FAP

Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.

Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM).

BR103354 is a selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 14 nM against human FAP. It effectively restores levels of phosphorylated ERK and Glut1, reduces non-fasting blood glucose concentrations, and enhances glucose tolerance, while also decreasing hepatic triglyceride content. This compound demonstrates potential in alleviating hepatic steatosis and fibrosis, making it a valuable tool for research into type 2 diabetes and non-alcoholic steatohepatitis.

FAPI-4 is a potent inhibitor of fibroblast activation protein (FAP), targeting FAP with high specificity. This compound demonstrates significant potential in cancer research, particularly in improving diagnostic imaging. The use of 68Ga-FAPI-4 in PET/CT scans offers enhanced tumor-to-background contrast ratios, making it an effective tool for visualizing various types of tumors.

PRMT5-IN-53 is a potent, orally bioavailable inhibitor of PRMT5, exhibiting pIC50 values of ≥ 9.7 against both human and mouse PRMT5. It demonstrates high affinity for the PRMT5:MEP50 complex with a KD of 11.3 pM. This compound effectively inhibits PRMT5 in the intestines of murine models, leading to a significant reduction in the number and size of polyps while minimizing systemic hematological toxicity. PRMT5-IN-53 is particularly valuable for research in colorectal cancer, especially in the context of familial adenomatous polyposis (FAP).

FAPI-mFS is an irreversible inhibitor of fibroblast activation protein (FAP), which targets FAP's enzymatic activity to enhance cancer cell uptake and retention through covalent binding. This compound is particularly useful for cancer imaging and therapy when labeled with radioisotopes such as 68Ga or 177Lu. Additionally, FAPI-mFS serves as a valuable tool in the synthesis and research of radionuclide-drug conjugates (RDCs), facilitating advancements in targeted cancer treatments.

NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor designed for targeted tumor imaging. This compound effectively binds to FAP, facilitating the visualization of tumors with high detection efficacy. NOTA-FAPI demonstrates superior imaging quality, making it a valuable tool for cancer research and diagnostic applications.

UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP), exhibiting an IC50 of 3.2 nM. In addition to FAP inhibition, UAMC-1110 also affects prolyl oligopeptidase (PREP) with an IC50 of 1.8 μM. This compound is primarily utilized in research applications targeting tumor microenvironment modulation and fibroblast-related pathologies.

AZD2389 is a potent and orally active inhibitor of fibroblast activation protein (FAP). It has demonstrated significant efficacy in research related to metabolic dysfunction-associated steatohepatitis. This compound serves as a valuable tool for studying the role of FAP in metabolic diseases and may aid in the development of therapeutic strategies aimed at targeting metabolic liver disorders.

FAP-IN-2 is a selective inhibitor of fibroblast activation protein (FAP), characterized by its isonitrile structure. This compound exhibits significant potential for therapeutic applications aimed at cancer treatment as well as for imaging purposes. When labeled with technetium-99m (99mTc), FAP-IN-2 can be utilized for targeted tumor single-photon emission computed tomography (SPECT) imaging, enhancing the visualization of FAP-expressing tumors.

ARI-3099 is a selective fibroblast activation protein (FAP) inhibitor that targets the proteolytic activity of FAP, preventing the cleavage of human FGF-21 between residues P171 and S172. By inhibiting this activity, ARI-3099 extends the half-life of circulating human FGF-21 in murine models. This compound is relevant for research focused on type 2 diabetes and various metabolic disorders, making it a valuable tool for investigating therapeutic strategies in these areas.

PNT6555 is a selective inhibitor of fibroblast activation protein-α (FAP), with notable antitumor activity. This compound is particularly valuable in the study of FAP-positive tumors, facilitating imaging applications that aid in tumor characterization and monitoring. Its specificity for FAP makes it a significant tool for cancer research, advancing the understanding of tumor microenvironments and potential therapeutic strategies.

DOTAGA-FAP-2286-ALB is a selective inhibitor of fibroblast activation protein (FAP) with an IC50 value of 67.5 nM. This compound enhances tumor retention through its interaction with albumin, thereby prolonging blood circulation and increasing the stability of radiometal complexes such as 111In and 225Ac. DOTAGA-FAP-2286-ALB is of particular interest for research applications in radionuclide therapy (TRT) targeting FAP-positive solid tumors.

FAPI-2 is a quinoline-based inhibitor targeting fibroblast activation protein (FAP). It exhibits rapid tracer kinetics and is suitable for use as a PET tracer in cancer diagnosis, labeled with 68Ga. Notably, FAPI-2 does not require fasting preparation and remains effective regardless of blood glucose levels, making it a valuable tool for oncological research and imaging applications.

FAP-IN-4 is a fibroblast activation protein (FAP) inhibitor that serves as an 18F-labeled PET tracer targeting FAP. This compound demonstrates significant potential in cancer research by facilitating the visualization of FAP-expressing tumors, thereby aiding in the understanding of tumor biology and treatment responses. It can be utilized in studies focused on tumor microenvironments and therapeutic interventions targeting FAP.

SB03178 is a selective inhibitor of fibroblast activation protein-alpha (FAP). This compound demonstrates significant potential in cancer research, particularly in modulating tumor microenvironments and enhancing the efficacy of cancer therapies. Additionally, SB03178 can be conjugated with DOTA for further applications in targeted imaging and therapeutic strategies.

FAP-IN-1 is a selective fibroblast activation protein (FAP) inhibitor that demonstrates potent activity with an IC50 value of 3.3 nM. This compound is valuable for investigating the role of FAP in the tumor microenvironment and its implications in cancer biology. FAP-IN-1 can be utilized in various research applications aimed at elucidating the mechanisms of tumor progression and the development of targeted therapeutic strategies.

QI-18 is a potent inhibitor of fibroblast activation protein (FAP) with an IC50 of 0.50 nM, exhibiting 6.5-fold increased potency compared to UAMC-1110. Its high affinity makes QI-18 suitable for the development of radiotracers with enhanced tumor selectivity and dosage for tumor diagnosis and research applications. This compound plays a significant role in studies focusing on tumor microenvironments and potential therapeutic interventions targeting FAP.

FAPI-P8PN is a selective inhibitor of fibroblast activation protein (FAP), exhibiting an IC50 value of 3.6 nM. This compound is particularly useful for investigating FAP-overexpressing solid tumors, providing insights into tumor microenvironments and potential therapeutic approaches. Its targeted activity makes it a valuable tool in cancer research aimed at developing FAP-focused therapies.

FAP-IN-8 is a selective inhibitor of fibroblast activation protein (FAP) and prolyl endopeptidase (PREP), exhibiting pIC50 values of 10.08 and 8.99 for these targets respectively. With IC50 values of 1 nM for FAP and 0.08 nM for PREP, FAP-IN-8 demonstrates potent inhibition that supports its utility in cancer research. This compound is valuable for studying tumor microenvironment interactions and the therapeutic targeting of cancer-associated fibroblasts.

FAP-IN-7 is a selective inhibitor of fibroblast activation protein (FAP), a serine protease implicated in tumor progression and immune modulation. This compound effectively hinders FAP activity, contributing to the investigation of cancer-associated fibroblasts in the tumor microenvironment. FAP-IN-7 is valuable for research applications focused on understanding cancer biology, developing therapeutic strategies, and exploring the role of FAP in various disease states.

DOTA-NI-FAPI-04 is a fibroblast activation protein (FAP) inhibitor with an IC50 of 7.44 nM, designed to enhance tumor uptake and retention using hypoxia-sensitive nitroimidazole groups. This compound forms stable complexes with metallic isotopes such as 68Ga and 177Lu through its DOTA moiety, serving as a foundation for the creation of radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04). DOTA-NI-FAPI-04 is valuable for research in cancer diagnostics, exploring the tumor microenvironment, and radionuclide therapy, particularly in the context of tumor stroma and hypoxic regions.

3BP-3580 is a potent inhibitor of fibroblast activation protein (FAP), exhibiting a pIC50 of 8.6. This compound is relevant for cancer research, specifically in studies investigating tumor microenvironments and the role of FAP in cancer progression. Its ability to modulate FAP activity makes it a valuable tool for exploring therapeutic strategies in oncology.

FAPI-X5 is a selective inhibitor of fibroblast activation protein (FAP) that binds to the catalytic domain, effectively disrupting its enzymatic activity through hydrogen bonding and π-π interactions. This compound exhibits significant cytostatic effects on glioblastoma tumors, resulting in reduced tumor growth without inducing regression. When radiolabeled with 68Ga, FAPI-X5 serves as a highly effective PET tracer, facilitating rapid tumor localization and high-contrast imaging in glioblastoma models. Additionally, FAPI-X5 can be labeled with 177Lu or 47Sc, functioning as a targeted radionuclide agent with extended tumor retention, making it valuable for glioblastoma research applications.

BR102910 is a selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 2 nM. Additionally, BR102910 exhibits inhibition of prolyl oligopeptidase (PREP) with an IC50 of 49.00 μM. This compound is primarily used in research focusing on type 2 diabetes and related metabolic disorders, making it a valuable tool for exploring FAP's role in these conditions.

FAP-PI3KI1 is a fibroblast-activated protein (FAP) inhibitor that selectively targets the phosphoinositide 3-kinase (PI3K) pathway in FAP-expressing human cells. This compound effectively inhibits collagen synthesis and reduces collagen deposition, making it a valuable tool for research in idiopathic pulmonary fibrosis (IPF) and related fibrotic conditions. Its targeted action facilitates investigating the role of the PI3K signaling pathway in fibrosis and offers potential insights into therapeutic strategies for IPF.