protein tyrosine phosphatase(ptp)

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]

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.

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

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.

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].

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.

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.

(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].

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.

MY33-3 is a powerful and specific inhibitor of receptor protein tyrosine phosphatase (RPTP)β/ζ, demonstrating an IC50 value of approximately 0.1 μM. Moreover, MY33-3 exhibits inhibitory activity against PTP-1B with an IC50 value of about 0.7 μM. Additionally, MY33-3 has been shown to effectively decrease ethanol consumption and alleviate neuroinflammation and cognitive dysfunction induced by Sevoflurane.

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.

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).

SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase ( LMW-PTP ) inhibitor ( IC 50 =4 nM, K i =1.2 nM). SPAA-52 can be used in diabete research [1] .

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.

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

VE-PTP-IN-1 (compound 2) is a selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP) with weakly acidic properties, and it plays a role in regulating vascular homeostasis and angiogenesis.

MY33-3 hydrochloride is a potent and selective inhibitor of the protein tyrosine phosphatase RPTPβ ζ (IC50~0.1 μM) and PTP-1B (IC50~0.7 μM). It also reduces ethanol consumption and alleviates Sevoflurane-induced neuroinflammation and cognitive dysfunction.

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

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.

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.

SHP844, a SHP2 inhibitor, exhibits an IC50 value of 18.9 µM. SHP2, a protein tyrosine phosphatase (PTP), plays a crucial role in modulating tyrosine phosphorylation levels, thereby influencing cell proliferation, differentiation, and survival.

PTP1B AKR1B1-IN-1 is a dual inhibitor targeting protein tyrosine phosphatase 1B (PTP1B) and aldose reductase (AKR1B1), with IC50s of 0.06 μM for PTP1B and 4.3 μM for AKR1B1. It also inhibits T-cell protein tyrosine phosphatase (TC-PTP) with an IC50 of 9 μM. This compound acts as an insulin-mimetic in murine myoblasts, reduces AKR1B1-mediated sorbitol accumulation, and aids in managing blood glucose levels and inhibiting type 2 diabetes mellitus (T2DM) development [1].

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.