BTB-1_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Libraries

www.MedChemExpress Data Sheet

实心盘

BIOLOGICAL ACTIVITY:

隔声工程BTB–1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC 50 of 1.69 μM.

IC50 & Target: IC50: 1.69 μM (Kif18A)[1]

In Vitro: BTB–1 blocks the motility of Kif18A in a reversible manner. BTB–1 inhibits Kif18A in an adenosine triphosphate

(ATP)–competitive but microtubule–uncompetitive manner and slows down the progression of cells through mitosis. 100 μM BTB–1does not significantly inhibit any of the other tested mitotic kinesins. BTB–1 competes with ATP for Kif18A binding only when the motor–protein is associated with its pseudosubstrate microtubules. HeLa cells treated with BTB–1 accumulate in mitosis in a dose–dependent manner [1]. BTB–1 shows cell toxicity with an EC 50 values of 35.8 μM. HeLa cells treated with 50 μM BTB–1 reveals severe defects in spindle morphology and chromosome alignment. Treatment with high concentrations of BTB–1 does not result in elongated spindles [2].

PROTOCOL (Extracted from published papers and Only for reference)

Kinase Assay:[1] BTB–1 is prepared in DMSO. The activity of His–Kif18A motor at increasing concentrations of ATP is monitored in the presence of 3 μM Mts and increasing concentrations of BTB–1 (0.21 μM, 0.42 μM, 0.85 μM, 1.7 μM) or DMSO as control [1].References:

[1]. Catarinella M, et al. BTB–1: a small molecule inhibitor of the mitotic motor protein Kif18A. Angew Chem Int Ed Engl. 2009;48(48):9072–6.

[2]. Braun J, et al. Synthesis and biological evaluation of optimized inhibitors of the mitotic kinesin Kif18A. ACS Chem Biol. 2015 Feb 20;10(2):554–60.

malaki paul

Product Name:

BTB–1Cat. No.:

生铁冶炼HY-101770CAS No.:j biol chem

86030-08-2Molecular Formula:

C 12H 8ClNO 4S Molecular Weight:

297.71Target:

Microtubule/Tubulin; Microtubule/Tubulin Pathway:

Cell Cycle/DNA Damage; Cytoskeleton Solubility:

10 mM in DMSO

外墙金属复合板

Caution: Product has not been fully validated for medical applications. For research use only.