mk-2-in-3

MK2-IN-3 (MK2 Inhibitor III) 是选择性的 MAPKAP-K2 (MK-2)抑制剂(IC50:8.5 nM)，能够抑制 U937 细胞及体内 TNFα 的生成。

MK2-IN-3 hydrate (MK-2 Inhibitor III) 是一种口服有活性的、ATP 竞争性的MAPKAP-K2 (MK-2)选择性抑制剂(IC50:0.85 nM)。

Ascr#2 (asc-C6-MK)是秀丽隐杆线虫中的糖苷类化合物，促进 dauer 形成。Ascr#2 在低浓度下与 ascr#3 的混合物可作为雄性引诱剂，可用于检测种群密度。

Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb MK cells (IC50 = 0.7 μg ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in osteoclasts with an IC50 value of 0.7 μM.

Reveromycin D is a bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb MK cells and has pH-dependent antifungal activity against C. albicans (MICs = 2 and >500 μg ml at pH 3 and 7.4, respectively). Reveromycin D also inhibits proliferation of KB and K562 cells (IC50s = 1.6 and 1.3 μg ml, respectively).

Dalotuzumab (MK-0646) 是一种靶向IGF-1R 的重组人源化单克隆抗体 (IgG1 型)。Dalotuzumab 通过抑制IGF-1和IGF-2介导的肿瘤细胞增殖、IGF-1R 自体磷酸化和Akt 磷酸化而发挥作用。Dalotuzumab 还可诱导细胞凋亡和周期停滞。Dalotuzumab 与其他抗癌活性分子（如他汀类活性分子）共同使用，可增强 Dalotuzumab 的体外和体内抗肿瘤活性。

Favezelimab（MK-4280）为人源化抗LAG-3单克隆抗体，能够抑制LAG-3与其配体MHC II类结合。该抗体联合PD-L1抑制剂Pembrolizumab在结直肠癌（CRC）治疗研究中展现出应用前景。