2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Phosphatase

Phosphatase

Phosphatase

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Phosphatases are enzyme that remove a phosphate group from a protein. Protein tyrosine phosphatases (PTPs) comprise a diverse family of transmembrane and cytoplasmic enzymes. PTPs play an important role in regulating the proliferative activity of cells and the integrity of cell-cell and cell-matrix contacts. Protein tyrosine phosphatase 1B (PTP1B) is a non-receptor PTP frequently associated with the endoplasmic reticulum and vesicles subjacent to the plasma membrane. PTP1B as a key negative regulator of leptin receptor pathways has been an attractive therapeutic target for the treatment of type 2 diabetes mellitus and obesity. Four major serine/threonine-specific protein phosphatase catalytic subunits are present in the cytoplasm of animal cells. Three of these enzymes, PP1, PP2A, and PP2B, are members of the same gene family, while PP2C appears to be distinct.The alkaline phosphatases comprise a heterogeneous group of enzymes that are widely distributed in mammalian cells. Acid phosphatase enzymes catalyze the hydrolysis of phosphate monoesters following the general equation.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-149097
    ITH12711
    		Activator
    ITH12711 is a PP2A ligand. ITH12711 is able to cross the blood-brain barrier (BBB). ITH12711 exerts neuroprotection via restoration of PP2A-phosphatase activity.
    ITH12711
  • HY-D1676
    Thymolphthalein monophosphate disodium hydrate
    Thymolphthalein monophosphate disodium hydrate is a chromogenic substrate for the determination of acid phosphatase and alkaline phosphatase. Thymolphthalein is released during the reaction, increases the pH of the medium for easy detection, produces color and stops hydrolysis. Thymolphthalein monophosphate disodium hydrate can be used for the specific detection of prostatic phosphatase in serum.
    Thymolphthalein monophosphate disodium hydrate
  • HY-P1799
    [pTyr5] EGFR (988-993)
    [pTyr5] EGFR (988-993) is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B).
    [pTyr5] EGFR (988-993)
  • HY-124152
    3,4-Dephostatin
    		Inhibitor
    3,4-Dephostatin (Methyl-3,4-dephostatin) is an inhibitor of protein-tyrosine phosphatase (PTPase). 3,4-Dephostatin accelerates nerve growth factor (NGF)-induced neurite formation in PC12h cells. 3,4-Dephostatin sustains the NGF-induced tyrosine phosphorylation of proteins, most prominently that of mitogen-activated protein (MAP) kinase. 3,4-Dephostatin also prolongs epidermal growth factor (EGF)-induced tyrosine phosphorylation and activation of MAP kinase.
    3,4-Dephostatin
  • HY-108599R
    DCP-LA (Standard)
    		Inhibitor
    DCP-LA (Standard) is the analytical standard of DCP-LA. This product is intended for research and analytical applications. DCP-LA (FR236924), a linoleic acid derivative, selectively and directly activates PKCε. DCP-LA activates Ca(2+)/calmodulin-dependent protein kinase II (CaMKII) and inhibits protein phosphatase-1 (PP-1) to stimulate AMPA receptor exocytosis. DCP-LA inhibits activation of caspase-3/-9 and protects neurons at least in part from oxidative stress-induced apoptosis[1][2][3].
    DCP-LA (Standard)
  • HY-N12353
    Stevisalioside A
    		Inhibitor
    Stevisalioside A (Compound 2) can be isolated from Stevia serrata roots. Stevisalioside A is an orally active antidiabetic agent. Stevisaliosides A inhibits PTP1B (IC50: 526.8 μM). Stevisalioside A reduces blood glucose levels and the postprandial peak in oral glucose and insulin tolerance tests in Streptozotocin (HY-13753) induced hyperglycemic mice.
    Stevisalioside A
  • HY-N15220
    Dipsacus saponin X
    		Activator
    Dipsacus saponin X (compound 7) is a triterpenoid saponin that stimulates the proliferation of UMR106 cells and increases alkaline phosphatase activity in UMR106 cells (4 μM).
    Dipsacus saponin X
  • HY-N7599
    Chrysophanol triglucoside
    		Inhibitor
    Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research.
    Chrysophanol triglucoside
  • HY-144396
    SHP2-IN-8
    		Inhibitor
    SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells.
    SHP2-IN-8
  • HY-117085
    Lobaric acid
    		Inhibitor
    Lobaric acid is a depsipeptide metabolite isolated from Stereocaulon lichen with antioxidant, antiproliferative, antiviral and enzyme inhibitory activities. Lobaric acid scavenges superoxide free radicals (IC50=97.9 μM) and inhibits cancer cell proliferation (EC50 of 15.2-63.9 μg/mL against leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic and lung cancer cell lines). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC50=0.87 μM for human recombinant enzyme) and 12(S)-HETE produced by 12(S)-lipoxygenase (IC50=28.5 μM). Lobaric acid (250 μM) also reduced pathological changes in tobacco leaves infected with tobacco mosaic virus (TMV).
    Lobaric acid
  • HY-125072
    Arabinose 1,5-diphosphate
    Arabinose 1,5-diphosphate serves as an inhibitor of bisphosphatase activity.
    Arabinose 1,5-diphosphate
  • HY-113976AR
    Endothall (Standard)
    		Antagonist
    Endothall (Standard) is the analytical standard of Endothall. This product is intended for research and analytical applications. Endothall (Endothal) is a protein phosphatase 2A (PP2A) inhibitor with IC50s of 90 nM and 5 µM for PP2A and PP1, respectively. Endothall can be used as an herbicide. Endothall also is useful in cancer chemotherapy.
    Endothall (Standard)
  • HY-126825
    NE21650
    		Inhibitor
    NE21650 potently inhibits farnesyl diphosphate (FPP) synthase. NE21650 is a weak inhibitor of isopentenyl diphosphate (IPP) isomerase. NE21650 is a potent inhibitor of protein prenylation in osteoclasts and macrophages and bone resorption in vitro.
    NE21650
  • HY-150609
    SHP2/CDK4-IN-1
    		Inhibitor
    SHP2/CDK4-IN-1 (compound 10) is an orally active and potent SHP2 and CDK4 dual inhibitor, with IC50 values of 4.3 and 18.2 nM, respectively. SHP2/CDK4-IN-1 effectively induces G0/G1 arrest to prevent the proliferation of TNBC cell lines. SHP2/CDK4-IN-1 shows significant antitumor efficacy in the EMT6 syngeneic mouse model. SHP2/CDK4-IN-1 can be used for triple-negative breast cancer (TNBC) research.
    SHP2/CDK4-IN-1
  • HY-156607
    Anticancer agent 143
    		Inhibitor
    Anticancer agent 143 (compound 369) is a dual PTPN2/PTP1B inhibitor with IC50 values <2.5 nM. Anticancer agent 143 can be used in cancer research.
    Anticancer agent 143
  • HY-P991210
    Efzimfotase alfa
    		Inhibitor
    Efzimfotase alfa (ALXN-1850) is enzyme replacement therapy agent targeting the deficiency of tissue-nonspecific alkaline phosphatase (TNSALP). Efzimfotase alfa functions by hydrolyzing the substrates of TNSALP, reducing the concentrations of substrates such as inorganic pyrophosphate (PPi) and pyridoxal 5′-phosphate (PLP). Efzimfotase alfa is promising for research of hypophosphatasia (HPP).
    Efzimfotase alfa
  • HY-169013
    DDO-3733
    		Activator
    DDO-3733 is a TRP-independent Protein Phosphatase 5 (PP5) allosteric activator that promotes dephosphorylation of downstream substrates.
    DDO-3733
  • HY-160151
    TP1L
    		Degrader
    TP1L is a potent and selective T-cell protein tyrosine phosphatase (TC-PTP) PROTAC degrader, with a DC50 value of 35.8 nM. TP1L elevates the phosphorylation level of TC-PTP substrates including pSTAT1 and pJAK1. TP1L selectively enhances IFN-γ signaling and increases MHC-I expression. TP1L activates TCR signaling through increases phosphorylation of LCK. TP1L enhances CAR-T cell mediated tumor killing efficacy through activation of the CAR-T cells. TP1L can be used for the study of cancer. (Pink: TC-PTP ligand: (HY-138964), Blue: E3 ligase CRBN Ligand (HY-A0003), Black: Linker: (HY-140002)).
    TP1L
  • HY-136595
    3,5-Difluoro-L-tyrosine
    		98.39%
    3,5-Difluoro-L-tyrosine is a functional, tyrosinase-resistant mimetic of tyrosine. 3,5-Difluoro-L-tyrosine can be used to analyze the substrate specificity of protein tyrosine phosphatases (PTPs).
    3,5-Difluoro-L-tyrosine
  • HY-117087
    K103
    K103 is an inhibitor discovered from the screen that is an analog of the serotonin antagonist benzazocine. K103 exhibited inhibition of SHIP homologues, labelling it a pan-SHIP1/2 inhibitor, but the molecule had no effect on another 5' inositol phosphatase, OCRL. In line with the "two PIPs hypothesis", the molecule exhibited significant anti-tumour effects against a variety of cell lines, particularly breast cancer cells. Additional studies with K103 revealed that inhibition of SHIP1/2 in multiple myeloma cells resulted in G2/M cell cycle arrest followed by extensive apoptosis via activation of the caspase cascade. K103 fits the commonly used small molecule agent property profile, but while this work was being conducted, it was discovered that K103 caused psychoactive effects in mice, which limited the utility of the molecule in vivo. Therefore, certain synthetic studies were conducted on this tryptamine to identify the features that needed to be present in the molecule to maintain pan-SHIP1/2 inhibition in order to design an inhibitor with favourable pharmacodynamic properties and an improved side effect profile.
    K103
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Cat. No. Product Name / Synonyms Application Reactivity