pp5

PP5-IN-1 is a potent and competitive serine threonine protein phosphatase-5 (PP5) inhibitor with potential anticancer activity that induces apoptosis in cancer cells.

Perfluorodecalin (PFD) is a chemically and biologically inert biomaterial, hydrophobic and radiolucent, used as artificial blood. Perfluorodecalin enhances bone regeneration and cell viability.

PP5-IN-2, a selective and orally active inhibitor of protein phosphatase 5 (PP5), exhibits an IC 50 of 0.9 μM. This compound activates p53 and leads to the downregulation of cyclin D1 and MGMT, thereby inducing cell cycle arrest and reversing Temozolomide (TMZ) resistance in the U87 MG cell line. Additionally, PP5-IN-2 has demonstrated effective inhibition of tumor growth in the xenograft mouse model.

PP58 is an inhibitor of PDGFR, FGFR and Src family.

Okadaic acid is a potent polyether marine toxin that primarily accumulates in the digestive glands of marine mollusks. It is a highly effective and selective inhibitor of protein phosphatases (PPs). By inhibiting these phosphatases, okadaic acid increases the phosphorylation levels of various proteins, acts as a tumor promoter, and induces tau protein phosphorylation. It can be used to establish models of Alzheimer’s disease and skin cancer.

Ro 90-7501 is an amyloid β42 (Aβ42) protofibrillar and TPR-dependent PP5 inhibitor, a novel radiosensitizer for cervical cancer cells, which inhibits ATM phosphorylation, promotes apoptosis, and induces cell-cycle arrest. Ro 90-7501 also exhibits antiviral activity and potential anticancer activity by inhibiting ATM phosphorylation and DNA repair, and by inhibiting HCMV.

DDO-3733 is a conformational activator of Protein Phosphatase 5 (PP5) that functions independently of TRP, facilitating the dephosphorylation of downstream substrates.

Cytostatin (sodium salt) is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin (sodium salt) potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.

Cytostatin is a natural antitumor inhibitor of cell adhesion to extracellular matrix, blocking adhesion of B16 melanoma cells to laminin and collagen type IV in vitro (IC50s = 1.3 and 1.4 μg/ml, respectively) and B16 cells metastatic activity in mice. It induces apoptosis of FS3 mouse fibrosarcoma cells (IC50 = 3.1 μg/ml). Cytostatin potently and selectively inhibits protein phosphatase 2A (PP2A; IC50 = 29 nM against the catalytic subunit), while having no effect against PP1, PP2B, or PP5.

Okadaic acid ammonium salt is a marine toxin that acts as an inhibitor of protein phosphatases (PP), with the highest affinity for PP2A (IC50 = 0.1–0.3 nM), while also inhibiting PP1, PP3, PP4, and PP5, but not PP2C. By increasing the phosphorylation of various proteins, it functions as a tumor promoter and induces tau protein phosphorylation, commonly used to establish Alzheimer's disease models.

DDO3711, a PP5-recruiting phosphatase recruitment chimera (PHORC), is created by chemically linking an apoptosis signal-regulated kinase 1 (ASK1) inhibitor with a PP5 activator. This compound selectively targets ASK1 (IC50=164.1 nM) over ASK2 (IC50 >20 μM), effectively dephosphorylating p-ASK1 T838 through PP5 recruitment. Exhibiting ASK1-dependent antiproliferative properties, DDO3711 demonstrates anti-cancer activity, making it a promising agent for research into the abnormal phosphorylation of oncoproteins.