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.
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 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).
A potent agonist of human STING and also weakly activates mouse STING. Suppresses the metastasis of human renal carcinoma cells.
Inhibits gene transcription driven by STAT3. Inhibits cancer cell stemness gene expression and blocks spherogenesis of stemness-high cancer cells isolated from a variety of cancer types.
Selectively inhibits the growth of cancer cells over normal cells. Induces non-apoptotic cell death in glioblastoma cells, and is active in vivo.
Plant growth inhibitor discovered using a resistance-gene-directed approach.