ptp

PTP inhibitor 1 is an inhibitor of cell-permeable protein tyrosine phosphatase (PTP) that covalently binds the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)),with Ki of128 μM.

VE-PTP-IN-1 (compound 2) is a selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP) with weakly acidic properties, and it plays a role in regulating vascular homeostasis and angiogenesis.

PTP Inhibitor IV is an effective protein tyrosine phosphatase (PTP) inhibitor, which can selectively inhibit DUSP14 phosphatase activity (IC50.5.21μm). PTP Inhibitor IV inhibited SHP-2, PTP1B, PTp-ε, PTP Meg-2, PTP-σ, PTP-β and PTP-μ, IC50 were 1.8 μM, 2.5 μM, 8.4 μM, 13 μM, 20 μM, 6.4 μM, and 6.7 μM, respectively. PTP Inhibitor IV affects cellular signaling by inhibiting PTP activity and may regulate specific pathways associated with PTP-mediated signaling events.

PTP1B-IN-22 is a protein tyrosine phosphatase 1B (PTP1B) inhibitor that inhibits glucose uptake in skeletal muscle L6 myotubes.

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.

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.

PTP1B-IN-2 is an effective protein tyrosine phosphatase 1B (PTP1B) inhibitor(IC50=50 nM).

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].

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.

PTP1B-IN-14 is a selective inhibitor of Protein Tyrosine Phosphatase 1B (PTP1B) that targets the enzyme's allosteric site, with an inhibitory concentration (IC50) of 0.72 μM.

PTP1B-IN-13, a potent and selective inhibitor of Protein Tyrosine Phosphatase 1B (PTP1B), effectively targets the allosteric site, exhibiting an IC50 value of 1.59 μM.

PTP1B AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1].

PTP1B-IN-4 (NUN-17724) is an allosteric PTP1B inhibitor with an IC50 of 8 μM. PTP1B-IN-4 can be used in studies about obesity and diabetes.

PTP1B-IN-3 diammonium is a highly effective and orally bioavailable inhibitor of the protein tyrosine phosphatase 1B (PTP1B) enzyme, with an IC50 value of 120 nM for both PTP1B and TCPTP, exhibiting potent antidiabetic and anticancer properties, as supported by extensive research [1] [2].

PTP1B-IN-17 (Compound 45) is a selective benzimidazole derivative with potential as a protein tyrosine phosphatase 1B (PTP1B) inhibitor (Ki: 30.2 μM). PTP1B-IN-17 can be used in the study of type 2 diabetes.

PTP1B-IN-16 is a promising and selective benzimidazole derivative and an inhibitor of protein tyrosine phosphatase 1B (PTP1B) (Ki: 12.6 μM).PTP1B-IN-16 can be used to study type 2 diabetes.

PTP1B-IN-15 is a potent, selective protein tyrosine phosphatase 1B (PTP1B) inhibitor with research potential in type II diabetes and obesity.

PTP1B-IN-20 is a selective PTP1B (protein tyrosine phosphatase 1B) inhibitor with an IC50 of 1.05 μM, demonstrating selectivity over TCPTP (T-cell protein tyrosine phosphatase) with an IC50 of 78.0 μM. It targets a crucial enzyme for inhibiting type 2 diabetes, showing preferential action on PTP1B over TCPTP.

PTP1B-IN-19 (Compound 43) is a promising selective benzimidazole derivative that acts as a protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 23.3 μM. This compound, along with PTP1B-IN-17, can be utilized in the study of type 2 diabetes.

PTPσ Inhibitor ISP is a compound that binds to recombinant human PTPs, thereby inhibiting PTPσ signaling. It has the capability to penetrate membranes and counteract the inhibitory effects of chondroitin sulfate proteoglycan (CSPG) on axonal sprouting in spinal cord injury models. Additionally, it fosters remyelination in lysolecithin (LPC)-induced demyelinated spinal cords and supports the migration and maturation of oligodendrocyte progenitor cells (OPCs), enhancing remyelination and functional recovery in Multiple Sclerosis (MS) animal models [1] [2].

PTP1B AKR1B1-IN-2 (Compound 7f) is a potent inhibitor targeting both PTP1B and AKR1B1 with IC50 values of 3.2 and 2.1 μM, respectively, and K i values of 4.0 and 0.9 μM. This compound acts as an insulin mimetic and enhances glucose uptake in murine C2C12 myoblasts, making it useful for Type 2 diabetes mellitus (T2DM) research [1].

PTP1B-IN-21 is a compound that functions as a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B; IC50=1.56 μM), demonstrating a marked preference over the structurally similar T-cell protein tyrosine phosphatase (TCPTP; IC50>100 μM). This specificity highlights its potential as a critical agent for type 2 diabetes management.

PTP1B-IN-18 is an orally active, fully mixed protein tyrosine phosphatase 1B (PTP1B) inhibitor with a Ki of 35.2 μM, and it can be used for the study of type 2 diabetes.

SF1670 (PTPase CD45 Inhibitor) is a specific PTEN inhibitor with IC50 of 2 μM.

MPTP hydrochloride is a precursor of MPP+, a dopamine neurotoxin with blood-brain barrier permeability. MPTP hydrochloride is toxic to dopaminergic neurons, which can lead to Parkinson's disease, and is widely used in the construction of animal models of Parkinson's disease.

RAMB4 (PTP1B-IN-9) is a ubiquitin-proteasome system (UPS)-stressor,with anticancer activity.

LMPTP INHIBITOR 1 hydrochloride is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM for LMPTP-A.

Purine riboside triphosphate, a derivative of purine riboside, exhibits structural similarity to adenosine. This naturally occurring base analog possesses inhibitory effects on carcinogenic growth, particularly in cancer ascites cells, by strongly impeding RNA and DNA synthesis.

PTP1B-IN-1 (PTP1B inhibitor) is a potent inhibitor of protein tyrosine phosphatase 1B (PTP1B) (IC50 : 1.6 mM)

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].

LMPTP Inhibitor 1 Dihydrochloride is a compound selectively targeting low molecular weight protein tyrosine phosphatase (LMPTP), exhibiting potent inhibitory activity with an IC50 value of 0.8 μM for LMPTP-A.

(Rac)-RK-682 is a racemic mixture that functions as a protein tyrosine phosphatases (PTPases) inhibitor, specifically targeting protein tyrosine phosphatase 1B (PTP-1B), low molecular weight protein tyrosine phosphatases (LMW-PTP), and cell division cycle 25B (CDC-25B), with inhibitory concentrations (IC50s) of 8.6 μM, 12.4 μM, and 0.7 μM, respectively [1].

PTPMT1-IN-1 is a PTEN-like mitochondrial phosphatase PTPMT1 inhibitor.

PROTAC PTPN2 degrader-2 (example 187B) is a potent PTPN2-degrading agent with potential applications in cancer and metabolic disease research [1].

mPTP-IN-22 is a novel mitochondrial permeability transition pore (mptp) inhibitor

MptpB-IN-1 is a potent, orally active MptpB inhibitor that targets the Mycobacterium tuberculosis protein-tyrosine-phosphatase B (MptpB), a secreted virulence factor evading host antimicrobial mechanisms. It effectively diminishes the survival and infection burden of multidrug-resistant Mycobacterium tuberculosis.

PROTAC PTPN2 Degrader-1 (compound example 77) is a potent entity capable of degrading PTPN2, showing promise for research applications in cancer or metabolic diseases [1].

PTPN22-IN-1, detailed in WO2021007491A1 as compound L-1, is a potent PTPN22 inhibitor, demonstrating an IC50 of 1.4 μM and a Ki of 0.50 μM. This compound achieves over 7-10 fold selectivity against PTPN22 relative to comparable phosphatases and enhances antitumor immune responses.

PROTAC PTPN2 degrader-2 (example 187B) TFA is a potent Protein Tyrosine Phosphatase Non-receptor Type 2 (PTPN2) degrader with potential applications in cancer and metabolic disease research [1].

MptpB-IN-2 (compound 20), a selective inhibitor for mycobacterium tuberculosis protein tyrosine phosphatase B (MptpB), exhibits half maximal inhibitory concentrations (IC50) of 0.64 μM for MptpB, 4.06 μM for MptpA, and 4.14 μM for PTP1B. Despite its inhibition potency, MptpB-IN-2 demonstrates limited antituberculosis efficacy, with a minimum inhibitory concentration (MIC) of 64.9 μM against Mtb H37Rv [1].

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.

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor that also inhibits lysine methyltransferase SETD8 (KMT5A) and various cytochrome P450 (P450) isoforms.

SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase ( LMW-PTP ) inhibitor ( IC 50 =4 nM, K i =1.2 nM). SPAA-52 can be used in diabete research [1] .

Compound 56 (Antidiabetic agent 2) is a glucose-uptake promoter that inhibits DPP-4, PTP-1B, α-amylase, and α-glucosidase, with IC50 values of 0.036, 0.042, 0.241, and 0.185 μM, respectively. This agent effectively decreases blood glucose levels [1].

MY33-3 is a powerful and specific inhibitor of receptor protein tyrosine phosphatase (RPTP)β/ζ, demonstrating an IC50 value of approximately 0.1 μM. Moreover, MY33-3 exhibits inhibitory activity against PTP-1B with an IC50 value of about 0.7 μM. Additionally, MY33-3 has been shown to effectively decrease ethanol consumption and alleviate neuroinflammation and cognitive dysfunction induced by Sevoflurane.

bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor (IC50s: 343 nM, 920 nM, and 38 nM for PTP-β, PTP-1B, and PTEN).

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

Ficusonolide exhibits significant antidiabetic activity through its interactions with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.