MELK-8a
Based on 3 publication(s) in Google Scholar
MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells.
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- 純度: 98.32%
- CAS 番号: 1922153-17-0
- 分子式: C25H32N6O
- 分子量:432.56
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 MELK-8a
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生物活性
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Cell Line
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Type | Value | Description | References |
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| MCF7 | IC50 |
3.68 μM
Compound: 8a
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Antiproliferative activity against MELK-independent ER-positive human MCF7 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay
Antiproliferative activity against MELK-independent ER-positive human MCF7 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay
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[PMID: 27187609] |
| MDA-MB-231 | CC50 |
2.3 μM
Compound: MELK-8a
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Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 to 96 hrs by CCK-8 method
Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 to 96 hrs by CCK-8 method
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[PMID: 39026635] |
| MDA-MB-468 | IC50 |
0.11 μM
Compound: 8a
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Antiproliferative activity against MELK-dependent human MDA-MB-468 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay
Antiproliferative activity against MELK-dependent human MDA-MB-468 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay
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[PMID: 27187609] |
| Ramos | IC50 |
3.4 μM
Compound: MELK-8a
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Cytotoxicity against human Ramos cells assessed as inhibition of cell growth measured after 72 to 96 hrs by CCK-8 method
Cytotoxicity against human Ramos cells assessed as inhibition of cell growth measured after 72 to 96 hrs by CCK-8 method
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[PMID: 39026635] |
化学情報
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CAS 番号 1922153-17-0
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性状 Solid
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分子量 432.56
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分子式 C25H32N6O
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Color Off-white to light yellow
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SMILES
CN(CC1)CCN1C2=CC=C(N3C=C(C4=CC=NC=C4OCC5CCNCC5)C=N3)C=C2
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別名
NVS-MELK8a
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 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 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 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 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 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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溶剤 & 溶解度
DMSO : 10 mg/mL (23.12 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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取扱説明書 (2659 KB)
参考文献
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. 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 | 1 mM | 2.3118 mL | 11.5591 mL | 23.1182 mL | 57.7955 mL |
| 5 mM | 0.4624 mL | 2.3118 mL | 4.6236 mL | 11.5591 mL | |
| 10 mM | 0.2312 mL | 1.1559 mL | 2.3118 mL | 5.7795 mL | |
| 15 mM | 0.1541 mL | 0.7706 mL | 1.5412 mL | 3.8530 mL | |
| 20 mM | 0.1156 mL | 0.5780 mL | 1.1559 mL | 2.8898 mL |
MELK-8a 関連分類
HY-100368 関連分類
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