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Tubulin polymerization-IN-41
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Tubulin polymerization-IN-41
CAS No. : 2804026-81-9
MCE 站:Tubulin polymerization-IN-41
产品活性:Tubulin polymerization-IN-41 是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂,IC50 为 2.61 μM。Tubulin polymerization-IN-41 靶向微管蛋白的秋水仙碱结合位点。Tubulin polymerization-IN-41 具有抗癌作用。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton | Apoptosis
作用靶点:Microtubule/Tubulin | Apoptosis
In Vitro: Tubulin polymerization-IN-41 (compound C3) displays remarkable antiproliferative activities with IC50 values of 6.3 nM, 9.2 nM, 8.3 nM, and 8.7 nM for K562, MCF-7, HT29, and HCT116 cells, respectively. Additionally, Tubulin polymerization-IN-41 shows marked activity against Paclitaxel-resistant MCF-7 cells and A549 cells.
Tubulin polymerization-IN-41 (compound C3; 5-20 nM) downregulates the expression of acetyl-α-tubulin (Ac-α-tubulin) and upregulated the expression of detyrosinated-α-tubulin (DeY-α-tubulin) in a concentration-dependent manner.
Tubulin polymerization-IN-41 (compound C3; 5-20 nM; 24 hours) could arrest cancer cells in the G2/M phase, and induces MCF-7 cells apoptosis in a concentration-dependent manner.
Tubulin polymerization-IN-41 (compound C3; 5-20 nM; 24 hours) reduces Ser216 phosphorylation, resulting in cdc2 Tyr15 dephosphorylation and Thr161 phosphorylation, which ultimately leads to the activation of subsequent cdc2/cyclin B1 complex.
In Vivo: Tubulin polymerization-IN-41 (compound C3; 5-20 mg/kg; i.p; every two days; for 21 consecutive days) exhibits the significant potency of tumor growth inhibition in a dose dependence without weight loss in the drug-treated period.
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