human primary fibroblasts

Nitisinone (SC0735) 是一种 4-羟基苯丙酮酸双加氧酶抑制剂。

VX-148是一种新型、非竞争性的IMPDH抑制剂，对IMPDH II型酶具有6 nM的K(i)值。在抑制原发性人类淋巴细胞（IC(50)值约为80 nM）的增殖方面，VX-148比麦考酚酸和VX-497略为有效。外源性鸟苷的存在可以缓解VX-148的抑制活性。VX-148不抑制如成纤维细胞等非淋巴细胞类型的增殖，显示出对IMPDH活性的选择性抑制。VX-148在大鼠和小鼠中具有口服生物利用度；口服VX-148以剂量依赖性抑制小鼠的初级抗体反应，ED(50)值为38 mg kg b.i.d。在小鼠中，VX-148以100 mg kg b.i.d.的剂量显著延长皮肤移植的存活时间。

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) 是一种分离自 Ulmus davidiana 根皮中的三萜类化合物，具有抗肿瘤作用，可以减缓人原始细胞的衰老。

4-CPPC 是一种巨噬细胞迁移抑制因子 2 (MIF-2; IC50= 27 μM) 的抑制剂。它对 MIF-2 的选择性高于 MIF-1 (IC50= 450 μM)。 当以 10 μM 浓度使用时，它在体外抑制 MIF-2，但不抑制 MIF-1，与 CD74 结合。 4-CPPC（5、10 和 25 μM）抑制原代人皮肤成纤维细胞中 MIF-2 诱导的 ERK1 2 磷酸化。

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），一种针对HDAC1 2的抑制剂，IC50分别为HDAC1和HDAC2的100 nM与92 nM。其对Caco-2细胞的IC50为4.1μM，并能下调原代正常人肺成纤维细胞中TGF-β1刺激的COL1A1 mRNA水平。此外，GK444还能抑制博来霉素诱发的小鼠肺纤维化。

1-花生四烯酰基溶血磷脂酸（1-arachidoyl LPA）是溶血磷脂酸受体1（LPA1）的激动剂，并且是一种含有花生四烯酸的甘油磷脂，花生四烯酸位于sn-1位置。它能在主要表达LPA1而非LPA2-LPA6的人类肺成纤维细胞中诱导钙离子动员（EC50 = 3.6 µM）。在无细胞试验中，1-Arachidoyl LPA（2.5 µM）还能结合到过氧化物酶体增殖物激活受体γ（PPARγ）的配体结合域。人类尿液中也发现了该化合物。