NH125

Uses

NH125 is an inhibitor of multiple kinases. It kills methicillin-resistant Staphylococcus.

Biological Activity

Histidine protein kinase and eukaryotic elongation factor 2 (eEF-2) kinase (CaMK III) inhibitor (IC 50 = 60 nM) that displays 125-fold, > 1300-fold and > 1500-fold selectivity over PKC, PKA and CaMK II respectively. Exhibits anticancer activity in a variety of malignant cell lines (IC 50 values are 0.7 - 4.8 μ M) and blocks G 1 /S cell cycle progression. Also is an effective antibacterial agent in vitro (IC 50 = 6.6 μ M) and in vivo .

Biochem/physiol Actions

NH125 exhibits anti-proliferation activity against many cancer cells. It also exhibits antibacterial effects by inhibiting bacterial histidine protein kinase.

IC 50

CaMK III: 60 nM (IC₅₀)

storage

Desiccate at -20°C

References

[1]. arora, s., et al., identification and characterization of an inhibitor of eukaryotic elongation factor 2 kinase against human cancer cell lines. cancer res, 2003. 63(20): p. 6894-9.
[2]. cheng, y., et al., integrated regulation of autophagy and apoptosis by eef2k controls cellular fate and modulates the efficacy of curcumin and velcade against tumor cells. autophagy, 2013. 9(2): p. 208-19.
[3]. usui, t., et al., eukaryotic elongation factor 2 kinase regulates the development of hypertension through oxidative stress-dependent vascular inflammation. am j physiol heart circ physiol, 2013. 305(5): p. h756-68.