MELK-8a Chemical Properties

Boiling point:

596.4±50.0 °C(Predicted)

Density 

1.25±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO: 3 mg/mL (5.93 mM);Water: 22 mg/mL (43.52 mM);Ethanol: Insoluble

form 

Solid

pka

10.28±0.10(Predicted)

color 

Off-white to light yellow

MELK-8a Usage And Synthesis

Uses

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].

References

[1] B Barry Touré, et al. Toward the Validation of Maternal Embryonic Leucine Zipper Kinase: Discovery, Optimization of Highly Potent and Selective Inhibitors, and Preliminary Biology Insight. J Med Chem. 2016 May 26;59(10):4711-23. DOI:10.1021/acs.jmedchem.6b00052