BTB-1|cas 86030-08-2|DC Chemicals

Cas No.:	86030-08-2
Chemical Name:	4-Chloro-2-nitro-1-(phenylsulfonyl)benzene
Synonyms:	Benzene,4-chloro-2-nitro-1-(phenylsulfonyl)-;1-(benzenesulfonyl)-4-chloro-2-nitrobenzene;1-Benzenesulfonyl-4-chloro-2-nitro-benzene;4-chloro-2-nitro-1-(phenylsulfonyl)benzene;4-CHLORO-2-NITRO-1-(PHENYLSULPHONYL)BENZENE;BTB1;(4-Chlor-2-nitro-phenyl)-phenyl-sulfon;4-Chlor-2-nitro-diphenylsulfon;4-chloro-2-nitrodiphenyl sulphone;4-Chloro-2-nitrodiphenylsulfone;4-chloro-2-nitrophenyl phenyl sulfone;BTB-1;4-Chloro-2-nitrodiphenyl sulfone;NSC156750;NSC658180;4-Chloranyl-2-Nitro-1-(Phenylsulfonyl)benzene;1-(benzenesulfonyl)-4-chloro-2-nitro-benzene;BTB 1;Maybridge1_000740;HMS543J14;ZX-A
SMILES:	ClC1C([H])=C([H])C(=C(C=1[H])[N+](=O)[O-])S(C1C([H])=C([H])C([H])=C([H])C=1[H])(=O)=O
Formula:	C₁₂H₈ClNO₄S
M.Wt:	297.7142
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC50 of 1.69 μM.
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].
Kinase Assay:	BTB-1 is prepared in DMSO. The activity of His-Kif18Amotor 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.

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