MELK-8a hydrochloride
Based on 3 publication(s) in Google Scholar
MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM.
For research use only. We do not sell to patients.
- Purity: 99.31%
- CAS No.: 2096992-20-8
- Formula: C25H33ClN6O
- Molecular Weight:469.02
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) MELK-8a hydrochloride
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Biological Activity
IC50: 2 nM (MELK)[1]
MELK-8a remains very potent (IC50=140 nM) when the ATP concentration in the biochemical assay is shifted from 20 μM to 2 mM. Its potency is well tracked between full-length MELK versus catalytic domain construct (5 nM versus 2 nM). It only inhibits seven off-target kinases in addition to MELK with >85% inhibition of binding at 1 μM demonstrating great selectivity. The compound is at least 90-fold more selective in targeting MELK in all cases. MELK-8a is fairly soluble (0.22 g/L at pH 6.8) and shows a good permeability in the Caco-2 assay. MELK-8a inhibits the growth of MDA-MB-468 cells and MCF-7 cells with an IC50 of approximately 0.06 and 1.2 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2096992-20-8
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Appearance Solid
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Molecular Weight 469.02
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Formula C25H33ClN6O
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Color Light yellow to yellow
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SMILES
CN(CC1)CCN1C2=CC=C(N3C=C(C4=CC=NC=C4OCC5CCNCC5)C=N3)C=C2.Cl
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Synonyms
NVS-MELK8a hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Rep
2017 Dec 5;21(10):2829-2841. PMID: 29212029
MELK-8a hydrochloride purchased from MedChemExpress. Usage Cited in: Cell Rep. 2017 Dec 5;21(10):2829-2841. [Abstract]
A375 cells are treated with MELK-8a for 48 h and analyzed for indicated proteins by immunoblot analysis. ACTINB is used for as a loading control.
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J Biol Chem
Mass spectrometry-based selectivity profiling identifies a highly selective inhibitor of the kinase MELK that delays mitotic entry in cancer cells. [Abstract]2020 Feb 21;295(8):2359-2374. PMID: 31896573
MELK-8a hydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374. [Abstract]
HeLaS3 cells treated with 8a complete mitosis and begin the subsequent cell cycle following delayed mitotic entry. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO or 3 μM 8a. Cells are collected starting at 6h post-release, with subsequent collections completed every 2h over a 20h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The split in the image indicates that the samples from DMSO and 3 μM 8a conditions are blotted sepa
MELK-8a hydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374. [Abstract]
Delayed mitotic entry caused by 8a is associated with delayed activation of Aurora A, Aurora B, and CDK1. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO or 3 μM 8a. Cells are collected starting at 6h post-release, with subsequent collections completed every 0.5 or 1h, over a 12h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The split in the image indicates that the samples from DMSO and 3 μM 8a conditions are blotted sepa.
MELK-8a hydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374. [Abstract]
MELK inhibition with 3 μM 8a causes delayed mitotic entry. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO, 1 μM, or 3 μM 8a. Cells are collected every 2h over a 12h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The splits in the image indicate that the samples from DMSO, 1 μM, and 3 μM 8a conditions are immunoblotted separately due to space constraints. Asynchronous HeLaS3 lysate is loaded in the lanes labeled “A” in order
MELK-8a hydrochloride purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374. [Abstract]
Asynchronous MDA-MB-468 cells are treated with DMSO or 0.5, 1, or 3 μM 8a for 1, 6, or 24h. Cells are harvested and immunoblotted with the indicated antibodies.
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Solvent & Solubility
H2O : ≥ 100 mg/mL (213.21 mM)
DMSO : 8.6 mg/mL (18.34 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (106.61 mM); Clear solution; Need ultrasonic
Protocol
MDA-MB-468 and MCF7 cells are seeded in growth medium into 96-well plates at 1000 and 4000 cells/well, respectively. Sixteen hours after plating, MELK-8a are added and incubated for 7 days. For each well, ATPLite reagent is added and incubated. Luminescence is measured on an multilabel plate reader[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: For pharmacokinetic studies, the intravenous and oral dose is prepared in a solution containing 5% ethanol, 100% PG, 5% CremophorEL, and 80% PBS. The subcutaneous dose is formulated in 10% PG and 25% (20%, v/v) Solutol. Plasma samples are collected at specified time points and stored frozen (−20 °C) until MELK-8a analysis. An LC−MS/MS method is used to quantitate MELK-8a drug levels in plasma[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.1321 mL | 10.6605 mL | 21.3211 mL | 53.3026 mL |
| 5 mM | 0.4264 mL | 2.1321 mL | 4.2642 mL | 10.6605 mL | |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1321 mL | 5.3303 mL | |
| 15 mM | 0.1421 mL | 0.7107 mL | 1.4214 mL | 3.5535 mL | |
| H2O | 20 mM | 0.1066 mL | 0.5330 mL | 1.0661 mL | 2.6651 mL |
| 25 mM | 0.0853 mL | 0.4264 mL | 0.8528 mL | 2.1321 mL | |
| 30 mM | 0.0711 mL | 0.3554 mL | 0.7107 mL | 1.7768 mL | |
| 40 mM | 0.0533 mL | 0.2665 mL | 0.5330 mL | 1.3326 mL | |
| 50 mM | 0.0426 mL | 0.2132 mL | 0.4264 mL | 1.0661 mL | |
| 60 mM | 0.0355 mL | 0.1777 mL | 0.3554 mL | 0.8884 mL | |
| 80 mM | 0.0267 mL | 0.1333 mL | 0.2665 mL | 0.6663 mL | |
| 100 mM | 0.0213 mL | 0.1066 mL | 0.2132 mL | 0.5330 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
MELK-8a hydrochloride Related Classifications
HY-100368A Related Classifications
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