ptp1b-in-1

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

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 TC-PTP IN-1 is a dual inhibitor of PTP1B and TC-PTP. It can be used as a target protein ligand for the synthesis of the PROTAC DU-14 (PTP1B TC-PTP PROTAC).

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

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]

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].

1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance the activities of PP2A and PTP1B in malignant pleural mesothelioma cells. Additionally, 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis in NCI-H28 malignant pleural mesothelioma cells.

OA-Br-1 is an orally active, selective inhibitor of PTP1B with an IC50 value of 7.08 μM. It induces apoptosis and exhibits broad-spectrum anti-cancer cell proliferation activity. OA-Br-1 exerts anti-breast cancer effects both in vitro and in vivo through the PTP1B PI3K AKT signaling pathway.

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].

MurA-IN-1 (compound 1a), a PTPRR inhibitor, exhibits IC50 values of 0.09 μM for PTPRR, 0.23 μM for PTP1B, 0.75 μM for PTPN7, and 0.8 μM for PTPN5, respectively, targeting a family of human MAPK-specific protein tyrosine phosphatases[1].

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].

Rubrofusarin 6-O-β-D-glucopyranoside, a glycosidic derivative of Rubrofusarin, functions as an inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 87.36 μM, and is utilized in research investigating comorbid diabetes and depression [1].

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].

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.

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].

Anticancer Agent 143 (Compound 369), a potent dual inhibitor targeting PTPN2 and PTP1B, exhibits IC50 values below 2.5 nM. It is employed in cancer research [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].