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.

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.

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.

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.

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.

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

Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

24-Norursodeoxycholic acid (nor-UDCA) is a side chain-shortened C23 homolog of UDCA.It has shown potent anti-inflammatory, anti-cholestatic, and anti-fibrotic properties.It is a Ursodeoxycholic Acid derivative. It is superior to Ursodeoxycholic acid in the treatment of sclerosing cholangitis in Mdr2 (Abcb4) knockout mice

Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.

PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2 3 (LOXL2 3) inhibitor with anti-fibrotic activity.

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

Cetaben, a PPARα-independent peroxisome proliferator, is a non-fibrotic lipid-lowering drug that effectively reduces cholesterol and triglyceride concentrations.

Chiglitazar is a PPAR α γ δ agonist and insulin sensitizer used in the treatment of type 2 diabetes mellitus to lower blood glucose, regulate blood lipids, and have anti-inflammatory and anti-fibrotic effects.

KIRA-7 is an imidazopyrazine compound. KIRA-7 has an anti-fibrotic effect. KIRA-7 binds the IRE1α kinase (IC50: 110 nM) to allosterically inhibit its RNase activity.

ML-290 is an effective relaxin insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes. It shows an EC50 of 94 nM.

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.

BPU17 interacts with PHB1 and disrupts the PHB1-PHB2 interaction, causing slight mitochondrial dysfunction. This damage hinders transcription dependent on SRF CArG-box, thereby inhibiting epithelial-mesenchymal transition (EMT) in retinal pigment epithelial cells (RPEs). BPU17 has demonstrated anti-fibrotic activity in vivo. It holds potential as a research agent for anti-angiogenic age-related macular degeneration (nAMD).

RIPK2-IN-6 (Compound 15a) is an inhibitor of RIPK that specifically targets the phosphorylation of RIPK2, thereby suppressing the NF-κB and MAPK signaling pathways. It has demonstrated anti-inflammatory and anti-fibrotic activities in a mouse model of colitis induced by Dextran sodium sulfate.

GED-0507-34 Levo ((S)-3-(4-Aminophenyl)-2-methoxypropanoic acid), an orally available PPARγ modulator for amelioration of inflammation-driven intestinal fibrosis, decreased the expression of the pro-fibrotic genes Acta2, COL1a1, and Fn1, reduced the protein levels of α-SMA and collagen I-II, the main markers of fibrosis, as well as the major components of the TGFβ Smad pathway, and decreased the expression of IL-13, CTGF, TGFB and ACTA1, and inhibited TGF-β-induced activation of fibroblasts and IECs cell lines.

Uridine triphosphate (UTP) is a purine nucleotide P2U receptor agonist with potential use in lung cancer treatment. By activating P2Y2 receptors, it enhances the proliferation of human cancerous ductal epithelial cells. Additionally, UTP induces fibrotic responses in cardiac fibroblasts through P2Y2 receptor activation and prolongs the action potential duration of guinea pig papillary muscles via the P2Y2 purinergic receptor.

STAT3-IN-39 (compound 10K) is an orally active inhibitor of STAT3, demonstrating effective inhibition of STAT3 phosphorylation with an IC50 of 0.47 μM in NIH-3T3 cells. It hinders TGF-β1-induced fibrotic responses and prevents epithelial-mesenchymal transition in A549 cells. STAT3-IN-39 is applicable for research related to idiopathic pulmonary fibrosis.