FAP

Cat. No.

A12986

CAS No.

886992-99-0

Ac-Gly-BoroPro

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

Cat. No.

A14079

CAS No.

149682-77-9

Talabostat

Synonyms: Val-boroPro; PT100

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).

Cat. No.

A24652

CAS No.

2374782-02-0

FAPI-4

Synonyms: DOTA-fapi-04

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.

Cat. No.

A36758

CAS No.

2505339-87-5

BR103354

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.

Cat. No.

A41622

CAS No.

2803421-14-7

3BP-3940

3BP-3940 is a highly potent and selective peptide inhibitor targeting fibroblast activation protein (FAP) in cancer-associated fibroblasts (CAFs) within the tumor microenvironment. This reagent exhibits significant potential for tumor imaging when labeled with radionuclides such as Ga-68 and for targeted anticancer therapies using Lu-177. 3BP-3940 selectively accumulates in tumor lesions, making it valuable for the diagnosis and treatment of various solid tumors and conditions related to CAFs.

Cat. No.

A41627

CAS No.

3023869-94-2

FAPI-mFS

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.

Cat. No.

A41634

CAS No.

2374782-03-1

NOTA-FAPI

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.

Cat. No.

A64612

CAS No.

1448440-52-5

UAMC-1110

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.

Cat. No.

A64613

CAS No.

80049-85-0

Suc-Gly-Pro-AMC

Suc-Gly-Pro-AMC is a fluorescent substrate designed specifically for the fibroblast activation protein (FAP). It is capable of reacting with recombinant porcine prolyl oligopeptidase, facilitating the study of FAP and prolyl endopeptidase (PREP) activity. This reagent is particularly valuable in glioma research, providing insights into the enzymatic functions associated with tumor progression and microenvironmental interactions.

Cat. No.

A64615

CAS No.

2990021-73-1

NH2-UAMC1110 TFA

NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110, designed for use as a precursor compound in the synthesis of FAP inhibitor probes. This compound incorporates an active amino group, enabling the formation of covalent bonds with various molecules, such as DOTA and radionuclide chelators, to create targeted molecular imaging probes. NH2-UAMC1110 TFA selectively binds to the FAP active site, inhibiting its serine protease activity and thereby blocking FAP-mediated tissue remodeling processes. It is particularly relevant for diagnostic imaging studies of tumors expressing FAP, including colorectal and pancreatic cancers, as well as research into FAP-related diseases like fibrosis and arthritis.

Cat. No.

A64618

CAS No.

2791472-12-1

AZD2389

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.

Cat. No.

A64619

CAS No.

2471983-20-5

FAP-IN-2

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.

Cat. No.

A64620

CAS No.

1432499-49-4

ARI-3099

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.

Cat. No.

A64622

CAS No.

1426305-25-0

ARI-3144

ARI-3144 is a specific substrate for fibroblast activation protein (FAP), designed for effective detection and quantification. When coupled with the fluorophore 7-Amino-4-methylcoumarin (AMC), this substrate facilitates sensitive analysis of FAP activity in various biological samples. ARI-3144 is valuable in research applications related to cancer biology and tissue remodeling, enabling deeper insights into FAP functions and its role in disease progression.

Cat. No.

A64624

CAS No.

2715113-34-9

PNT6555

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.

Cat. No.

A64625

CAS No.

3114056-16-2

DOTAGA-FAP-2286-ALB

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.

Cat. No.

A64628

CAS No.

2370952-98-8

FAPI-2

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.

Cat. No.

A64629

CAS No.

3020777-05-0

FAP-IN-4

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.

Cat. No.

A64630

CAS No.

2952588-12-2

SB03178

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.

Cat. No.

A64631

CAS No.

2956858-96-9

FAP-IN-1

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.

Cat. No.

A64632

CAS No.

3093894-38-0

QI-18

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.

Cat. No.

A64635

CAS No.

2921619-09-0

FAPI-P8PN

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.

Cat. No.

A64637

CAS No.

3075119-33-1

FAP-IN-8

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.

Cat. No.

A64639

CAS No.

3020777-28-7

FAP-IN-7

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.

Cat. No.

A64641

CAS No.

3078291-78-5

DOTA-NI-FAPI-04

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.