protein phosphatase 5

DJ001 is a highly specific, selective, and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with an IC50 of 1.43 μM, and it promotes the regeneration of hematopoietic stem cells.

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.

Endothall is a protein phosphatase 2A (PP2A) inhibitor, capable of inhibiting PP2A (IC50: 90 nM) and PP1 (IC50: 5 uM). It acts as a herbicide and can also be useful in cancer chemotherapy.

Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride may cause sensitization. Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride promotes apoptosis in HepG2 (IC50= 62 μM) and SK-Hep1 (IC50= 151 μM) cells and inhibits protein phosphatase 2A.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

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

BRD6257 is an orally active inhibitor of protein phosphatase 1D (proteinphosphatase, Mg2+ Mn2+ dependent 1D, PPM1D) with an IC50 of 5 nM. It activates the p53 signaling pathway (EC50 of 51 nM), enhances p21 expression, and inhibits the proliferation of cancer cells MOLM13 (IC50 = 2.8 μM). BRD6257 demonstrates good metabolic stability in human and rat liver microsomes.

TRC-766, a negative control of RTC-5 (TRC-382), is a compound that exhibits protein phosphatase 2A (PP2A) binding properties while lacking phosphatase activation capabilities.

TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), exhibiting psychotropic activity and low acute toxicity. It enhances the expression of brain-derived neurotropic factor (BDNF) in the brain, reduces mRNA levels of MAOA and 5-HT1A receptors in the midbrain, and inhibits 5-HT2A receptor-mediated signaling.

SHP2-IN-5 (compound 1) is a non-receptor protein tyrosine phosphatase inhibitor targeting SHP2, with an IC50 value of 97 nM, and is associated with regulating cell growth and proliferation. This compound exhibits potential therapeutic properties in inhibiting cancer and other SHP2-related human diseases [1].

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.

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.

Cassiaside B2 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A).Cassiaside B2 is an agonist of the 5-HT2C receptor with anti-allergic activity.Cassiaside B2 is one of the active ingredients in the naphthylpyrone reference extract (NRE).