dpp-2

DPP-21是一种能有效抑制微管蛋白聚合的化合物（IC50: 2.4 μM）。它对多种癌细胞系表现出显著的抗增殖效果，各自的IC50值分别为0.38 nM （HCT116）、11.69 nM （B16）、5.37 nM （HeLa）、9.53 nM （MCF7）、8.94 nM （H23）和9.37 nM （HepG2）。DPP-21能引起癌细胞在有丝分裂G2 M期的细胞周期停滞，并诱导肿瘤细胞走向凋亡（Apoptosis），此作用通过降低Bcl-2和提高Bax蛋白水平实现。

Iptacopan (LNP023) 是一种与factor B 亲和力较高的抑制剂,其KD值为7.9 nM，其IC50:值为10 nM。

Cameglipti, a dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type 2 diabetes.

Denagliptin是一种小分子二肽基肽酶IV（DPP-4）抑制剂，可用于治疗内分泌于代谢疾病，可用于研究2型糖尿病。

TS-021 是一种具有选择性的二肽基肽酶 4 (DPP-4) 抑制剂，具有抗糖尿病活性，可用于研究2 型糖尿病。

Trelagliptin (SYR-472) 是一种有效的，具有口服活性的DPP-4抑制剂，IC50=4 nM。它可以改善体内血糖控制，能够用于2 型糖尿病 (T2DM) 的研究。

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。

Saxagliptin hydrate (Onglyza hydrate) 是一种选择性，竞争性，可逆性和口服活性的二肽基肽酶 4 (DPP-4) (Ki= 0.6-1.3 nM) 抑制剂。Saxagliptin hydrate 能够用于 2 型糖尿病的研究。

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。

Nateglinide (Senaglinide) 是 D-苯丙氨酸的一种衍生物，是口服有效的、短效促胰岛素释放化合物，也是 DPP IV 抑制剂。 Nateglinide 抑制胰岛 β 细胞中 ATP 敏感的 K+通道。Nateglinide 在 2 型糖尿病中具有研究价值。

Vildagliptin (LAF237) 是一种选择性二肽基肽酶IV (DPP-IV) 抑制剂，在人 Caco-2 细胞中抑制 DPP-IV 的IC50为 3.5 nM。它具有出色的口服生物利用度和降血糖活性。

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) 是一种有效的 DPP-IV 抑制剂，在 Caco-2 细胞提取物中的 IC50 为 19 nM。

Trelagliptin succinate (SYR-472 succinate) 是一种有效的，具有口服活性的DPP-4抑制剂，IC50=4 nM。它可以改善体内血糖控制，能够用于2 型糖尿病(T2DM) 的研究。

Sitagliptin (MK0431) 是一种有效的 DPP4抑制剂，在 Caco-2 细胞中，IC50值为 19 nM。它是一种新型口服降糖药，可单独使用或与二甲双胍或噻唑烷二酮联合用于治疗 2 型糖尿病。

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-4-IN-11 (compound 10) 为一种抗2型糖尿病活性的口服DPP-4抑制剂,其IC50值为2.75 μM.该化合物通过抑制α-葡萄糖苷酶(IC50=3.02 μM)和α-淀粉酶(IC50=3.3 μM)来降低血糖.

Vildagliptin-d7 是 Vildagliptin 的氘代化合物。Vildagliptin 的 CAS 号为 274901-16-5。Vildagliptin 是一种选择性二肽基肽酶IV (DPP-IV) 抑制剂，在人 Caco-2 细胞中抑制 DPP-IV 的IC50为 3.5 nM。它具有出色的口服生物利用度和降血糖活性。

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.

Saxagliptin is a new oral hypoglycemic of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Saxagliptin is a competitive DPP4 inhibitor that slows the inactivation of the incretin hormones and reducing fasting and postprandial glucose conce

BMS-767778, a DPP-4 inhibitor, is used potentially for the treatment of type 2 diabetes.

Antidiabetic agent 2 (Compound 56) 作为一种葡萄糖摄取促进剂，能有效地抑制DPP-4, PTP-1B, α-淀粉酶和α-葡萄糖苷酶，其IC50s分别达到0.036、0.042、0.241、0.185 μM，表现出显著的降血糖作用。

DPP-4 GPR119 modulator 2 是二肽基肽酶 IV (DPP-IV) 抑制剂 (IC50: 0.22 μM)，也是一种 GPR119 激动剂 (EC50: 0.95 μM)。DPP-4 GPR119 modulator 2 能够用于研究糖尿病。

VAMP 是一种四肽和竞争性二肽基肽酶 IV (DPP-IV) 抑制剂，其 IC50 为 1.00 μM，Kd 为 6.89 μM。VAMP 有效靶向 DPP-IV-GLP-1 轴，适用于 2 型糖尿病的研究。

Fluostatin A是一种最初从链霉菌中分离出的荧光酮类化合物。它对二肽基肽酶3（DPP-3）的选择性抑制作用优于对DPP-1、DPP-2和DPP-4的抑制作用（IC50s分别为0.44, >100, >100, 和 >100 µg/ml）。