PTP1B inhibitor 2

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.

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]

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.

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.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

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

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.

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.

Sodium stibogluconate (Stibogluconate trisodium nonahydrate) is a potent inhibitor of protein tyrosine phosphatase.

Razuprotafib (AKB-9778) is a protein tyrosine phosphatase ß (HPTPß) inhibitor with an IC50 of 50 nM. It effectively activates Tie-2 and provides protection against acute kidney injury.

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.

LXQ-87 is an orally administered, non-competitive inhibitor of PTP1B with an IC50 of 1.061 μM, demonstrating hypoglycemic activity. It alleviates insulin resistance and enhances cellular glucose uptake, making it useful for type 2 diabetes research.

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.

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].

PHPS1 is an inhibitor of Shp2. PHPS1 efficiently inhibits activation of Erk1 2 by the leukemia-associated Shp2 mutant, Shp2-E76K, and blocks the anchorage-independent growth of a variety of human tumor cell lines.

Aquastatin A is a fungal metabolite originally isolated fromF. aquaeductuumthat has diverse biological activities.1It is active againstS. aureus(MIC = 32 μg/ml) and inhibits enoyl-acyl carrier protein reductase (Fabl; IC50= 3.2 μM) andS. aureusfatty acid synthesis (IC50= 3.5 μM).2Aquastatin A also inhibits the Na+/K+-ATPase and H+/K+-ATPase (IC50s = 7.1 and 6.2 μM, respectively), as well as protein tyrosine phosphatase 1B (PTP1B; IC50= 0.19 μM).1,3 1.Hamano, K., Kinoshita-Okami, M., Minagawa, K., et al.Aquastatin A, an inhibitor of mammalian adenosine triphosphatases from Fusarium aquaeductuum. Taxonomy, fermentation, isolation, structure determination and biological propertiesJ. Antibiot. (Tokyo)46(11)1648-1657(1993) 2.Kwon, Y.-J., Fang, Y., Xu, G.-H., et al.Aquastatin A, a new inhibitor of enoyl-acyl carrier protein reductase from Sporothrix sp. FN611Biol. Pharm. Bull.32(12)2061-2064(2009) 3.Seo, C., Soh, J.H., Oh, H., et al.Isolation of the protein tyrosine phosphatase 1B inhibitory metabolite from the marine-derived fungus Cosmospora sp. SF-5060Bioorg. Med. Chem. Lett.19(21)6095-6097(2009)

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-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.