ntpdase

Ticlopidine (PCR 5332) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor.

h-NTPDase-IN-2 is a broad-spectrum NTPDase inhibitor that inhibits multiple h-NTPDas isoforms.

h-NTPDase-IN-3 is an h-NTPDase inhibitor that inhibits h-NTPDase1, h-NTPDase2, h-NTPDase3 and h-NTPDase8.

NTPDase/NPP1-IN-1 is an inhibitor of ectonucleotidase (NTPDase) and phosphodiesterase-1 (NPP1), with IC50 values of 0.28, 0.92, 0.82, and 0.73 μM for h-NTPDase1, h-NTPDase2, h-NTPDase3, and h-NPP1, respectively. This compound acts as a membrane interaction agent, localizing to the plasma membrane and interacting with cancer cells. NTPDase/NPP1-IN-1 is applicable in breast cancer research.

NTPDase-IN-1 (compound 5a) is a selective inhibitor of NTPDase enzymes with IC50 values of 0.05 μM, 0.23 μM, and 0.54 μM against h-NTPDase-1, h-NTPDase-2, and h-NTPDase-8, respectively. It exerts non-competitive inhibition on h-NTPDase-1 and h-NTPDase-2, with a Km value of 21 μM for h-NTPDase-1. This compound is useful for investigating conditions such as cancer, immunologic disorders, and bacterial infections [1].

NTPDase-IN-3 (Compound 5e), an inhibitor of NTPDase, exhibits IC50 values of 0.38 μM (NTPDase3), 0.05 μM (NTPDase8), 0.21 μM (NTPDase1), and 1.07 μM (NTPDase2). It is utilized in cancer and thrombosis research [1].

NTPDase-IN-2 (compound 5g) selectively inhibits NTPDase-2 and NTPDase-8 with IC50 values of 0.04 µM and 2.27 µM, respectively, and exhibits non-competitive inhibition toward h-NTPDase-1 and h-NTPDase-2, with a Km of 74 µM for h-NTPDase-2. This compound is applicable in researching cancer, immunological disorders, and bacterial infections [1].

h-NTPDase-IN-4 is a pan-inhibitor of NTPDase, which can inhibit h-NTPDase1, 1h-NTPDase2, h-NTPDase3, h-NTPDase8. The IC50 values were 3.58 μM, 10.21 μM, 0.13 μM and 13.57 μM, respectively.

h-NTPDase-IN-1 (Compound 3i) is an inhibitor of human NTPDase with IC50 values of 2.88 μM for h-NTPDase1 and 0.72 μM for h-NTPDase3, indicating potential utility for thrombosis, inflammation, diabetes, and cancer research [1].

h-NTPDase-IN-5 (compound 3b) serves as a pan-inhibitor of NTPDase, exhibiting inhibitory concentration 50 (IC50) values of 1.10 μM [h-NTPDase1], 44.73 μM [h-NTPDase2], 26.14 μM [h-NTPDase3], and 0.32 μM [h-NTPDase8].

h-NTPDase8-IN-1 is a specific aminosulfonylbenzamide inhibitor of h-NTPDases8 (IC 50 = 0.28 ± 0.07 μM). h-NTPDase8-IN-1 can be used to study diseases brought about by aberrant h -NTPDase expression.

TcNTPDase1-IN-1 (compound 16) serves as an inhibitor of nucleoside triphosphate diphosphohydrolase 1 (TcNTPDase1) from Trypanosoma cruzi in vitro. This compound is applicable in research related to antibacterial, antitoxic, and antitumor activities.

Sodium metatungstate (Sodium polyoxotungstate) is a potent inhibitor of ecto-nucleoside triphosphate diphosphohydrolase (NTPDase), with Ki values of 2.58 μM for NTPDase 1, 3.26 μM for NTPDase 3, and 28.8 μM for NTPDase 2.

PSB-06126 is a selective NTPDase3 (nucleotide triphosphate diphosphate hydrolase 3) inhibitor with a Ki of 1.5 μM for rat NTPDase3 and an IC50 of 7.76 μM for human NTPDase3 (Ki = 4.39 μM). It is suitable for investigating cancer and immune-related diseases.

NTPDase inhibitor

ARL 67156 is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12 μM, respectively[1]. ARL67156 trisodium salt is an inhibitor of ecto-ATPase.

PSB-6426 is the first potent and selective human nucleoside triphosphate diphosphohydrolase-2 inhibitor.

PSB-16131 is the Lp1NTPDase inhibitor.

Sodium metatungstate (Sodium polyoxotungstate; POM-1) hydrate is an inhibitor of NTPDase, with Ki values for NTPDase1 (CD39), NTPDase 3, and NTPDase 2 being 2.58 μM, 3.26 μM, and 28.8 μM, respectively. It exhibits anti-inflammatory and anticancer properties and inhibits ATP hydrolysis while also blocking central synaptic transmission.

Ticlopidine-d6 hydrochloride is a deuterium-labeled version of Ticlopidine hydrochloride. Ticlopidine (PCR 5332) hydrochloride acts as an antithrombotic prodrug and non-competitive allosteric CD39 inhibitor with an IC50 of 81.7 μM. It inhibits NTPDase isoenzymes, showing IC50 values of 170 μM for NTPDase2 and 149 μM for NTPDase3. Additionally, Ticlopidine hydrochloride acts as an inhibitor of the human liver enzyme CYP2C19 and inhibits CYP2C9 and CYP3A4 with IC50 values of 26.0 μM and 32.3 μM, respectively.

Apyrase is an extracellular nucleoside triphosphate diphosphate hydrolase (NTPDase) that catalyzes the hydrolysis of ATP and ADP to form AMP and inorganic phosphate. Apyrase is commonly used to regulate extracellular nucleotide levels and plays a significant role in studies of platelet aggregation, purine signaling, and cellular energy metabolism.