dpp-iv-in-1

DPP-IV-IN-1 is an effective inhibitor of dipeptidyl peptidase IV (DPP-IV), a serine protease (IC50: 4.6 nM).

DPP IV hCA II-IN-1 is a potent, selective inhibitor of dipeptidyl peptidase IV (DPP IV) and carbonic anhydrase (CA), exhibiting an IC50 of 0.049 μM for DPP IV and K_i values of 0.0361, 0.0428, 0.0941, 0.1328, 0.2615, and 3.034 μM for CA II, CA VB, CA VA, CA IX, CA I, and CA IV, respectively [1].

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

ASP8497 is a potent, long-acting DPP-IV inhibitor that improves glucose tolerance by elevating GLP-1 levels in a glucose-dependent insulin-stimulating manner. The compound is used as a therapeutic agent for impaired glucose tolerance and type 2 diabetes.

DPP, a Platinum(IV) complex with a pterostilbene-derived axial ligand, inhibits the JAK2-STAT3 pathway in breast cancer (BC) cells, demonstrating antiproliferative activity. It activates caspase-3 and cleaved poly ADP-ribose polymerase, inducing apoptosis. Furthermore, DPP enhances the maturation and antigen presentation of dendritic cells and exhibits in vivo safety [1].

VAMP is a tetrapeptide that acts as a competitive dipeptidyl peptidase IV (DPP-IV) inhibitor, exhibiting an IC50 of 1.00 μM and a Kd of 6.89 μM. It effectively targets the DPP-IV-GLP-1 axis and is utilized in the research of type 2 diabetes.

DPP-4 GPR119 modulator 1 (Compound 22) is an orally active compound that acts as both a dipeptidyl peptidase IV (DPP-IV) inhibitor and GPR119 agonist, demonstrating a glucose-lowering effect in blood and moderate inhibition of the hERG channel with an IC50 value of 4.9 µM. This compound is applicable in diabetes research [1].

Fotagliptin benzoate, a Dipeptidyl Peptidase IV (DPP-4) inhibitor with an inhibitory concentration (IC50) of 2.27 nM, demonstrates significant safety in both rat and dog models. It is utilized in Type 2 diabetes mellitus research [1].

Dipeptidyl peptidase-IV (DPP-IV) is an enzyme that deactivates incretin hormones such as glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which are crucial in regulating blood glucose levels. Additionally, DPP-IV functions as a binding protein and ligand for various extracellular molecules. This enzyme is instrumental in research related to diabetes and cancer.

Vildagliptin dihydrate (LAF237 dihydrate) is a potent and stable dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells, exhibiting exceptional oral bioavailability and significant antihyperglycemic activity [1].

DPP-IV-IN-5, derived from Lycium barbarum fruits, demonstrates moderate agonistic activity towards peroxisome proliferator-activated receptor (PPARγ), showing EC50 values between 10.09 and 44.26 μM, and exhibits inhibitory activity against dipeptidyl peptidase-4 (DPPIV) with an IC50 of 47.13 μM [1].