tyrosine phosphatase 1b

1. Stearic acid (Cetylacetic acid) can reduce metastatic tumor burden. 2. Stearic acid leads to dramatically reduced visceral fat likely by causing the apoptosis of preadipocytes. 3. Stearic acid and its derivatives have been used as gelators in food and pharmaceutical gel formulations. 4. Stearic acid is a potent phosphatase 1B inhibitor, possibly causing an enhancement in the insulin receptor signaling to stimulate glucose uptake into adipocytes. 5. Stearic acid has the potential to increase dry matter intake and yields of milk and milk components, without affecting conversion of feed to milk, body condition score, or body weight.

Rhein-8-O-beta-D-glucopyranoside(Rhein-8-glucoside calcium (Rhein-8-glucoside calcium salt) salt) shows moderate bioactivity against human Protein Tyrosine Phosphatase 1B (hPTP1B) in vitro.

(Rac)-RK-682 is a racemic mixture that functions as a protein tyrosine phosphatases (PTPases) inhibitor, specifically targeting protein tyrosine phosphatase 1B (PTP-1B), low molecular weight protein tyrosine phosphatases (LMW-PTP), and cell division cycle 25B (CDC-25B), with inhibitory concentrations (IC50s) of 8.6 μM, 12.4 μM, and 0.7 μM, respectively [1].

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

KY-226 is a potent inhibitor of protein tyrosine phosphatase 1B (PTP1B)(IC50: 0.25 μM,)

bpV(phen) is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor (IC50s: 343 nM, 920 nM, and 38 nM for PTP-β, PTP-1B, and PTEN).

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 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B) with an IC50 of approximately 1 μM.

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).

(Rac)-Hesperetin is the racemic mixture of hesperetin. Hesperetin is a potent, broad-spectrum inhibitor of human UGT activity and an apoptosis inducer. (Rac)-Hesperetin inhibits protein tyrosine phosphatase 1B (IC₅₀ = 20.16 µM).

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.

Isotanshinone IIA, could non-competitively inhibit Protein Tyrosine Phosphatase 1B (PTP1B) activity with an IC50 0f 11.4 μM. is an abietane-type diterpene metabolite.

IONIS PTP1BRx (ISIS 404173) acts as an antisense inhibitor of protein tyrosine phosphatase 1B (PTP-1B). This compound exhibits anti-diabetic properties, making it suitable for research into insulin resistance related to obesity and type 2 diabetes.

bpV(bipy) hydrate acts as an inhibitor for phosphoinositide 3-phosphatase (PTEN) and protein tyrosine phosphatases PTP-β and PTP-1B, with IC50 values of 18, 60.3, and 164 nM, respectively.

PTP1B-IN-29 (Compound A2B5) is a phosphatase inhibitor that targets protein tyrosine phosphatase 1B (PTP1B), TCPTP, and λPPase, with IC50 values of 1.27 μM, 4.38 μM, and 8.79 μM, respectively. PTP1B-IN-29 is applicable in the research of diabetes and obesity.

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.

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).

PTP1B-IN-26 (compound 7a) is a derivative of phenylthiourea-semicarbazone-aryloxy-1,2,3-triazolyl-N-phenylacetamide. It acts as a competitive inhibitor of protein tyrosine phosphatase 1B (PTP-1B) and is applicable in type 2 diabetes research.

MY17 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 0.41±0.05 μM. It alleviates insulin resistance induced by palmitic acid (PA) by enhancing the expression of phosphorylated insulin receptor substrate (IRS1) and protein kinase B (AKT). By binding to PTP1B, MY17 inhibits its activity, thereby improving insulin signaling and exhibiting antidiabetic properties. MY17 is useful in the study of type 2 diabetes.

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.

CX08005 is a protein tyrosine phosphatase 1B inhibitor. CX08005 reduces hepatic lipid accumulation and microcirculatory impairment associated with non-alcoholic fatty liver disease.

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)

Ficusonolide exhibits significant antidiabetic activity through its interactions with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.