Biotin-itaconate is a biotin-labeled itaconic anhydride that targets PD-L1. Biotin-itaconate acts as a biotin probe for in vitro alkylation assays to identify itaconate-modified protein substrates-typically substrates containing cysteine residues. Biotin-itaconate is applicable to cancer research [1] [2].
In Vitro, Biotin-itaconate (50 μM; 4 h) covalently alkylates the Cys272 residue of wild-type PD-L1 in HEK293T cells, while the C272A mutation abolishes this alkylation[1].
References:
[1]. Fan Y, et al. Itaconate transporter SLC13A3 confers immunotherapy resistance via alkylation-mediated stabilization of PD-L1. Cell Metab. 2025;37(2):514-526.e5.
[2]. Yang Y, et al. Itaconate modifications: Mechanisms and applications. J Intensive Med. 2025 Dec 1;6(2):114-127.
In Vitro, Biotin-itaconate (50 μM; 4 h) covalently alkylates the Cys272 residue of wild-type PD-L1 in HEK293T cells, while the C272A mutation abolishes this alkylation[1].
References:
[1]. Fan Y, et al. Itaconate transporter SLC13A3 confers immunotherapy resistance via alkylation-mediated stabilization of PD-L1. Cell Metab. 2025;37(2):514-526.e5.
[2]. Yang Y, et al. Itaconate modifications: Mechanisms and applications. J Intensive Med. 2025 Dec 1;6(2):114-127.