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MELK-T1 hydrochloride

Chemical Structure : MELK-T1 hydrochloride

CAS No.: 1610536-69-0

MELK-T1 hydrochloride (JNJ-47117096 hydrochloride)

Catalog No.: PC-70139Not For Human Use, Lab Use Only.

MELK-T1 (JNJ-47117096) hydrochloride is a cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM.

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Biological Activity

MELK-T1 (JNJ-47117096) hydrochloride is a cell-permeable, potent and selective inhibitor of MELK kinase domain with IC50 of 37 nM.
MELK-T1 shows >50% inhibition at 1 uM against 6 kianses in a panel of 235 kinases (Flt3 IC50=18 nM);.
MELK-T1 triggers a rapid and proteasome-dependent degradation of the MELK protein, induces the accumulation of stalled replication forks and DSBs in MCF-7 cells.
MELK-T1 induces a strong phosphorylation of p53, a prolonged up-regulation of p21 and a down-regulation of FOXM1 target genes.

Physicochemical Properties

M.Wt 398.891
Formula C21H23ClN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-methoxy-4-(1H-pyrazol-4-yl)-N-(2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yl)benzamide hydrochloride

References

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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