fibrotic

AMG-25 (c-Kit-IN-5-1) is a selective and potent c-Kit inhibitor that inhibits c-Kit, KDR, p38, Lck, and Src, and can be used in the study of mast cell-associated fibrosis.

Malotilate (Kantec) is a medicine used for the therapy of liver cirrhosis.

Ogerin is a selective GPR68 positive allosteric modulator (pEC50: 6.83) that blocks recall in fear conditioning in mice. It exhibits inverse agonist and antagonist activity (Ki, 220 nM) at the A2A receptor and weak antagonist activity (Ki, 736 nM) at the 5-HT2B receptor.

HA 155 (Autotaxin Inhibitor IV) is a boronic acid-based compound, inhibiting ATX with IC50 of 5.7 nM by selectively binding to its catalytic threonine.

Aucubin (Rhinanthin) is an iridoid glycoside with anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.

Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM).

SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects.

Antifibrotic agent 1 is an orally active medication designed to treat idiopathic pulmonary fibrosis (IPF). It effectively mitigates IPF-related processes, including TGF-β-induced epithelial-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT), as well as profibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α, and Src family kinases (SFKs), while sparing VEGFR, FGFR, and Abl to minimize off-target toxicity. In a bleomycin (BLM)-induced pulmonary fibrosis mouse model, it demonstrates strong antifibrotic activity.

Taxifolin (Dihydroquercetin) is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.

Ro24-7429 is a small molecule inhibitor, an HIV-1 Tat antagonist and RUNX1 inhibitor, with oral activity, cell permeability, and anti-inflammatory effects, used for anti-HIV, anti-fibrotic, and inflammation-related research.

Cilofexor inhibits binding of a synthetic peptide, Cilofexor is a farnesoid X receptor (FXR) agonist.

OATD-01 is a highly active inhibitor of both Chitotriosidase (CHIT1) and acidic mammalian chitinase (AMCase).

AZD-8055 is an orally bioavailable, highly selective, ATP-competitive mTOR kinase inhibitor that directly binds to the ATP-binding pocket of the mTOR kinase domain, while potently inhibiting both mTORC1 and mTORC2 complexes (IC₅₀ values of 0.8 nM and 0.1 nM, respectively). AZD-8055 is suitable for research in oncology, metabolic diseases, and fibrotic disorders.

Selvigaltin (GB1211) is an orally administered, highly selective small-molecule inhibitor of galectin-3 (Gal-3) with an IC₅₀ value of 12 nM in rabbits, exhibiting anticancer and anti-fibrotic activity. Selvigaltin reduces galectin-3 levels in the liver and decreases biomarkers of inflammation (cellular foci) and fibrosis (PSR, SHG), while simultaneously lowering the mRNA and protein expression of inflammatory and fibrotic biomarkers (IL-6, TGF-β3, SNAI2, collagen). Selvigaltin also restores T-cell activity and reduces tumor growth and metastasis. Selvigaltin is suitable for use in studies of liver fibrosis, non-alcoholic steatohepatitis (NASH), and tumors.

GPR84 antagonist 8 is a selective GPR84 antagonist applicable for investigating inflammatory and fibrotic diseases.

PAT-1251 is an inhibitor of LOXL2 with IC50s of 10, 0.12, and 0.16 μM for the mouse, rat, and dog and can be used in studies about fibrotic diseases.

Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.

TD139 is a small molecule inhibitor of inhaled galectin-3 (Gal-3) with potential anti-fibrotic activity, commonly used in the study of idiopathic pulmonary fibrosis.

UK-396082 is a thrombin-activated fibrinolysis inhibitor (TAFI) that inhibits Carboxypeptidase B. It is used in the study of thrombosis, atherosclerosis, cancer, and fibrotic conditions.

Lenumlostat is an orally available, selective and potent lysyl oxidase-like protein 2 (LOXL2) inhibitor with inhibitory effects on hLOXL2, hLOXL3 and LOXL2 for the study of fibrotic diseases.

4-aminobenzoic acid is an organic acid with UV-absorbing and antifibrotic properties. When exposed to light, 4-aminobenzoic acid absorbs UV light and releases excess energy through a photochemical reaction, which may cause DNA damage.4-aminobenzoic acid also increases oxygen uptake at the tissue level and may enhance monoamine oxidase (MAO) activity to promote serotonin degradation, which in excess may lead to fibrotic Changes.

Idoxifene (CB7432) is a selective and tissue-specific estrogen receptor modulator (SERM) that reduces collagen and malondialdehyde (MDA) levels in rat liver, exhibiting anti-fibrotic effects.

AZD0233 is an orally active CX3CR1 antagonist that immunomodulates the CX3CR1/CX3CL1 signaling axis. It improves cardiac function in dilated cardiomyopathy mouse models while reducing macrophage infiltration and fibrotic scarring.

KBP-7018 is a potent and highly selective tyrosine kinase inhibitor that simultaneously targets three key fibrotic-associated kinases, including c-KIT, RET, and PDGFR, with IC50 values of 10 nM, 7.6 nM, and 25 nM respectively, and is therefore widely applicable for mechanistic research into fibrotic signaling pathways, kinase-driven disease progression, and pharmacological intervention strategies aimed at modulating aberrant tyrosine kinase activity.