fap inhibitor

BR102910 (4-Thiazolecarboxamide, N-[2-[(2S)-2-cyano-4,4-difluoro-1-pyrrolidinyl]-2-oxoethyl]-2-[(3,4-dichlorophenyl)methyl]-) 是一种选择性的成纤维细胞活化蛋白（FAP）的抑制剂。

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.

Ac-Gly-BoroPro is a selective FAP inhibitor (Ki: 23 nM).

FAPI-2 是一种基于放射性示踪剂 FAP 标记的成纤维细胞活化蛋白特异性抑制剂，具有抗癌活性，可用于研究胰腺癌。

FAPI-4 是一种成纤维细胞激活蛋白 (FAP) 抑制剂，是FAPI配体，在原发性肝癌肝细胞癌（HCC）的PET成像中显示出强烈的肝脏摄取作用，常用于 PET 成像，可用于研究癌症。

FAPI-mFS，作为一种不可逆的成纤维细胞活化蛋白 (FAP) 抑制剂，通过与FAP形成共价结合来提高在癌细胞中的摄取与滞留。此化合物在标记放射性68Ga或177Lu后，可应用于癌症的成像与治疗领域。

3BP-3580 是一种靶向成纤维细胞活化蛋白 (FAP) 的抑制剂 (pIC50: 8.6)，适用于癌症研究。

DOTA-NI-FAPI-04 是一种强效的FAP抑制剂 (IC50= 7.44 nM)，通过结合FAP靶向机制和携带缺氧敏感基团 (硝基咪唑)，显著增加了在肿瘤内的摄取和滞留。该化合物利用 DOTA 螯合金属同位素(如68Ga和177Lu)，可生成放射性探针([68Ga]Ga DOTA-NI-FAPI-04 和 [177Lu]Lu DOTA-NI-FAPI-04)，推动肿瘤诊断与治疗剂研究。在癌症成像以及肿瘤微环境研究中，它具有双重靶向潜力，尤其适合研究肿瘤基质和低氧区域协同效应的应用。

FAPI-34, a fibroblast-activating protein (FAP) inhibitor, boasts advantageous pharmacokinetic and biochemical attributes.

BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, in association with increased intact form of hFGF21 in ob ob mice. BR103354 acts as an effective FAP inhibitor in vitro and in vivo, thereby demonstrating its potential application as an anti-diabetic and anti-NASH agent.

NOTA-FAPI-4 is an analogue of FAPI-4 and a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI-4 is useful in the diagnosis or treatment of a disease characterized by overexpression of fibroblast activation protein (FAP). NOTA-FAPI-4 can be used as a PET tracer for detection of diseases or disorders related to fibroblast activation protein.

FAP-PI3KI1 是一种成纤维细胞活化蛋白 (FAP) 靶向 PI3K 抑制剂，可选择性靶向表达 FAP 的人特发性肺纤维化 (IPF)细胞并有效抑制胶原蛋白合成，减少胶原蛋白沉积。

NH2-UAMC1110 TFA 是 UAMC1110 带有氨基丁氧基的衍生物，用于合成 FAPI-QS。UAMC1110 是一种新型选择性成纤维细胞活化蛋白 (fap) 抑制剂，对相关二肽基肽酶 (dpps) dppiv、dpp9、dppii、和（prep）表现出低纳摩尔抑制力和高选择性。

FAP-IN-2 TFA为99mTc标记的异腈类FAP抑制剂衍生物，适用于肿瘤显像。

SP-13786 是成纤维细胞活化蛋白 (FAP)和脯氨酰寡肽酶 (PREP)的抑制剂，IC50值分别为3.2 nM和1.8μM。

FAP-IN-1，一种FAP (成纤维细胞激活蛋白)抑制剂，具有3.3 nM的IC50值，适用于癌症研究。

FAP-IN-2，一种标记有99mTc的含异腈FAPI（成纤维细胞活化蛋白）抑制剂衍生物，适用于肿瘤显像。

FAPI-2 TFA为一种针对成纤维细胞活化蛋白（FAP）的抑制剂，适用于癌症研究领域。

ARI-3144 是一种成纤维细胞激活蛋白 (FAP) 的优良底物，同时也是一种FAP激活的蛋白酶体抑制剂，适用于实体瘤研究。

SB03178是一种成纤维细胞活化蛋白-α (FAP) 的抑制剂，可通过与DOTA偶联，用于癌症研究。

Anti-MouseFAPAntibody (73.3) 是源自小鼠的IgG1, κ 抗体抑制剂，专门针对小鼠FAP。