pp-1

PP1 (AGL 1872), a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.

Calyculin A ((-)-Calyculin A), a toxicant in the Japanese marine sponge CDiscodermia calyxC, is a selective and potent inhibitor of protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A), inducing hyperactivation of cryopreserved bovine spermatozoa and inhibiting radiation-induced gammaH2AX DNA repair disease in human lymphocytes. gammaH2AX DNA repair foci in human lymphocytes.

Okadaic acid is a potent polyether marine toxin that primarily accumulates in the digestive glands of marine mollusks. It is a highly effective and selective inhibitor of protein phosphatases (PPs). By inhibiting these phosphatases, okadaic acid increases the phosphorylation levels of various proteins, acts as a tumor promoter, and induces tau protein phosphorylation. It can be used to establish models of Alzheimer’s disease and skin cancer.

3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor. In cells expressing analog-sensitive Plk1 alleles, 3MB-PP1 blocks mitotic progression and cell division arise by targeting Plk1. 3MB-PP1 specifically inhibits analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase with IC50 of 2 μM. 3MB-PP1 can be used for the research of cell division and hypha formation of Candida albicans.

1-NM-PP1 (PP1 Analog II) is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.

1-Naphthyl PP1 (1-NA-PP 1) is a selective Src inhibitor, targeting v-Src and c-Fyn, c-Abl, CDK2, and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18, and 22 μM, respectively.

3BrB-PP1 is an ATP-competitive analog that exhibits specific inhibitory activity towards protein kinase, particularly effective against protein kinases with mutations in the ATP-binding pocket, such as the Thr97 mutation within Sty1's ATP-binding pocket.

1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases v-Src.

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].

DSPE-PEG1000-PP1 is a PEG compound composed of DSPE and the PP1 peptide. The PP1 peptide targets inflammatory atherosclerotic plaques. DSPE-PEG1000-PP1 is suitable for drug delivery applications.

DSPE-PEG5000-PP1 is a PEG compound composed of DSPE and the PP1 peptide, which targets inflammatory atherosclerotic plaques. It can be used for drug delivery.

DSPE-PEG2000-PP1 is a PEG compound composed of DSPE and the PP1 peptide. The PP1 peptide specifically targets inflammatory atherosclerotic plaques. DSPE-PEG2000-PP1 is utilized in drug delivery applications.

DSPE-PEG3400-PP1 is a PEG compound composed of DSPE and PP1 peptide. The PP1 peptide targets inflammatory atherosclerotic plaques. DSPE-PEG3400-PP1 can be utilized for drug delivery.

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-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.

DPP-1-IN-1 (Compound 14) is an orally active inhibitor of cathepsin C (also known as dipeptidyl peptidase I), with an IC50 of 5.31 nM. It effectively suppresses downstream neutrophil elastase activity in neutrophils mediated by cathepsin C. DPP-1-IN-1 is applicable for studying inflammatory diseases.

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.