New Products

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.