human primary fibroblasts

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

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.

1(R)-(Trifluoromethyl)oleyl alcohol is an analog of oleic acid .1It inhibits ferroptosis induced by erastin in primary fibroblasts isolated from patients with Friedreich ataxia, a neuro- and cardiodegenerative disorder characterized by loss or impaired activity of frataxin (FXN), when used at concentrations of 5, 10, or 20 μM. 1(R)-(Trifluoromethyl)oleyl alcohol (5 μM) reduces lipid peroxidation induced byFXNsiRNA knockdown in NBT human myoblasts. 1.Cotticelli, M.G., Forestieri, R., Xia, S., et al.Identification of a novel oleic acid analog with protective effects in multiple cellular models of Friedreich ataxiaACS Chem. Neurosci.11(17)2535-2542(2020)

S-Acetyl-L-glutathione is a derivative of glutathione .1 It increases intracellular GSH levels in primary fibroblasts derived from patients with glutathione synthetase deficiency when used at a concentration of 50 μM. S-Acetyl-L-glutathione (5 mM) induces apoptosis in Daudi, Raji, and Jurkat lymphoma cells.2 It inhibits the replication of herpes simplex virus 1 (HSV-1) in human foreskin fibroblasts when used at concentrations of 5 and 10 mM.3 S-Acetyl-L-glutathione (6.25 μg/g per day) increases survival in a mouse model of HSV-1 infection.

Epifriedelanol (Epifriedelinol) suppresses adriamycin-induced cellular senescence, replicative senescence in human fibroblasts (HDFs) and HUVECs. Because of Epifriedelanol can reduce cellular senescence in human primary cells, it may be used to develop dietary supplements or cosmetics that modulate tissue aging or aging-associated diseases.

4-CPPC is an inhibitor of macrophage migration inhibitory factor-2 (MIF-2; IC50= 27 μM).1It is selective for MIF-2 over MIF-1 (IC50= 450 μM). It inhibits MIF-2, but not MIF-1, binding to CD74in vitrowhen used at a concentration of 10 μM. 4-CPPC (5, 10, and 25 μM) inhibits MIF-2-induced ERK1 2 phosphorylation in primary human skin fibroblasts. 1.Tilstam, P.V., Pantouris, G., Corman, M., et al.A selective small-molecule inhibitor of macrophage migration inhibitory factor-2 (MIF-2), a MIF cytokine superfamily member, inhibits MIF-2 biological activityJ. Biol. Chem.294(49)18522-18531(2019)

Clobetasol propionate-d5 is intended for use as an internal standard for the quantification of clobetasol propionate by GC- or LC-MS. Clobetasol propionate is a corticosteroid. It binds to glucocorticoid receptors in a cell-free assay and inhibits proliferation of primary human skin fibroblasts when used at a concentration of 5 µg ml. Topical administration of clobetasol propionate reduces croton oil-induced ear edema in mice. Formulations containing clobetasol propionate have been used in the treatment of inflammatory skin conditions.

GK444 (Compound 15a), a selective HDAC1 2 inhibitor with IC50 values of 100 nM and 92 nM for HDAC1 and HDAC2 respectively, demonstrates an IC50 of 4.1 μM in Caco-2 cell inhibition. Additionally, GK444 attenuates TGF-β1-induced COL1A1 mRNA expression in primary normal human lung fibroblasts and mitigates Bleomycin-induced lung fibrosis in mice [1].

1-Arachidoyl lysophosphatidic acid (1-arachidoyl LPA), a glycerophospholipid with arachidic acid at the sn-1 position, functions as an agonist for lysophosphatidic acid receptor 1 (LPA1). It effectively induces calcium mobilization in primary human lung fibroblasts at an EC50 value of 3.6 µM, given these cells inherently express LPA1 but lack expression of LPA2-LPA6 receptors. Additionally, at a concentration of 2.5 µM, 1-arachidoyl LPA binds to the ligand-binding domain of peroxisome proliferator-activated receptor γ (PPARγ) in a cell-free environment. This compound has also been detected in human urine.