With the progressive elucidation of the biological functions of SIRT4, multiple regulatory mechanisms in cancer have been unveiled, thus positioning SIRT4 as a prospective therapeutic target for various malignancies (Table 2). Nevertheless, the development of small molecule inhibitors targeting SIRT4 remains considerably constrained, with the majority of investigations yielding inhibitors of low potency and non-selectivity. Here, SIRT4 is linked to cancer.