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Chemical Structure| 2183470-12-2 Chemical Structure| 2183470-12-2

Structure of GCN2iB
CAS No.: 2183470-12-2

Chemical Structure| 2183470-12-2

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GCN2iB is an ATP-competitive inhibitor of the serine/threonine-protein kinase GCN2, with an IC50 of 2.4 nM.

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Product Details of GCN2iB

CAS No. :2183470-12-2
Formula : C18H12ClF2N5O3S
M.W : 451.83
SMILES Code : FC1=C(C(F)=C(NS(C2=CC(Cl)=CN=C2OC)(=O)=O)C=C1)C#CC3=CN=C(N)N=C3
MDL No. :MFCD32015941

Safety of GCN2iB

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
HEK293-Gcn2 KO 50 nM 6 h To measure the activity of certain mutant Gcn2 proteins and the induction of the ISR via Gcn2iB. PMC10124904
mandarin fish brain cells 1 μM 120 minutes Inhibition of the GCN2 signaling pathway, blocking eIF2α phosphorylation, thereby suppressing npy transcription PMC9223478

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice ob/ob and HFD-fed mice Intraperitoneal injection 3 mg/kg every other day for 6 weeks GCN2iB inhibited hepatic steatosis and oxidative stress. PMC8718669
Mice HFD/STZ-induced type 2 diabetic mouse model Intraperitoneal injection 3 mg/kg Every other day for 6 weeks GCN2iB ameliorated hyperglycemia, insulin resistance, hepatic steatosis, and oxidative stress PMC9404927

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.07mL

2.21mL

1.11mL

22.13mL

4.43mL

2.21mL

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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