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Metabolism

ATP Citrate Lyase

(11)

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(35)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(31)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(80)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(47)

Stearoyl-CoA Desaturase (SCD)

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

Filter HomeSignaling PathwaysMetabolismPhosphatase

Osunprotafib

T616992489404-97-7In house

Osunprotafib (ABBV-CLS-484) is a potent, orally bioavailable PTP1B PTPN2 inhibitor in clinical trials for solid tumors. [1] Osunprotafib (ABBV-CLS-484) stimulates the tumor microenvironment and promotes natural killer cell and CD8 T cell function and enhances T cell anti-tumor immunity by enhancing JAK-STAT signaling and reducing T cell dysfunction. [2]

$455

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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.

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SHP099 hydrochloride

T35442200214-93-1

SHP099 hydrochloride is a potent, selective, orally bioavailable SHP2 inhibitor with IC50 of 70 nM, which inhibits ERK1 2 activation in cancer cells. [2]

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TNO155

T131761801765-04-7

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

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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.

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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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RMC-4630

T396582172652-48-9

RMC-4630 (SHP2-IN-7) is an inhibitor of SHP2.

$148

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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.

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Voclosporin

T17235515814-01-4

Voclosporin (ISAtx-247) is a novel, orally available calcium-modulated phosphatase (CN; PP2B) inhibitor and immunosuppressant used for treating lupus nephritis.

$139

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MY10

T616782204270-73-3

MY10, a potent and orally active inhibitor of the receptor protein tyrosine phosphatase (RPTPβ ζ), effectively reduces binge-like ethanol consumption and diminishes the rewarding effects of ethanol.

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Ertiprotafib

T15243251303-04-5In house

Ertiprotafib (PTP 112), a selective and potent inhibitor of protein tyrosine phosphate 1B (PTP1B) and IkappaB kinase β (IKK-β), is a novel insulin sensitizer with potential anticancer activity for the study of type 2 diabetes and breast cancer.

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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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BCI

T104861245792-51-1

BCI ((E)-BCI) is an allosteric inhibitor of dual-specificity phosphatases (DUSP), with EC50 values of 13.3 μM for DUSP6 and 8.0 μM for DUSP1 in cells, and does not inhibit DUSP5.

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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.

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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.

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SC-43

T84781400989-25-4

SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects.

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Razuprotafib

T167241008510-37-9

Razuprotafib (AKB-9778) is a protein tyrosine phosphatase ß (HPTPß) inhibitor with an IC50 of 50 nM. It effectively activates Tie-2 and provides protection against acute kidney injury.

$253

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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 is utilized in neuropathic pain research.

$148

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LB100

T44491632032-53-1

LB100 (LB-100) is a water soluble protein phosphatase 2A (PP2A) inhibitor.

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LUPENONE

T57081617-70-5

Lupenone is a natural product isolated from Rhizoma Musae and has good anti-diabetic activity,and has anti-inflammatory activity.lupenone were potent PTP1B inhibitors with IC50 values of 15.11±1.23μM.

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CaMKP Inhibitor

T215952789-62-5

CaMKP Inhibitor can inhibit CaMKP.

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CCT007093

T1927176957-55-4

CCT007093 is an effective PPM1D (WIP1) inhibitor (IC50: 8.4 μM).

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RMC-4550

T167622172651-73-7

RMC-4550 is an effective and allosteric inhibitor of SHP2 (IC50: 0.583 nM).

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CDP-Star

T75349160081-62-9

CDP-Star is a luminescent substrate for 1,2-dioxetane and a substrate for alkaline phosphatase.CDP-Star can be used for in vivo imaging by detecting mRNA on Northern blot.

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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 sensitizer and has been 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, respectively [1][2].

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DA-3003-1

T16357383907-43-5In house

DA-3003-1 (DA-3003-1) is a membrane-permeable, potent and selective Cdc25 dual specificity phosphatase inhibitor with antitumor activity that inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.

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Mulberrofuran G

TN195687085-00-5

Mulberrofuran G, isolated from Morus alba L., has anti-hepatitis B virus activity and protects against ischemic injury-induced cell death. Mulberrofuran G is a dual inhibitor of PTP1B and alpha-glucosidase for use in the study of Alzheimer's disease.

$263

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GSK 2830371

T65211404456-53-6

GSK 2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.

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D-ERYTHRO-SPHINGOSINE

T5891123-78-4

D-erythro-Sphingosine (trans-4-Sphingenine) is a protein kinase C (PKC) inhibitor. D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator

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Tegeprotafib

T790492407610-46-0

Tegeprotafib (PTPN2 1-IN-1) is an orally active and potent PTPN1 2 inhibitor with potential anticancer and antitumor activity for the study of cancer and immune system diseases.

$440

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LFHP-1c

T781412102347-47-5

LFHP-1c is a novel PGAM5 inhibitor that shows neuroprotective activity in an ischemic stroke model, preventing BBB destruction after transient middle cerebral artery occlusion (tMCAO) in rats.LFHP-1c can be used to study cerebral ischemic stroke.

$198

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TPI-1

T396279756-69-7

TPI-1 is a SHP-1 inhibitor.

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NSC 95397

T707893718-83-3

NSC 95397 is a potent inhibitor of Cdc25 dual specificity phosphatase(Ki of 32, 96, and 40 nM for Cdc25A, Cdc25B, and Cdc25C, respectively).

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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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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.

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NCGC00378430

T9205920650-00-6

NCGC00378430 is a potent SIX1 EYA2 interaction inhibitor that disrupts the [SIX1 EYA2] complex, EMT, and metastasis.

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Ascomycin

T2481104987-12-4

Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.

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KY-226

T77041621673-53-7

KY-226 is a potent inhibitor of protein tyrosine phosphatase 1B (PTP1B)(IC50: 0.25 μM,)

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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

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SBI-425

T168591451272-71-1

SBI-425 is an effective and orally bioavailable inhibitor of tissue-nonspecific alkaline phosphatase (TNAP). SBI-425 effectively inhibits TNAP in the vasculature and improves cardiovascular parameters and survival without a detectable change in the bone.

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BTdCPU

T71501257423-87-2

BTdCPU is a potent activator of heme-regulated eIF2α kinase (HRI) . BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.

$148

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Sal003

T24171164470-53-4

Sal003, an effective cell-permeable analog, inhibitis the eIF2α phosphatase.

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Pentamidine

T23133100-33-4

Pentamidine is an antifungal and antiprotozoal agent, interacting directly with the pathogen genome by binding to AT-rich regions of duplex DNA and the minor groove of DNA, thereby interfering with DNA replication.

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Pentamidine dihydrochloride

T2313250357-45-4In house

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent effective against various microorganisms, including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). It is a potent and selective inhibitor of protein tyrosine phosphatases and phosphatase of regenerating liver. Pentamidine dihydrochloride inhibits the parasite Leishmania infantum with an IC50 of 2.5 μM.

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BN82002

T4671396073-89-5

BN82002 (CDC25 Phosphatase Inhibitor I) is a synthetic inhibitor of CDC25 phophatases

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BCI-215

T73231245792-67-9

BCI-215 causes selective cancer cell cytotoxicity in part through non-redox-mediated activation of MAPK signaling

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Sephin1

T2182413098-73-2

Sephin1 (IFB-088) is reportedly a selective inhibitor of GADD34 (PPP1R15A), which is a stress-induced regulatory subunit of protein phosphatase 1 complex that dephosphorylates eIF2α

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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.

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