Peptidyl-prolyl isomerases (PPIases) assist in the folding of newly-synthesized proteins, regulating the stability, localization, and activity of mature proteins. PPIase-Parvulin Inhibitor is a cell-permeable inhibitor of the PPIases Pin1 and Pin4 (IC50s = 1.5 and 1.0 μM, respectively), interacting with the PPIase domain. It blocks the proliferation of cancer cells that overexpress Pin1 and Pin4 (IC50 range = 2-5 μM), and similarly inhibits wild type mouse embryonic fibroblasts (MEFs) but not Pin1-/- MEFs. PPIase-Parvulin Inhibitor does not inhibit topoisomerase I or bind DNA. Also referred to as PiB, this compound is commonly used to determine the role of Pin1 in regulating various substrates and cellular functions.