Able to decrease plasma triglycerides levels, increase HDL cholesterol levels in human studies, and improve hepatic and peripheral insulin sensitivity.
Inhibits the PP2A methylesterase maintaining PP2A in a highly active state leading to hyperphosphorylated α-synuclein.
Potent, reversible competitive inhibitor of ABHD12 (α/β-hydrolase domain-containing 12) which shows negligible interaction with other serine hydrolases.
Potent PARP1 inhibitor. Cytotoxic to human cancer cells or xenograft tumors with mutated or epigenetically silenced BRCA1/2.
Inhibits the E3 ubiquitin ligase cereblon (CRBN). Displays antiangiogenic and immunomodulatory activity in vivo potently inhibiting the production of TNF alpha and IL-2.
Toll-like receptor 7/8 agonist with anti-viral and anti-tumor properties. Enhances innate immune system leading to Th1-mediated antitumor immune response.
Induces long QT syndrome via slow delayed rectifier potassium current block. Time dependent inhibitor of CYP2C19 and CYP3A4.
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.
Very potent (IC50 = 0.5nM) irreversible inhibitor of Bruton tyrosine kinase (BTK) that blocks activation of the B-cell antigen receptor (BCR).
RORγt agonist that drives proliferation of Th17 cells and decrease levels of the immune checkpoint protein PD-1.
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.
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.
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.
Endogenous STING (stimulator of interferon genes) agonist. Induces autophagy which is a mechanism for clearance of DNA and viruses in the cytosol.
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.
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.
Potent IDO pathway inhibitor (Ki = 7nM). Synergizes with chemo-radiation therapy to promote T cell dependent complement deposition in a murine model of glioblastoma.
Potent (IC50 = 12 nM) and selective allosteric inhibitor of MEK1/2.
Inhibitor of the JAK2/STAT3 pathway as well as STAT5 and AKT. Enhances T-cell cytotoxicity via inhibition of regulatory T-cells.
Inhibits (IC50 = <100nM) the formation of the PD-1/PD-L1 complex via binding to PD-L1 and inducing dimerization.
Inhibits formation of the PD-1/PD-L1 complex via binding to PD-L1 and inducing dimerization.
Potent and selective inhibitor of Indoleamine-2,3-dioxygenase (IDO1).
Potent (IC50 = 10nM) and selective inhibitor of Indoleamine-2,3-dioxygenase 1 (IDO1) with no activity at IDO2 or TDO.
Potent and selective dual PI3Kδ/γ inhibitor. It inhibits B and T cell proliferation, blocks neutrophil migration, and inhibits basophil activation.
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.
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.
Potent and selective dual inhibitor of CSF1R (IC50 = 20nM) and c-KIT (IC50 = 10nM).
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.
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>
Potent and selective inhibitor of p38 MAP kinases, p38α MAPK and p38β (KD = 3.7 and 17 nM respectively)
Selective serotonin reuptake inhibitor (SSRI) with high selectivity for the serotonin transporter over the norepinephrine and dopamine transporters.
Inhibits cholesterol absorption in the intestine by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter.
Potent, irreversible monoamine oxidase (MAO) inhibitor selective for MAO-B (IC50=4.43 nM) over MAO-A (IC50=412 nM).
A novel tool compound for exploring the potential of ACL inhibition as a target for metabolic disorders such as obesity and dyslipidemia.
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
Reactivates mutant p53, an important tumor suppressor gene, in cancer cells. Induces p53-dependent mitochondrial apoptosis via activation of caspase-2.
TGF-β kinase (ALK5) antagonist. Stimulated hematopoiesis from primary myelodysplastic syndrome bone marrow specimens via downregulation of SMAD2 phosphorylation.
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.
Inhibits oxidative stress-induced decrease in mitochondrial membrane potential and associated release of pro-apoptotic factors. Displays neuroprotective and anti-antiinflammatory effects.
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
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).
Broad spectrum receptor tyrosine kinase inhibitor. Its targets include Axl, c-Met, PDGFR, VEGFR, Ephrin receptor family, and FLT3 among others at nanomolar levels..
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.
Potent and selective σ1 antagonist with weak binding at σ2 (IC50 σ1 = 17nM, σ2 = 9300nM).
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.
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.
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.
Potent pan-Bromodomain (BRD) inhibitor. Bromosporine was able to reactivate HIV-1 replication in different latency models.
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
Potent inhibitor of the sigma receptor (σ) with selectivity for sigma-1 (IC50 = 1.5 nM) over sigma-2 (IC50 = 85 nM).