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FAP Inhibitor

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48

Inhibitors & Agonists

1

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4

Peptides

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13233A
    Talabostat mesylate
    Maximum Cited Publications
    42 Publications Verification

    Val-boroPro mesylate; PT100 mesylate

    		 Dipeptidyl Peptidase Inflammation/Immunology Cancer
    Talabostat mesylate (Val-boroPro mesylate; PT100 mesylate) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities .
    Talabostat mesylate
  • HY-128643
    FAPI-4
    30+ Cited Publications

    		 FAP Cancer
    FAPI-4 is a potent fibroblast activation protein (FAP) inhibitor for the targeting FAP. FAPI-4 can be used in cancer research. 68Ga-FAPI-4 PET/CT is a promising new diagnostic method for imaging various kinds of cancer, with good tumor-to-background contrast ratios .
    FAPI-4
  • HY-100684
    UAMC-1110
    2 Publications Verification

    		 Prolyl Endopeptidase (PREP) FAP Cancer
    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 .
    UAMC-1110
  • HY-101801
    Ac-Gly-BoroPro
    5 Publications Verification

    		 FAP Cancer
    Ac-Gly-BoroPro is a selective FAP inhibitor with a Ki of 23 nM.
    Ac-Gly-BoroPro
  • HY-W010991
    N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly
    1 Publications Verification

    FAPGG

    		 Angiotensin-converting Enzyme (ACE) Others
    N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly (FAPGG) is a specific substrate of angiotensin converting enzyme (ACE) with a Ki of 2.546×10 -4 M. It is used as a chromogenic probe for quantitative detection of ACE activity. N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly can be hydrolyzed by ACE to generate N-[3-(2-furyl)acryloyl]-Phe (FAP) and Gly-Gly, and the ACE inhibitory effect is monitored by photometry. FAPGG competitively binds to the active center of ACE and is a key tool for screening ACE inhibitors such as Captopril (HY-B0368) and Dioscorin. Its reversible mechanism of action supports hypertension research and drug development targeting the renin-angiotensin system .
    N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly
  • HY-47979
    FAP-IN-2
    1 Publications Verification

    		 FAP Cancer
    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 .
    FAP-IN-2
  • HY-13233
    Talabostat

    Val-boroPro; PT100

    		 Dipeptidyl Peptidase Inflammation/Immunology Cancer
    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), inhibits DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM), quiescent cell proline dipeptidase (QPP) (IC50 = 310 nM), DPP2, and some other DASH family enzymes. Antineoplastic and hematopoiesis- stimulating activities .
    Talabostat
  • HY-172317
    AZD2389

    		FAP Metabolic Disease
    AZD2389 is a potent and orally active FAP inhibitor. AZD2389 can be used for the study of metabolic dysfunction-associated steatohepatitis .
    AZD2389
  • HY-136641
    NOTA-FAPI

    		Radionuclide-Drug Conjugates (RDCs) FAP Cancer
    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 .
    NOTA-FAPI
  • HY-153552A
    NH2-UAMC1110 TFA

    		FAP Cancer
    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 .
    NH2-UAMC1110 TFA
  • HY-D2363
    DOTA.SA.FAPi TFA

    		Radionuclide-Drug Conjugates (RDCs) FAP Prolyl Endopeptidase (PREP) Cancer
    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 .
    DOTA.SA.FAPi TFA
  • HY-153552
    NH2-UAMC1110

    		FAP Cancer
    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 .
    NH2-UAMC1110
  • HY-160289
    ARI-3144

    		FAP Cancer
    ARI-3144 is an excellent and specific substrate for fibroblast activation protein (FAP). ARI-3144 is usually coupled with the fluorophore 7-Amino-4-methylcoumarin (HY-D0027) (AMC) for detection and quantification of FAP .
    ARI-3144
  • HY-125366
    ARI-3099

    		FAP Metabolic Disease
    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 .
    ARI-3099
  • HY-P10131
    3BP-3940

    		Radionuclide-Drug Conjugates (RDCs) FAP Cancer
    3BP-3940 is a highly potent and selective peptide inhibitor of FAP that targets cancer-associated fibroblasts (CAFs) in the tumor microenvironment. 3BP-3940 can be labeled with radionuclides (such as Ga-68) for precise tumor imaging or Lu-177 for the development of targeted anticancer technologies. 3BP-3940 accumulates in tumor lesions and can be used to diagnose and inhibit various solid cancers and CAFs-related diseases .
    3BP-3940
  • HY-W404002
    BR102910

    		Prolyl Endopeptidase (PREP) Metabolic Disease
    BR102910 is a selective fibroblast activation protein (FAP) inhibitor with the IC50 of 2 nM. BR102910 also inhibits prolyl oligopeptidase (PREP) with the IC50 of 49.00 μM. BR102910 can be used for the researchof type 2
    BR102910
  • HY-173374
    DOTAGA-FAP-2286-ALB

    		FAP Drug Derivative Cancer
    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 .
    DOTAGA-FAP-2286-ALB
  • HY-161074
    PNT6555

    		FAP Cancer
    PNT6555 is a fibroblast activation protein-α (FAP) inhibitor. PNT6555 has antitumor activity. PNT6555 can be used for imaging of FAP-positive tumors .
    PNT6555
  • HY-175350
    OncoFAP-GlyPro-MMAE

    OncoFAP glidotin

    		 FAP Microtubule/Tubulin Cancer
    OncoFAP-GlyPro-MMAE is a FAP small molecule-drug conjugate (SMDC) with an IC50 of 0.49  nM. OncoFAP-GlyPro-MMAE consists of a FAP Ligand OncoFAP (HY-145938), a Tubulin inhibitor (MMAE) (HY-15162) and a linker. OncoFAP-GlyPro-MMAE can be used for cancers like renal cancer research .
    OncoFAP-GlyPro-MMAE
  • HY-175613
    DOTA-ALB-02

    		FAP Cancer
    DOTA-ALB-02 is an albumin-bound FAP inhibitor (FAPI) ligand. DOTA-ALB-02 labeled with 177Lu has a high FAP-binding affinity and enhanced tumor uptake and retention with a significant tumor/nontarget ratio. DOTA-ALB-02 can be used for PET/CT and SPECT/CT imaging of cancers, especially late-stage cancers .
    DOTA-ALB-02
  • HY-177435
    FAPI-800CW

    		FAP Inflammation/Immunology
    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 .
    FAPI-800CW
  • HY-148128
    TAM470

    		Microtubule/Tubulin ADC Payload Cancer
    TAM470 is a novel cytolysin, inhibiting tubulin polymerization and microtubule depolymerization. TAM470 can be used in the synthesis of OMTX705 as payload molecule, OMTX705 is a novel FAP-targeting antibody-drug conjugates (ADCs) with antitumor activity .
    TAM470
  • HY-164725
    FAPI-mFS

    		Radionuclide-Drug Conjugates (RDCs) FAP 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).
    FAPI-mFS
  • HY-170779
    DOTA-NI-FAPI-04

    		FAP Cancer
    DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact .
    DOTA-NI-FAPI-04
  • HY-175612
    DOTA-ALB-01

    		FAP Cancer
    DOTA-ALB-01 is an albumin-bound FAP inhibitor (FAPI) ligand. DOTA-ALB-01 labeled with 68Ga or 177Lu has a high FAP-binding affinity and enhanced tumor uptake and retention. DOTA-ALB-01 can be used for PET/CT and SPECT/CT imaging of cancers, especially late-stage cancers .
    DOTA-ALB-01
  • HY-149860
    FAP-IN-1

    		FAP Cancer
    FAP-IN-1 is a fibroblast activation protein (FAP) inhibitor with an IC50 value of 3.3 nM. FAP-IN-1 can be used for the research of cancer .
    FAP-IN-1
  • HY-175685
    FAP-IN-7

    		FAP Cancer
    FAP-IN-7 (Compound 5b) is a FAPinhibitor. FAP-IN-7 labeled with 18F enhances tumor retention with high selectivity and favorable pharmacokinetics. FAP-IN-7 can be used as a radiotracer for PET imaging and radionuclide therapy of cancers research .
    FAP-IN-7
  • HY-47979A
    FAP-IN-2 TFA
    1 Publications Verification

    		 FAP Cancer
    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 .
    FAP-IN-2 TFA
  • HY-145358
    FAP-PI3KI1

    		PI3K Cancer
    FAP-PI3KI1 is a fibroblast-activated protein (FAP)-targeted PI3K inhibitor that selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells and effectively inhibits collagen synthesis and reduces collagen deposition .
    FAP-PI3KI1
  • HY-128642
    FAPI-2

    		FAP Cancer
    FAPI-2 is a quinoline-based fibroblast activation protein (FAP)-targeting ligand that can be labeled as 68Ga-FAPI-2 and used as a PET tracer for cancer diagnosis. FAPI-2 has advantages such as fast tracer kinetics, no need for fasting preparation, and being unaffected by blood glucose .
    FAPI-2
  • HY-175322
    FAPI-P8PN

    		FAP Cancer
    FAPI-P8PN is a fibroblast activation protein (FAP) inhibitor (IC50=3.6 nM). FAPI-P8PN is promising for research of FAP-overexpressing solid tumors .
    FAPI-P8PN
  • HY-174421
    FAPI-JNU

    		FAP Cancer
    FAPI-JNU is a molecule targeting fibroblast activation protein (FAP). FAPI-JNU specifically binds to FAP highly expressed in the tumor microenvironment, and uses radionuclides [ 68Ga]Ga or [ 177Lu]Lu to achieve tumor imaging diagnosis. [177Lu]Lu−FAPI−JNU can effectively target and inhibit tumor growth in tumor-bearing mice. FAPI-JNU is promising for research of FAP-positive tumors (such as various solid tumors) .
    FAPI-JNU
  • HY-W668749
    3BP-3580

    		FAP Cancer
    3BP-3580 is a fibroblast activation protein (FAP) inhibitor (pIC50: 8.6), and can be used for cancer research .
    3BP-3580
  • HY-175330
    FAP-IN-6

    		FAP Cancer
    FAP-IN-6 (Compound 21) is a selectivity FAP inhibitor with an IC50 of 13 pM. FAP-IN-6 has a high metabolic stability. FAP-IN-6 labeled with 18F can be used as a positron emission tomography (PET) tracer. FAP-IN-6 can be used for microenvironment of cancers research .
    FAP-IN-6
  • HY-158326
    FAP-IN-4

    		FAP Cancer
    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 .
    FAP-IN-4
  • HY-178981
    FAP-IN-8

    		FAP Prolyl Endopeptidase (PREP) Cancer
    FAP-IN-8 (Compound 12i) is a potent inhibitor of PREP and FAP, with pIC50 values ​​of 8.99 and 10.08 for FAP and PREP, and IC50 values ​​of 1 and 0.08 nM, respectively. FAP-IN-8 may be used in cancer research .
    FAP-IN-8
  • HY-128642A
    FAPI-2 TFA

    		FAP Cancer
    FAPI-2 TFA is a quinoline-based fibroblast activation protein (FAP)-targeting ligand that can be labeled as 68Ga-FAPI-2 and used as a PET tracer for cancer diagnosis. FAPI-2 TFA has advantages such as fast tracer kinetics, no need for fasting preparation, and being unaffected by blood glucose .
    FAPI-2 TFA
  • HY-164364B
    DOTAGA.(SA.FAPi)2 analogue TFA

    		FAP Cancer
    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) .
    DOTAGA.(SA.FAPi)2 analogue TFA
  • HY-161262
    SB03178

    		FAP Cancer
    SB03178 is a fibroblast activation protein-alpha (FAP) inhibitor. SB03178 can be conjugated with DOTA and can be used for cancer research .
    SB03178
  • HY-159934
    QI-18

    		FAP Cancer
    QI-18 is a fibroblast activation protein (FAP) inhibitor with the IC50 of 0.50 nM, which is a 6.5-fold increase in potency over that of UAMC-1110 (HY-100684，IC50 of 3.25 nM). QI-18 can be used to synthesize high tumor selectivity and high dose radiotracers for the diagnosis and study of tumors .
    QI-18
  • HY-178028
    PRMT5-IN-53

    		Histone Methyltransferase Cancer
    PRMT5-IN-53 is a gut-restricted and orally active PRMT5 inhibitor with pIC50s of ≥ 9.7 against hPRMT5 and mPRMT5. PRMT5-IN-53 binds to the PRMT5:MEP50 complex with a KD of 11.3 pM. PRMT5-IN-53 effectively inhibits PRMT5 locally in the intestines of mice, significantly reducing the number and area of polyps, while avoiding systemic hematological toxicity (such as anemia, neutropenia). PRMT5-IN-53 can be used for the study of colorectal cancer especially for familial adenomatous polyposis (FAP) .
    PRMT5-IN-53
  • HY-179348
    DPP9-IN-2

    		Dipeptidyl Peptidase HIV Pyroptosis Cancer
    DPP9-IN-2 is a selective, potent and orally active inhibitor of Dipeptidyl Peptidase 9 (DPP9 ) with an IC50 of 12.9 nM. DPP9-IN-2 shows a SI of 59 over DPP8, and shows no significant inhibitory activity against related peptidases including DPP2, DPP4, FAP, and PREP. DPP9-IN-2 can induce cancer cells pyroptosis and has weak synergistic anti-HIV-1 activity when combined with non-nucleoside reverse transcriptase inhibitor. DPP9-IN-2 can be used for the researches of cance rand infection .
    DPP9-IN-2
  • HY-173319
    FAP-IN-5

    		FAP Cancer
    FAP-IN-5 (Compound 4a) is an FAP inhibitor with an IC50 of 1.7 nM. FAP-IN-5 can be used in the research of tumor positron emission tomography (PET) imaging .
    FAP-IN-5
  • HY-182272
    FAP-IN-9

    		FAP Cancer
    FAP-IN-9 (compound P12) is a fibroblast activation protein (FAP) inhibitor with an IC50 of 0.38 nM against human FAP. FAP-IN-9 functionally inhibits FAP activity, and its specific binding is verified by in vitro and in vivo blocking assays. FAP-IN-9 forms stable complexes and acts as a tumor-targeting agent. When labeled with 99mTc, FAP-IN-9 serves as a SPECT probe and is applicable to research related to glioblastoma .
    FAP-IN-9
  • HY-182250
    BR103354

    		FAP ERK GLUT Metabolic Disease Inflammation/Immunology
    BR103354 is an orally active, selective fibroblast activation protein (FAP) inhibitor with an IC50 value of 14 nM against hFAP. BR103354 restores the levels of phosphorylated ERK and Glut1 that are reduced by co-treatment with hFGF21 and FAP, decreases non-fasting blood glucose concentrations, improves glucose tolerance, and reduces hepatic triglyceride content. BR103354 ameliorates hepatic steatosis and hepatic fibrosis. BR103354 can be used in the research of type 2 diabetes and non-alcoholic steatohepatitis .
    BR103354
  • HY-186190
    I-FAPI-04 prodrug-1

    		Drug Intermediate FAP Cancer
    I-FAPI-04 prodrug-1 is a prodrug of I-FAPI-04, which is an inhibitor targeting fibroblast activation protein (FAP). I-FAPI-04 prodrug-1 can be used as a radioactive tracer in cancer .
    I-FAPI-04 prodrug-1
  • HY-100684R
    UAMC-1110 (Standard)

    		Prolyl Endopeptidase (PREP) FAP Reference Standards Cancer
    UAMC-1110 (Standard) is the analytical standard of UAMC-1110 (HY-100684). This product is intended for research and analytical applications. 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 .
    UAMC-1110 (Standard)
  • HY-181494
    FAPI-X5

    		FAP Cancer
    FAPI-X5 is a fibroblast activation protein (FAP) inhibitor. FAPI-X5 binds to the FAP catalytic domain, forming hydrogen bonds with key active residues and engaging in π-π stacking to drive functional inhibition. FAPI-X5 exhibits albumin binding activity to prolong systemic circulation half-life. FAPI-X5 induces cytostatic effects on glioblastoma tumors, slowing tumor growth without regression. FAPI-X5, when labeled with 68Ga, acts as a PET tracer with rapid tumor uptake and high-contrast imaging in glioblastoma tumor-bearing mice. FAPI-X5, when labeled with 177Lu or 47Sc, functions as a targeted radionuclide agent with prolonged tumor retention. FAPI-X5 can be used for the research of glioblastoma .
    FAPI-X5

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