2. PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. MELK PDGFR Haspin Kinase
  4. MELK-8a

MELK-8a  (Synonyms: NVS-MELK8a)

Cat. No.: HY-100368 Purity: 98.32%
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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.

For research use only. We do not sell to patients.

MELK-8a Chemical Structure

MELK-8a Chemical Structure

CAS No. : 1922153-17-0

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50 mg USD 469 In-stock
100 mg USD 750 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of MELK-8a:

MELK-8a Related Antibodies

Top Publications Citing Use of Products

    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]

    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]

    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.

    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: 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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    Description

    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[1].

    Cellular Effect
    Cell Line Type Value Description References
    MCF7 IC50
    3.68 μM
    Compound: 8a
    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
    		[PMID: 27187609]
    MDA-MB-468 IC50
    0.11 μM
    Compound: 8a
    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
    		[PMID: 27187609]
    Molecular Weight

    432.56

    Formula

    C25H32N6O
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    CN(CC1)CCN1C2=CC=C(N3C=C(C4=CC=NC=C4OCC5CCNCC5)C=N3)C=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3118 mL 11.5591 mL 23.1182 mL
    5 mM 0.4624 mL 2.3118 mL 4.6236 mL
    View the 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.

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    Purity & Documentation
    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. 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
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    MELK-8a Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    MELK-8a1922153-17-0NVS-MELK8aMELKPDGFRHaspin KinaseMaternal embryonic leucine zipper kinasePlatelet-derived growth factor receptormaternal embryonic leucine zipper kinaseMELK inhibitorcell mitosiscancer cellsInhibitorinhibitorinhibit

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