Tubulin inhibitor 23

Tubulin inhibitor 23 is a potent Tubulin inhibitor with an IC50 of 4.8 µM. Tubulin inhibitor 23 induces cell apoptosis. Tubulin inhibitor 23 shows antiangiogenic activity in a dose-dependent manner. Tubulin inhibitor 23 has the potential for the research of leukaemia[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

IC50: 4.8 µM (Tubulin)[1]

Tubulin inhibitor 23 (compound 29e) (0-100 µM) inhibits tubulin polymerisation (IC50=4.8 µM) and anti-angiogenesis (IC50=3.4 µM) in Zebrafish[1]. Tubulin inhibitor 23 (0-200 nM; 48 h) induces cell apoptosis in a concentration-dependent manner[1]. Tubulin inhibitor 23 (0-20 µM; 0-29 min) binds to the colchicine site of tubulin and inhibit the microtubule polymerisation[1]. Tubulin inhibitor 23 (0.1, 1, 10 µM; 1 h) shows anti-angiogenesis activity with low toxicity (IC50=58.6 µM) in Human umbilical vein endothelial cells (HUVECs)[1]. Cell Proliferation Assay[1] Cell Line: MV4-11, HL60, K562, THP-1,CCRF-CEM, Jurkat, HuT 78 cells Concentration: Incubation Time: 72 h Result: Showed potent growth inhibitory activity with IC50s of 0.25, 0.18, 0.09, 0.37, 0.84, 1.22, 0.26 µM for MV4-11, HL60, K562, THP-1,CCRF-CEM, Jurkat, HuT 78 cells, respectively. Apoptosis Analysis[1] Cell Line: K562 cells Concentration: 0, 50, 100, 200 nM Incubation Time: 48 h Result: The percentage of apoptotic cell significantly increased from 5.95% to 45.81%. Western Blot Analysis[1] Cell Line: K562 cells Concentration: 0, 50, 100, 200 nM Incubation Time: 48 h Result: Increased the expression of cleaved caspase-3 and PARP.

Tubulin inhibitor 23 (2, 6 µM; add into embryo water) shows antiangiogenic activity in a dose-dependent manner[1]. Tubulin inhibitor 23 (2, 6 µM; add into embryo water) suppresses the proliferation and metastasis of K562 cells in zebrafish xenografts in a dose-dependent manner[1]. Animal Model: 3hpf zebrafish embryos[1] Dosage: 2.0, 6.0 µM Administration: Add into embryo water Result: Decreased the number and length of ISVs (intersegmental vessels) in a dose-dependent inhibition pattern. Animal Model: Transgenic zebrafish (fil1:EGFP) (K562 cell xenograft)[1] Dosage: 2, 6 µM Administration: Add into embryo water Result: Reduced intensities and decreased tumour area.

[1]. Yao Y,wt al. Angiogenesis and anti-leukaemia activity of novel indole derivatives as potent colchicine binding site inhibitors. J Enzyme Inhib Med Chem. 2022 Dec;37(1):652-665.