GCN2iB

Name: GCN2iB
Brand: MedChemExpress
SKU: HY-112654
Rating: 5.0 (30 reviews)

Cat. No.: HY-112654 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC₅₀ of 2.4 nM.

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

GCN2iB Chemical Structure

CAS No. : 2183470-12-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 275	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 275	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2100	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of GCN2iB:

GCN2iB acetate Get quote

29 Publications Citing Use of MCE GCN2iB

: GCN2iB purchased from MedChemExpress. Usage Cited in: FASEB J. 2023 Mar;37(3):e22820. [Abstract]; GCN2iB (1 μM; 12 h) significantly inhibits Cholic acid (CA)-induced phosphorylation of GCN2 and eIF2α in HTR8/SVneo cells.

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Biological Activity
Protocol
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References
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Description

GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC₅₀ of 2.4 nM.

IC₅₀ & Target

eIF2

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 μM GCN2iB, demonstrating high kinase selectivity^[1].

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

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/GCN2iB-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].

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

Molecular Weight

451.83

Formula

C₁₈H₁₂ClF₂N₅O₃S

CAS No.

2183470-12-2

Appearance

Solid

Color

Off-white to light yellow

SMILES

O=S(C1=CC(Cl)=CN=C1OC)(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	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (110.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.67 mg/mL (3.70 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (248 KB) HNMR (132 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Nakamura A, et al. Inhibition of GCN2 sensitizes ASNS-low cancer cells by disrupting the amino acid response. Proc Natl Acad Sci U S A. 2018 Aug 14;115(33):E7776-E7785. [Content Brief]

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

[1]. Nakamura A, et al. Inhibition of GCN2 sensitizes ASNS-low cancer cells by disrupting the amino acid response. Proc Natl Acad Sci U S A. 2018 Aug 14;115(33):E7776-E7785. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2132 mL	11.0661 mL	22.1322 mL	55.3305 mL
	5 mM	0.4426 mL	2.2132 mL	4.4264 mL	11.0661 mL
	10 mM	0.2213 mL	1.1066 mL	2.2132 mL	5.5331 mL
	15 mM	0.1475 mL	0.7377 mL	1.4755 mL	3.6887 mL
	20 mM	0.1107 mL	0.5533 mL	1.1066 mL	2.7665 mL
	25 mM	0.0885 mL	0.4426 mL	0.8853 mL	2.2132 mL
	30 mM	0.0738 mL	0.3689 mL	0.7377 mL	1.8444 mL
	40 mM	0.0553 mL	0.2767 mL	0.5533 mL	1.3833 mL
	50 mM	0.0443 mL	0.2213 mL	0.4426 mL	1.1066 mL
	60 mM	0.0369 mL	0.1844 mL	0.3689 mL	0.9222 mL
	80 mM	0.0277 mL	0.1383 mL	0.2767 mL	0.6916 mL
	100 mM	0.0221 mL	0.1107 mL	0.2213 mL	0.5533 mL

GCN2iB Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GCN2iB2183470-12-2Eukaryotic Initiation Factor (eIF)AutophagyInhibitorinhibitorinhibit

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GCN2iB

Customer Review

Other Forms of GCN2iB:

GCN2iB Related Antibodies

29 Publications Citing Use of MCE GCN2iB

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Biological Activity

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GCN2iB Related Antibodies

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Complete Stock Solution Preparation Table

GCN2iB Related Classifications

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