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].

PDE IV-IN-1 is a potent phosphodiesterase 4 (PDE4) inhibitor with anti-inflammatory activity for the treatment of asthma, chronic obstructive pulmonary disease and other inflammatory diseases, and is a potential compound for the study of depression.

1-Dehydroxybaccatin IV is a natural product from Taxus mairei.

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

DPP-4-IN-1 (compound d1) is a highly potent inhibitor of DPP-4 (dipeptidyl peptidase 4) with an IC 50 of 49 nM, making it suitable for diabetes research [1]. It shares structural similarities to Alogliptin and can be effectively utilized for studying diabetes-related mechanisms.

DPP-IV-IN-2 (H-Lys(4-nitro-Z)-pyrrolidide) is an inhibitor of both DP8/9 and dipeptidyl peptidase IV (IC50s: 0.1 and 0.95 μM).

Topoisomerase IV inhibitor 2 (compound 7d) is a potent inhibitor of DNA topoisomerase IV (TOPO IV), exhibiting IC50 values of 0.23 μM for TOPO IV and 0.43 μM for DNA gyrase. It also demonstrates antibacterial efficacy, with minimum inhibitory concentrations (MICs) of 0.972 μM against Staphylococcus aureus Newman and 0.608 μM against Escherichia coli ATCC8739 [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.

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].

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].

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.

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].

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