1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease

GCN2iB 

Cat. No.: HY-112654 Purity: 97.26%
Handling Instructions

GCN2iB is an ATP-competitive GCN2 inhibitor, with an IC50 of 2.4 nM.

For research use only. We do not sell to patients.

GCN2iB Chemical Structure

GCN2iB Chemical Structure

CAS No. : 2183470-12-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 Get quote
50 mg USD 1500 Get quote
100 mg USD 2100 Get quote
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GCN2iB is an ATP-competitive GCN2 inhibitor, with an IC50 of 2.4 nM.

IC50 & Target

IC50: 2.4 nM (GCN2)[1].

In Vitro

GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity. In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μmol/L GCN2iB, demonstrating high kinase selectivity. Unlike GCN2iA, GCN2iB does not inhibit GSK3β (0% inhibition)[1].

In Vivo

In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth. Notably, a combination of ASNase and GCN2iB elicit potent antitumor activity (P=0.0002) with synergistic effects. In MV-4-11 and SU.86.86 xenografts, robust antitumor activity of the combination of GCN2iB and ASNase is observed with synergistic effect, respectively. ASNase/GCN2i-treated tumors do not show significant growth even after drug cessation. The combination of ASNase and GCN2iB yield survival advantage compared with the vehicle treated control with synergistic effect[1].

Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (331.98 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2132 mL 11.0661 mL 22.1322 mL
5 mM 0.4426 mL 2.2132 mL 4.4264 mL
10 mM 0.2213 mL 1.1066 mL 2.2132 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.53 mM); Clear solution

References
Animal Administration
[1]

Mice[1]
A suspension of CCRF-CEM, HPB-ALL, MV-4-11, or SU.86.86 cells (1×107 cells/site) is subcutaneously injected into the right flanks of 6-week-old female SCID mice. Tumor volume is calculated as volume =L×l2×1/2, where L represents the longest diameter across the tumor and l represents the corresponding perpendicular distance. Body weight is also measured. To assess the anti-tumor activity, mice with tumor mass ~200 mm3 are sorted into treatment groups (N=5/group). The tumors are monitored and mice are euthanized when an endpoint is reached, or at the end of the study, whichever comes first. From the next day of randomization, GCN2 inhibitors (e.g., GCN2iB, 10 mpk, twice a day) or ASNase is orally or intraperitoneally administered to mice bearing the xenografts for 7 to 10 days, respectively. T/C (%), an index of anti-tumor activity, is calculated by comparing the mean change in tumor volume during the treatment period in the control and treated groups[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

451.83

Formula

C₁₈H₁₂ClF₂N₅O₃S

CAS No.

2183470-12-2

SMILES

O=S(C1=CC(Cl)=CN=C1OC)(NC2=CC=C(F)C(C#CC3=CN=C(N)N=C3)=C2F)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GCN2iB
Cat. No.:
HY-112654
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GCN2iB

Cat. No.: HY-112654