ptp1b-in-3

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-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-30 (Compound 3j) is an inhibitor of PTP1B with an IC50 of 0.51 µM. It suppresses the proliferation of T47D cancer cells with an IC50 of 21.21 µM, induces cell cycle arrest at the S phase, and triggers apoptosis in T47D cells.

PTP1B-IN-31 (Compound (S,S)-3ak) is a PTP1B inhibitor with an IC50 of 0.81 μM. It works synergistically with cytokine IFNγ to inhibit the growth of tumor cells, making it useful for cancer research.

PTP1B-IN-33 is a protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC₅₀ of 2.45 μM against human PTP1B, showing more than 20-fold selectivity over SHP2. It enhances π-alkyl interactions with PTP1B, thereby promoting closure of the WPD loop. PTP1B-IN-33 can be used in studies on cancer, diabetes, and autoimmune deficiency diseases.

PTP1B-IN-34 is an orally active, selective, and non-competitive inhibitor of PTP1B, with an IC50 value of 0.64 μM and a Ki of 1.15 μM for human PTP1B. It effectively reduces blood glucose levels in diabetic mice and is applicable for research related to type 2 diabetes.

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.

PPARα agonist5 is an orally active, selective partial agonist of PPARα with an EC50 of 3 nM. It reduces lipid accumulation and upregulates PPARα target genes, exhibiting anti-hepatic steatosis properties. Additionally, PPARα agonist5 demonstrates significant lipid-lowering and glucose-lowering effects through partial PPARγ agonist activity and mild inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 79.1 μM. It has favorable safety and is applicable in the study of dyslipidemia in type 2 diabetes.

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].

3,8'-Biapigenin is a polyketide synthase-derived biflavonoid identified in Hypericum species and has been reported to exhibit diverse biological activities. 3,8'-Biapigenin inhibits protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 4.5 µM and stimulates glucose uptake in 3T3-L1 adipocyte cells at concentrations of 5 and 10 µM. 3,8'-Biapigenin also inhibits the cytochrome P450 isoforms CYP3A4, CYP2C9, and CYP1A2, with Ki values of 0.038, 0.32, and 0.95 µM, respectively. In isolated rat embryonic hippocampal neurons, 3,8'-Biapigenin reverses cell death induced by kainate and NMDA when applied at a concentration of 10 µM. Furthermore, 3,8'-Biapigenin administered at 8 mg/kg decreases carrageenan-induced paw edema and protects against gastric lesions induced by indomethacin in rats. These findings support the application of 3,8'-Biapigenin as a research tool for investigations involving metabolic regulation, enzyme modulation, neurobiology, inflammatory processes, and xenobiotic metabolism.

Cyanidin 3-arabinoside (Cyanidin 3-monoarabinoside) is an anthocyanin extracted from blueberries that is a selective protein tyrosine phosphatase 1B (PTP1B) inhibitor, with potential anticancer activity, and can be used in the study of type 2 diabetes.

5-O-Coumaroylquinic acid (3-O-Coumaroylquinic acid), exhibits significant inhibition of PTP1B and a concentration-dependent inhibitory effect on α-glucosidase, thereby demonstrating anti-hyperglycemic properties. Additionally, this compound enhances glucose uptake and inhibits PTP1B in vitro, emphasizing its potential therapeutic applications in glucose regulation.