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Chemical Structure| 278603-08-0 Chemical Structure| 278603-08-0

Structure of NH125
CAS No.: 278603-08-0

Chemical Structure| 278603-08-0

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NH125 is a selective eEF-2 kinase inhibitor with IC50 of 60 nM, also a potent histidine kinase inhibitor.

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Product Details of NH125

CAS No. :278603-08-0
Formula : C27H45IN2
M.W : 524.56
SMILES Code : CC1=[N+](CC2=CC=CC=C2)C=CN1CCCCCCCCCCCCCCCC.[I-]
MDL No. :MFCD07370143
InChI Key :RVWOHCBHAGBLLT-UHFFFAOYSA-M
Pubchem ID :10436839

Safety of NH125

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • CaMKIII

    eEF-2 kinase, IC50:60 nM

In Vitro:

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 Drug Des Devel Ther. 2018 Aug 29;12:2655-2663.
Rheumatoid arthritis fibroblast-like synoviocytes (RA FLSs) 1.0 μM 24 hours NH125 inhibited TNF-α-induced phosphorylation of IKK and IκBα, reduced nuclear translocation of p65, thereby suppressing NF-κB pathway activation. J Inflamm Res. 2022 Mar 10;15:1729-1744.
Rheumatoid arthritis fibroblast-like synoviocytes (RA FLSs) 0.1, 0.5, 1.0 μM 24 hours 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.

In Vivo:

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. J Inflamm Res. 2022 Mar 10;15:1729-1744.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.53mL

1.91mL

0.95mL

19.06mL

3.81mL

1.91mL

References

 

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