Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
BTB-1 is a novel, potent and the first small molecule inhibitor of the mitotic motor protein Kif18A. It exhibits selectivity within the Kif4, Eg5, MKLP-1, MKLP-2, MPP1, CENP-E, and MCAK kinesin subgroups. Antimitotic medications target kinesin motors because they have a variety of functions during mitosis. Kif18A is frequently overexpressed in solid tumors, so drugs such as BTB-1 are not only very interesting for basic research but may also lead to new approaches in the treatment of human diseases. BTB-1 was added during in vitro motility tests, and this reversibly inhibited Kif18A's ability to glide through MT. Surprisingly, BTB-1 traps Kif18A on the microtubule, while its binding site is similar to that of well-studied Kif11 inhibitors that prevent tight microtubule binding.
Targets |
Kif18A (IC50 = 1.69 μM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
In DMSO, BTB-1 is prepared. The His-Kif18Amotor sactivityis observed as ATP concentration increases when 3 μM Mts and increasing BTB-1 concentrations (0.21 μM, 0.42 μM, 0.85 μM, 1.7 μM) or DMSO as a control are present[1].
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Cell Assay |
In a reversible way, BTB-1 inhibits Kif18A motility. Cell division is slowed down by BTB-1, which inhibits Kif18A in a way that is competitive for adenosine triphosphate (ATP) but uncompetitive for microtubules. It was found that none of the other tested mitotic kinesins are significantly inhibited by 100 μM BTB-1. BTB-1 and ATP are only in competition for Kif18A binding when the motor protein is attached to its pseudosubstrate microtubules. BTB-1 treatment causes dose-dependent accumulation of HeLa cells during mitosis. With an EC50 value of 35.8 μM, BTB-1 exhibits cell toxicity. Severe defects in spindle morphology and chromosome alignment are observed in HeLa cells treated with 50 μM BTB-1. Longitudinal spindles are not produced by treatment with high BTB-1 concentrations.
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Animal Protocol |
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References |
Molecular Formula |
C12H8CLNO4S
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Molecular Weight |
297.71
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Exact Mass |
296.99
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Elemental Analysis |
C, 48.41; H, 2.71; Cl, 11.91; N, 4.70; O, 21.50; S, 10.77
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CAS # |
86030-08-2
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
C1=CC=C(C=C1)S(=O)(=O)C2=C(C=C(C=C2)Cl)[N+](=O)[O-]
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InChi Key |
VZDUQPHKUBZMLW-UHFFFAOYSA-N
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InChi Code |
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
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Chemical Name |
1-(benzenesulfonyl)-4-chloro-2-nitrobenzene
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.3590 mL | 16.7949 mL | 33.5897 mL | |
5 mM | 0.6718 mL | 3.3590 mL | 6.7179 mL | |
10 mM | 0.3359 mL | 1.6795 mL | 3.3590 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inhibition of Kif18A activities by BTB-1. Modeling of the putative BTB-1 binding site.ACS Chem Biol.2015 Feb 20;10(2):554-60. th> |
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Conformation of the MT-bound Kif18A motor domain in the presence of BTB-1.ACS Chem Biol.2015 Feb 20;10(2):554-60. td> |
Effect of point mutations of Kif18A around the putative BTB-1–binding pocket on BTB-1 inhibition of MT gliding activity.ACS Chem Biol.2015 Feb 20;10(2):554-60. td> |