PTP1B inhibitor

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

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]

Infliximab is a monoclonal antibody, a human-mouse chimeric monoclonal antibody that inhibits TNF-α and prevents TNF-α from interacting with TNFR1 and TNFR2. Infliximab can be used to treat Crohn's disease and rheumatoid arthritis.

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.

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.

Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an aromatic diamidine agent effective against various microorganisms, including protozoa (Trypanosoma brucei, Leishmania spp., and Babesia spp.) and fungi (Pneumocystis jirovecii). It is a potent and selective inhibitor of protein tyrosine phosphatases and phosphatase of regenerating liver. Pentamidine dihydrochloride inhibits the parasite Leishmania infantum with an IC50 of 2.5 μM.

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

Pentamidine is an antifungal and antiprotozoal agent, interacting directly with the pathogen genome by binding to AT-rich regions of duplex DNA and the minor groove of DNA, thereby interfering with DNA replication.

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.

RA371 (EX-A4742) is a derivative of PTP1B-IN-8, an inhibitor of PTP1B.

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.

MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B) with an IC50 of approximately 1 μM.

PTP1B-IN-8 is a potent and selective inhibitor of protein tyrosine phosphatase-1B (PTP1B).

RAMB4 (PTP1B-IN-9) is a ubiquitin-proteasome system (UPS)-stressor,with anticancer activity.

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

Masticadienonic acid is a compound derived from Chios mastic gum, with potential anti-inflammatory and anti-cancer activities. It alleviates colitis in mice by modulating inflammatory responses, gut barrier integrity, and the microbiome. Masticadienonic acid is a potential protein tyrosine phosphatase 1B (PTP1B) inhibitor and can be used for research on diabetes.

DPM-1001 is an orally bioavailable and non-competitive protein-tyrosine phosphatase (PTP1B) inhibitor (IC50: 100 nM) with the anti-diabetic property.

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.

3-O-Dihydro-p-coumaroyltohogenol functions as a PTP1B inhibitor (IC50 = 6.27 μM), exhibiting anti-diabetic and anti-obesity activities.

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.