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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) PMC3552884
T98G cells 0.25 μM 48 hours Inhibiting EEF2K activity enhances tumor cell sensitivity to ER stress inducers (e.g., curcumin and velcade) PMC3552884
Mycoplasma genitalium 3.13 µM Evaluate the antibacterial activity of NH125 analogues against Mycoplasma genitalium, showing MIC of 3.13 µM PMC6395908
Mycoplasma pneumoniae 3.13 µM Evaluate the antibacterial activity of NH125 analogues against Mycoplasma pneumoniae, showing MIC of 3.13 µM PMC6395908
Ureaplasma urealyticum 12.5 µM Evaluate the antibacterial activity of NH125 analogues against Ureaplasma urealyticum, showing MIC50 of 12.5 µM PMC6395908
Ureaplasma parvum 6.25 µM Evaluate the antibacterial activity of NH125 analogues against Ureaplasma parvum, showing MIC50 of 6.25 µM PMC6395908
Vero cells 10 µM 2 hours Screening NH125 for antiviral activity against VSV, results showed NH125 significantly inhibited VSV entry. PMC6024324
HK296 GSC 2.50 μmol/L 24 hours NH125 significantly reduces GSC viability and induces EIF2α phosphorylation and expression of ATF4, CHOP, and DR5. PMC8797269
NS039 GSC 1.90 μmol/L 24 hours NH125 significantly reduces GSC viability and induces EIF2α phosphorylation and expression of ATF4, CHOP, and DR5. PMC8797269
T4213 GSC 1.25 μmol/L 24 hours NH125 significantly reduces GSC viability and induces EIF2α phosphorylation and expression of ATF4, CHOP, and DR5. PMC8797269
U251 2.5 μmol/L 24 hours NH125 induces DR5 expression by activating the EIF2α-ATF4-CHOP axis. PMC8797269
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 PMC6120571
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 PMC6120571
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. PMC8922331
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. PMC8922331
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. PMC6024324
Mouse cerebellar stellate cells 1 μM 3 hours Had little effect on the expression of CPEB3-ir PMC4592363
Mouse cerebellar stellate cells 0.5 μM 3 hours Had little effect on the expression of CPEB3-ir PMC4592363
Mouse cerebellar stellate cells 10 μM 3 hours Reduced the level of CPEB3-ir to ~50% relative to control values PMC4592363

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 PMC8961175
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. PMC8797269
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 PMC6120571
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. PMC8922331

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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