ptp1b in 1

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

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.

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/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].

DU-14 (PTP1B/TC-PTPPROTAC) is a potent and selective dual PROTAC degrader for PTP1B and TC-PTP, exhibiting IC50 values of 24.2 nM and 30.1 nM for the phosphatase activity of PTP1B and TC-PTP, respectively. It enhances IFN-γ signaling, promotes T cell activation, and possesses antitumor activity.

PROTAC PTP1B degrader 1 (compound 75) is a CRBN-based PTP1B PROTAC degrader with DC50 values of 0.2 μM at 48 hours and 0.05 μM at 72 hours.

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-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]

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].

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.

PTP1B-IN-27 (Compound 7i) is an inhibitor of protein tyrosine phosphatase 1-B (PTP-1B) with an IC50 of 8.2 µM. Additionally, it inhibits α-glucosidase with an IC50 of 120 µM and exhibits competitive inhibition characteristics (Ki=118 µM).

TC-PTP-IN-1 (compound 8) is a potent inhibitor of TC-PTP, with an IC50 value of 9.2 nM and Ki values of 4.3 nM and 34 nM for TC-PTP and PTP1B, respectively. TC-PTP-IN-1 increases the expression of pSre416 protein. TC-PTP-IN-1 (compound 3) also acts as a TC-PTP ligand for TP1L.

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].