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Phosphatase inhibitors act on protein, lipid and inositol phosphatases that hydrolyze phosphate esters. A 2004 survey of the human genome counted 107 genes for protein tyrosine phosphatases (PTPs). Serine/threonine phosphatases such as protein phosphatases 1 and 2A (PP1, PP2A) reverse many kinase-driven signals. Calyculin A, reported in 1989 as an inhibitor of protein phosphatase activity, blocks both PP1 and PP2A. LB-100 targets PP2A, tautomycetin prefers PP1, and sodium orthovanadate inhibits PTPs broadly and is a common lysis buffer additive. Among lipid and inositol phosphatases, 3AC inhibits Src homology 2 (SH2) domain-containing inositol 5-phosphatase 1 (SHIP1), and L-690330 targets inositol monophosphatase.
Synonyms: Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
Synonyms: Acetyl ceramide; N-Acetyl-D-sphingosine
Ceramide is a ceramide shown to be a potent modulator of proliferation and differentiation, used as a tool for studying the complex signaling associated with the ceramides.
DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.
Synonyms: DT1154
SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A.
Synonyms: AQX-1125
Rosiptor (AQX-1125) is a selective and orally active phosphatase SHIP1 activator with anti-inflammatory effects.
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
Synonyms: DT061
(1S,2S,3R)-DT-061 is an enantiomer of DT-061. DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
AQX-016A is a potent activator of SHIP-1 that induces apoptosis of the cancer cell lines in vitro in both a time and dose dependant manner.
Synonyms: L-Ascorbic acid 2-phosphate trisodium
2-Phospho-L-ascorbic acid trisodium acts as an antioxidant and a stimulator of hepatocyte growth factor (HGF) production.
PROTAC PTPN2 degrader-1 is an effective degrader of the protein tyrosine phosphatase PTPN2. This compound facilitates target protein degradation through the proteasome pathway, enabling the modulation of cellular signaling related to cancer and metabolic diseases. Its application in research may provide insights into the therapeutic potential of targeting PTPN2 in various disease contexts.
PPA24 is a potent activator of protein phosphatase 2A (PP2A), with a KD of 8.465 μM for PP2ACα. It promotes apoptosis in cancer cells, leverages reactive oxygen species (ROS) generation, and reduces c-Myc expression levels. PPA24 is applicable for research in colorectal cancer, particularly in studies involving FOLFOX-resistant CRC and melanoma.
AQX-435 is a potent activator of SHIP1 phosphatase. This compound effectively reduces PI3K activation downstream of the B-cell receptor (BCR), leading to the induction of apoptosis in malignant B cells and demonstrating significant inhibition of lymphoma growth. It serves as a valuable tool for research into targeted therapies for B-cell malignancies.
Guaiacin is an arylnaphthalene-type lignin that acts as a potent phosphatase activator. Isolated from the bark of Machilus thunbergii, Guaiacin significantly enhances alkaline phosphatase activity and promotes osteoblast differentiation. Its biological activity makes it a valuable reagent for research applications focused on bone health and metabolic pathways involving phosphate metabolism.
P5SA-2 is a selective allosteric activator of the phosphatase PPP5C. By modulating the phosphatase domain, P5SA-2 enhances PPP5C activity by up to 3.2-fold at a concentration of 100 μM, with an apparent affinity constant of 7.8 μM. This compound is valuable for research in cancer biology and Alzheimer’s disease, providing insights into therapeutic mechanisms involving PPP5C modulation.
Anticancer Agent 7 is a PP2A modulator that facilitates the translocation of the FOXO1 transcription factor to the nucleus. This compound exhibits significant anti-proliferative activity against H1650 lung cancer cells, demonstrating an IC50 value of 5 μM. It serves as a valuable tool in cancer research, particularly in studies focused on signaling pathways involving PP2A and FOXO1.
Synonyms: AQX-1125 acetate
Rosiptor acetate is a selective activator of the SHIP1 phosphatase, known for its anti-inflammatory properties. It effectively inhibits Akt phosphorylation and reduces the production of inflammatory mediators and leukocyte chemotaxis in vitro. This compound is valuable for research applications focused on inflammation and immune response modulation.
ITH12711 is a potent activator of protein phosphatase 2A (PP2A), which plays a crucial role in various cellular signaling pathways. This compound effectively crosses the blood-brain barrier, resulting in neuroprotective effects through the restoration of PP2A-phosphatase activity. ITH12711 is valuable for research in neurobiology and pharmacology, particularly in studies focusing on neurodegenerative diseases and molecular mechanisms of neuroprotection.
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DDO-3733 is an allosteric activator of Protein Phosphatase 5 (PP5), functioning independently of TRP. It enhances the dephosphorylation of downstream substrates, making it a valuable tool for investigating the regulatory mechanisms of PP5 in various signaling pathways. This compound can be utilized in research applications focused on cellular signaling, phosphatase activity modulation, and the study of related metabolic processes.
ATUX-8385 is a potent activator of Protein Phosphatase 2A (PP2A), specifically binding to the PR65 subunit. This compound demonstrates significant potential for the investigation of various cancers and chronic conditions, including Alzheimer’s disease and chronic obstructive pulmonary disease (COPD). Its mechanism of action may provide insights into therapeutic strategies aimed at modulating PP2A activity in these diseases.
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SMAPP1 is a potent activator of protein phosphatase-1 (PP1). This compound effectively enhances the phosphorylation of CDK9 at Ser90 and Thr186, while leaving Ser175 unaffected. SMAPP1 has been shown to induce HIV-1 replication and significantly upregulate HIV-1 transcription, contributing to the reactivation of latent HIV-1 provirus. Its properties make it a valuable tool for studies related to HIV latency and viral reactivation.
