LOX-IN-3, an orally active inhibitor of lysyl oxidase (LOX), holds potential application in the fields of fibrosis, cancer, and angiogenesis research[1].
LOX-IN-3 dihydrochloride monohydrate (Compound 33) is a lysyl oxidase (LOX) inhibitor with oral activity. It is specifically designed for research purposes in the areas of fibrosis, cancer, and angiogenesis [1].
COX-2 5-LOX-IN-3 (compound 5b) is a powerful and dual inhibitor of COX-2 and 5-LOX, with IC50 values of 45.73 μM, 5.45 μM, and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. This compound, COX-2 5-LOX-IN-3, shows promise for the investigation of inflammatory diseases [1].
BX-320 is an inhibitor of the serine/threonine kinase 3-phosphoinositide-dependent protein kinase 1 (PDK1; IC50= 30 nM).1It is selective for PDK1 over a panel of 10 additional kinases (IC50s = >820 nM for all). BX-320 inhibits Akt and p70S6K1 phosphorylation in PC3 cells (IC50s = 1-3 μM). It induces apoptosis in, and inhibits the growth of, MDA-MB-468 breast cancer cells (IC50s = 0.5 and 0.6 μM, respectively), as well as inhibits cell growth in a panel of cancer cells (IC50s = 0.12-1.2 μM). BX-320 (200 mg/kg) inhibits the growth of lung tumors in a LOX melanoma mouse model of blood-borne metastasis. 1.Feldman, R.I., Wu, J.M., Polokoff, M.A., et al.Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1J. Biol. Chem.280(20)19867-19874(2005)
Angiotensin II human TFA 是肾素-血管紧张素系统中的强效血管收缩剂,通过与 AT1R 和 AT2R 受体作用调节血压,可激活交感神经、促进醛固酮合成和肾功能,诱导血管平滑肌细胞增殖及成纤维细胞中 I 型和 III 型胶原合成,导致血管和心肌增厚、纤维化,并诱导凋亡及促进毛细血管生成,可用于构建心脏肥大、高血压和腹主动脉瘤模型。
Selaginellin has a neuroprotective effect against L-glutamate-induced neurotoxicity through mechanisms related to anti-oxidation and anti-apoptosis via scavenging reactive oxygen species and up-regulating the expression of klotho gene. Selaginellin shows