collagen-1

SRI-011381 hydrochloride, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.

Sinefungin (Adenosyl-Ornithine) belongs to natural products and is an mRNA methyltransferase inhibitor with broad-spectrum antiviral activity. This compound possesses cell permeability and is commonly used in antiviral mechanism research and antiviral drug development.

SRI-011381, a new-type agonist of the TGF-beta signaling pathway, is utilized in the treatment of Alzheimer's disease.

Halofuginone (RU-19110), the competitive inhibitor of prolyl-tRNA synthetase(Ki=18.3 nM), could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in the mammal.

Collagen proline hydroxylase inhibitor-1 exhibits antifibroproliferative activity.

Tipelukast (KCA 757) is a novel, orally available leukotriene receptor antagonist with anti-inflammatory properties, capable of reducing fibrosis and down-regulating TIMP-1 and type 1 collagen. Tipelukast is utilized in asthma research.

3-Aminopropionitrile fumarate (2:1) [β-Aminopropionitrile fumarate] is an organic compound and antirheumatic agent utilized in veterinary medicine.

Collagenase Type I is a proteolytic enzyme that primarily targets collagen and is able to break down peptide bonds in collagen. Collagenase is used as a potential therapeutic option to break up the herniated disc material, thereby reducing compression of nearby nerves. Collagenase may aid in the breakdown and reorganization of excessive scar tissue, potentially improving tissue function and appearance. Collagenase has the potential to treat intervertebral disc herniation, keloid, fat mass, lipoma, as well as Peyronie's disease and palmar fibromatosis.

SR 1903 is an inverse agonist of RORγ and PPARγ (IC₅₀ = 100 nM and 209 nM, respectively) and an agonist of LXR (EC₅₀ = 154 nM). It exerts anti-inflammatory and anti-diabetic effects in mouse models of collagen-induced arthritis and diet-induced obesity.

4-Deoxypyridoxine (4-DPD) is a vitamin B6 antimetabolite with diverse biological activities. It inhibits transport of pyridoxine , pyridoxal, and pyridoxamine in and reduces growth of S. carlsbergensis cells. 4-DPD inhibits sphingosine-1-phosphate (S1P) lyase and reduces cyclic stretch-induced apoptosis in alveolar epithelial MLE-12 cells. 4-DPD (5 mg, i.p.) reduces lysyl oxidase activity by 26% and reduces collagen and elastin crosslinking, resulting in limb abnormalities in chick embryos. It decreases latency to first seizure in mice (ED50 = 1 mmol/kg) and increases the occurrence and duration of myoclonic responses in baboons with photosensitive epilepsy. 4-DPD reduces TNF-α and IL-6 production in mice infected with T. spiralis.

JTE-952 is a oral, potent active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse

Benzyl-α-GalNAc (O-glycosylation-IN-1) is an effective inhibitor of O-glycosylation used to reduce the levels of mucin on the cell surface; it can inhibit the synthesis of O-glycosylated mucin in a human pancreatic cancer cell model. Benzyl-α-GalNAc effectively inhibits the proliferation and activation of LX-2 cells and suppresses the expression of collagen I/III, making it suitable for studies on liver fibrosis. Benzyl-α-GalNAc can be used in research on glycobiology, tumor metastasis, liver fibrosis, and chemotherapeutic sensitization.

ALK5-IN-82 is a potent and selective inhibitor of activin receptor-like kinase 5 (ALK5), demonstrating an IC50 value of 9.1 nM. This compound effectively suppresses the expression of α-smooth muscle actin (α-SMA), collagen I, and the proteinases tissue inhibitor of metalloproteinase 1 (TIMP-1) and matrix metalloproteinase 13 (MMP-13) in human umbilical vein endothelial cells induced by transforming growth factor-β. ALK5-IN-82 shows potential for use in research related to cardiac fibrosis.

Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by hindering HDAC6 activity, with an IC50 value of 63 nM for HDAC6. It exhibits superior selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat effectively reduces the expression of fibrosis markers, fibronectin and collagen 1, in fibroblasts. It shows no toxicity in rat perfused heart and zebrafish larvae studies. Fibrostat holds promise for research on fibrosis-related diseases.

ERBB agonist-1 (Compound EF-1) is an ERBB4 agonist (EC50=10.5 μM) that induces ERBB4 receptor dimerization and phosphorylation of Akt and ERK1/2. It exhibits cardioprotective effects in mouse models and prevents myocardial fibrosis.

FGFRs-IN-1 (Compound A16) is an orally active inhibitor targeting FGFR1/2/3/4, with IC50 values of 2.3, 7, 11, and 163 nM respectively. It also inhibits VEGFR1/2/3, Abl, and Flt3, with IC50 values of 61, 176, 112, 26, and 353 nM. The compound shows weak inhibition of CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and it inhibits epithelial-mesenchymal transition (EMT) in A549 cells stimulated by TGF-β1. Additionally, FGFRs-IN-1 demonstrates anti-inflammatory activity in mouse models of lung fibrosis induced by Bleomycin and liver fibrosis induced by CCl4.

ATX-IN-1 (compound 35) is an ATX inhibitor with an IC50 of 0.7 nM, demonstrating anti-inflammatory properties. It effectively suppresses the TGF-β/Smad pathway and reduces collagen deposition, alleviating fibrosis in a Bleomycin-induced mouse model. This compound also exhibits good oral bioavailability (F=69.5%) and microsomal stability.

Galectin-3-IN-6 (Compound 12) is an orally active galectin-3 (Gal-3) inhibitor, with an IC50 of 12 nM and a Kd of 13 nM for Gal-3. In a CCl4-induced mouse model of acute liver injury and fibrosis, Galectin-3-IN-6 significantly reduces fibrosis markers collagen-1 and α-smooth muscle actin (αSMA) by 64% and 71%, respectively, demonstrating notable anti-fibrotic activity. Galectin-3-IN-6 is applicable for research in fibrosis-related diseases, cancer, and cardiovascular disorders.

1-Methylnicotinamide is the active metabolite of nicotinamide, formed by nicotinamide N-methyltransferase. 1-Methylnicotinamide induces the secretion of nitric oxide by human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner. When administered at a dose of 30 mg/kg, it can increase the level of 6-keto-prostaglandin F1α in rat plasma and inhibit collagen-induced thrombosis at the same dose.

NCGC00685960 is a potent inhibitor of nicotinamide N-methyltransferase (NNMT) with an IC50 of less than 10 nM. This compound exhibits strong anti-tumor activity, enhances H3K27 trimethylation in ovarian cancer cells, and suppresses α-SMA expression in NNMT-expressing ovarian fibroblasts. It also reduces 1-MNA levels in cancer-associated fibroblasts (CAFs), reverses low SAM and H3K27 methylation, and significantly diminishes collagen contractility. NCGC00685960 is valuable for cancer research.

LOXL2/sGC modulator-1 (Compound 11k) is an LOXL2 inhibitor with an IC₅₀ of 0.13 μM and acts as an sGC activator. It shows good selectivity for LOX (IC₅₀ > 45.9 μM) and LOXL3 (IC₅₀ = 1.30 μM). In the presence of the gGC inhibitor ODQ, it significantly increases intracellular cGMP levels. LOXL2/sGC modulator-1 effectively inhibits hypoxia-induced collagen deposition and cross-linking while promoting vasodilation. This compound is useful for researching pulmonary arterial hypertension.

Calcium glucoheptonate is a highly water-soluble calcium supplement. It enhances the proliferation rate and calcium uptake of MG-63 cells, while also boosting alkaline phosphatase (ALP) activity. This compound upregulates the expression of osteogenesis-related genes and proteins, including collagen-1, osteocalcin, and osteopontin (osteocalcin). Calcium glucoheptonate is applicable in research related to osteoporosis and hypocalcemia.

SP-100030 is a dual inhibitor of NF-κB and activator protein-1 (AP-1), demonstrating potent inhibition with IC50 values of 50 nM for both. It effectively reduces the production of IL-2, IL-8, and TNF-alpha in Jurkat and other T cell lines. Additionally, SP-100030 has been shown to decrease the severity of murine collagen-induced arthritis (CIA).

Allylpyrocatechol is an antioxidant. Allylpyrocatechol attenuates collagen-induced arthritis via attenuation of oxidative stress secondary to modulation of the MAPK, JAK/STAT, and Nrf2/HO-1 pathways.