1. Cell Cycle/DNA Damage
  2. Eukaryotic Initiation Factor (eIF)
  3. GCN2-IN-6

GCN2-IN-6 

Cat. No.: HY-130240 Purity: 98.47%
Handling Instructions

GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).

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

GCN2-IN-6 Chemical Structure

GCN2-IN-6 Chemical Structure

CAS No. : 2183470-09-7

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
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2800 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells)[1].

IC50 & Target

IC50: 1.8 nM (GCN2, in-house enzymatic) and 9.3 nM (GCN2, cellular assays); 0.26 nM (PERK, in-house enzymatic) and 230 nM (PERK, cellular assays)[1]

In Vitro

To examine the impact of GCN2 inhibition on cancer cell proliferation, acute lymphoblastic leukemia (ALL) CCRFCEM cells are treated with GCN2-IN-6 (Compound 6d) in the presence of asparaginedepleting agent asparaginase. Treatment with GCN2-IN-6 greatly sensitizes CCRF-CEM cells to asparaginase. The moderate antiproliferative effects achieved by combining asparaginase and GCN2-IN-6 treatment are observed in GCN2-wildtype (WT) mouse embryonic fibroblast (MEF) cells but not in GCN2-knockout (KO) MEF. GCN2-IN-6 demonstrates suppression on p-GCN2, p-eIF2α, and ATF4 activated by asparaginase[1].

In Vivo

GCN2-IN-6 (Compound 6d; 0.3-3 mg/kg; oral administration; for 8 hours; mice) treatment at 3 mg/kg suppresses both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase[1].

Animal Model: Mice bearing CCRF-CEM cells xenografts[1]
Dosage: 0.3 mg/kg, 1 mg/kg, and 3 mg/kg
Administration: Oral administration; for 8 hours
Result: Suppressed both self-phosphorylation of GCN2 and the downstream effector ATF4 to the basal level following pretreatment with asparaginase.
Molecular Weight

485.29

Formula

C₁₉H₁₂Cl₂F₂N₄O₃S

CAS No.

2183470-09-7

SMILES

O=S(C1=CC(Cl)=CC(CO)=C1Cl)(NC2=CC=C(F)C(C#CC3=CN=C(N)N=C3)=C2F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (515.16 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0606 mL 10.3031 mL 20.6062 mL
5 mM 0.4121 mL 2.0606 mL 4.1212 mL
10 mM 0.2061 mL 1.0303 mL 2.0606 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (4.29 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

GCN2-IN-6Eukaryotic Initiation Factor (eIF)Inhibitorinhibitorinhibit

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Product name:
GCN2-IN-6
Cat. No.:
HY-130240
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