fibrotic diseases

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.

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.

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.

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.

SR-302 is a potent and selective inhibitor of DDR p38, with IC50 values of 0.125 μM for p38α, 0.023 μM for DDR1, and 0.018 μM for DDR2. It is utilized in research related to fibrotic diseases, such as kidney and lung fibrosis, atherosclerosis, and various types of cancer.

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

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).

S1P2 antagonist 1 is an orally bioavailable S1P2 antagonist used in the treatment of fibrotic diseases.

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.

TGFβ1-IN-1 is an orally active TGF-β1 inhibitor that inhibits the production of TGF-β1-induced fibrotic markers (α-SMA and fibronectin) and can be used for the study of cancer and autoimmune diseases.

ALK5-IN-28 is a selective inhibitor of ALK-5 with an IC50 ≤ 10 nM that inhibits TGF-β-induced SMAD signalling.ALK5-IN-28 has the potential to inhibit tumour growth in vivo.ALK5-IN-28 can be used to study proliferative diseases (e.g. cancer, fibrotic diseases, systemic sclerosis).

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-32 is a selective inhibitor of ALK-5 (10 nMdiseases (e.g. cancer, fibrotic diseases, systemic sclerosis). .

SGC agonist 2 is a potent soluble guanylate cyclase (SGC) agonist with potential therapeutic applications for cardiovascular diseases (heart failure, angina, pulmonary hypertension, myocardial infarction) and fibrotic diseases (renal fibrosis, 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.

PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others.

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].

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].

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].

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].

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.