Tubulin degrader 1

Tubulin degrader 1 (Compound 5i) potently inhibits the proliferation of human cancer cell lines HeLa, HCT116, MCF-7, K562 and Molm-13, with IC₅₀ values ranging from 0.02 to 0.05 μM after 72 h of incubation. It also potently inhibits the proliferation of multidrug-resistant human cancer cell lines A2780T, A549T, MCF-7/ADR and their sensitive parental cells, with IC₅₀ values ranging from 16 to 37 nM after 72 h of incubation, and shows a low drug resistance index^[1].
Tubulin degrader 1 (0.5-50 μM; 24 h) promotes α-tubulin degradation in a concentration-dependent manner in HeLa cells^[1].
Tubulin degrader 1 (5-10 μM; 5 min preincubation) inhibits tubulin polymerization in a cell-free system in a concentration-dependent manner when preincubated at concentrations of 5 μM or 10 μM for 5 minutes prior to the initiation of polymerization^[1].
Tubulin degrader 1 (0.2-25 μM) directly binds to the colchicine-binding site of tubulin in HeLa cells^[1].
Tubulin degrader 1 (100 nM; 24 h) disrupts the cellular microtubule network in HeLa cells and induces microtubule depolymerization^[1].
Tubulin degrader 1 (10-40 nM; 6 h) inhibits capillary network formation in human umbilical vein endothelial cells (HUVECs) in a concentration-dependent manner, and does not induce cytotoxicity at the aforementioned concentrations^[1].
Tubulin degrader 1 (3-300 nM; 24 h) induces concentration-dependent G₂/M cell cycle arrest in A2780S and A2780T ovarian cancer cells^[1].
Tubulin degrader 1 (3-300 nM; 48 h) induces concentration-dependent apoptosis in A2780S and A2780T ovarian cancer cells^[1].

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