enpp 1 in 1

Enpp-1-IN-1 is an inhibitor of Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1)

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-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].

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].

Enpp-1-IN-13 is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP) inhibitor that is able to act on ENPP1 (IC50: 1.29 μM) and ENPP3 (IC50: 20.2 μM), exhibiting anticancer effects.

Compound 88a (Enpp-1-IN-15) is an inhibitor of Ectonucleotide Pyrophosphatase/Phosphodiesterase 1 (Enpp-1), exhibiting a Ki value of 0.00586 nM [1].

Enpp-1-IN-17 (example 274) is a potent inhibitor of ENPP1, with inhibition constants (Ki values) ranging from 100 nM to 1 μM for cGAMP hydrolysis and greater than 1 μM for ATP hydrolysis, demonstrating a selectivity ratio of over 6.4 favoring cGAMP hydrolysis inhibition [1].

Enpp-1-IN-19 (compound 29f) is an orally active inhibitor of ENPP1 that effectively blocks cGAMP hydrolysis with an IC50 of 68 nM. It not only enhances anti-PD-L1 responses and curtails tumor growth in CT26 syngeneic models but also boosts STING-mediated type I interferon responses. Additionally, Enpp-1-IN-19 fosters immune memory and aids in preventing tumor recurrence [1].

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-1-IN-22 is a potent oral bioavailable prodrug of the ENPP1 inhibitor dimeric paraformaldehyde ester, exhibiting anticancer activity.

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.

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.

Enpp-1-IN-29 (Compound 1) is a highly selective inhibitor of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) with an IC50 of 0.05 nM. This compound shows potential for research into cancers with overexpressed ENPP1, such as breast cancer, head and neck cancer, and metastatic chromosomal instability tumors, as well as immunological disorders like autoimmune diseases and tumor immune evasion.

Enpp-1-IN-30 (compound 44a) is an ENPP1 inhibitor with oral bioavailability and a human IC50 of 13.1 nM. It prevents cGAMP degradation and activates the STING pathway. Enpp-1-IN-30 induces cytokine release to enhance the innate immune response and demonstrates antitumor efficacy in syngeneic mouse models. This compound is applicable for 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.