collagen deposition

TB-500 is a synthesised peptide, essentially a short-chain version of the naturally occurring Thymosin Beta-4.

safironil is a novel antifibrotic compound and a competitive inhibitor of collagen synthesis. safironil inhibited in vitro experiments on fibroblast activation monitored by collagen I mRNA or smooth muscle alpha-actin levels, and fibrogenesis as judged by type I and type III collagen and laminin production. safironil had no effect on the size of liver granulomas without altering total hydroxyproline, but altered the pattern of fibrosis by increasing type III and decreasing type I collagen deposition.

cis-L-Hydroxyproline inhibits the synthesis and extracellular deposition of collagen. The growth inhibition of pancreatic cancer cells induced by the Hyp isomer could be due to endoplasmatic reticulum stress.

PXS-4787 hydrochloride is a specific and potent pan-lysyl oxidase inhibitor that effectively eliminates the activity of lysyl oxidase. It exhibits varying IC50 values against different forms of the enzyme, including 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), and 0.2 μM (rh LOXL4). In addition, PXS-4787 hydrochloride reduces the deposition and cross-linking of collagen I secreted by human fibroblasts.

TRPV1-IN-3 (compound 14) is a TRPV1 inhibitor utilized in idiopathic pulmonary fibrosis research. It demonstrates antifibrotic activity in vitro (IC50 = 0.51 μM) by inhibiting the TGF-β/Smads and MAPK pathways, thereby affecting the expression of fibrosis markers collagen I and α-SMA. In vivo, TRPV1-IN-3 significantly reduces collagen deposition in lung tissue, improves alveolar structure, and increases survival rates in mice with Bleomycin-induced pulmonary fibrosis.

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.

ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. It effectively inhibits cell migration and collagen gel contraction. Additionally, ATX inhibitor 26 demonstrates significant antifibrotic activity, reducing collagen deposition in a Bleomycin (BLM)-induced pulmonary fibrosis model.

L-Ascorbic acid (L-Ascorbate) magnesium is an electron donor and an endogenous antioxidant. It selectively inhibits Cav3.2 channels with an IC50 of 6.5 μM. Additionally, L-Ascorbic acid promotes collagen deposition and inhibits elastin production. It also exhibits anticancer effects by generating reactive oxygen species (ROS) and selectively damaging cancer cells.

SGLT2-IN-2 (Compound E9) is an inhibitor of SGLT2 and significantly enhances the inhibition of SGLT2, NHE1, and SOD enzyme activities. It provides protection against myocardial cell damage induced by glucose-free DMEM. Additionally, SGLT2-IN-2 markedly improves cardiac function in TAC-induced heart failure (HF) mice, suppressing myocardial cell hypertrophy and collagen deposition. It reduces myocardial tissue damage and boosts autophagy in damaged myocardial cells, increasing the survival rate of HF mice.

ATX-IN-3 is an orally active autotaxin (ATX) inhibitor with an IC50 of 46 nM. It effectively ameliorates pulmonary fibrosis in mouse models by significantly reducing collagen deposition. ATX-IN-3 demonstrates excellent metabolic stability and drug-like properties, making it suitable for research on idiopathic pulmonary fibrosis (IFP).

TGF-β/Smad-IN-2 is an orally active TGF-β/Smad inhibitor. It suppresses TGF-β-induced differentiation of fibroblasts into myofibroblasts and collagen deposition, with an IC50 value of 102 μM for reducing collagen in LL29 cells. TGF-β/Smad-IN-2 acts by modulating the SMAD3/SMAD7 signaling pathway and decreases lung index in mice with pulmonary fibrosis. This compound is applicable in pulmonary fibrosis research.

ROCK2-IN-12 (Compound A25) is a selective inhibitor of ROCK2, exhibiting an IC50 of 7.0 nM for ROCK2, demonstrating greater efficacy compared to ROCK1 inhibition. It exerts potent anti-fibrotic effects via the TGF-β/Smad and ROCK2/STAT3 signaling pathways. In a Bleomycin-induced mouse pulmonary fibrosis (PF) model, ROCK2-IN-12 significantly reduces collagen deposition and reverses fibrosis progression. This compound is applicable in research on pulmonary diseases such as lung fibrosis.

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.

PI3K/mTOR-IN-20 is a selective dual inhibitor of PI3K/mTOR. It demonstrates nanomolar anti-proliferative effects in MRC-5 and Mlg2908 cells with IC50 values of 0.380 and 0.090 μM, respectively. In a Bleomycin-induced pulmonary fibrosis model, PI3K/mTOR-IN-20 reduces Ashcroft scores, decreases hydroxyproline content and collagen deposition, downregulates fibrosis-related protein expression, and aids in the repair of lung tissue structure. This compound exhibits good safety, as indicated by stable weight recovery in mice without significant hepatic or renal toxicity. PI3K/mTOR-IN-20 is useful for research on pulmonary fibroblasts.

KS370G (Caffeic Acid Phenethyl Amide) inhibits UUO-induced renal fibrosis marker expression. KS370G is an orally active hypoglycemic and cardioprotective agent that reduces collagen deposition in obstructed kidneys and significantly decreases renal expression of inflammatory chemokines/adhesion molecules and monocyte markers and improves left ventricular hypertrophy and function in the heart of pressure-overloaded mice.KS370G can be used to study renal obstructive nephropathy.

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

CAY10678 is an mPGES-1 inhibitor that inhibits PD-1.CAY10678 reduces collagen deposition and T-cell depletion, and may be used to study melanoma.CASHIPS

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.

J-1063 is a selective, orally active and potent inhibitor of ALK5 (IC50: 0.039 μM). J-1063 inhibits inflammatory infiltration, collagen deposition, hepatocyte necrosis and exhibits anti-fibrotic effects. j-1063 has potential for liver fibrosis studies.

FAP-PI3KI1, a fibroblast-activated protein (FAP)-targeted PI3K inhibitor, selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells. It effectively inhibits collagen synthesis and reduces collagen deposition [1].

ALK5-IN-79 (compound 57), an ALK inhibitor, exhibits anticancer activity by inhibiting the TGF-β1/SMAD signaling pathway. It effectively reduces the production of extracellular matrix (ECM) and collagen deposition. Moreover, ALK5-IN-79 demonstrates satisfactory pharmacokinetic (PK) properties and favorable in vivo tolerance.

Elastin Methacrylated (ElaMA) is a protein that can recruit and modulate innate immune cells, enhancing vascular formation at wound sites and thereby improving tissue regeneration. This compound attracts large numbers of neutrophils and key M2 macrophages to wounds, inducing their infiltration into hydrogels. It exhibits excellent immunomodulatory properties, promoting superior angiogenesis, collagen deposition, and dermal regeneration. When used in combination with the photoinitiator LAP , ElaMA self-assembles into fibrous hydrogels, targeting bioactive adhesion sites and providing intrinsic support and biodegradation for tissue cells. It is applicable in fields such as cell culture, bio 3D printing, and tissue engineering.

L-Ascorbic acid-D2 is the deuterated form of L-Ascorbic acid. L-Ascorbic acid (T0928) (L-Ascorbate) acts as an electron donor and is an endogenous antioxidant. It selectively inhibits Cav3.2 channels (Cav3.2 channels) with an IC50 of 6.5 μM. Additionally, L-Ascorbic acid (T0928) serves as a promoter of collagen deposition and an inhibitor of elastin production.

L-Ascorbic acid-13C-1 is a 13C-labeled version of L-Ascorbic acid. L-Ascorbic acid (T0928) (L-Ascorbate), known as an electron donor, functions as an endogenous antioxidant. It selectively inhibits Cav3.2 channels with an IC50 value of 6.5 μM. Additionally, L-Ascorbic acid (T0928) acts as a promoter of collagen deposition and an inhibitor of elastin formation.