BTB1, a novel inhibitor of the mitotic motor protein Kif18A.

BTB1 an ATP-competitive and selective inhibitor of the mitotic motor protein Kif18A with IC50 value of 17 M

Product information

CAS Number: 86030-08-2

Molecular Weight: 297.71

Formula: C12H8ClNO4S

Chemical Name: 4-chloro-2-nitro-1-(phenylsulfonyl)benzene

Smiles: [O-][N+](=O)C1=CC(Cl)=CC=C1S(=O)(=O)C1C=CC=CC=1

InChiKey: VZDUQPHKUBZMLW-UHFFFAOYSA-N

InChi: InChI=1S/C12H8ClNO4S/c13-9-6-7-12(11(8-9)14(15)16)19(17,18)10-4-2-1-3-5-10/h1-8H

Technical Data

Appearance: Solid powder

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 60 mg/mL(201.53 mM). Water: Insoluble.

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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-1 does 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 EC50 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].

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.

Products are for research use only. Not for human use.