Topoisomerase I IIinhibitor 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 IIinhibitor 3抑制细胞增殖、侵袭和迁移,诱导细胞凋亡(apoptosis)。Topoisomerase I IIinhibitor 3 在肝癌中具有研究价值。
Adenosine receptorinhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptorinhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].
Topoisomerase IIinhibitor 3 (Compound 6 h) is an acridone derivative that acts as a Type II DNA topoisomerase (topo II) inhibitor. It specifically inhibits the topo IIα β subtypes, with an IC50 value of 0.17 μM for topo IIα and 0.23 μM for topo IIβ. This compound elicits significant DNA damage and induces apoptosis by triggering the loss of mitochondrial membrane potential [1].
Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitorII is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitorII blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively).
β-Secretase InhibitorII is a tripeptide aldehyde compound that acts as an inhibitor of β-Secretase. It exhibits a simple structure and has an inhibitory potency of IC50 = 700 nM against total Aβ and IC50 = 2.5 μM specifically against Aβ 1-42. This compound is particularly useful in research related to Alzheimer's disease.
ALK5 InhibitorII is an ALK5 inhibitor. IC50: 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively.
Heat shock protein (Hsp) inhibitorII is the active form of Hsp inhibitor I and a benzylidene lactam compound that prevents the synthesis of inducible Hsps, such as Hsp105, Hsp72, and Hsp40. Hsp inhibitorII decreases Hsp72 synthesis in vivo and reduces thermotolerance of tumors in SCC VII tumor-containing mice. At 100 μM, it inhibits the development of thermotolerance in COLO 320 DM cells. Inhibition of Hsp70 with Hsp inhibitorII in combination with amphotericin B increases susceptibility of AmB-susceptible (MICs = 0.058 versus 0.27 μg ml for combined and AmB alone, respectively) and AmB-resistant (MICs = 21.33 versus >32 μg ml for combined and AmB alone, respectively) strains of A. fumigatus.
Lck inhibitorII is a cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a highly potent Lck (lymphocyte specific kinase) inhibitor
Type II topoisomerase inhibitor 1 可用于抗菌领域。Type II topoisomerase inhibitor 1 是大肠杆菌DNA 旋转酶的选择性抑制剂,IC50值为 1.7 nM,并能与 Asp73 残基形成氢键。Type II topoisomerase inhibitor 1 抑制拓扑异构酶 IV 的活性,IC50值为 0.98 μM。
JTE-952 is a oral, potent active and selective Type IIinhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse