Tubulin polymerization-IN-41 

Tubulin polymerization-IN-41 is a potent tubulin polymerization inhibitor with the IC₅₀ of 2.61 μM. Tubulin polymerization-IN-41 targets the Colchicine-binding site of tubulin. Tubulin polymerization-IN-41 has anticancer effects^[1].

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^[1].
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^[1].
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^[1].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

435.26

C₂₀H₁₆Cl₂N₂O₅

2804026-81-9

O=C(N1[C@@H](C2=CC3=C(C=C2C[C@H]14)OCCO3)C5=CC(Cl)=C(C(Cl)=C5)OC)NC4=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jiafu Leng, et al. Discovery of Novel N-Heterocyclic-Fused Deoxypodophyllotoxin Analogues as Tubulin Polymerization Inhibitors Targeting the Colchicine-Binding Site for Cancer Treatment. J Med Chem. 2022 Dec 22;65(24):16774-16800.  [Content Brief]