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Thiocolchicine, a derivative of colchicine, exhibits potent inhibition of microtubule assembly (IC50 = 2.5 µM). By impeding the binding of colchicine to tubulin (Ki = 0.7 µM in a radioligand binding assay), it exerts its inhibitory effects. Thiocolchicine proves effective in suppressing the proliferation of MDA-MB-231. Functioning as an antimitotic alkaloid, thiocolchicine plays a role as an inhibitor of tubulin polymerization and microtubule assembly, thereby modulating the axonal cytoskeleton. It also serves as an apoptosis inducer. Notably, the presence of thiocolchicine-dimers demonstrates potent inhibition of topoisomerase I activity. Structurally analogous to colchicine, thiocolchicine replaces the C-10 methoxy group with a thiomethyl moiety. This substitution enables high-affinity binding to the colchicine site on tubulin (Ka = 1.07 +/- 0.14 x 10 M-1). Additionally, the formation of thiocolchicine-dimers further enhances its potency as a topoisomerase I inhibitor.
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Thiocolchicine, 5 mg | sc-202838A | 5 mg | $125.00 | |||
Thiocolchicine, 100 mg | sc-202838 | 100 mg | $194.00 |