Recent studies revealed that in addition to its localization in membrane, PD‐L1 also resides in cytoplasm and other subcellular structures.[2] Hence, it exerts an impact on immune suppression function through a PD‐1‐dependent pathway, while also facilitating tumor invasion and proliferation via mechanisms independent of PD‐1.[3] Thus, developing PD‐L1 small molecular modulators, such as degraders, down‐regulators, and covalent inhibitors, is essential to block related PD‐L1 processes and to reverse immunosuppression in tumor microenvironment.[4]. Here, CD274 is linked to neoplasm.