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