FAP Inhibitor

UAMC-1110 is a highly potent and selective inhibitor of fibroblast activation protein (FAP) with an IC₅₀ of 3.2 nM. UAMC-1110 also inhibits prolyl oligopeptidase (PREP) with an IC₅₀ of 1.8 μM.

GFAP/NF-κB/APOE/NLRP3-IN-1 is an orally active, blood-brain barrier-permeable multi-target inhibitor with an IC₅₀ of 3.50 nM against Acetylcholinesterase. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits BACE-1 with an IC₅₀ of 14.61 nM. GFAP/NF-κB/APOE/NLRP3-IN-1 inhibits Aβ_1-42 aggregation with an IC₅₀ of 8.63 μM. GFAP/NF-κB/APOE/NLRP3-IN-1 reduces the levels of GFAP, NLRP3 inflammasome, NF-κB and APOE. GFAP/NF-κB/APOE/NLRP3-IN-1 is applicable for the research of Alzheimer's disease and neuroblastoma.

NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 TFA is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose effect, and has been used in tumor diagnosis. NH2-UAMC1110 TFA structurally incorporates an active amino group, allowing it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.) to synthesize molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 TFA specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling-related processes. Its key activity is high targeting and high affinity, and its core function is to act as a targeting module coupled with bifunctional chelators (such as DOTA, DATA5m). NH2-UAMC1110 TFA can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis.

Anti-Mouse FAP Antibody (73.3) is an anti-mouse FAP IgG1 monoclonal antibody. Anti-Mouse FAP Antibody (73.3) can be used to accurately detect the expression and localization of FAP protein in mice. Anti-Mouse FAP Antibody (73.3) can be used for research on cancer.

FAPI-mFS is an irreversible fibroblast activation protein (FAP) inhibitor, that enhances the uptake and retention time in cancer cells through its covalent binding property for FAP. FAPI-mFS can be used for cancer imaging the therapy, when labeled with radioactive 68Ga or 177Lu. FAPI-mFS can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

ARI-3099 is an oral fibroblast activation protein (FAP) inhibitor. ARI-3099 specifically inhibits the proteolytic activity of FAP and blocks the cleavage of human FGF-21 between residues P171 and S172. ARI-3099 extends the half-life of circulating human FGF-21 in mice. ARI-3099 can be used in the research of type 2 diabetes and metabolic disorders.

AZD2389 is a potent and orally active FAP inhibitor. AZD2389 can be used for the study of metabolic dysfunction-associated steatohepatitis.

FAP-IN-2 is an isonitrile-containing fibroblast activation protein (FAP) inhibitor. FAP-IN-2 can be labeled with technetium-99m (^99mTc) for targeted tumor SPECT imaging.

NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor. NOTA-FAPI can be used as a probe for FAP-targeted tumour imaging. NOTA-FAPI has good tumour detection efficacy and excellent imaging quality.

3BP-4089 TFA is a highly efficient fibroblast activation protein (FAP) targeting peptide. 3BP-4089 TFA is often conjugated with radionuclides for tumor diagnosis and research.

DOTA.SA.FAPi TFA is a selective FAP inhibitor with an IC₅₀ value of 0.9 nM against FAP. DOTA.SA.FAPi TFA forms stable complexes with ⁶⁸Ga and serves as a PET radiotracer for preclinical imaging of FAP-expressing tumors. DOTA.SA.FAPi TFA can be used in the research of colorectal adenocarcinoma and various other cancers.

DOTAGA.(SA.FAPi)2 TFA is a potent dimeric fibroblast-activation protein inhibitor (FAPi). DOTAGA.(SA.FAPi)2 TFA has the potential for cancer diagnosis research.

FAPI-800CW is a near-infrared (NIR) fluorescent-labeled fibroblast activation protein (FAP) inhibitor. FAPI-800CW shows specific uptake in inflamed paws in collagen-induced arthritis (CIA) model mice. FAPI-800CW can be used for in vivo molecular imaging of FAP expression in inflammatory diseases such as rheumatoid arthritis (RA) to monitor joint inflammation and disease activity.

FAP-IN-2 TFA is an isonitrile-containing fibroblast activation protein (FAP) inhibitor. FAP-IN-2 TFA can be labeled with technetium-99m (^99mTc) for targeted tumor SPECT imaging.

DOTAGA-FAP-2286-ALB is a derivative of Rofapitide tetraxetan (HY-147057). DOTAGA-FAP-2286-ALB is a selective fibroblast activation protein (FAP) inhibitor with an IC₅₀ value of 67.5 nM. DOTAGA-FAP-2286-ALB enhances tumor retention via albumin interaction, prolonging blood circulation and improving radiometal complex stability (e.g., with 111In and 225Ac). DOTAGA-FAP-2286-ALB is promising for research of radionuclide therapy (TRT) of FAP-positive solid tumors.

NH2-UAMC1110 is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose-response, and has been used for tumor diagnosis. NH2-UAMC1110 introduces an active amino group into its structure, enabling it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.), thereby synthesizing molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling processes. Its key activity is high targeting and high affinity, and its core function is to be coupled with bifunctional chelators (such as DOTA, DATA5m) as a targeting module. NH2-UAMC1110 can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis.

Zilganersen (ION373) sodium is a gapmer antisense oligonucleotide targeting glial fibrillary acidic protein (GFAP). Zilganersen sodium reduces excess glial fibrillary acidic protein produced by disease-causing variants in the GFAP gene and inhibits synthesis of GFAP. Zilganersen sodium can be used for the research of Alexander disease.

OMTX005 (OMTX705 antibody) is a humanized anti-FAP IgG1 monoclonal antibody that specifically binds to human (EC₅₀: 0.33 nM)/mouse (EC₅₀: 0.14 nM) FAP proteins and FAP-positive cells. OMTX005 exhibits no cytotoxicity when used alone and fails to induce an increase in caspase 3/7 activity in relevant cells. OMTX005 can be used to synthesize the ADC molecule OMTX705 for tumor research.

DOTAGA.(SA.FAPi)2 analogue TFA is a DOTAGA.(SA.FAPi)2 TFA (HY-164364A) analogue, in which the ligand and the chelator are identical to those of DOTAGA.(SA.FAPi)2 TFA. DOTAGA.(SA.FAPi)2 TFA is a potent dimeric fibroblast-activation protein inhibitor (FAPi).

FAP-IN-4 (Comp 10) is a fibroblast activation protein (FAP) inhibitor and a ¹⁸F-labeled PET tracer targeting FAP. FAP-IN-4 can be used for cancer research.