ptp1b-in-2

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

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

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-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 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-29 (Compound A2B5) is a phosphatase inhibitor that targets protein tyrosine phosphatase 1B (PTP1B), TCPTP, and λPPase, with IC50 values of 1.27 μM, 4.38 μM, and 8.79 μM, respectively. PTP1B-IN-29 is applicable in the research of diabetes and obesity.

PTP1B-IN-24 (Compound 9), a reversible PTP1B inhibitor, exhibits an IC 50 value of 1.4 μM and can increase the thermal stability of PTP1B. This compound is capable of reversing PA-induced insulin resistance by enhancing the phosphorylation levels of IRS1 and AKT [1].

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]

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].

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].

Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α-glucosidase, PTP1B, and RLAR. Vicenin 2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen-independent prostate cancer. Vicenin 2 might be a useful lead for the development of multiple target-oriented therapeutic modalities for the treatment of diabetes and diabetes-associated complications. Vicenin 2 could act as a UV light barrier to protect the plants.

JTT 551 can be used in the research of type 2 diabetes mellitus. JTT 551 is selective a protein tyrosine phosphatase 1B (PTP1B) inhibitor, with Kis of 0.22 μM and 9.3 μM for PTP1B and TCPTP (T-cell protein tyrosine phosphatase), respectively.

α-glucosidase PTP1B-IN-1 (compound 8a) is an effective inhibitor of both α-glucosidase and PTP1B, with IC50 values of 66.3 μM and 47.0 μM, respectively. It also exhibits strong inhibitory activity against α-amylase, having an IC50 of 30.62 μM. This compound is capable of binding to the active sites of α-glucosidase and PTP1B. α-glucosidase PTP1B-IN-1 holds potential for reducing postprandial blood glucose levels and may be useful in managing type 2 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-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.

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.

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 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].

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].

Stevisalioside A (Compound 2), isolated from the roots of Stevia serrata, is an orally active antidiabetic agent that inhibits Protein Tyrosine Phosphatase 1B (PTP1B) with an IC50 value of 526.8 μM. It effectively lowers blood glucose levels and attenuates the postprandial peak observed in oral glucose and insulin tolerance tests in Streptozotocin-induced hyperglycemic mice [1].

LXQ46 is an orally effective inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 0.190 μM. It enhances insulin and leptin signaling pathways in insulin-resistant C2C12 cells. Additionally, LXQ46 improves type 2 diabetes and increases insulin tolerance in mouse models.

Momordicoside A is a triterpenoid saponin compound isolated from bitter melon (Momordica charantia L.), which possesses a variety of biological activities, including inhibition of protein tyrosine phosphatase (PTP1B), and can be used in the treatment of type 2 diabetes. In addition, Momordicoside A has anti-inflammatory, antioxidant, antitumor, and anti-HIV AIDS potentials.