Phosphatase

Fumonisin B1 is a fungal metabolite produced by Fusarium moniliforme, that has been shown to inhibit protein serine/threonine phosphatases (PP1, PP2A, PP2B, PP2C, and PP5/T/K/H), and is most effective with PP5.

Osunprotafib hydrochloride is a selective inhibitor of protein tyrosine phosphatases PTPN1 and PTPN2, exhibiting IC50 values of 2.5 nM and 1.8 nM, respectively. This compound demonstrates significantly reduced activity against PTPN9 and no activity on SHP-1 or SHP-2. Osunprotafib hydrochloride enhances the sensitivity of human cancer cell lines to interferon-gamma (IFNγ) and promotes robust anti-tumor immunity through the activation of JAK-STAT signaling pathways while mitigating T cell dysfunction. This makes it a valuable reagent for research into cancer immunotherapy and signaling modulation.

Calcium glucoheptonate is a highly soluble calcium supplement that primarily targets calcium deficiency. It enhances the proliferation rate and calcium uptake in MG-63 osteoblast-like cells and increases the activity of alkaline phosphatase (ALP). Additionally, it upregulates the expression of osteogenic markers such as collagen-1 and osteocalcin. This compound is valuable for research applications focused on osteoporosis and hypocalcemia.

Pimecrolimus is a natural ascomycin macrolactam that binds to macrophilin-12 (FKBP-12) and inhibits calcineurin as well as prolyl isomerase (rotamase).

Sodium orthovanadate is the chemical compound Na3VO4. It is an inhibitor of protein tyrosine phosphatases, alkaline phosphatases and a number of ATPases, most likely acting as a phosphate analogue.

D-3, a phosphorpeptide, is an efficient, simple, and specific iPSC-eliminating agent.

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.

Nodularin is a potent hepatotoxin, tumor promoter, and protein phosphatase inhibitor.

Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction.

bpV(phen) is a potent inhibitor of protein tyrosine phosphatases (PTPs) and PTEN, exhibiting IC50 values of 38 nM, 343 nM, and 920 nM for PTEN, PTP-β, and PTP-1B, respectively. This compound demonstrates significant anti-proliferative effects on the protozoan parasite Leishmania in vitro. Additionally, bpV(phen) enhances the secretion of various chemokines and pro-inflammatory cytokines while promoting a Th1-type immune response characterized by IL-12 and IFNγ production. It also induces apoptosis and exhibits anti-angiogenic and anti-tumor properties, making it valuable for research in cancer and inflammation biology.

PTPN2/1-IN-4 is a potent dual inhibitor of PTPN1 and PTPN2, exhibiting IC50 values of 12.8 nM and 5.8 nM, respectively. This compound effectively modulates the IFNγ-JAK-STAT signaling pathway, resulting in enhanced CD8+ T-cell infiltration into tumors. PTPN2/1-IN-4 demonstrates significant anticancer activity, inhibiting tumor growth both as a standalone treatment and in combination with anti-PD-1 antibodies in B16-OVA syngeneic mouse models, making it a valuable tool for cancer research.

Migoprotafib (GDC-1971; compound 199) is a selective SHP2 inhibitor that suppresses the MAPK/ERK signaling pathway. It exhibits antitumor activity and is under investigation for its potential in targeting SHP2-driven cancers.

HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC).

Isosinensetin is a bioactive flavonoid compound with diverse pharmacological properties. It acts as a dual inhibitor of HIV-1 protease and protein tyrosine phosphatase 1B (PTP1B), with an IC₅₀ of 2.61 µM and a Kᵢ of 0.92 µM for PTP1B, indicating its potential in antiviral and metabolic disease research. Additionally, isosinensetin inhibits P-glycoprotein (P-gp) activity in MDR1-MDCKII cells, suggesting its utility in overcoming multidrug resistance. Isosinensetin exhibits multiple therapeutic effects, including anti-tumor, anti-viral, anti-inflammatory, and antioxidant activities. These properties support its application in the research of various conditions such as cancer, chronic inflammation, osteoporosis, diabetes, and infectious diseases.

β-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a widely used phosphatase inhibitor. It plays a critical role in promoting and sustaining osteoblast differentiation, supporting mineral metabolism, and modulating cellular signal transduction pathways. In tissue engineering and drug delivery, it is commonly utilized as a component in the formation of heat-sensitive hydrogels due to its thermoresponsive properties. Additionally, β-glycerophosphate disodium salt accelerates calcification in vascular smooth muscle cells, making it a valuable tool for studying vascular calcification and related pathologies.