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Purity: ≥98%
MELK-8a is a novel, highly potent and selective MELK (Maternal Embryonic Leucine Zipper Kinase) inhibitor.MELK kinase has been suggested to be a key player in the development of tumors. A subset of basal-like breast cancer cell lines with high MELK expression experience growth inhibition as a result of genetic MELK depletion. MELK is involved in the regulation of cell cycle. Short hairpin ribonucleic acid (shRNA)-mediated MELK knockdown in cellular models is recapitulated by MELK inhibitors 8a. It was discovered that a novel hydrophobic collapse caused by fluorine locked the ligand in its bioactive conformation and produced a 20-fold increase in potency. These brand-new pharmacological inhibitors had a good safety profile and high levels of in vivo exposure, which may open the door for more in vivo testing.
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| Enzyme Assay |
MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM.
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| Cell Assay |
MELK is involved in the regulation of cell cycle and its genetic depletion leads to growth inhibition in a subset of high MELK-expressing basal-like breast cancer cell lines. 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.
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| References |
| Molecular Formula |
C25H32N6O
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| Molecular Weight |
432.56
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| CAS # |
1922153-17-0
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| Related CAS # |
MELK-8a hydrochloride;2096992-20-8
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| SMILES |
CN1CCN(CC1)C2=CC=C(C=C2)N3C=C(C=N3)C4=C(C=NC=C4)OCC5CCNCC5
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| InChi Key |
BLFBSGVUERKSST-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H32N6O/c1-29-12-14-30(15-13-29)22-2-4-23(5-3-22)31-18-21(16-28-31)24-8-11-27-17-25(24)32-19-20-6-9-26-10-7-20/h2-5,8,11,16-18,20,26H,6-7,9-10,12-15,19H2,1H3
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| Chemical Name |
1-methyl-4-[4-[4-[3-(piperidin-4-ylmethoxy)pyridin-4-yl]pyrazol-1-yl]phenyl]piperazine
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2312 mL | 1.1559 mL | 2.3118 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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