MDL-27048 

MDL-27048, a tubulin inhibitor, binds competitively, reversibly to the Colchicine (HY-16569)-binding site on tubulin heterodimers. MDL-27048 inhibits microtubule assembly, induces slow depolymerization of preassembled microtubules, disrupts microtubule polymerization-depolymerization dynamics, and disrupts cytoplasmic microtubule networks. MDL-27048 exerts growth inhibitory effects on human cancer cells, induces mitotic arrest, and does not disrupt actin filaments at microtubule-depolymerizing concentrations. MDL-27048 can be used for the research of malignant tumors^[1][2].

MDL-27048 (0.4-20 μM; 40 min, 25 °C) binds reversibly to one site per purified porcine brain tubulin heterodimer with an apparent equilibrium constant of (2.1-3.5) × 10⁶ M^-1, and its binding site overlaps with the podophyllotoxin/colchicine-binding site^[2].
MDL-27048 (0.5-20 μM; 30-96 min) inhibits in vitro assembly of purified porcine brain tubulin into microtubules with an IC₅₀ of 1 μM at 1 mg/mL tubulin, induces slow depolymerization of pre-assembled microtubules, and its inhibitory effect is reversible with taxol^[2].
MDL-27048 (0.2-10 μM; 10 min-4 h, monitored 2-30 min after wash-off) induces concentration- and time-dependent reversible depolymerization of PtK2 cell cytoplasmic microtubules, with maximal depolymerization achieved at 2-5 μM for 3 h, and complete repolymerization within 15-30 min after drug removal^[2].
MDL-27048 (0.05-1 μM; 3-27 h) induces mitotic arrest in SV40-3T3 cells, with significant arrest at 0.2 μM and a mitotic index increase to 12.7% at 1 μM after 9 h, causing accumulation of cells with doubled DNA content^[2].

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

325.40

C₂₀H₂₃NO₃

124711-23-5

CN(C)C(C=C1)=CC=C1/C=C(C)/C(C2=C(C=CC(OC)=C2)OC)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Kim DY, et al. Design and biological evaluation of novel tubulin inhibitors as antimitotic agents using a pharmacophore binding model with tubulin. J Med Chem. 2006;49(19):5664-5670.  [Content Brief]

  [2]. Peyrot V, et al. Interaction of tubulin and cellular microtubules with the new antitumor drug MDL 27048. A powerful and reversible microtubule inhibitor. J Biol Chem. 1989 Dec 15;264(35):21296-301.