dpp-8

Anagliptin (SK-0403) 是一种选择性的二肽酰肽酶 4 抑制剂，IC50=3.8 nM，对 DPP-8/9 的选择性相对较弱，IC50分别为 68 和 60 nM。

Teneligliptin hydrobromide (MP-513(hydrobromide)) 是β2肾上腺素能受体 (β2AR) 阻滞剂，具有抗高血压、抗氧化、清除自由基的活性。

DPP8/9-IN-1 (Compound 16) 是一种具有选择性共价作用的二肽基肽酶 8 和 9 (DPP8/9) 抑制剂，其IC50值分别为 14 和 298 nM。通过含磷酸酯的弹头不可逆地结合活性位点丝氨酸（例如 DPP9 的 S730），DPP8/9-IN-1 阻断底物结合，从而抑制 DPP8/9 介导的蛋白加工。该化合物有望应用于癌症和炎症性疾病的研究。

1G244 是DPP8 9的抑制剂，具有抗动脉粥样硬化和抗骨髓瘤作用的特性。1G244对DPP8和DPP9的IC50值分别为14和53 nM, DPP8和DPP9的Ki 值分别为0.9和4.2 nM

Anagliptin (SK-0403) hydrochloride 是一种有效的、高度选择性的、口服具有活力的二肽酰肽酶 4 (DPP-4) 抑制剂 (IC50: 3.8 nM)，对 DPP-8 (IC50: 68 nM) 和 DDP-9 (IC50: 60 nM) 的选择性相对较弱。

DPP9-IN-1 (Compound 42) 是一种二肽基肽酶 9 (DPP9) 抑制剂，对 DPP9 的 IC50 为 3 nM，而对 DPP8 的 IC50 为 0.6 μM。在 THP-1 细胞中，DPP9-IN-1 可诱导浓度依赖性 LDH 释放。

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.

Alogliptin Benzoate (SYR 322) 是一种有效且特异性的 DPP-4 抑制剂 ，IC50值小于 10 nM，其选择性比 DPP-8 9 高 10,000 倍以上，可用于研究 2 型糖尿病。

Alogliptin (SYR-322) 是一种具有选择性口服活性的DPP-4的抑制剂，IC50值小于 10 nM，比对 DPP-8 和 DPP-9 的抑制性高 10000 倍以上，可研究 2 型糖尿病。

DPP-4-IN-8 (compound 27) 是一种高效的选择性DPP4抑制剂，具有 0.96 μM 的 Ki。该化合物能够抑制 Caco-2 和 HepG-2 细胞中的 DPP4 二肽酶活性，并剂量依赖性地降低 TNF-α、IL-6 和 IL-1β 的表达水平[1]。