fs-3

ATX inhibitor 1是一种 ATX(IC50=1.23 nM, FS-3; 2.18 nM, bis-pNPP) 抑制剂。

GRI918013 是一种具有选择性且竞争性的自分泌运动因子(ATX/NPP2)抑制作用的化合物，能够抑制肿瘤细胞的侵袭和转移。GRI918013 通过与 ATX 的活性位点竞争结合，阻止溶血磷脂酰胆碱(LPC)等脂质底物进入，从而减少 ATX 催化 LPC 水解生成溶血磷脂酸(LPA)的过程，抑制 ATX-LPA 轴相关的细胞侵袭与转移。GRI918013 对 ATX 催化的 LPL 底物 FS-3 的抑制作用表现为 IC50 为 31.42 nM，Ki 为 12.98 nM。GRI918013可作为黑色素瘤等癌症侵袭与转移研究的工具，同时也适用于纤维化疾病、神经性疼痛及胆汁淤积性瘙痒等与 ATX-LPA 轴相关的疾病研究。

Heliquinomycin is a bacterial metabolite originally isolated fromStreptomycesthat has diverse biological activities.1It is active against a variety of Gram-positive bacteria, including strains ofB. anthracis, B. subtilis, and methicillin-sensitive or -resistantS. aureus(MICs = <0.05-0.39 μg/ml). Heliquinomycin inhibits the activity of DNA helicase with a Kivalue of 6.8 μM. It reduces the growth of L1210 leukemia, B16 melanoma, and FS-3 fibrosarcoma cells (IC50s = 0.97, 0.89, and 0.83 μg/ml, respectively). 1.Chino, M., Nishikawa, K., Umekita, M., et al.Heliquinomycin, a new inhibitor of DNA helicase, produced by Streptomyces sp. MJ929-SF2 I. Taxonomy, production, isolation, physico-chemical properties and biological activitiesJ. Antibiot. (Tokyo)49(8)752-757(1996)

1-Decarboxy-3-oxo-ceanothic acid shows in vitro cytotoxic activity in a human ovarian adenocarcinoma cell line, the cytotoxic effect is mediated, at least in part, by the induction of apoptosis. It shows cytotoxic against OVCAR-3 and HeLa cancer cell line

Lactonamycin 对革兰氏阳性菌具有显著的活性，包括葡萄球菌、链球菌、肠球菌、MRSA（MIC 为 0.39-0.78 μg/mL）以及 VRE（MIC 为 0.39-0.78 μg/mL）。同时，它也对多种肿瘤细胞株如 L-1210、P388、S180、FS-3、Ehrlich、B16-BL5 示现抑制作用（IC50为 0.06-3.3 μg/mL）。