tumor-associated macrophages (tams)

Antitumor agent-19 is a modulator of tumor-associated macrophages with EC50s of 17.18 μM and 18.87 μM in the RAW 264.7 cells and the BMDM cells.

Conophyllidine is a bisindole alkaloid and functions as a selective inhibitor of M2 polarization. It inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. The IC50 of Conophyllidine for IL-4-induced arginase inhibition is 0.31 μM. This compound effectively induces tumor-associated macrophages (TAMs) to shift from an anti-inflammatory to an inflammatory state, thereby enhancing the recruitment and function of cytotoxic CD8+ T cells in the tumor microenvironment. Conophyllidine is useful for studying tumor-associated macrophages.

Emactuzumab(RG 7155) is a monoclonal antibody against colony-stimulating factor-1 receptor targeting tumor-associated macrophages (TAMs) Emactuzumab has antitumor activity and inhibits activation of colony-stimulating factor 1 receptor (CSF1R) Emactuzumab has a high affinity for CSF-1R with a Ki value of 0.2 nM. Emactuzumab blocks CSF-1R dimerization and can be used to study cancers such as diffuse tenosynovial giant cell tumor (dt-GCT).

CSF1R-IN-22 (Compound C19), a potent orally administered CSF-1R selective inhibitor (IC50 <6 nM), significantly enhances CXCL9 secretion from M2 macrophages and promotes CD8+ T cell infiltration. Moreover, it amplifies the anti-tumor immune responses in conjunction with anti-PD-1 and triggers apoptosis in tumor cells. Additionally, CSF1R-IN-22 effectively reprograms M2-like TAMs (tumor-associated macrophages) to an M1 phenotype, modulates the tumor microenvironment (TME) by fostering the recruitment of CD8+ T cells, and diminishes the presence of immunosuppressive Tregs and MDSCs [1].

M2 Peptide is a targeting peptide specific to M2-like tumor-associated macrophages (TAMs). It serves as a carrier for drugs or small interfering RNA (siRNA) to facilitate the repolarization of M2-like macrophages to M1-like macrophages. This shift alters the immunosuppressive state within the tumor microenvironment, enhancing the antitumor immune response. M2 Peptide is used in research to study its effects on macrophage polarization and the implications of this polarization on tumor growth and metastasis.