fibrotic

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.

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.

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.

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.

Apamin acetate (Apamine acetate) is a selective Ca2+-activated blocker of K+ (SK) channels, an 18-amino acid peptide neurotoxin found in bee toxins.Apamin acetate enhances synapse growth and regeneration following laceration injury to cortical neurons.Apamin acetate has anti-inflammatory and anti-fibrotic effects.

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.

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.

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

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

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.

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

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

PDE1-IN-7 (Compound 13h), with an IC50 value of 10 nM, selectively inhibits bPDE1. This compound demonstrates significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model and is useful for research purposes in studying liver fibrosis [1].

DDR1/2 Inhibitor-2 (Example 31) serves as an inhibitor of DDR1/DDR2, exhibiting IC50 values below 100 nM. It is applicable in cancer and fibrotic disease research [1].

FT011, a direct anti-fibrotic agent,attenuates cardiac remodelling and dysfunction in experimental diabetic cardiomyopathy.

KBP-7018 is a potent, selective tyrosine kinase inhibitor with effects on three fibrotic kinases c-KIT, RET, and PDGFR (IC50 values are 10nM, 7.6 nM and 25nM respectively).

(S,R,S)-AHPC-C2-amide-benzofuranylmethyl-pyridine is a dual-target PROTAC capable of directing ubiquitination and degradation of Smad3 while also elevating HIF-α protein levels, exhibiting multipath anti-fibrotic and renal protective functions, making it valuable for renal anemia research [1].

DS89002333 is a potent, orally active PRKACA inhibitor (IC50: 0.3 nM).DS89002333 has shown good antitumor effects in a patient-derived xenograft model of FL-HCC expressing a DNAJB1-PRKACA fusion gene.DS89002333 can be used to study fibrotic hepatocellular carcinoma ( FL-HCC).

ALK5-IN-31 is a selective inhibitor of ALK-5 (IC50≤10 nM) and also inhibits TGF-β-induced SMAD signalling.ALK5-IN-31 has the potential to inhibit tumour growth in vivo.ALK5-IN-31 can be used in the study of proliferative diseases (e.g. cancer, fibrotic diseases, systemic sclerosis).

ALK5-IN-6 is a potent inhibitor of ALK5 with potential applications for TGF-β-related diseases and conditions, including tumors, inflammatory diseases, fibrotic diseases, and autoimmune diseases. Transforming growth factor β (TGF-β) is a multifunctional cytokine that regulates cell proliferation, differentiation, and apoptosis through a complex receptor signaling pathway on the cell surface in an autocrine, paracrine, and endocrine manner.

PXS-6302 is an irreversible inhibitor of lysyl oxidase with IC50s of 3.7 μM for Bovine LOX, 3.4 μM for rh LOXL1, 0.4 μM for rh LOXL2, 1.5 μM for rh LOXL3, 0.3 μM for rh LOXL4, respectively. PXS-6302 can readily penetrate the skin, reduces collagen deposition and cross-linking, and significantly improves scar appearance without reducing tissue strength. PXS-6302 also has potentially broader applications in other fibrotic diseases.

ATX inhibitor 12 is an orally active ATX inhibitor (IC50: 1.72 nM). In C57Bl/6J mice, oral administration of ATX inhibitor 12 at a dose of 60 mg/kg was effective in inhibiting structural lung damage and reducing fibrotic lesions.

Naproxcinod, a nitric oxide-releasing NSAID derivative, significantly improved skeletal muscle strength and fatigue resistance in sedentary and exercise mice, reducing inflammatory infiltration and fibrotic deposition in the myocardium and diaphragm. In a

Tulisokibart (PRA023) is a humanized IgG1-κ monoclonal antibody targeting TNFSF15 TL1A, with potential applications in researching inflammatory and fibrotic diseases, including Crohn's Disease (CD) [1] [2].

Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom) that selectively blocks Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity. This component of bee venom is strongly basic in nature.

MnTBAP chloride (Mn(III)TBAP) is a cell-permeable superoxide dismutase (SOD) mimetic and peroxynitrite scavenger that reduces the doubling time of SOD-E. coli by a factor of 2. MnTBAP chloride exhibits anti-inflammatory effects through upregulation of BMPR-II and inhibition of NFκB signaling. mnTBAP chloride is a manganese porphyrin complex with antioxidant properties and has potential for use in the study of fibrotic responses in chronic kidney diseases (CKDs).

ACT-1016-0707 (Compound 49), a selective antagonist of the LPA1 receptor, is effective when administered orally. It is utilized in the study of fibrotic diseases [1].

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.

Pentabromopseudilin (PBrP), a marine antibiotic derived from Pseudomonas bromoutilis and Alteromonas luteoviolaceus, demonstrates antimicrobial, antitumor, and phytotoxic properties. It acts as a reversible, allosteric inhibitor of myosin Va (MyoVa) and robustly inhibits transforming growth factor-β (TGF-β) activity. PBrP is utilized in researching fibrotic diseases and cancer [1].

VCP-746 is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling. VCP746 reduces hypertrophy in a rat neonatal cardiac myocyte model. VCP746 is a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia.

KBP-7018 Hydrochloride is a novel, tyrosine kinase-selective inhibitor with potent effects on three fibrotic kinases (c-KIT, PDGFR, and RET).

Halofuginone hydrochloride (RU-19110), a derivative of Febrifugine, functions as a competitive inhibitor of prolyl-tRNA synthetase, displaying a Ki value of 18.3 nM. This compound effectively inhibits type-I collagen synthesis, providing therapeutic benefits in osteoarthritis (OA) by impeding TGF-β signaling. Additionally, it serves as a potent pulmonary vasodilator, mainly through the activation of Kv channels and the inhibition of various calcium channels including voltage-gated, receptor-operated, and store-operated ones. Beyond its vascular effects, Halofuginone hydrochloride exhibits a broad spectrum of biological activities, including anti-malarial, anti-inflammatory, anti-cancer, and anti-fibrotic properties, supported by multiple studies.

Angiogenin (108-122) is an angiogenin peptide that serves as a therapeutic agent for the prophylaxis and or treatment of cancer, infectious diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, autoimmune diseases, and heart and vascular diseases.

Tranilast Sodium has been used for the treatment of bronchial asthma. Tranilast is also used to autoimmune diseases, atopic and fibrotic pat.

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

Cortistatin 29, a neuropeptide, alleviates neuropathic pain and exhibits anti-fibrotic effects. It binds with high affinity to all somatostatin (SS) receptor subtypes, displaying IC 50 values of 2.8 nM for SSTR1, 7.1 nM for SSTR2, 0.2 nM for SSTR3, 3.0 nM for SSTR4, and 13.7 nM for SSTR5, respectively [1] [2] [3] [4].

Hedgehog IN-5, an orally active small molecule inhibitor of the hedgehog pathway, can be used for the research of fibrotic disease [1].

Ac-D-DGla-LI-Cha-C is a potent peptide inhibitor of the HCV protease, useful in research targeting various diseases, including cancer, autoimmune, fibrotic, inflammatory, neurodegenerative, infectious, lung, heart and vascular, and metabolic diseases [1].

PF-03671148 is a potent ALK inhibitor. PF-03671148 inhibits the expression of fibrotic genes and protein markers both in vitro in human fibroblasts and in vivo in a rat wound repair model. Wound healing is not inhibited by the topical application of the ALK5 inhibitor to the wound. PF-03671148 may have potential utility for the prevention of dermal scarring.

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.

ATX inhibitor 15 (compound 30) is an indole-based carbamate derivative with a strong inhibitory effect on autotaxin (ATX), demonstrated by an IC50 of 2.17 nM. It effectively inhibits ATX activity in vivo, suppresses the expression of pro-fibrotic genes, and exhibits protective effects in Bleomycin-induced lung fibrosis in mice [1].

Bexotegrast, also known as PLN-74809, is a small-molecule, dual selective inhibitor of αVβ1 / αVβ6 for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). These integrins cause upstream activation of TGF-β1 in actively fibrotic tissue. Inhibition of these integrins will block TGF-β1 activation, thereby preventing the growth of fibrotic tissue within the lung and bile ducts.

Angiogenin (108-122) TFA is an angiogenin peptide.Angiogenin (108-122) acts as a therapeutic agent for the prophylaxis and/or treatment of cancer, an infectious disease, a fibrotic disease, an inflammatory disease, a neurodegenerative disease, an autoimmu

Physalin A is an anti-inflammatory compound isolated from P. alkekengi with anti-fibrotic effects, regulating the Nrf2 pathway through ERK and p38 to induce detoxification enzymes. Physalin A blocks the activation of the NF-kappaB signaling pathway. Physalin A reduces mammosphere formation by reducing the expression of the GLI1 gene and the YAP1 gene.

HYOU1-IN-1 (Compound 33), an inhibitor of hypoxia-upregulated protein 1 (HYOU1), exhibits anti-inflammatory properties. It is applicable in studies focusing on fibroblast activation, chronic inflammation, and fibrotic diseases [1].

MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor that specifically targets the Mixed Lineage Kinase domain-like (MLKL) protein. It effectively prevents MLKL phosphorylation and oligomerization, which are critical steps in cell necrosis. Additionally, MLKL-IN-6 restrains immune cell death, diminishes adhesion factor expression, exhibits low cytotoxicity, impedes hepatic stellate cell activation, decreases liver fibrosis marker levels, and exerts anti-fibrotic effects [1].

Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.