research use only
Cat.No.S7336
| 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) Combretastatin A4 Epothilone A ABT-751 (E7010) TAI-1 Cucurbitacin B INH1 |
| Molecular Weight | 500.33 | Formula | C23H21IN2O3 |
Storage (From the date of receipt) | |
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| CAS No. | 1594094-64-0 | Download SDF | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | C1=CC=C(C=C1)CC(C(=O)NC2=C(C=C(C=C2)I)C(=O)O)NCC3=CC=CC=C3 | ||
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In vitro |
DMSO
: 100 mg/mL
(199.86 mM)
Ethanol : 4 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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
| Features |
Allosteric, HSET-selective inhibitor.
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| Targets/IC50/Ki |
HSET
75 μM
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| In vitro |
CW069 increases multipolar spindles in N1E-115 cells with supernumerary centrosomes without altering bipolar spindle morphology in normal human dermal fibroblast cells. This compound inhibits growth in cancer N1E-115 cells with IC50 of 10 μM, but not in NHDF or primary human bone marrow cells.
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| Kinase Assay |
In Vitro Enzymatic ATPase Assay
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The protocol is optimized for use with full-length, N-terminal, 6His-tagged HSET and KSP, and measured the MT-stimulated activity of the proteins. Inhibition of the Gsp synthetase activity of HSET/KSP is observed spectrophotometrically by coupling the hydrolysis of ATP to oxidation of NADH via pyruvate kinase/lactate dehydrogenase reactions. The assay is initiated by adding purified Gsp synthetase/amidase (12.8 nM) to an assay mixture containing the following components (final concentration): 6 nM protein, 0.07 mg/ml MTs (University Biologicals), 1.56 mM glutathione, 10 mM spermidine, 2 mM ATP, 2.7 mM MgCl2, 1 mM phospho(enol)-pyruvate, 0.2 mM NADH, 50 μg/ml lactate dehydrogenase, 100 μg/ml pyruvate kinase, and various concentrations of this compound all in 50 mM Na PIPES (pH 6.8) at 37°C. The ADP-Glo detection assay (Promega) is performed as described in the manufacturer’s instructions. All compound additions were performed using a multidrop BioMek Nxp. Plates were read using a Pherastar microplate reader.
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References |
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