H125 is a selective eEF2K inhibitor with IC50 value of 60nM in vitro. It blocked the phosphorylation of eEF-2 in intact C6 glioma cells at 1μM post 12h. It decreased the viability of 10 cancer cell lines from rat glioblastoma, human glioblastoma, human ovarian carcinoma, human cervical carcinoma, human prostate carcinoma, human ovarian carcinoma and human breast carcinoma with IC50 values ranging from 0.7 to 4.7μM[3]. On the contrary, some study showed that NH125 was more correlated with induction of eEF2 phosphorylation than inhibition of eEF2K[4].
NH125 细胞实验
Cell Line
Concentration
Treated Time
Description
References
LN-229 cells
0.25 μM
48 hours
Inhibiting EEF2K activity enhances tumor cell sensitivity to ER stress inducers (e.g., curcumin and velcade)
Autophagy. 2013 Feb 1;9(2):208-19.
T98G cells
0.25 μM
48 hours
Inhibiting EEF2K activity enhances tumor cell sensitivity to ER stress inducers (e.g., curcumin and velcade)
Autophagy. 2013 Feb 1;9(2):208-19.
Mycoplasma genitalium
3.13 µM
Evaluate the antibacterial activity of NH125 analogues against Mycoplasma genitalium, showing MIC of 3.13 µM
Antimicrob Agents Chemother. 2019 Feb 26;63(3):e02265-18.
Mycoplasma pneumoniae
3.13 µM
Evaluate the antibacterial activity of NH125 analogues against Mycoplasma pneumoniae, showing MIC of 3.13 µM
Antimicrob Agents Chemother. 2019 Feb 26;63(3):e02265-18.
Ureaplasma urealyticum
12.5 µM
Evaluate the antibacterial activity of NH125 analogues against Ureaplasma urealyticum, showing MIC50 of 12.5 µM
Antimicrob Agents Chemother. 2019 Feb 26;63(3):e02265-18.
Ureaplasma parvum
6.25 µM
Evaluate the antibacterial activity of NH125 analogues against Ureaplasma parvum, showing MIC50 of 6.25 µM
Antimicrob Agents Chemother. 2019 Feb 26;63(3):e02265-18.
Vero cells
10 µM
2 hours
Screening NH125 for antiviral activity against VSV, results showed NH125 significantly inhibited VSV entry.
Viruses. 2018 Jun 5;10(6):306.
HK296 GSC
2.50 μmol/L
24 hours
NH125 significantly reduces GSC viability and induces EIF2α phosphorylation and expression of ATF4, CHOP, and DR5.
Mol Cancer Res. 2019 May;17(5):1102-1114.
NS039 GSC
1.90 μmol/L
24 hours
NH125 significantly reduces GSC viability and induces EIF2α phosphorylation and expression of ATF4, CHOP, and DR5.
Mol Cancer Res. 2019 May;17(5):1102-1114.
T4213 GSC
1.25 μmol/L
24 hours
NH125 significantly reduces GSC viability and induces EIF2α phosphorylation and expression of ATF4, CHOP, and DR5.
Mol Cancer Res. 2019 May;17(5):1102-1114.
U251
2.5 μmol/L
24 hours
NH125 induces DR5 expression by activating the EIF2α-ATF4-CHOP axis.
Mol Cancer Res. 2019 May;17(5):1102-1114.
C666-1 cells
0.25 µM
72 hours
To evaluate the effect of NH125 combined with MK-2206 on the growth and proliferation of C666-1 cells, the results showed that the combination significantly enhanced the growth-inhibitory effect of MK-2206
Drug Des Devel Ther. 2018 Aug 29;12:2655-2663.
CNE-2 cells
0.25 µM
72 hours
To evaluate the effect of NH125 combined with MK-2206 on the growth and proliferation of CNE-2 cells, the results showed that the combination significantly enhanced the growth-inhibitory effect of MK-2206
NH125 significantly reduced TNF-α-induced expression of CCL-2, IL-6, IL-8, and CXCL-10, and decreased inflammation in RA FLSs.
J Inflamm Res. 2022 Mar 10;15:1729-1744.
BHK-21 cells
10 µM
24 hours
Assessing NH125 cytotoxicity, results showed NH125 at 10 µM concentration caused about 50% cell death after 24 hours.
Viruses. 2018 Jun 5;10(6):306.
Mouse cerebellar stellate cells
1 μM
3 hours
Had little effect on the expression of CPEB3-ir
Neuropharmacology. 2016 Feb;101:531-7.
Mouse cerebellar stellate cells
0.5 μM
3 hours
Had little effect on the expression of CPEB3-ir
Neuropharmacology. 2016 Feb;101:531-7.
Mouse cerebellar stellate cells
10 μM
3 hours
Reduced the level of CPEB3-ir to ~50% relative to control values
Neuropharmacology. 2016 Feb;101:531-7.
NH125 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
B16F10 melanoma model
Intraperitoneal injection
500 μg/kg
Once daily for 2 weeks
NH125 alone or in combination with PD-1 mAb inhibited tumor growth and increased CD8+ T cell infiltration and granzyme B secretion
J Immunother Cancer. 2022 Mar;10(3):e004026
Athymic nude mice
NS039 GSC xenograft model
Intratumoral injection
3 mg/kg
Two treatments, 24 hours apart
PEG-PCL-NH125 treatment led to a sustained decrease in tumor volume, with significant reduction in four out of six treated tumors.
Mol Cancer Res. 2019 May;17(5):1102-1114.
BALB/c nude mice
CNE-2 xenograft model
Intraperitoneal injection
500 µg/kg
Once daily for 2 weeks
To evaluate the inhibitory effect of NH125 combined with MK-2206 on tumor growth in the CNE-2 xenograft model, the results showed that the combination significantly enhanced the tumor-inhibitory effect of MK-2206
Drug Des Devel Ther. 2018 Aug 29;12:2655-2663.
DBA/1 mice
Collagen-induced arthritis (CIA) mouse model
Intraperitoneal injection
1 mg/kg/d
Once daily for 14 consecutive days
NH125 treatment attenuated the severity of arthritis in CIA mice, reduced inflammatory cell infiltration, synovial hyperplasia, and bone erosion, and decreased serum levels of TNF-α, IL-6, IL-1β, IL-8, CCL-2, and CXCL-10.
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