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Chemical Structure| 2009273-71-4 Chemical Structure| 2009273-71-4

Structure of GNE-6776
CAS No.: 2009273-71-4

Chemical Structure| 2009273-71-4

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GNE-6776 is selective ubiquitin specific protease-7 (USP7) inhibitor with IC50 of 1.34 μM through binding to acidic amino acid residues.

Synonyms: GEN-6776

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Product Details of GNE-6776

CAS No. :2009273-71-4
Formula : C20H20N4O2
M.W : 348.40
SMILES Code : O=C(C1=CC=C(C2=C(CC)C(C3=CC=C(O)C=C3)=C(N)N=C2)C=N1)NC
Synonyms :
GEN-6776
MDL No. :MFCD31657364

Safety of GNE-6776

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
T47D 10 µM 72 hours To evaluate the effect of GNE-6776 on T47D cell viability, showing an IC50 value of 31.8 µM. Cancer Cell Int. 2025 Feb 21;25(1):60
MCF7 10 µM 72 hours To evaluate the effect of GNE-6776 on MCF7 cell viability, showing an IC50 value of 27.2 µM. Cancer Cell Int. 2025 Feb 21;25(1):60
H1299 cells 0, 6.25, 25, 100 µM 24 or 48 hours GNE-6776 inhibited the proliferation, migration, and invasion of H1299 cells in a concentration- and time-dependent manner, induced apoptosis, and arrested cells in the G1 phase. Pharmaceuticals (Basel). 2025 Feb 12;18(2):245
A549 cells 0, 6.25, 25, 100 µM 24 or 48 hours GNE-6776 inhibited the proliferation, migration, and invasion of A549 cells in a concentration- and time-dependent manner, induced apoptosis, and arrested cells in the G1 phase. Pharmaceuticals (Basel). 2025 Feb 12;18(2):245
BL28 cells 15 µM 24 hours and 4 days To evaluate the effect of USP7 inhibition on p53 and its inhibitory genes. Results showed that in EBNA1-harboring cells, MDM2 mRNA expression was significantly upregulated, while p53 mRNA expression was downregulated after 24 hours and upregulated after 4 days, though not significantly. Rep Biochem Mol Biol. 2023 Jan;11(4):672-683
MKN-45 cells 15 µM 24 hours and 4 days To evaluate the effect of USP7 inhibition on the expression of p53 and its inhibitory genes. Results showed that in EBNA1-transfected cells, MDM4, MDM2, and PSMD10 genes were significantly upregulated after 24 hours, while their expression was no longer significantly upregulated after 4 days. Additionally, USP7 inhibition induced apoptosis. Iran Biomed J. 2023 Jan 1;27(1):34-45
Beas2B cells 0, 6.25, 25, and 100 µM GNE-6776 had virtually no effect on Beas2B cells, demonstrating its high safety for in vitro applications. Pharmaceuticals (Basel). 2025 Feb 12;18(2):245

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice A549 xenograft model Intraperitoneal injection 15 mg/kg and 30 mg/kg Administered every other day for 7 days GNE-6776 significantly inhibited tumor growth without affecting body weight, reduced the expression of CDK6, C-myc, and N-cadherin, and increased GSK3β expression in tumor tissue. Pharmaceuticals (Basel). 2025 Feb 12;18(2):245

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.87mL

0.57mL

0.29mL

14.35mL

2.87mL

1.44mL

28.70mL

5.74mL

2.87mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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