoride group, which react with conserved lysine residue within kinase ATP binding site.
SML0835   PF74 ≥98% (HPLC) PF74 (PF-3450074) is a HIV-1 inhibitor that targets HIV capsid protein. PF74 binds specifically to HIV-1 particles and triggers premature HIV-1 uncoating in target cells.
SML0715   PF-8380 ≥98% (HPLC) PF-8380 [6-(3-(piperazin-1-yl)propanoyl)benzo[d]oxazol-2(3H)-one] has the ability to change the resistant and invasive features of glioblastoma and helps to improve the response to radiation therapy.
PF-8380 is a potent orally bioavailable inhibitor of autotaxin (ATX), the enzyme that synthesize lysophosphatidic acid (LPA) from lysophosphatidyl choline, and is an emerging target for treatment of inflammatory conditions, including cancer, arthritis and multiple sclerosis. PF-8380 blocks inflammation-induced LPA synthesis. PF-8380 works both in vitro and in vivo through direct inhibition of autotaxin. In human whole blood PF-8380 inhibited autotaxin with an IC50 of 101 nM.
PZ0400 PF-915275 ≥98% (HPLC) PF-915275 is an orally active, potent and selective 11beta-hydroxysteroid dehydrogenase type 1 (11&szlig;-HSD1, HSD11B1) inhibitor (human 11&szlig;-HSD1 Ki &lt;1 nM; cellular IC50 = 5 nM using human 11&szlig;-HSD1-transfected HEK293) with reduced potency toward non-human species (human/monkey/dog hepatocytes EC50 = 20/100/120 nM; mouse 11&szlig;-HSD1 Ki = 750 nM, rat hepatoma EC50 = 14 &mu;M). PF-915275 (0.1-3-mg/kg via nasogastric intubations) inhibits prednisone-to-prednisolone conversion in cynomolgus monkeys (by 87% with 3 mg/kg) in vivo and reduces plasma insulin increase following prednisone & resumed feeding (4 hrs post PF-915275) among overnight fasted monkeys.
PZ0403 PF-9366 ≥98% (HPLC) New PF-9366 is a methionine adenosyltransferase 2A allosteric inhibitor (human Mat2A IC50/Kd = 420 nM/170 nM) whose binding site overlaps with that of the Mat2A regulator, Mat2B. PF-9366 inhibits cellular SAM production in a Mat2B-competitive manner (IC50 post 6-hr treatment = 1.2 μM wihout vs. 0.86 μM with Mat2B knockdown; H520 lung carcinoma cells) without antiproliferation efficacy in cancer cultures due to an induction of Mat2A upregulation upon allosteric inhibition. Similar to Mat2B, PF-9366 allosteric binding alters Mat2A active site, causing increased substrate affinity and decreased enzyme turnover.
PZ0151 PF-956980 hydrate ≥98% (HPLC) PF-956980 is a FGF1 receptor antagonist; PDGF receptor modulator; Flt3 tyrosine kinase modulator; and VEGF antagonist.
SML0587   PF9601N ≥98% (HPLC) PF9601N is a selective and potent monoamine oxidase B inhibitor that exhibit anti-Parkinsonian effects in several models of PD.
PZ0131 PF-998425 ≥98% (HPLC) PF-998425 is a novel, nonsteroidal androgen receptor antagonist.
PZ0325   PF-CBP1 ≥98% (HPLC) CBP is a transcriptional coactivator. The protein is a link between the DNA-associated transcription factors and the RNA polymerase 2 complex. It also exhibits histone acetyltransferase activity.
PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons. Also, PF-CBP1 significantly reduces levels of RGS4 mRNA levels in neurons.
SML2679 PFF-1 ≥97% (HPLC) PFF-1 is a robust, cell penetrant and long time-laps (>30 min) fluorophore suitable for single-molecule localization microscopy experiments (SMLM). PFF-1 exhibits minimal phototoxicity and no apparent photobleaching. It was used to visualize movement of vesicles within cultured neurons.
SML0352 PFI-1 ≥98% (HPLC) PFI-1 is a quinazolinone inhibits androgen receptor (AR) mediated signaling in prostate cancer cells. It elicits minimum toxicity and is effective for anti-HIV-latency therapy. In leukemia cells, PFI-1 inhibits Aurora B kinase and promotes caspase-dependent apoptosis.
The human BET family, which includes BRD2, BRD3, BRD4 and BRDT, play a role in regulation of gene transcription. PFI-1 is a selective BET bromodomain inhibitor with activity at BRD2 (IC50 = 98 nM) and BRD4 (IC50 = 220 nM). For full characterization details, please visit the PFI-1 probe summary on the Structural Genomics Consortium (SGC) website.

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

(S)-PFI-2, an enantiomer of (R)-PFI-2, is used as a negative control. (S)-PFI-2 is available from Sigma. To learn more about and purchase (S)-PFI-2, click here.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
PZ0312 (S)-PFI-2 (S)-PFI-2 is the negative control probe for (R)-PFI-2 hydrochloride, which is a histone-lysine N-methyltransferase (HKMT) inhibitor selective for SETD7 (SET9). (R)-PFI-2 has 1000-fold selectivity for SETD7 (SET9) over other methyltransferases and other non-epigenetic targets and an IC50 value of 2 nM. (S)-PFI-2 is 500-fold less active.

For characterization details of (R)-PFI-2 and (S)-PFI-2, please visit the PFI-2 probe summary on the Structural Genomics Consortium (SGC) website.

(R)-PFI-2, the active SETD7 probe, is available from Sigma. To learn more about and purchase (R)-PFI-2, click here.

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

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

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
SML1009   PFK15 ≥98% (HPLC) PFK15 is also referred as 1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one. It prevents autophagy and multiplication in rhabdomyosarcoma cells. PFK15 results in cell death in gastric cancer cells via mitochondrial pathway. It also blocks MKN45 (human gastric cancer cell lines) tumor growth in vivo. PFK15 promotes cell cycle arrest and changes the upregulation of key cell cycle proteins.
PFK15 is potent and selective antagonist of PFKB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3) that causes a rapid induction of apoptosis in cancer and transformed cells. PFK15 inhibits the growth of LLC xenografts.
SML1839 PFM39 ≥98% (HPLC) PFM39 is a potent cell-permeable Mirin analog that selectively inhibits MRE11 exo-, but not endo-, nuclease activity. PFM39 targets MRE11 in a fashion similar to Mirin, but distinct from that of PFM01 to allow a blockage of dsDNA phosphate backbone rotation and selective inhibition against MRE11 exo-, but not endo-, nuclease activity. FM39 potently impairs G2-phase double-strand break (DSB) repair in 1BR3-hTERT fibrolasts following ionizing irradiation (IR).
P3998 PGL-135 hydrochloride monohydrate ≥98% (HPLC), solid Cell-permeable polyglutamine aggregation inhibitor