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Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(50)

Glyoxalase

(2)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(40)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(116)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(53)

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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Cyclosporin A

T094559865-13-3

Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a/CD18 adhesion molecules. It is commonly used to induce uremia models.

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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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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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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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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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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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RMC-4630

T396582172652-48-9

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

$137

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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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Tacrolimus

T2144104987-11-3

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

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LB100

T44491632032-53-1

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

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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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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.

$136

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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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β-Glycerophosphate disodium salt hydrate

T4915154804-51-0

β-Glycerophosphate is a classical serine-threonine phosphatase inhibitor used in kinase reaction buffers. BGP is often used in combination with other phosphatase protease inhibitors for broad spectrum inhibition. It functions as an organic phosphate donor

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D-Glucose 6-phosphate

T1926356-73-5

D-Glucose 6-phosphate (G6P) is glucose that hydroxyl group on carbon 6 is phosphorylated by hexose kinase and is involved in glycolysis, gluconeogenesis, and the pentose phosphate pathway, as well as being converted to glycogen or starch storage. G6P serves as a substrate for glucose 6-phosphatase in the liver and hexose 6-phosphate dehydrogenase (H6PDH) in the lumen of the endoplasmic reticulum.

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Rosiptor

TQ0032782487-28-9

Rosiptor (AQX-1125) (AQX-1125) is an orally-active and specific phosphatase SHIP1 activator with anti-inflammatory effects.

$113

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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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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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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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NSC-87877

T1635056990-57-9

NSC-87877 is an effective inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (IC50=0.318 μM, 0.355 μM of shp2 and shp1, respectively).It also inhibits dual-specificity phosphatase 26 (DUSP26).

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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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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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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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