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Chemical Structure : MELK-T1 hydrochloride
Catalog No.: PC-70139Not For Human Use, Lab Use Only.
A novel, cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM.
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A novel, cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM; shows >50% inhibition at 1 uM against 6 kianses in a panel of 235 kinases (Flt3 IC50=18 nM); triggers a rapid and proteasome-dependent degradation of the MELK protein, induces the accumulation of stalled replication forks and DSBs in MCF-7 cells; induces a strong phosphorylation of p53, a prolonged up-regulation of p21 and a down-regulation of FOXM1 target genes.
| M.Wt | 398.891 | |
| Formula | C21H23ClN4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Beke L, et al. Biosci Rep. 2015 Oct 2;35(6). pii: e00267.
2. Johnson CN, et al. ACS Med Chem Lett. 2014 May 23;6(1):25-30.
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