fibroblast activation

Flunisolide (Rhinalar) is a synthetic corticosteroid with anti-inflammatory and antiallergic properties.

Trimethylamine N-oxide (TMAO) is a gut microbiota-dependent metabolite derived from dietary choline, betaine, and carnitine. It induces inflammation by activating the ROS/NLRP3 inflammasome and promotes fibroblast differentiation through the activation of the TGF-β/Smad2 signaling pathway. TMAO is commonly used to induce cardiac fibrosis models.

safironil is a novel antifibrotic compound and a competitive inhibitor of collagen synthesis. safironil inhibited in vitro experiments on fibroblast activation monitored by collagen I mRNA or smooth muscle alpha-actin levels, and fibrogenesis as judged by type I and type III collagen and laminin production. safironil had no effect on the size of liver granulomas without altering total hydroxyproline, but altered the pattern of fibrosis by increasing type III and decreasing type I collagen deposition.

The FAP-targeting peptide for FXX489 constitutes the peptide moiety of FXX489, suitable for biochemical assays and drug synthesis studies. FXX489 is a fibroblast activation protein (FAP)-targeting ligand employed in radioligand therapy (RLT) for multiple cancers.

TGFβ1-IN-2, a derivative of diarylacylhydrazones, effectively inhibits fibroblast activation and proliferation and holds potential for idiopathic pulmonary fibrosis (IPF) research [1].

TGFβ1-IN-3, a diarylhydrazone derivative, inhibits fibroblast activation and proliferation, positioning it as a candidate compound for the treatment of idiopathic pulmonary fibrosis (IPF).

FAPI-2 is a specific inhibitor of fibroblast-activated protein based on the radiotracer FAP labeling. It has anticancer activity and can be used in the study of pancreatic cancer.

FAPI-4 FAPI-4 is a fibroblast activating protein (FAP) inhibitor, a FAPI ligand, which shows strong liver uptake in PET imaging of primary liver cancer hepatocellular carcinoma (HCC) and is commonly used in PET imaging for the study of cancer.

ML334 (LH601A) is a transmembrane and potent NRF2 activator that inhibits Keap1-NRF2 protein interactions to ameliorate myocardial infarction-induced cardiac fibrosis by inhibiting cardiac fibroblast activation and proliferation.

DOTAGA.(SA.FAPi)2 TFA is an effective dimeric fibroblast activation protein inhibitor (FAPi). This compound holds potential for use in cancer diagnostic research.

FAPI-mFS, an irreversible fibroblast activation protein (FAP) inhibitor, enhances uptake and retention in cancer cells through its covalent binding properties with FAP. When labeled with radioactive 68Ga or 177Lu, FAPI-mFS can be utilized for cancer imaging and therapy.

3BP-3580 is an inhibitor of fibroblast activation protein (FAP) with a pIC50 value of 8.6, utilized in cancer research.

QI-18 is a fibroblast activation protein (FAP) inhibitor with an IC50 value of 0.50 nM, offering a 6.5-fold increase in activity compared to UAMC-1110 (IC50 3.25 nM). It can be utilized in the synthesis of highly tumor-selective and high-dose radiotracers for the diagnosis and treatment of tumors.

FAP-targeting peptide-PEG2 conjugate (Example A1) is the polypeptide and linker conjugate component of Unlabeled FXX489. Unlabeled FXX489 serves as a ligand targeting fibroblast activation protein (FAP).

DOTAGA-FAP-2286-ALB is a derivative of Rofapitide tetraxetan. It functions as a selective inhibitor of fibroblast activation protein (FAP) with an IC50 value of 67.5 nM. By interacting with albumin, DOTAGA-FAP-2286-ALB enhances tumor retention, prolongs circulation time in the bloodstream, and improves the stability of radiometal complexes [such as 111In and 225Ac]. This compound shows promise for use in targeted radionuclide therapy (TRT) research for FAP-positive solid tumors.

PNT6555 acts as an inhibitor of fibroblast activation protein-α (FAP). It possesses anti-tumor properties and is applicable for imaging FAP-positive tumors.

BR-cpd7 is a PROTAC degrader of fibroblast growth factor receptors (FGFR1/2) with a DC50 of 10 nM. It is capable of arresting the cell cycle and inhibiting the proliferation of tumor cells with aberrant activation of FGFR1/2.

FAP-IN-4 (Comp 10) is an inhibitor of fibroblast activation protein (FAP) and serves as a targeted FAP-specific radiotracer for PET imaging labeled with 18F. It is applicable in tumor research.

Antitumor agent-176 (Compound 22) is an antitumor agent that binds effectively to FGF2, inhibits the activation of fibroblast growth factor receptor (FGFR) in multiple myeloma (MM) cells, and demonstrates significant antitumor activity against MM both in vivo and in vitro.

FAPI-JNU is a molecule that targets fibroblast activation protein (FAP). It binds specifically to FAP, which is highly expressed in the tumor microenvironment, enabling tumor imaging and diagnosis using radionuclides [68Ga]Ga or [177Lu]Lu. The compound [177Lu]Lu−FAPI−JNU can effectively target and inhibit tumor growth in mice with tumors. FAPI-JNU holds potential for research on FAP-positive tumors, such as various solid tumors.

TriOncoFAP-GlyPro-MMAE is a small molecule drug conjugate (SMDC) that targets fibroblast activation protein (FAP), with an IC50 value of 13 pmol/L. It comprises a ligand targeting FAP (TriOnco), a cleavable glycine-proline linker, and a cytotoxic payload (MMAE).

Faridoxorubicin (AVA-6000) is a prodrug that targets fibroblast activation protein alpha (FAPα). It releases active doxorubicin through FAPα-mediated cleavage, enhancing drug exposure within tumors while reducing cardiac toxicity. Faridoxorubicin holds potential for research in solid tumors, such as liver metastases from colorectal cancer.

FAPI-P8PN is an inhibitor of fibroblast activation protein (FAP) with an IC50 value of 3.6 nM. It holds potential for research involving solid tumors with overexpression of FAP.

ARI-3099 inhibits fibroblast activation protein, alpha (FAP).