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New Products
We continue to add new products to our already extensive portfolio so check back often for the latest breakthroughs. If you can’t find what you need, contact us for information on custom synthesis.
Catalog# Product
10-4635
PF-9366 | Methionine adenosyltransferase 2A inhibitor
Allosteric inhibitor of methionine adenosyltransferase 2A (Mat2A), the primary enzyme responsible for extrahepatic synthesis of S-adenosyl-L-methionine (SAM).
11/5/19
10-3768
Eltrombopag | Small molecule thrombopoietin agonist
Novel, orally active, small molecule human thrombopoietin receptor (TPO-R) agonist, EC50=0.27 μM. Maintains human hematopoietic stem and progenitor cells under inflammatory conditions.
11/5/19
10-4103
N6022 | S-Nitrosoglutathione reductase inhibitor
Potent and reversible inhibitor of GSNOR with significant efficacy in mouse models of ovalbumin-induced asthma, chronic obstructive pulmonary disease and irritable bowel syndrome.
11/1/19
10-4011
Selinexor | Inhibitor of the nuclear export receptor CRM1/XPO1
Exhibited potent growth suppression in various T-cell acute lymphoblastic leukemia (T-ALL) cells (IC50’s = 34-203 nM)1 and pancreatic cancer cells (IC50 ~ 150 nM)2.
11/1/19
10-3904
ZJ43 | Potent inhibitor of glutamate carboxypeptidases II and III
Potently (IC50 = 2.4 nM) inhibits the ability of glutamate carboxypeptidase II to hydrolyze the neurotransmitter N-acetylaspartylglutamate (NAAG) resulting in an increase in synaptic levels of group II mGluRs.
11/1/19
10-3903
SI-2 | Potent inhibitor of steroid receptor coactivator-3 (SRC-3)
Blocks MDA-MB-468 cell growth with an IC50 = 3.4 nM without effecting normal cells. Significantly inhibited breast cancer cell growth in an orthotopic MDA-MD-468 mouse model.
11/1/19
10-4219
SA4503 | Potent and selective sigma 1 agonist
Potent and selective sigma 1 agonist (sigma 1 IC50 = 17.4 nM, sigma 2 IC50 = 1784 nM).
11/1/19
10-4840
NH125 | Eukaryotic elongation factor 2 (eEF-2) kinase inhibitor
NH125 has also been shown to engage the EIF2a-ATF4-CHOP axis resulting in induction of DR5 expression
11/1/19
10-4493
CYM-5541 | Allosteric sphingosine-1-phosphate receptor 3 agonist
Potent and selective allosteric agonist of the sphingosine-1-phosphate receptor 3 (S1P3; EC50’s = 72.3-132 nM).
11/1/19
10-3902
Lipofermata | Fatty acid transport protein 2 (FATP2) inhibitor
Inhibitor of fatty acid transport protein 2 (FATP2) that does not inhibit glucose transport or the activity of long chain acyl-CoA synthase. Inhibition is specific for long and very long chain fatty acids.
11/1/19
10-4028
GSK3326595 | Selective PRMT5 inhibitor
Potent, selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5
11/1/19
10-3730
Fasentin | Glucose uptake inhibitor
Novel inhibitor of glucose uptake which acts via inhibition if glucose transporter GluT1 and GluT4.
10/11/19
10-3780
Loxoribine | TLR7 agonist
Potent immunostimulant with a relatively broad spectrum of immunobiological activities including upregulation of the activity of B cells, T cells, NK cells, macrophages and LAK cells
10/11/19
10-3613
Santacruzamate A | Uktrapotent HDAC2 inhibitor
Highly potent and selective inhibitor of HDAC2, IC50=0.119 and 434 nM for HDAC2 and HDAC6 respectively.
10/11/19
10-4810
NU7441 | DNA-PK inhibitor
Potent and selective ATP-competitive inhibitor of DNA-dependent protein kinase. Increases radio/chemosensitivity of various cancer cell lines.
9/2/19
10-4782
Crenolanib | PDGFR and FLT3 inhibitor
Potent inhibitor of PDGFR and FLT3 that binds only to the active kinase configuration
9/2/19
10-4778
AZ3146 | Mps1 kinase inhibitor
Potent and selective inhibitor of monopolar spindle 1 that decreases hepatocellular carcinoma growth in vitro.
9/2/19
10-4771
AZD7762 | Checkpoint Kinase 1/2 inhibitor
Potent and selective inhibitor of checkpoint kinases 1 and 2. It abrogates DNA damage-induced S and G2 checkpoints and enhances the efficacy of DNA damaging agents such as gemcitabine and irinotecan
8/30/19
10-4779
SNS-314 mesylate | Aurora kinase inhibitor
Potent and selective Aurora kinase inhibitor. Able to inhibit proliferation in a wide panel of human cancer cell lines.div>
8/30/19
10-3901
Elafibranor | PPARalpha/delta agonist
Able to decrease plasma triglycerides levels, increase HDL cholesterol levels in human studies, and improve hepatic and peripheral insulin sensitivity.
8/30/19
10-2040
Levetiracetam | Anticonvulsant
Clinically useful non classical anticonvulsant believed to act through binding to SV2A. No effect on voltage-dependent Na+ channels, GABAergic transmission, or affinity for either GABAergic or glutaminergic receptor.
8/29/19
10-3900
Tigecycline | Antibiotic
Clinically useful antibiotic that has also been shown to be selectively toxic to human acute myeloid leukemia cells over normal hematopoietic cells.
8/25/19
10-4818
Volasertib | Potent and selective inhibitor of Polo-like kinase 1
Potent and selective inhibitor of Polo-like kinase 1 that has shown efficacy in multiple solid xenograft tumor models and in clinical studies of patients with acute myeloid leukemia.
8/25/19
10-4784
Fruquintinib | Potent and selective inhibitor of VEGFR kinase
Potently and selectively inhibits VEGF/VEGFR signaling and cell proliferation in HUVECs and HLECs and prevents angiogenesis in vitro.
8/25/19
10-4675
AZ20 | ATR kinase inhibitor
Combination therapy with AZ20 and gemcitabine resulted in synergistic inhibition of tumor cell growth and cell death initiation in pancreatic cancer cell lines.
8/25/19
10-4804
AZD1152-HQPA | Aurora B kinase inhibitor
Highly selective inhibitor of Aurora kinase B that inhibits the growth of tumors in multiple cancer models
8/17/19
10-4017
Lomeguatrib | MGMT inhibitor
Potent inhibitor of O6-Methylguanine-DNA Methyltransferase (MGMT), an important DNA repair protein.
8/17/19
10-4531
Methoprene Acid | Selective RXR agonist
Binds directly and selectively to the retinoid X receptor (RXR) acting as a transcriptional activator with no activity at RAR. Negatively regulates thrombosis and hemostasis.
7/22/19
10-3648
ML-335 | Trek-1,2 activator
Novel, selective TREK-1,2 activator with EC50s of 14.3 and 5.2 μM
7/21/19
10-3756
NOTUMib-1 | NOTUM inhibitor, restores Wnt signaling
Inhibits the carboxylesterase activity of NOTUM, IC50=0.085 μM, and restores Wnt signaling.
7/21/19
10-1525
MitoBloCK-12 | Mitochondrial import inhibitor
Blocks translocation of a mutant form of alanine: glyoxylate aminotransferase (AGT) to the mitochondria and restores AGT trafficking to peroxisomes.
7/21/19
10-3631
N-Eicosanoyl serotonin | Neuroprotective
Inhibits the PP2A methylesterase maintaining PP2A in a highly active state leading to hyperphosphorylated α-synuclein.
5/12/19
10-3712
DO264 | ABHD12 inhibitor
Potent, reversible competitive inhibitor of ABHD12 (α/β-hydrolase domain-containing 12) which shows negligible interaction with other serine hydrolases.
5/12/19
10-3321
Rucaparib phosphate | PARP1 inhibitor
Potent PARP1 inhibitor. Cytotoxic to human cancer cells or xenograft tumors with mutated or epigenetically silenced BRCA1/2.
4/10/19
10-2768
Pomalidomide | Cereblon ubiquitination inhibitor
Inhibits the E3 ubiquitin ligase cereblon (CRBN). Displays antiangiogenic and immunomodulatory activity in vivo potently inhibiting the production of TNF alpha and IL-2.
4/101/19
10-4230
Imiquimod | TLR7 agonist
Toll-like receptor 7/8 agonist with anti-viral and anti-tumor properties. Enhances innate immune system leading to Th1-mediated antitumor immune response.
3/29/19
10-2671
Norfluoxetine HCl | Fluoxetine Metabolite
Induces long QT syndrome via slow delayed rectifier potassium current block. Time dependent inhibitor of CYP2C19 and CYP3A4.
3/29/19
10-4806
Acalabrutinib | Highly selective BTK inhibitor
hHghly selective, potent (IC50 = 3nM), and irreversible inhibitor of Bruton’s tyrosine kinase (BTK). Significantly inhibits BCR signaling, inhibits tumor proliferation, and reduces tumor burden.
3/29/19
10-4757
Ibrutinib | BTK inhibitor
Very potent (IC50 = 0.5nM) irreversible inhibitor of Bruton tyrosine kinase (BTK) that blocks activation of the B-cell antigen receptor (BCR).
3/29/19
10-4008
SR0987 | RORγt agonist
RORγt agonist that drives proliferation of Th17 cells and decrease levels of the immune checkpoint protein PD-1.
3/29/19
10-4035
CPI-455 | Lysine demethylase KDM5 inhibitor
Potent (IC50 = 10 nM) and selective inhibitor of the lysine demethylase KDM5. Reduced the number of drug-tolerant persister cancer cells (DTPs) in a dose-dependent, KDM5-dependent manner in multiple cell lines treated with standard chemotherapy or targeted agents.
3/29/19
10-4920
Motolimod | TLR8 agonist
A selective Toll-like receptor 8 (TLR8) agonist (EC50 = 100 nM). Stimulates the production of TNFα and IL-12 from monocytes and myeloid dendritic cells.
3/29/19
10-4261
PF-4136309 | CCR2 antagonist
Potent and selective inhibitor of CCR2 (hIC50 = 5.2 nM, mIC50 = 13 nM, rIC50 = 17 nM). Significantly decreased inflammatory monocytes in a mouse model of pancreatic cancer.
3/29/19
10-1639
2’,3’-cGAMP | Endogenous STING agonist
Endogenous STING (stimulator of interferon genes) agonist. Induces autophagy which is a mechanism for clearance of DNA and viruses in the cytosol.
3/29/19
10-4101
CPI-444 | Adenosine A2A receptor antagonist
Potent (Ki = 3.54 nM) and selective adenosine A2A receptor antagonist. CPI-444 monotherapy or in combination with anti-PD-1, anti-PD-L1, and anti-CTLA-4 induced T-cell-mediated tumor responses, inhibited tumor growth, and enabled antitumor immune memory.
3/29/19
10-4006
Grapiprant | EP4 Receptor antagonist
Potent and selective prostaglandin EP4 receptor antagonist. Produces antihyperalgesic effects in animal models of pain, and has significant anti-inflammatory effects in a rat model of adjuvant-induced arthritis.
3/29/19
10-4564
NLG919 | IDO pathway inhibitor
Potent IDO pathway inhibitor (Ki = 7nM). Synergizes with chemo-radiation therapy to promote T cell dependent complement deposition in a murine model of glioblastoma.
3/29/19
10-4789
Binimetinib | MEK1/2 inhibitor
Potent (IC50 = 12 nM) and selective allosteric inhibitor of MEK1/2.
3/29/19
10-4831
WP1066 | JAK2/STAT3 inhibitor
Inhibitor of the JAK2/STAT3 pathway as well as STAT5 and AKT. Enhances T-cell cytotoxicity via inhibition of regulatory T-cells.
3/29/19
10-4901
PD-1/PD-L1 Inhibitor 1 | PD-1/PD-L1 inhibitor
Inhibits (IC50 = <100nM) the formation of the PD-1/PD-L1 complex via binding to PD-L1 and inducing dimerization.
3/29/19
10-4900
BMS-202 | PD-1/PD-L1 inhibitor
Inhibits formation of the PD-1/PD-L1 complex via binding to PD-L1 and inducing dimerization.
3/29/19
10-4498
PF-06840003 | IDO1 inhibitor
Potent and selective inhibitor of Indoleamine-2,3-dioxygenase (IDO1).
3/29/19
10-4499
Epacadostat | IDO1 inhibitor
Potent (IC50 = 10nM) and selective inhibitor of Indoleamine-2,3-dioxygenase 1 (IDO1) with no activity at IDO2 or TDO.
3/29/19
10-4788
Duvelisib | PI3Kdelta/gamma inhibitor
Potent and selective dual PI3Kδ/γ inhibitor. It inhibits B and T cell proliferation, blocks neutrophil migration, and inhibits basophil activation.
3/29/19
10-4676
R428 | Potent and selective AXL inhibitor
Potent and selective inhibitor of AXL kinase (IC50 = 1.4nM). R428 has been shown to overcome chemotherapy resistance to various agents in multiple cancer models.
3/29/19
10-4828
Defactinib | Potent FAK inhibitor
Potent inhibitor of FAK and Pyk2 that is active in vivo (EC50 = 26nM). FAK inhibition prevents tumor invasion and dissemination rather than tumor size reduction.
3/29/19
10-4829
Pexidartinib | CSF1R inhibitor
Potent and selective dual inhibitor of CSF1R (IC50 = 20nM) and c-KIT (IC50 = 10nM).
3/29/19
10-4033
(R)-PFI-2 HCl | Methyltransferase SETD7 inhibitor
Potent and selective SAM-dependent inhibitor of the lysine methyltransferase SETD7. Alters Hippo pathway signaling in MCF7 cells by altering YAP nuclear localization in a SETD7-dependent manner.
3/29/19
10-4018
A-196 | SUV420H1/H2 methyltransferase inhibitor
Potent and selective inhibitor of the protein lysine methyltransferases SUV420H1 and SUV420H2. Substantially inhibited non-homologous end-joining (NHEJ)-directed DNA repair but not homology-directed repair(HDR) in cells treated with ionizing radiation. div>
3/3/19
10-2181
VX-702 | P38alpha MAP kinase inhibitor
Potent and selective inhibitor of p38 MAP kinases, p38α MAPK and p38β (KD = 3.7 and 17 nM respectively)
3/1/19
10-2728
Fluoxetine HCl | Serotonin reuptake inhibitor
Selective serotonin reuptake inhibitor (SSRI) with high selectivity for the serotonin transporter over the norepinephrine and dopamine transporters.
2/15/19
10-2027
Ezetimibe | Cholesterol absorption inhibitor
Inhibits cholesterol absorption in the intestine by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter.
2/15/19
10-2315
Rasagiline mesylate | MAO-B inhibitor, neuroprotective
Potent, irreversible monoamine oxidase (MAO) inhibitor selective for MAO-B (IC50=4.43 nM) over MAO-A (IC50=412 nM).
2/15/19
10-1414
BMS-303141 | ATP citrate lyase (ACL) inhibitor
A novel tool compound for exploring the potential of ACL inhibition as a target for metabolic disorders such as obesity and dyslipidemia.
2/13/19
10-4791
BI-D1870 | p90 Ribosomal S6 kinase inhibitor.
Inhibitor of p90 ribosomal S6 kinase (RSK) with selectivity over other AGC kinases. Protected mice from experimental autoimmune encephalomyelitis suggesting a new strategy to treat multiple sclerosis
2/3/19
10-4175
PRIMA-1(MET) | Reactivates mutant p53
Reactivates mutant p53, an important tumor suppressor gene, in cancer cells. Induces p53-dependent mitochondrial apoptosis via activation of caspase-2.
1/15/19
10-4110
Galunisertib | Potent TGFB receptor 1
TGF-β kinase (ALK5) antagonist. Stimulated hematopoiesis from primary myelodysplastic syndrome bone marrow specimens via downregulation of SMAD2 phosphorylation.
1/15/19
10-4029
RGFP966 | Selective HDAC3 inhibitor
Selective inhibitor of HDAC3. Facilitates the extinction of cocaine-seeking behavior in mice and transforms subthreshold learning events into robust long-term memory, suggesting a potential therapeutic target for memory enhancement and neurodegenerative diseases.
1/15/19
10-3161
Bakuchiol | Antioxidant
Inhibits oxidative stress-induced decrease in mitochondrial membrane potential and associated release of pro-apoptotic factors. Displays neuroprotective and anti-antiinflammatory effects.
1/8/19
10-4105
Divin | Divisome assembly inhibitor
Divin is an iron, cobalt, and copper chelator that arrests the late stages of cytokinesis in bacteria by blocking the physical process of constriction in dividing cells without affecting FtsZ
1/8/19
10-4813
Quizartinib | Selective FLT3 Inhibitor
Potent and selective inhibitor of FLT3 (Kd = 1.6nM, IC50 = 0.56 nM MV4-11 cells). It is in clinical trials for treatment of Acute Myelogenous Leukemia (AML).
1/5/19
10-4826
Sitravatinib | Multikinase inhibitor / Immuno-oncology agent
Broad spectrum receptor tyrosine kinase inhibitor. Its targets include Axl, c-Met, PDGFR, VEGFR, Ephrin receptor family, and FLT3 among others at nanomolar levels..
1/5/19
10-4827
IPI-549 | Selective PI3Kγ inhibitor / Immuno-oncology agent
Potent and highly selective inhibitor of PI3K-γ in both biochemical (IC50 = 16 nM) and cellular (IC50 = 12.2 nM) assays. Macrophage PI3K-γ has been found to be a critical switch between immune stimulation and suppression.
1/5/19
10-4201
S1RA | Selective sigma-1 antagonist
Potent and selective σ1 antagonist with weak binding at σ2 (IC50 σ1 = 17nM, σ2 = 9300nM).
1/5/19
10-4202
Siramesine | Selective sigma-2 antagonist
σ2 selective agonist (IC50’s: σ1 = 17nM, σ2 = 0.2nM). Produced non-sedating potent and long-last anxiolytic effects in rodents. Siramesine induced caspase-independent programmed cell death in various cancer cell lines via increased levels of ROS and lysosomal leakage.
1/5/19
10-4203
PRE084 | Selective sigma-1 agonist
Agonist of the σ receptor with selectivity for the σ1 subtype (IC50’s: σ1 = 2.2nM, σ2 = 13091nM). PRE-084 has demonstrated neuroprotective/restorative effects in brain injury and neurodegenerative conditions.
1/5/19
10-4020
GSK2879552 | Potent and selective LSD1 inhibitor
Potent, selective, and irreversible inhibitor of Lysine Demethylase 1 (LSD1) via covalent modification of the LSD1 cofactor FAD (Ki = 1.7 µM). It is selective for LSD1 over the closely related LSD2, MAO-A, MAO-B, and the FAD dependent enzymes D-amino acid oxidase and glutathione reductase.
1/5/19
10-4030
Bromosporine | Pan-bromodomain inhibitor
Potent pan-Bromodomain (BRD) inhibitor. Bromosporine was able to reactivate HIV-1 replication in different latency models.
1/5/19
10-4031
EPZ015666 | Potent and selective PRMT5 inhibitor
Selective and potent (IC50 = 22nM) inhibitor of arginine methyltransferase 5 (PRMT5). PRMT5 inhibition with EPZ015666 potently suppressed in vivo glioblastoma tumors and significantly inhibited the growth of multiple myeloma cell lines
1/5/19
10-4200
NE-100 | Selective sigma-1 antagonist
Potent inhibitor of the sigma receptor (σ) with selectivity for sigma-1 (IC50 = 1.5 nM) over sigma-2 (IC50 = 85 nM).
1/5/19
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