human fibroblasts

CP-640186 is an isozyme-nonselective Acetyl-CoA carboxylase (ACCase) inhibitor. The IC50s of CP-640186(CP 640186) is 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively.

1,4-DPCA is an inhibitor of prolyl-hydroxylase with an IC50 of 2.4 µM for collagen hydroxylation in human foreskin fibroblasts and 60 μM for factor inhibiting HIF (FIH).

Azalanstat (RS 21607) is an orally available selective mammalian lanosterol 14-alpha-demethylase inhibitor with hypocholesterolemic activity that inhibits cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster livers through inhibition of the cytochrome P450 enzyme, lanosterol 14 alpha demethylase.

Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.

Nitisinone (SC0735)(SC0735) is an enzyme 4-hydroxyphenylpyruvate dioxygenase inhibitor.

Addition of the Rhamnose (6-Deoxy-L-mannose)-rich polysaccharide, RROP-1, to normal human dermal fibroblasts (NHDFs) and human endothelial cells produced a dose-dependent stimulation of the calcium-signaling pathway, inducing fast and transient increases in Ca2 influx and intracellular free Ca2 level.

1-Hydroxyoctadecane (OctadecanolOctadecanol) is a fatty alcohol present in human and is normally incorporated into plasmalogen lipids. Sjogren-Larsson syndrome is defined by the triad of ichthyosis, mental retardation, and spasticity, and patients accumulate fatty alcohols such as Octadenol in the plasma and cultured fibroblasts.

AS8351 (NSC51355) is a histone demethylase inhibitor. It has been used in combination with CHIR99021, A 83-01, BIX01294, SC-1, Y-27632, OAC2, SU 16f, and JNJ-10198409 to induce reprogramming of human fetal lung fibroblasts into functional cardiomyocytes.

Dieckol, a rhizomycin found in some brown algae species, has antimicrobial, anticancer, antioxidant, antiaging, antidiabetic, and neuroprotective effects, ameliorates acute hearing loss, and inhibits cell proliferation through cell cycle arrest in human tracheal fibroblasts via Hs680.Tr.

HG-6-63-01 serves as a type II RET tyrosine kinase inhibitor (TKI). It effectively targets and inhibits REarranged during Transfection (RET) kinase, disrupting signaling pathways in human thyroid cancer cell lines possessing oncogenic RET alleles. Moreover, this compound reduces the phosphorylation and signaling of RET oncogenic mutants. HG-6-63-01 further suppresses the proliferation of fibroblasts transformed by RET C634R and RET M918T, as well as thyroid cancer cells with RET mutations, showing potential as a therapeutic option for cancers with oncogenic activation of RET.

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.

Uridine triphosphate (UTP) is a purine nucleotide P2U receptor agonist with potential use in lung cancer treatment. By activating P2Y2 receptors, it enhances the proliferation of human cancerous ductal epithelial cells. Additionally, UTP induces fibrotic responses in cardiac fibroblasts through P2Y2 receptor activation and prolongs the action potential duration of guinea pig papillary muscles via the P2Y2 purinergic receptor.

VX-148 is a novel, non-competitive IMPDH inhibitor with a K(i) value of 6 nM for IMPDH Type II enzyme. It is slightly more effective than mycophenolic acid and VX-497 in inhibiting the proliferation of primary human lymphocytes (IC(50) approximately 80 nM). The presence of exogenous guanosine can mitigate VX-148's inhibitory activity. Notably, VX-148 does not impede the proliferation of non-lymphocyte types such as fibroblasts, indicating selective inhibition of IMPDH activity. The compound exhibits oral bioavailability in rats and mice; oral administration of VX-148 inhibits the primary antibody response in mice in a dose-dependent manner, with an ED(50) of 38 mg kg b.i.d. Additionally, in mice, VX-148 at a dosage of 100 mg kg b.i.d. significantly prolongs skin graft survival time.

Anticanceragent 271 (compound 5C) exhibits antiproliferative activity against lung cancer (A549), colon cancer (Caco-2) cell lines, and human lung fibroblasts (WI38), with an IC50 value of 9.18 μM for A549 cells. This compound can downregulate PI3K and mTOR gene expression and is applicable in cancer research.

Zoniporide (CP-597396) is an NHE-1 inhibitor that inhibits the uptake of 22Na+ by fibroblasts expressing human NHE-1 in a concentration-dependent manner, inhibits platelet swelling, and can be used in the study of cardiovascular diseases.

Induces p21 expression and S-phase arrest in cancer cells via ERK-mediated pathways. IC50 values are 0.89 and 12.6 μM for LoVo human colon cancer cell line and normal human fibroblasts respectively.

O4I2 is an effective Oct3 4 inducer in various human cell lines including human fibroblasts.

RBC10 inhibits the binding of Ral to its effector RALBP1, as well as inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines.

alpha-RA-F can modulate collagen synthesis and matrix metalloproteinases (MMPs) expression levels by boosting collagen synthesis and reducing MMPs expression levels in human fibroblasts without cytotoxicity.

Dracorhodin perchlorate inhibits cell growth, and induces apoptosis in fibroblasts in a dose-and time-dependent manner, arresting cell cycle at G1 phase, may as a candidate for anti-breast cancer. Dracorhodin perchlorate can inhibit high glucose-induced serum and glucocorticoid induced protein kinase 1 (SGK1) and fibronectin(FN) expression in human mesangial cells, and this may be part of the mechanism of preventing and treating renal fibrosis of DN.

AR 12465 is a trapidil derivative which may affect LDL receptor mediated uptake and degradation of 125 I-LDL by human skin fibroblasts (HSF) and human hepatic cells (HEP G2).

C012 Dihydrochloride is a novel small molecule compound that sensitized BRAF wild-type melanoma cells to verofenib. It can significantly reduce the activity of melanoma cells and has limited toxicity to normal human fibroblasts.

Terrain, also known as NSC 291308, is a fungal metabolite with diverse biological activities. Terrein reduces age-related inflammation induced by oxidative stress through Nrf2 ERK1 2 HO-1 signalling in aged HDF cells. (+)-terrein suppresses interleukin-6

Adenosine 5'-methylenediphosphate is an inhibitor of ecto-5'-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5'-monophosphate , adenosine 5'-diphosphate , or adenosine 5'-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5'-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) cells in a migration assay.2,3It increases tumor infiltration of CD3+CD8+T cells and reduces tumor growth in a K1735 murine melanoma model when administered at a dose of 400 μg mouse.4 1.Bruns, R.F.Adenosine receptor activation by adenine nucleotides requires conversion of the nucleotides to adenosineNaunyn Schmiedebergs Arch. Pharmacol.315(1)5-13(1980) 2.Braganhol, E., Tamajusuku, A.S.K., Bernardi, A., et al.Ecto-5′-nucleotidase CD73 inhibition by quercetin in the human U138MG glioma cell lineBiochim. Biophys. Acta1770(9)1352-1359(2007) 3.Shali, S., Yu, J., Zhang, X., et al.Ecto 5′ nucleotidase (CD73) is a potential target of hepatocellular carcinomaJ. Cell Physiol.234(7)10248-10259(2018) 4.Forte, G., Sorrentino, R., Montinaro, A., et al.Inhibition of CD73 improves B cell-mediated anti-tumor immunity in a mouse model of melanomaJ. Immunol.189(5)2226-2233(2021)