research use only
Cat.No.S7493
| Related Targets | Akt Wnt/beta-catenin PKC HSP ROCK Integrin Bcr-Abl Actin FAK Kinesin |
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| Other Microtubule Associated Inhibitors | Nocodazole MMAF Patupilone (Epothilone B) Lexibulin (CYT997) CW069 Combretastatin A4 Epothilone A ABT-751 (E7010) TAI-1 Cucurbitacin B |
| Molecular Weight | 308.40 | Formula | C18H16N2OS |
Storage (From the date of receipt) | |
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| CAS No. | 313553-47-8 | Download SDF | Storage of Stock Solutions |
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| Synonyms | IBT 13131 | Smiles | CC1=CC(=C(C=C1)C2=CSC(=N2)NC(=O)C3=CC=CC=C3)C | ||
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In vitro |
DMSO
: 61 mg/mL
(197.79 mM)
Ethanol : 61 mg/mL Water : Insoluble |
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In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Targets/IC50/Ki |
Hec1
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| In vitro |
INH1 reduces the association of Hec1 with kinetochore and decreases global Nek2 protein level in cells. This compound effectively inhibits the proliferation of human breast cancer lines with GI50 of 10-21 μM. Moreover, it also elicits cell killing activity in part through impairing the Hec1/Nek2 pathway for the spindle checkpoint regulation.
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| Kinase Assay |
Binding assays
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Surface plasma resonance (SPR) assays are performed at 22.5°C in HBSD buffer [10 mmol/L HEPES, 150 mmol/L NaCl, 0.1% DMSO (pH 7.5)] on Biacore 3000. 6×His-Hec1 and GST-Nek2 are purified. NTA sensor chip or glutathione-modified CM5 chip are used to capture His-Hec1 and GST-Nek2, respectively. The capture level is about 140 to 180 resonance units (RU) at the flow rate of 5 μL/min. For the binding assay, chips are sequentially treated with this compound (1 or 20 μmol/L) and then proteins (50 μg/mL). Retained RUs are recorded and processed (triplicate experiments).
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| In vivo |
INH1 (100 mg/kg i.p.) inhibits breast tumour growth in mice bearing MDA-MB-468 human breast cancer xenograft.
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References |
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