npp 1

NPP1-IN-1 is a highly potent inhibitor of NPP enzymes, effectively inhibiting NPP1 with an IC 50 value of 0.15 μM and NPP3 with an IC 50 value of 40 μM [1].

NPP1-IN-2 (compound 3h) is a potent and selective inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase-1 (NPP1), with IC50 values of 0.55 µM for NPP1 and 3.73 µM for NPP3.

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.

NPP3-IN-1 (Compound 3e) is an inhibitor of phosphodiesterase/pyrophosphatase-3 (NPP3), exhibiting IC50 values of 0.24 μM for NPP3 and 1.37 μM for NPP1.

Enpp-1-IN-16 is an inhibitor targeting ENPP1 with potential anti-cancer activity.Enpp-1-IN-16 can be used to study insulin resistance in relation to type II diabetes mellitus and various ENPP1-mediated diseases in the chondrocalcinosis and osteoarthritis classes.

Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase, exhibiting IC50s of 1.36, 1.35, 3.00, 0.88, and 1.02 µM for NPP1, NPP2, NPP3, CA-II, and CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 also demonstrates selective antiproliferative activity for cancer cells.

Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.07, 0.74, 0.33, 0.68, respectively.Enpp/Carbonic anhydrase-IN-2 induced apoptosis.Enpp/Carbonic anhydrase-IN-2 has antiproliferative activity against cancer cells and low cytotoxicity against normal cells.

2OH-BNPP1 is a BUB1 kinase, a Ser/Thr kinase inhibitor, it used for the treatment of cancer.

Enpp-1-IN-23 (compound 27) is an Enpp-1 inhibitor with an IC50 value of 1.2 nM. This compound is utilized in cancer research.

Enpp-1-IN-24 (compound 7) is an ENPP1 inhibitor that, when used in combination with anti-PD-1 antibodies, achieves a tumor growth inhibition rate of 77.7% and enhances survival rates in a mouse model.

ENPP1 inhibitor 32 is an ENPP1 inhibitor with antitumor activity.

Enpp-1-IN-21 (compound 4g) is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1), with IC50 values of 0.45 μM for ENPP1 and 0.19 μM for ENPP3.

Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and exhibits low oral bioavailability. By inhibiting cGAMP degradation, it effectively activates the intracellular STING pathway. Enpp-1-IN-25 can enhance immune cell infiltration and type I interferon response in the tumor microenvironment, thereby increasing the antitumor efficacy of anti-PD-L1 antibodies. It is applicable for research in cancer immunotherapy.

Enpp-1-IN-20 (Compound 31) is an inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) with an IC50 of 0.09 nM. It demonstrates the most potent inhibitory activity in cell assays, with an IC50 of 8.8 nM. Enpp-1-IN-20 significantly inhibits ENPP1 in vitro and activates the STING pathway. This compound can be utilized in cancer research.

Enpp-1-IN-26 (Compound 4e) is an ENPP1 inhibitor with an IC50 value of 0.188 μM. By preventing ENPP1 from hydrolyzing cGAMP, Enpp-1-IN-26 enhances the expression levels of IFN-β in vivo and can be used in studies on metastatic breast cancer.

Enpp-1/3-IN-1 (Compound 5j) serves as an inhibitor for ENPP1 and ENPP3, with IC50 values of 0.59 μM for h-ENPP1 and 0.62 μM for h-ENPP3, respectively. This compound also inhibits e5′NT (CD73) and TNAP, exhibiting IC50 values of 0.89 μM for h-e5′NT, 5.12 μM for r-e5′NT, and 1.68 μM for h-TNAP. Enpp-1/3-IN-1 is applicable in cancer research.

Enpp-1-IN-28 is an ENPP1 inhibitor with IC50 values of 0.188 µM at the molecular level and 0.732 µM at the cellular level. By preventing ENPP1 from hydrolyzing cGAMP, Enpp-1-IN-28 enhances the expression level of IFN-β in vivo, thereby triggering a stronger innate immune response. Enpp-1-IN-28 is applicable in metastatic breast cancer research.

Enpp-1-IN-27 is a selective ENPP1 inhibitor with an IC50 of 14.68 nM, exhibiting approximately 410-fold selectivity over ENPP2 and roughly 10-fold selectivity over ENPP3. This compound stabilizes cGAMP levels and activates the STING pathway, leading to cytokine release and an enhanced innate immune response. In addition, Enpp-1-IN-27 activates ISRE and boosts cGAMP-mediated immune responses, demonstrating significant antitumor effects in 4T1 and CT26 syngeneic mouse models. It is applicable to breast cancer and colon cancer research.

ENPP1 Inhibitor C is an ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor with potential anticancer activity for the study of triple-negative breast cancer.

Enpp-1-IN-14 is a potent inhibitor of Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1) with an IC50 value of 32.38 nM for recombinant human ENPP-1. Enpp-1-IN-14 has anti-tumor activity.

Enpp-1-IN-10 (compound 1) is a potent inhibitor of Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) with a Ki value of 3.866 μM, suitable for anticancer research [1].

3-IN-PP1, a potent protein kinase D (PKD) inhibitor, exhibits pan-PKD inhibitory activity with IC50 values of 108 nM for PKD1, 94 nM for PKD2, and 108 nM for PKD3. Additionally, it serves as a broad-spectrum anticancer agent by inhibiting the growth of various tumor cells. 3-IN-PP1 is utilized in cancer research [1].

Enpp-1-IN-11 (compound 23) is a highly potent inhibitor of Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1), with a Ki value of 45 nM. It demonstrates excellent stability in human and mouse plasma and exhibits low clearance in both human and mouse liver microsomes, holding promise for anticancer research [1].

Enpp-1-IN-12 (compound 43), an orally active and potent inhibitor of ecto-nucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) with a K_i of 41 nM, exhibits anti-tumor activity [1].