Glyoxalase I inhibitor 6 (Compound 9j) is an inhibitor of glyoxalase I (Glo-I) with an IC50 value of 1.13 μM. This compound shows potential as an anticancer agent, demonstrating low toxicity [1].
Glyoxalase I inhibitor 7 (Compound 6) is a potent inhibitor of glyoxalase I (Glo-I) with an IC50 of 3.65 μM. It exhibits potential as an anticancer agent [1].
Topoisomerase I inhibitor 7 (Compound 8) 是有效的Topoisomerase I 抑制剂。Topoisomerase I inhibitor 7 显著抑制肿瘤生长(高达 79%)。在接受 P388 淋巴瘤移植的小鼠模型中,Topoisomerase I inhibitor 7延长了小鼠寿命(153%)。
Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1].
Topoisomerase I II inhibitor 3 (化合物7) 是拓扑异构酶 I (Topo I)和 II (Topo II)的有效双抑制剂。 通过抑制 PI3K Akt mTOR 信号通路,Topoisomerase I II inhibitor 3抑制细胞增殖、侵袭和迁移,诱导细胞凋亡(apoptosis)。Topoisomerase I II inhibitor 3 在肝癌中具有研究价值。
Human PD-L1 inhibitor I is a peptide ligand that specifically inhibits the interaction between human PD-L1 and human PD-1. It exhibits a KD value of 3.39 μM, indicating its binding affinity. The presence of Human PD-L1 inhibitor I disrupts the binding between human PD-L1 and human PD-1, thereby attenuating their respective functions.
MMP inhibitor I is a peptide inhibitor of matrix metalloproteinase-1 (MMP-1), MMP-2, and MMP-3 (IC50s = 1.3, 30, and 150 μM, respectively). It is selective for MMP-1, MMP-2, and MMP-3 over the proteases thermolysin, urease, trypsin, α-chymotrypsin, plasmin, and elastase at concentrations up to 4 mM.
Topoisomerase I inhibitor 4 (compound 7a) is a potent inhibitor of topoisomerase I activity. It effectively inhibits the proliferation of various cancer cell lines including HepG2, A549, MCF-7, and HeLa, with IC50 values of 1.20 μM, 2.09 μM, 1.56 μM, and 1.92 μM, respectively. Thus, Topoisomerase I inhibitor 4 holds promise for cancer research applications [1].
GSK-3β inhibitor 6 is a highly potent inhibitor of GSK-3β, with an IC50 value of 24.4 μM. It demonstrates significant enhancement of hepatocyte glucose uptake (38%). This compound holds great potential for studying various diseases including diabetes, inflammation, cancer, Alzheimer's disease, and bipolar disorder [1].
Factor D inhibitor 6 is a potent, highly selective, orally active compound that specifically inhibits the activity of factor D (FD). It demonstrates an IC50 of 30 nM and a Kd of 6 nM. Notably, Factor D inhibitor 6 does not exhibit any inhibitory effects against factor B, classical and lectin complement-pathway activation, nor does it interfere with a broad array of receptors, ion channels, kinases, and proteases.