Potent and specific inhibitor of T cell antigen receptor (TCR)-dependent T cell activation.
Potent inhibitor of tropomyosin receptor kinases A,B and C. Greater than 100-fold selective against a panel of 229 kinases. Attenuated bone cancer pain and blocked the formation neuroma-like structures and sprouting of sensory nerve fibers
Selective and potent inhibitor of RIP2 kinase. Also inhibits isolated RIP3 kinase but is inactive against RIP3 in cellular assays.
Potent and selective inhibitor of the excitatory amino acid transporter 1. Significantly increased survival in glioma-bearing mice.
Inhibitor of the RNA helicase DDX3. Inhibition of DDX3 lead to activation of cell death pathways, inhibition of Wnt pathway signaling, and abrogation of non-homologous end-joining DNA repair.
Causes G1 cell cycle arrest in colo-205 colorectal cells, MDA-MB-361 breast cancer cells and MV4-11 AML cells.
Indirectly inhibits the NFkB pathway via inhibition of store operated calcium entry. Displays neuroprotective effects in transgenic fly and mouse models of Huntington’s disease.
Potent and selective allosteric inhibitor of the EED subunit of the methyltransferase polycomb repressive complex.
Potent and selective inhibitor of fatty-acid-binding protein aP2. Demonstrated reductions in atherosclerotic lesions, improved glucose metabolism, reduced inflammation and increased insulin sensitivity in mouse models.
Allosteric inhibitor of methionine adenosyltransferase 2A (Mat2A), the primary enzyme responsible for extrahepatic synthesis of S-adenosyl-L-methionine (SAM).
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.
Potent and reversible inhibitor of GSNOR with significant efficacy in mouse models of ovalbumin-induced asthma, chronic obstructive pulmonary disease and irritable bowel syndrome.
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.
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.
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.
Potent and selective sigma 1 agonist (sigma 1 IC50 = 17.4 nM, sigma 2 IC50 = 1784 nM).
NH125 has also been shown to engage the EIF2a-ATF4-CHOP axis resulting in induction of DR5 expression
Potent and selective allosteric agonist of the sphingosine-1-phosphate receptor 3 (S1P3; EC50’s = 72.3-132 nM).
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.
Potent, selective (>4000-fold over 20 other methyltransferases), SAM uncompetitive, peptide competitive inhibitor of PRMT5
Novel inhibitor of glucose uptake which acts via inhibition if glucose transporter GluT1 and GluT4.
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
Highly potent and selective inhibitor of HDAC2, IC50=0.119 and 434 nM for HDAC2 and HDAC6 respectively.
Potent and selective ATP-competitive inhibitor of DNA-dependent protein kinase. Increases radio/chemosensitivity of various cancer cell lines.
Potent inhibitor of PDGFR and FLT3 that binds only to the active kinase configuration
Potent and selective inhibitor of monopolar spindle 1 that decreases hepatocellular carcinoma growth in vitro.
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
Potent and selective Aurora kinase inhibitor. Able to inhibit proliferation in a wide panel of human cancer cell lines.div>
Able to decrease plasma triglycerides levels, increase HDL cholesterol levels in human studies, and improve hepatic and peripheral insulin sensitivity.
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.
Clinically useful antibiotic that has also been shown to be selectively toxic to human acute myeloid leukemia cells over normal hematopoietic cells.
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.
Potently and selectively inhibits VEGF/VEGFR signaling and cell proliferation in HUVECs and HLECs and prevents angiogenesis in vitro.
Combination therapy with AZ20 and gemcitabine resulted in synergistic inhibition of tumor cell growth and cell death initiation in pancreatic cancer cell lines.
Highly selective inhibitor of Aurora kinase B that inhibits the growth of tumors in multiple cancer models
Potent inhibitor of O6-Methylguanine-DNA Methyltransferase (MGMT), an important DNA repair protein.
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.
Novel, selective TREK-1,2 activator with EC50s of 14.3 and 5.2 μM
Inhibits the carboxylesterase activity of NOTUM, IC50=0.085 μM, and restores Wnt signaling.
Blocks translocation of a mutant form of alanine: glyoxylate aminotransferase (AGT) to the mitochondria and restores AGT trafficking to peroxisomes.
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.