ptp-β

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].

PTP inhibitor 1 is an inhibitor of cell-permeable protein tyrosine phosphatase (PTP) that covalently binds the catalytic domain of the Src homology region 2 domain-containing phosphatase (SHP-1(ΔSH2)),with Ki of128 μM.

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor that also inhibits lysine methyltransferase SETD8 (KMT5A) and various cytochrome P450 (P450) isoforms.

Purine riboside triphosphate, a derivative of purine riboside, exhibits structural similarity to adenosine. This naturally occurring base analog possesses inhibitory effects on carcinogenic growth, particularly in cancer ascites cells, by strongly impeding RNA and DNA synthesis.

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.

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.

7-BIA is a receptor-type protein tyrosine phosphatase D (PTPRD) inhibitor with anti-addictive properties, and is utilized in neuropathic pain research.

Cyt-PTPε Inhibitor-1 (A Inhibitor-1) is an inhibitor of cytosolic protein tyrosine phosphatase ε. Cyt-PTPε Inhibitor-1 blocks the dephosphorylation of c-Src and exhibits anti-osteoclastic activity.

DJ001 is a highly specific, selective, and non-competitive protein tyrosine phosphatase σ (PTPσ) inhibitor with an IC50 of 1.43 μM, and it promotes the regeneration of hematopoietic stem cells.

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.

Etidronic acid (HEDP) is a diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover.

Sodium etidronate (Didronel) is a synthetic therapeutic diphosphonate analog of endogenous pyrophosphate. As a member of the family of drugs known as bisphosphonates, Sodium etidronate differs from endogenous pyrophosphate in its resistance to enzymatic hydrolysis. This agent adsorbs to hydroxyapatite cells and reduces the number of osteoclasts, thereby inhibiting abnormal bone resorption. Etidronate may also directly stimulate bone formation by osteoblasts.

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].

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).

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.

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.

Purine riboside-5'-O-triphosphate sodium is an active metabolite of Nebularine and acts as an inhibitor of DNA primase ATP and GTP polymerization activities, with IC50 values of 35 µM and 28 µM, respectively. It also inhibits calmodulin-dependent protein kinase II (CaMKII), with a Ki value of 590 µM.

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).

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.

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.

LMPTP Inhibitor 1 Dihydrochloride is a compound selectively targeting low molecular weight protein tyrosine phosphatase (LMPTP), exhibiting potent inhibitory activity with an IC50 value of 0.8 μM for LMPTP-A.

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

MY10, a potent and orally active inhibitor of the receptor protein tyrosine phosphatase (RPTPβ/ζ), effectively reduces binge-like ethanol consumption and diminishes the rewarding effects of ethanol.