tubulin polymerization inhibitor

Names

[ Name ]:
tubulin polymerization inhibitor

[Synonym ]:
9(10H)-Anthracenone, 10-[(3-hydroxy-4-methoxyphenyl)methylene]-
10-(3-Hydroxy-4-methoxybenzylidene)-9(10H)-anthracenone
10-(3-hydroxy-4-methoxybenzylidene)anthracen-9(10H)-one

Biological Activity

[Description]:

Tubulin polymerization-IN-24 (compound HMBA) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-24 inhibits MCF-7 cells proliferation. Tubulin polymerization-IN-24 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-24 increase the GTP hydrolysis rate and inhibits microtubule assembly[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin

Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

[In Vitro]

Tubulin polymerization-IN-24 (compound HMBA) inhibits the assembly of purified tubulin (MAPs-free) in a concentration dependent manner[1]. Tubulin polymerization-IN-24 (0-100 nM) inhibits MCF-7 proliferation in a concentration dependent fashion with an IC50 value of 47 nM[1]. Tubulin polymerization-IN-24 competitively inhibits colchicine binding to tubulin with a Ki value of 3.6 μM[1]. Tubulin polymerization-IN-24 inhibits the progression of MCF-7 cells in mitosis and induces apoptotic cell death involving p53 pathway[1].

[References]

[1]. Chatterji BP, et al. HMBA depolymerizes microtubules, activates mitotic checkpoints and induces mitotic block in MCF-7 cells by binding at the colchicine site in tubulin. Biochem Pharmacol. 2010 Jul 1;80(1):50-61.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
524.7±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₂H₁₆O₃

[ Molecular Weight ]:
328.361

[ Flash Point ]:
188.8±23.6 °C

[ Exact Mass ]:
328.109955

[ LogP ]:
3.80

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.700

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

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Exp. Hematol. 43 , 393-403.e2, (2015)

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J. Virol. 89 , 9841-52, (2015)

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Related Compounds

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