P21d

P21d (also known as BRK inhibitor P21d) is a potent, selective, and cell-permeable small molecule inhibitor of breast tumor kinase (BRK, also known as protein tyrosine kinase 6 or PTK6) with an IC50 of 30 nM. It was originally discovered by Merck Research Laboratories as a tool compound to explore PTK6 as an oncology target. P21d inhibits PTK6 kinase activity, leading to the downregulation of SNAIL (a transcriptional driver of epithelial-mesenchymal transition) and the restoration of E-cadherin expression in triple-negative breast cancer (TNBC) cells. In vivo, P21d treatment suppresses TNBC tumor growth and metastasis in immunocompetent mouse models by promoting an anti-tumor immune response, characterized by increased infiltration of cytotoxic CD8+ T cells and NK cells mediated by CXCL10 induction.

Other names

BRK inhibitor P21dBRK inhibitor P21d hydrochlorideP21d hydrochlorideP-21d hydrochlorideP 21d hydrochloridePTK6 inhibitor P21dPTK-6 inhibitor P21dPTK 6 inhibitor P21dPyrazin-21dPyrazin21dPyrazin 21d