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).

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).

TFAP2β modulator-1 is a potent modulator of the transcription factor TFAP2β, promoting its condensation through the induction of conformational changes within its intrinsically disordered region. This compound exhibits significant anti-tumor activity by inducing apoptosis in esophageal squamous cell carcinoma (ESCC) cells, as well as in relevant mouse models and organoids. TFAP2β modulator-1 serves as a valuable tool for investigating the role of TFAP2β in ESCC research and therapeutic development.

Simlukafusp alfa is an immunocytokine composed of an antibody targeting fibroblast activation protein α (FAPα) and a variant of interleukin-2 (IL-2) that selectively engages the IL-2 receptor βγ chain. This unique structure enhances the immune response against FAPα-expressing tumors while promoting T-cell activation and proliferation. Simlukafusp alfa is suitable for research applications focused on cancer immunotherapy and the study of tumor microenvironments, particularly in evaluating the efficacy of targeted immune modulation.

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.

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.

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.

FAP targeting peptide for FXX489 is a polypeptide that specifically targets fibroblast activation protein (FAP). This ligand plays a crucial role in the development of therapeutic agents aimed at modulating FAP-related pathways. It is particularly applicable in cancer research, where FAP is associated with tumor stroma and cancer progression, facilitating targeted delivery of therapeutic compounds.

DOTAGA.Glu.(FAPi)2 is a targeted agent that functions as a homodimer specific to fibroblast activation protein (FAP). This compound, which features a central glutamic acid linker connecting FAPi to a chelator, is suitable for radiolabeling with gallium-68, lutetium-177, or terbium-161, making it valuable for PET imaging studies in cancers expressing FAP. Its primary research applications include investigations related to prostate adenocarcinoma and recurrent glioblastoma multiforme, facilitating enhanced imaging and assessment of these malignancies.

FAP targeting peptide-PEG2 conjugate is a peptide-PEG2 linker conjugate of Unlabeled FXX489, a ligand specifically targeting fibroblast activation protein (FAP). This conjugate facilitates targeted delivery and enhances bioavailability in therapeutic applications. It is primarily employed in research focusing on FAP-related diseases, offering valuable insights into cancer progression and tissue remodeling.

TAM470 is a novel cytolysin that functions by inhibiting tubulin polymerization and facilitating microtubule depolymerization. This compound serves as a valuable payload molecule in the synthesis of OMTX705, a groundbreaking antibody-drug conjugate (ADC) targeting fibroblast activation protein (FAP) and demonstrating significant antitumor activity. TAM470 is of interest for research into cancer therapeutics and the development of targeted delivery systems.

TAM558 Intermediate-5 is a pivotal intermediate in the synthesis of TAM558, which serves as the payload molecule for the formation of OMTX705. OMTX705 is a humanized antibody targeting fibroblast activation protein (FAP), facilitating cytolysis via binding to TAM470. This intermediate is essential for research into anti-tumor therapies and the development of novel cancer treatments targeting the tumor microenvironment.

TAM558 intermediate-2 is a critical intermediate in the synthesis of TAM558, a payload molecule used in the preparation of OMTX705. OMTX705 is a humanized antibody targeting fibroblast activation protein (FAP), which exhibits significant anti-tumor activity by binding to the cytolysin TAM470. This intermediate plays a vital role in facilitating the development of innovative therapeutic agents for cancer treatment.

TAM558 is a payload molecule utilized in the synthesis of OMTX705, a humanized anti-fibroblast-activating protein (FAP) antibody conjugated to the cytolysin TAM470. This conjugation enhances the antitumor activity of OMTX705, making it a valuable tool in cancer research. The combination of TAM558 with targeted antibodies facilitates the development of innovative therapeutic strategies against tumor-associated fibroblasts.

OncoFAP-GlyPro-MMAE is a small molecule-drug conjugate (SMDC) targeting fibroblast activation protein (FAP) with an IC50 of 0.49 nM. This compound combines the selective FAP ligand OncoFAP with the tubulin inhibitor MMAE, linked for optimized delivery. OncoFAP-GlyPro-MMAE demonstrates significant cytotoxic activity and is suitable for research applications in renal cancer and related malignancies.

Rofapitide tetraxetan is a highly selective fibroblast activation protein (FAP)-binding peptide, exhibiting a mean IC50 of 2.7 nM for FAP binding. This compound demonstrates significant antitumor activity and can be effectively labeled with radionuclides for use in diagnostic imaging. Its specific targeting of FAP makes it a valuable tool for research applications in cancer diagnosis and therapy.

FAPI-46 is a quinoline-based tracer that selectively targets fibroblast activation protein (FAP). Labeled with radioactive isotopes like 68Ga or 177Lu, FAPI-46 is utilized for tumor imaging across various cancer types. Its high tumor uptake and prolonged tumor accumulation make it a valuable tool for assessing tumor burden and progression in clinical and research settings.

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.

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.

FAPI-74 is a positron emission tomography (PET) tracer that specifically targets fibroblast activation protein (FAP). This compound is valuable in the study of FAP-positive tumors, enabling researchers to visualize and assess tumor metabolism and progression. FAPI-74 offers significant potential for applications in cancer imaging and therapeutic monitoring.

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.

OncoFAP is a high-affinity ligand for fibroblast activation protein (FAP), designed for targeted applications in cancer research. Its pan-tumoral potential allows for effective identification and localization of tumors, aiding in the investigation of tumor microenvironments. This reagent is particularly useful in studies focused on cancer diagnostics and therapeutics, providing a valuable tool for enhancing the precision of tumor targeting.

Unlabeled FXX489 is a fibroblast activation protein (FAP)-targeting ligand. This compound possesses anticancer properties and can be utilized in conjunction with isotopes such as 68Ga and 177Lu for imaging and therapeutic applications. Unlabeled FXX489 is particularly relevant for research on pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC), aiding in the exploration of FAP's role in tumor biology and treatment strategies.

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.

FT-FAPI-12_9 is a fibroblast activation protein (FAP) ligand designed for the synthesis of FAPI-46, a radiotracer that selectively targets FAP. This compound exhibits specific binding properties that facilitate the imaging of tumors and inflammatory conditions associated with FAP expression. Its application in cancer research and molecular imaging underscores its utility in evaluating FAP as a potential therapeutic target.

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.

FAPI-34 is a radiolabeled imaging agent that specifically targets fibroblast activation protein (FAP). It demonstrates high affinity for FAP-expressing cells, resulting in significant internalization and accumulation in FAP-positive tumor lesions while exhibiting minimal uptake in normal tissues, with the exception of the kidneys. This compound is particularly useful for tumor-related research applications, including imaging studies and the assessment of FAP's role in tumor biology.

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.

NH2-UAMC1110 is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110, functioning as a precursor for the synthesis of FAP-targeted radiotracers. This compound is integral in producing the radiotracer FAPI-QS, known for its high tumor selectivity and dose-response, facilitating tumor diagnosis. NH2-UAMC1110 features an active amino group, allowing for covalent bonding with various molecules including bifunctional chelators like DOTA and DATA5m. It specifically binds to the FAP active site, inhibiting its serine protease activity, thereby blocking FAP-mediated tissue remodeling. Suitable for diagnostic imaging of tumors expressing FAP, NH2-UAMC1110 serves as a valuable tool in the study of FAP-related diseases such as fibrosis and arthritis.

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.

3BP-4089 is a potent fibroblast activation protein (FAP)-targeting peptide designed for theranostic applications. This peptide effectively facilitates the targeting of tumor microenvironments, allowing for enhanced imaging and therapeutic strategies. Coupling 3BP-4089 with radionuclides supports its utility in tumor diagnosis and advanced cancer research.

DOTA-C1-FAP-2286 is a cysteic acid-modified radioligand that specifically targets fibroblast activation protein (FAP). With an IC50 of 127.64 nM, it binds competitively to FAP-expressing cells, allowing for targeted accumulation and expedited renal clearance. This compound is suitable for use as a PET/CT tracer in cancer research and can aid in the imaging of tumors with high FAP expression.

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.

FAP6-19 is a radioligand targeting fibroblast activation protein (FAP) with a Kd of 18.2 nM. This compound selectively delivers therapeutic radioactive isotopes, such as 177Lu, directly to tumors that overexpress FAP in the microenvironment, enabling targeted destruction of malignant cells while preserving healthy tissues. FAP6-19 demonstrates high total cellular uptake and excellent intracellular retention in HT1080 cells. When labeled with 111In, it achieves favorable tumor/kidney and tumor/liver dose ratios in mouse models with 4T1 tumors. This reagent is valuable for research involving solid tumors that express FAP.

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.

R-75317 is a selective antagonist of platelet-activating factor (PAF). It has demonstrated the ability to prevent the decline in creatinine clearance in a rat model of antibody-induced glomerulonephritis, delay the onset of proteinuria, and ameliorate glomerular hypertrophy, mesangial matrix proliferation, and interstitial fibrosis. This compound may serve as a valuable tool in the investigation of glomerulonephritis and related renal pathologies.