86030-08-2
86030-08-2 structure
- Name: BTB1
- Chemical Name: 1-(benzenesulfonyl)-4-chloro-2-nitrobenzene
- CAS Number: 86030-08-2
- Molecular Formula: C12H8ClNO4S
- Molecular Weight: 297.71400
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Microtubule/Tubulin
- Create Date: 2018-04-20 08:00:00
- Modify Date: 2024-01-11 16:06:04
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BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC50 of 1.69 μM.
| Name | 1-(benzenesulfonyl)-4-chloro-2-nitrobenzene |
|---|---|
| Synonyms |
4-Chloro-2-nitrodiphenylsulfone
4-Chlor-2-nitro-diphenylsulfon 4-Chloro-2-nitro-1-(phenylsulfonyl)benzene (4-Chlor-2-nitro-phenyl)-phenyl-sulfon 4-chloro-2-nitrodiphenyl sulphone 4-chloro-2-nitrophenyl phenyl sulfone BTB-1 |
| Description | BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC50 of 1.69 μM. |
|---|---|
| Related Catalog | |
| 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-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 |
| Density | 1.476g/cm3 |
|---|---|
| Boiling Point | 471.2ºC at 760mmHg |
| Melting Point | 115ºC |
| Molecular Formula | C12H8ClNO4S |
| Molecular Weight | 297.71400 |
| Flash Point | 238.8ºC |
| Exact Mass | 296.98600 |
| PSA | 88.34000 |
| LogP | 4.68500 |
| Index of Refraction | 1.623 |
| Storage condition | 2-8℃ |
| Risk Phrases | 36/37/38 |
|---|---|
| Safety Phrases | S26-S36-S37-S39 |
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| Literature: Journal of the Chemical Society, , p. 1618,1621 |
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| Literature: Journal of the Chemical Society, , p. 1618,1621 |
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| Literature: Journal of the Chemical Society [Section] B: Physical Organic, , p. 260 - 266 |
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| Literature: Journal of the Chemical Society, Perkin Transactions 2: Physical Organic Chemistry (1972-1999), , p. 105 - 108 |
