collagen-1

Collagen proline hydroxylase inhibitor-1 exhibits antifibroproliferative activity.

Collagen-IN-1 (compound 3) is an ortho-carbonyl hydroquinone derivative that selectively inhibits collagen. It non-competitively inhibits agonist-induced platelet aggregation, with an IC50 value of 1.77 μM. Collagen-IN-1 reduces P-selectin expression, glycoprotein IIb IIIa activation, and the release of adenosine triphosphate and CD63 from platelets. This compound is promising for research into platelet-related thrombosis diseases [1].

This is a peptide inhibitor of collagen fibrillar matrix assembly.

Sinefungin (Adenosyl-Ornithine) is an effective inhibitor of virion mRNA(guanine-7-)-methyltransferase, mRNA(nucleoside-2'-)-methyltransferase, and viral multiplication. Sinefungin is a SET7 9 inhibitor and ameliorates renal fibrosis by inhibiting H3K4 methylation.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

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

Fasudil (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK.

Cirsiumaldehyde is a compound isolated from the mature fruits of Lobelia chinensis, Cornus officinalis, and the fruits of Hippophae rhamnoides.Cirsiumaldehyde in the presence of collagen inhibited U46619-induced (1~5 uM) The inhibitory concentration of Cirsiumaldehyde on U46619-induced (1~5 uM) rat platelet aggregation in the presence of collagen was 0.8~1.0 ug mL.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

1. Glaucocalyxin A (Leukamenin F)-SBE-β-CD could be useful with a better solubility and sustained function in drug delivery. 2. Glaucocalyxin A activates caspase-3, decreases BAD phosphorylation, and reduces the expression of X-linked inhibitor of apoptosis protein. 3. Glaucocalyxin A inhibits Akt phosphorylation, suppresses proliferation, and promotes apoptosis in a dose-dependent manner, but not in normal glial cells. 4. Glaucocalyxin A inhibits collagen-stimulated tyrosine phosphorylation of Syk, LAT, and phospholipase Cγ2, the signaling events in collagen receptor GPⅥ pathway. 5. Glaucocalyxin A could potentially be developed as an antiplatelet and antithrombotic agent, can inhibit platelet p-selectin secretion and integrin activation by convulxin, is a GPVI selective ligand.

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

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).

Osteostatin, derived from parathyroid hormone-related protein (PTHrP) 107-111, has demonstrated properties conducive to bone repair in animal models presenting with bone defects and exhibits efficacy in mitigating bone erosion associated with inflammatory arthritis. Additionally, it possesses the capacity to inhibit both collagen-induced arthritis and direct osteoclastic bone resorption, marking its potential utility in inflammation and immunology research [1] [2] [3] [4].

Endotrophin (Mus musculus), a cleavage product of collagen 6 (Col6), induces upregulation of profibrotic and proinflammatory genes [1].

Caprooyl-tetrapeptide-3 acetate, employed for diminishing fine lines and wrinkles, enhances collagen VII and laminin-5 expression in corticoid-induced skin aging models [1].

Oleic acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic acid is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma, cell membranes, and adipose tissue.1,2 It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets.1 Oleic acid inhibits collagen-stimulated platelet aggregation by approximately 90% when used at a concentration of 10 μg/ml. It also inhibits fMLF-induced neutrophil aggregation and degranulation by 55 and 68%, respectively, when used at a concentration of 5 μM, similar to arachidonic acid .3 Oleic acid (60 μM) induces release of intracellular calcium in human platelets.4

GPVI antagonist 2 (Compound 1) is a potential Glycoprotein VI (GPVI) antagonist, showing activity against collagen (IC50: 0.35 μM), CRP (IC50: 0.80 μM), convulxin (IC50: 195.2 μM), and thrombin (IC50: 81.38 μM), and is a promising anti-platelet agent.

ENMD-1068 hydrochloride, a selective protease-activated receptor 2 (PAR2) antagonist, inhibits TGF-β1/Smad signaling, thereby reducing hepatic stellate cell activation and collagen expression. It also suppresses the proliferation of endometrial cells and triggers apoptosis in epithelial lesion cells. This compound is utilized in researching endometriosis and liver fibrosis [1] [2].

MMP13-IN-2 is a highly potent, selective, and orally active inhibitor of MMP-13. It demonstrates exceptional potency against MMP-13, with an IC50 value of 0.036 nM, and exhibits selectivities greater than 1,500-fold over MMP-1, 3, 7, 8, 9, 14, and TACE. Moreover, MMP13-IN-2 possesses the capability to effectively inhibit collagen release from cartilage in vitro. Consequently, MMP13-IN-2 holds great potential for advancing research on collagenase-related diseases.

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.

Galactosylhydroxylysine hydrochloride, a bone collagen component generated through hydroxylysine's post-translational glycosylation, is liberated during bone resorption. Its levels increase in cases of metabolic bone loss [1].

TGFβ-IN-2 (Compound 9d) effectively inhibits TGF-β-induced accumulation of total collagen in NRK-49F cells, with an IC50 value of 4.31 μM. It also suppresses the TGF-β-induced in vitro expression of COL1A1, α-SMA, and p-Smad3. Additionally, TGFβ-IN-2 shows promise as a potential anti-fibrosis compound for in vivo applications through oral administration [1].

GPVI antagonist 3 (Compound 2) is a promising antiplatelet agent that selectively inhibits the interaction between the Glycoprotein VI (GPVI) receptor and its ligands. It demonstrates potent inhibitory effects with IC50 values of 1.01 μM for collagen, 1.92 μM for CRP, 7.24 μM for convulxin, and 51.74 μM for thrombin, positioning it as a potential novel antithrombotic treatment [1].

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)

Tetrapeptide-11 is the reaction product of Acetic Acid and tetrapeptide-11, containing leucine, proline, and tyrosine residues. It boosts cell growth, Syndecan-1, and Collagen XVII synthesis. Tetrapeptide-11 has a face and body anti-wrinkle and anti-aging

Collagen type IV alpha1 (531-543) is a protein that in humans is encoded by the COL4A1 gene on chromosome 13. It is ubiquitously expressed in many tissues and cell types. COL4A1 is a subunit of type IV collagen and plays a role in angiogenesis.

Kartogenin (KGN) sodium acts as an inducer of chondrogenic tissue formation (EC 50: 100 nM). It promotes chondrogenesis by binding to fibrin A, disrupting its interaction with the transcription factor core binding factor beta subunit (CBFβ), and modulating the CBFβ-RUNX1 transcriptional program. Additionally, Kartogenin sodium aids tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. It is extensively utilized in cell-free therapies for cartilage regeneration and protection, tendon-bone healing, wound healing, and limb development. The compound is also vital for cartilage repair, coordinating limb development, and osteoarthritis (OA) research [1] [2] [3] [4].

Tetrapeptide-4 is a peptide commonly incorporated into skincare formulations for its anti-aging benefits, which include diminishing wrinkles and fortifying collagen, elastin, and fibronectin [1].

Collagen Type II Fragment is a peptide with anti-inflammatory properties that effectively inhibits collagen-induced arthritis (CIA) in mice. It is useful for research focused on inflammation and immunity [1].

Angiotensin II human TFA, a potent vasoconstrictor within the renin/angiotensin system, plays a pivotal role in human blood pressure regulation primarily through interactions with the G-protein-coupled receptors Angiotensin II type 1 receptor (AT1R) and Angiotensin II type 2 receptor (AT2R). It not only prompts sympathetic nervous stimulation, aldosterone biosynthesis, and renal effects but also fosters growth in vascular smooth muscle cells and boosts collagen type I and III synthesis in fibroblasts. This action results in the thickening of the vascular wall and myocardium, alongside fibrosis. Additionally, Angiotensin II human TFA triggers apoptosis and encourages capillary formation from endothelial cells through the LOX-1 dependent redox-sensitive pathway [1] [2] [3] [4].

TP0556351, a potent and selective inhibitor of matrix metalloproteinase-2 (MMP2), exhibits significant efficacy with an IC50 of 0.2 nM and demonstrates the capability to decrease collagen accumulation in a Bleomycin-induced pulmonary fibrosis mouse model. This compound shows promise as a research tool for idiopathic pulmonary fibrosis (IPF) [1].

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 μM), showing no effect on PAR-2, PAR-3, or PAR-4. It inhibits the aggregation of human platelets induced by SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), with high selectivity relative to U46619. RWJ-56110 dihydrochloride also blocks angiogenesis and the formation of new vessels in vivo, and induces cell apoptosis[1][2].

PalMitoyl Tripeptide-1 affects the synthesis of collagen, fibronectin and hyaluronic acid in human skin fibroblasts and can be used to prepare anti-aging cosmetics.

GRGESP, a collagen gel contraction inhibitor, impedes human fibroblast spreading within collagen gels and significantly reduces gel contraction, making it a valuable agent for research in connective tissue morphogenesis [1].

1. Darutoside (Darutin) can as an appropriate treatment for wounds. 2. Darutoside can improve skin elasticity, surface appearance and stretch mark removal, through soothing the skin, decreasing inflammation, restoring collagen and promoting collagen production.

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

GPR183 antagonist-2 (compound 32), a selective antagonist of GPR183, exhibits excellent water solubility and pharmacokinetic properties. This compound effectively diminishes paw and joint swelling, and reduces gene expression of pro-inflammatory cytokines (MCP-1, MMPs, and VEGF) in a dose-dependent manner within a collagen-induced arthritis (CIA) mouse model. GPR183 antagonist-2 is applicable in researching autoimmune diseases [1].

NJK14047 inhibits p38 MAPK and prevents the differentiation of naive T-cells into Th1 and Th17 cells, thereby ameliorating collagen-induced rheumatoid arthritis and Imiquimod-induced psoriasis in mice [1].

MCI, a chemical compound demonstrating significant anti-inflammatory effects, particularly in collagen-induced arthritis (CIA) models, modulates inflammation through macrophage reprogramming by enhancing ROS scavenging and promoting COX-2 downregulation. It effectively inhibits COX-2, exhibiting an IC50 of 1.23 μM. Additionally, MCI holds potential for research applications in rheumatoid arthritis (RA) [1].

Diethyl pyimDC is an inhibitor of human collagen prolyl 4-hydroxylase 1 (CP4H1).

Ganodermaones B is a renal fibrosis inhibitor. Ganodermaones B inhibits TGF-β1-induced collagen I and fibronectin expression .

Pal-KTTKS is a lipidated pentapeptide consisting of a fragment of the type I collagen C-terminal propeptide conjugated to palmitic acid .1 It increases collagen production in human corneal and dermal fibroblasts when used at concentrations of 0.002, 0.004, and 0.008 wt%.2 Following topical administration, pal-KTTKS (50 μg/cm2) is found in the stratum corneum, epidermis, and dermis of isolated hairless mouse skin.1 It can self-assemble into flat tapes and extended fibrillar structures.3 Pal-KTTKS has been detected in anti-wrinkle creams.4 |1. Choi, Y.L., Park, E.J., Kim, E., et al. Dermal stability and in vitro skin permeation of collagen pentapeptides (KTTKS and palmitoyl-KTTKS). Biomol. Ther. (Seoul) 22(4), 321-327 (2014).|2. Jones, R.R., Castelletto, V., Connon, C.J., et al. Collagen stimulating effect of peptide amphiphile C16-KTTKS on human fibroblasts. Mol. Pharm. 10(3), 1063-1069 (2013).|3. Castelletto, V., Hamley, I.W., Whitehouse, C., et al. Self-assembly of palmitoyl lipopeptides used in skin care products. Langmuir 29(29), 9149-9155 (2013).|4. Chirita, R.-I., Chaimbbault, P., Archambault, J.-C., et al. Development of a LC-MS/MS method to monitor palmitoyl peptides content in anti-wrinkle cosmetics. Anal. Chim. Acta 641(1-2), 95-100 (2009).

4-hydroxy Valsartan is a major metabolite of the angiotensin II type 1 (AT1) receptor antagonist valsartan . It reduces platelet aggregation induced by epinephrine and collagen but not ADP in human whole blood.

SR-1903 is a modulator of retinoic acid receptor-related orphan receptor γ (RORγ) and liver X receptor (LXR). It is an inverse agonist of RORγ and an agonist of LXR. It also binds to peroxisome proliferator-activated receptor γ (PPAR) but does not activate it. SR-1903 inhibits LPS-induced expression of triggering receptor expressed on myeloid cells 1 (TREM-1). It also inhibits LPS-induced expression of the LXR target genes IL-6 and IL-33 and increases expression of ABCG1, FASN, and SCD-1. SR-1903 reduces the severity of collagen-induced arthritis. It reduces blood glucose levels in a glucose tolerance test, serum levels of total cholesterol and LDL, body weight, and fat mass in a mouse model of high-fat diet-induced obesity.

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

CD36 Peptide P (93-110), Cys conjugated, a Cys-labelled CD36 Peptide, blocks the binding of CD36 to immobilized thrombospondin and partially inhibits collagen-induced platelet aggregation [1].

AF299 decreases collagen-related peptide-induced platelet Ca2+ levels and inhibits collagen-induced platelet aggregation. It is applicable for antiplatelet research [1].

N-Acetyldopamine dimers A (Compound (+)-2) can be isolated from the cast-off shell of the cicada Cryptotympana sp. and increase collagen and α-SMA expression [1].