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Phosphatase

A phosphatase is an enzyme that uses water to cleave a phosphoric acid monoester into a phosphate ion and an alcohol. Because a phosphatase enzyme catalyzes the hydrolysis of its substrate, it is a subcategory of hydrolases. Phosphatase enzymes are essential to many biological functions, because phosphorylation (e.g. by protein kinases) and dephosphorylation (by phosphatases) serve diverse roles in cellular regulation and signaling. Whereas phosphatases remove phosphate groups from molecules, kinases catalyze the transfer of phosphate groups to molecules from ATP. Together, kinases and phosphatases direct a form of post-translational modification that is essential to the cell's regulatory network. Phosphatase enzymes are not to be confused with phosphorylase enzymes, which catalyze the transfer of a phosphate group from hydrogen phosphate to an acceptor. Due to their prevalence in cellular regulation, phosphatases are an area of interest for pharmaceutical research

  • Osunprotafib
    T616992489404-97-7In house
    ABBV-CLS-484 (Osunprotafib) is a potent PTPN2 inhibitor with subnanomolar activity and antitumor activity that enhances T-cell anti-tumor immunity.ABBV-CLS-484 can be used for the treatment of neoplasms, esophageal cancer, and digestive disorders.
    • $455
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  • SHP099 hydrochloride
    T35442200214-93-1
    SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor.
    • $32
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  • Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride
    T650862746-19-2
    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.
    • $37
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  • Cyclosporin A
    T094559865-13-3
    Cyclosporin A is a naturally occurring cyclic polypeptide that is the active metabolite of a fungus. Cyclosporin A is an immunosuppressant that binds to procyclins and inhibits calcineurin (IC50=7 nM).
    • $36
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  • Neomangiferin
    T380464809-67-2
    Neomangiferin (Mangiferin 7-glucoside) has beneficial effects on high fat diet-induced nonalcoholic fatty liver disease in rats. Neomangiferin and mangiferin inhibit tartrate-resistant acid phosphatase, a biochemical marker of osteoclast function and bone resorption.
    • $130
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  • Stearic acid
    T2P292357-11-4
    1. Stearic acid (Cetylacetic acid) can reduce metastatic tumor burden. 2. Stearic acid leads to dramatically reduced visceral fat likely by causing the apoptosis of preadipocytes. 3. Stearic acid and its derivatives have been used as gelators in food and pharmaceutical gel formulations. 4. Stearic acid is a potent phosphatase 1B inhibitor, possibly causing an enhancement in the insulin receptor signaling to stimulate glucose uptake into adipocytes. 5. Stearic acid has the potential to increase dry matter intake and yields of milk and milk components, without affecting conversion of feed to milk, body condition score, or body weight.
    • $33
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  • Cyclosporine
    T645979217-60-0
    Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation.
    • $30
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  • Disodium monofluorophosphate
    T074510163-15-2
    Disodium monofluorophosphate (NSC248) is a competitive inhibitor of pyruvate kinase and alkaline phosphatase, which also irreversibly inhibits phosphorylase phosphatase.
    • $50
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  • Cyt-PTPε Inhibitor-1
    T10927428478-94-8In house
    Cyt-PTPε Inhibitor-1 (A Inhibitor-1) is an inhibitor of cytosolic protein tyrosine phosphatase ε. Cyt-PTPε Inhibitor-1 blocks the dephosphorylation of c-Src and exhibits anti-osteoclastic activity.
    • $58
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  • BN82002
    T4671396073-89-5
    BN82002 (CDC25 Phosphatase Inhibitor I) is a synthetic inhibitor of CDC25 phophatases
    • $38
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  • NSC 65809
    T857394023-67-3
    NSC-65809 (Raphin1) is a selective inhibitor of R15B.
    • $133
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  • ML400
    T258241908414-42-5In house
    ML400 (CID73050863) is an allosteric inhibitor of LMPTP with an EC50 of 1μM. ML400 displays good cell-based activity and rodent pharmacokinetics.
    • $98
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  • CX08005
    T371841256341-22-6
    CX08005 is a protein tyrosine phosphatase 1B inhibitor. CX08005 reduces hepatic lipid accumulation and microcirculatory impairment associated with non-alcoholic fatty liver disease.
    • $94
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  • h-NTPDase8-IN-1
    T79492716358-51-9In house
    h-NTPDase8-IN-1 is a specific aminosulfonylbenzamide inhibitor of h-NTPDases8 (IC 50 = 0.28 ± 0.07 μM). h-NTPDase8-IN-1 can be used to study diseases brought about by aberrant h -NTPDase expression.
    • $54
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  • h-NTPDase-IN-2
    T796072939933-03-4In house
    h-NTPDase-IN-2 is a broad-spectrum NTPDase inhibitor that inhibits multiple h-NTPDas isoforms.
    • $479
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  • Managlinat dialanetil
    T16009L280782-97-0In house
    Managlinat dialanetil (MB06322) is an orally available and potent fructose 1,6-bisphosphatase (FBPase) inhibitor with hypoglycaemic activity for the study of type 2 diabetes.
    • $233
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  • (E,E)-RAMB4
    T12578919091-61-5
    PTP1B-IN-8 is a potent and selective inhibitor of protein tyrosine phosphatase-1B (PTP1B).
    • $148
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  • h-NTPDase-IN-3
    T796222939933-10-3In house
    h-NTPDase-IN-3 is an h-NTPDase inhibitor that inhibits h-NTPDase1, h-NTPDase2, h-NTPDase3 and h-NTPDase8.
    • $462 TargetMol
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  • Calcineurin Autoinhibitory Peptide acetate
    TP2054L
    Calcineurin Autoinhibitory Peptide acetate is a selectivecalcineurin phosphatase inhibitor(IC50 ~ 10 μM). Calcineurin Autoinhibitory Peptide acetate can be used in the protection of neurons from excitatory neuronal death.
    • $193
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  • MB-07729
    T11955882755-95-5In house
    MB-07729 is a potent non-competitive inhibitor of fructose-1,6-bisphosphate with IC50 values of 189, 121 and 31 nM in rat, monkey and human, respectively, for the study of diabetes.
    • $380
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  • BPDA2
    T735522907659-86-1In house
    BPDA2 is a selective and potent SHP2 inhibitor with IC50 values of 92.0 nM, 33.39 μM, and 40.71 μM for SHP2, SHP1, and SHP1B, respectively.DBDA2 possesses anticancer and antitumor activity and inhibits anchorage-independent growth of breast cancer cells and cancer stem cell properties in a concentration-dependent manner.BPDA2 can be used to study of breast cancer.
    • $293 TargetMol
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  • Pentamidine dihydrochloride
    T2313250357-45-4In house
    Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent with activity against a number of microorganisms including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases and phosphatase of regenerating liver inhibitor. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM.
    • $50
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  • LMPTP INHIBITOR 1 hydrochloride
    T44912310135-38-5
    LMPTP INHIBITOR 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase ( LMPTP ), with an IC 50 of 0.8 μM for LMPTP-A.
    • $258
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  • 7-BIA
    T101901313403-49-4In house
    7-BIA is a receptor-type protein tyrosine phosphatase D (PTPRD) inhibitor with anti-addictive properties and can be used in the study of neuropathic pain.
    • $148
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  • Ro 90-7501
    T16773293762-45-5In house
    Ro 90-7501 is an amyloid β42 (Aβ42) protofibrillar and TPR-dependent PP5 inhibitor, a novel radiosensitiser for cervical cancer cells, which inhibits ATM phosphorylation, promotes apoptosis, and induces cell-cycle arrest.Ro 90-7501 exhibits antiviral activity and potential anticancer activity by inhibiting ATM phosphorylation and DNA repair, and by inhibiting HCMV.
    • $30
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  • MLS000544460
    T12080352336-36-8In house
    MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor (Kd: 2.0 μM, IC50: 4 μM).MLS000544460 exhibits inhibitory effects on Eya2 phosphatase-mediated cell migration and has anticancer activity.
    • $82
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  • PTP1B-IN-22
    T6789386109-60-6In house
    PTP1B-IN-22 is a protein tyrosine phosphatase 1B (PTP1B) inhibitor that inhibits glucose uptake in skeletal muscle L6 myotubes.
    • $39
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  • Endothall
    T2747145-73-3In house
    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.
    • $38
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  • Vutiglabridin
    T612681800188-47-9In house
    Vutiglabridin (HSG4112) is a novel and safe modulator of PON2, a racemic compound. vutiglabridin is an optimized structural analogue of Glabridin and is superior to Glabridin in terms of weight loss and chemical stability. vutiglabridin ameliorates mptp-induced neurodegeneration in Parkinson's disease mice by targeting mitochondrial paraoxonase-2. Vutiglabridin is a clinical phase 2 drug for the treatment of obesity and has therapeutic effects on p-mitochondrial PON2 in a PD model. vutiglabridin penetrates the brain, binds PON2, and restores 1-methyl-4-phenylpyridine (MPP*)-induced neuroblastoma in SH-SY5Y Vutiglabridin significantly attenuated 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced dyskinesia and dopaminergic neuronal damage in mice modeled with PD in mouse experiments.
    • $100
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  • DT-061
    T10060L1809427-19-7In house
    DT-061 is an orally bioavailable protein phosphatase 2A (PP2A) activator. It could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
    • $1,230
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  • DJ001
    T110532161305-12-8In house
    DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with IC50 of 1.43 μM. DJ001 promotes the regeneration of hematopoietic stem cells.
    • $58
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  • CDC25B-IN-1
    T107232374831-10-2In house
    CDC25B-IN-1 is an inhibitor of CDC25B with a Ki of 8.5 μM. CDC25B-IN-1 increases the G2/M phase by inhibiting cell proliferation and colony formation.
    • $69
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  • PTP1B-IN-3
    T12577809272-64-8In house
    PTP1B-IN-3 is a selective and potent PTP1B inhibitor with anticancer activity that inhibits PTP1B and TCPTP.PTP1B-IN-3 is used in the study of diabetes.
    • $289
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  • SPI-112
    T43401051387-90-6
    SPI-112, the SPI-112 methyl ester analog, can inhibit cellular Shp2 PTP activity. SPI-112 bound to Shp2 by surface plasmon resonance (SPR) and displayed competitive inhibitor kinetics to Shp2.
    • $43
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  • PTP1B-IN-2
    T42561919853-46-5
    PTP1B-IN-2 is an effective protein tyrosine phosphatase 1B (PTP1B) inhibitor(IC50=50 nM).
    • $42
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  • Ebselen
    T082560940-34-3
    Ebselen (CCG-39161) is a organoselenium compound with anti-inflammatory, anti-oxidant and cytoprotective activity. Ebselen acts as a glutathione peroxidase mimetic and is thereby able to prevent cellular damage induced by reactive oxygen species (ROS). In addition, this agent inhibits the activity of a variety of enzymes including nitric oxide synthase (NOS), 5-lipoxygenase, cyclooxygenase, protein kinase C (PKC), NADPH oxidase and gastric H+/K+-ATPase. Furthermore, ebselen may be neuroprotective due to its ability to neutralize free radicals upon NMDA receptor activation thus, reducing lipoperoxidation mediated by glutamate-induced excitotoxicity.
    • $42
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  • Tacrolimus
    T2144104987-11-3
    Tacrolimus (Fujimycin) can bind FKBP12 to form a high-affinity complex (Ki: 0.2 nM) which inhibits the activity of the calcium/calmodulin-dependent protein phosphatase.
    • $38
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  • Bis(maltolato)oxovanadium(IV)
    T2227638213-69-3
    Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases)inhibitor with insulin-mimicking effects and anti-diabetic properties. BMOV is a potent insulin sensitize. BMOV is shown to improve cardiac dysfunctions in diabetic models. BMOV inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectivelyr[1][2].
    • $39
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  • Sodium metatungstate
    T1251912141-67-2
    Sodium metatungstate (Sodium polyoxotungstate) is a potent inhibitor of ecto-nucleoside triphosphate diphosphohydrolase (NTPDase)(Ki values of 2.58 μM, 3.26 μM, and 28.8 μM for NTPDase 1, NTPDase 3 and NTPDase 2 respectively).
    • $43
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  • SF1670
    T6667345630-40-2
    SF1670 (PTPase CD45 Inhibitor) is a specific PTEN inhibitor with IC50 of 2 μM.
    • $37
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  • kuwanon G
    T3S161275629-19-5
    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.
    • $100
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  • SHP099
    T35641801747-42-1
    SHP099 (SHP099 free base) free base is an effective, selective, orally bioavailable, and efficacious SHP2 inhibitor (IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM). SHP099 shows dose-dependent pathway inhibition and antitumor activity in xenograft models.
    • $31
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  • (Rac)-LB-100
    T20682061038-65-9
    LB-100, a novel Protein Phosphatase 2A (PP2A) inhibitor, sensitizes malignant meningioma cells to the therapeutic effects of radiation
    • $59
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  • Salubrinal
    T3045405060-95-9
    Salubrinal, a phosphatases (PP1) inhibitor(IC50=1.7 μM), exhibits function on the eukaryotic translation initiation factor 2 subunit (eIF2α).
    • $35
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  • 2-Bromo-4'-hydroxyacetophenone
    T70842491-38-5
    2-Bromo-4'-hydroxyacetophenone(PTP Inhibitor I) is a cell-permeable, protein tyrosine phosphatase (PTP) inhibitor that covalently blocks the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)) with a Ki value of 43 μM and PTP1B with a Ki value of 42 μM [1]. SHP-1 and PTP1B both have known roles in regulating insulin signaling as well as myeloid and lymphoid cell differentiation, making inhibitors of these phosphatases of interest in diabetes, cancer, allergy, and inflammation research [2].
    • $55
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  • LB100
    T44491632032-53-1
    LB100 (LB-100) is a water soluble protein phosphatase 2A (PP2A) inhibitor.
    • $51
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  • Suramin Sodium Salt
    T2160129-46-4
    Suramin Sodium Salt (BAY-205) is a sodium salt form of suramin, a polysulphonated naphthylurea with potential antineoplastic activity. Suramin blocks the binding of various growth factors, including insulin-like growth factor I (IGF-I), epidermal growth factor (EGF), platelet-derived growth factor (PDGF), and tumor growth factor-beta (TGF-beta), to their receptors, thereby inhibiting endothelial cell proliferation and migration. This agent also inhibits vascular endothelial growth factor (VEGF)- and basic fibroblast growth factor (bFGF)-induced angiogenesis; retroviral reverse transcriptase; uncoupling of G-proteins from receptors; topoisomerases; cellular folate transport; and steroidogenesis.
    • $41
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  • Taraxerol acetate
    T39302189-80-2
    Taraxeryl acetate shows the significant antiviral activity against herpes simplex virus (type II). It has less effect on cell cycle arrest and apoptosis of AGS cells than taraxerol. A. roxburghiana has antidiabetic activity, could be attributed due to PTP
    • $232
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  • JAB-3068
    T396402169223-48-5
    JAB-3068 (SHP2-IN-6) is a potent SHP2 inhibitor with anticancer and antitumor activity for the study of breast, lung, and esophageal cancers.
    • $397
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  • Tetramisole hydrochloride
    T04945086-74-8
    Tetramisole hydrochloride (Tetramisole HCl) inhibits alkaline phosphatase and is a high-purity antiparasitic agent.
    • $30
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