NH125 278603-08-0

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Molecular Weight:

524.56 NH125 is a Selective EEF-2 Kinase Inhibitor with IC50 of 60 nM, >125-fold selectivity over PKC, PKA, and CaMKII, and also a potent histidine kinase inhibitor.

Biological Activity

In C6 glioma cells, NH125 decreases the cellular content of
phospho-eEF-2 without affecting total content eEF-2 content, and blocks
Cell Cycle transit at the G1-S boundary. NH125 potently inhibits cell
viability of 10 cancer cells with IC50 ranging from 0.7 to 4.8 μM.


NH125 effectively inhibits histidine protein kinases, including Envz,
PhoQ, BvgS, EvgS, and thus produces potent anti-bacteria activities on
oxacillin-resistant Staphylococcus aureus (ORSA), vancomycin-resistant
Enterococcus faecalis (VRE), penicillin-resistant Streptococcus
pneumoniae (PRS), and other Gram-positive and Gram-negative bacteria.


EEF2K inhibition by NH125 renders tumor cells more sensitive to curcumin and velcade, which possess ER stress-inducing action.


NH125 reduces blood pressure in SHR and ROS production, induction of
inflammatory molecules, and hypertrophy in SHR superior mesenteric
artery.

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Product Categories : Neuronal Signaling > CaMK Inhibitor