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CTLA-4

CTLA-4 antibodies and inhibitors target cytotoxic T-lymphocyte-associated protein 4 (CTLA-4). CTLA-4 is an inhibitory T-cell receptor, a homolog of the costimulatory receptor cluster of differentiation 28 (CD28) that binds the same ligands, B7-1 (CD80) and B7-2 (CD86), on antigen-presenting cells. It binds them with higher affinity than CD28 and so limits costimulation and T-cell activation. Mice lacking CTLA-4 develop massive lymphoproliferation and fatal multiorgan tissue destruction. Most products here are antibodies, such as the anti-CTLA-4 antibodies quavonlimab and gotistobart. Vudalimab is a bispecific antibody against CTLA-4 and programmed cell death protein 1 (PD-1). Davoceticept is listed as a dual inhibitor of CTLA-4 and programmed death-ligand 1 (PD-L1), and AN02 as a CTLA-4 degrader.

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  • AN02
    Cat. No.
    A37044
    CAS No.
    1246964-08-8

    AN02

    AN02 is a CTLA-4 degrader that demonstrates potent anti-cancer activity in ovarian cancer research. This compound inhibits cell proliferation, clonogenicity, migration, and invasion of ovarian cancer cells while upregulating the expression of antigen-presenting cells (APC). AN02 mediates CTLA-4 degradation through the SMAD4 pathway, significantly reducing tumor growth in small xenograft models and reversing the immune-suppressive tumor environment. Additionally, when used in combination with Ipilimumab, AN02 enhances therapeutic efficacy and inhibits epithelial-mesenchymal transition, making it a valuable tool for studying ovarian cancer.

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