GCN2-IN-7

Name: GCN2-IN-7
Brand: MedChemExpress
SKU: HY-151460
Rating: 4.5 (1 reviews)

Cat. No.: HY-151460 Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC₅₀=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo.

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

GCN2-IN-7 Chemical Structure

CAS No. : 2396465-33-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 1102	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 1102	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1600	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 3350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 5350	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 8450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC₅₀=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo^[1].

IC₅₀ & Target

IC50: 5 nM (GCN2)^[1]

In Vitro

GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	CD8⁺ T cells from WT and GCN2KO cells
Concentration:	600 nM
Incubation Time:	3 days
Result:	Relieved MDSC suppression of proliferation of the co-cultured CD8⁺ T cells with significant relief at 600 nM.

In Vivo

GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose^[1].
GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model^[1].

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

Animal Model:	Balb/c mice injected with RENCA cells^[1]
Dosage:	15 mg/kg
Administration:	Oral gavage; 15 mg/kg; BID; 17 days
Result:	Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues. Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.

Animal Model:	LL2 syngeneic mouse model^[1]
Dosage:	50 mg/kg
Administration:	Oral gavage; 50 mg/kg; BID; 17 days
Result:	Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.

Molecular Weight

527.44

Formula

C₂₂H₂₃BrN₈OS

CAS No.

2396465-33-9

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@]1(C)C[C@H](NC2=NC=C3C(N(C4=CC=C(C5=NN=C(C)S5)C=C4)N=C3Br)=N2)CC1)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (94.80 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	1.8960 mL	9.4798 mL	18.9595 mL
5 mM	0.3792 mL	1.8960 mL	3.7919 mL
10 mM	0.1896 mL	0.9480 mL	1.8960 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.74 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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: 99.85%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (254 KB) HNMR (277 KB) RP-HPLC (260 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Jackson JJ, et al. Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy. J Med Chem. 2022 Sep 20. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8960 mL	9.4798 mL	18.9595 mL	47.3988 mL
	5 mM	0.3792 mL	1.8960 mL	3.7919 mL	9.4798 mL
	10 mM	0.1896 mL	0.9480 mL	1.8960 mL	4.7399 mL
	15 mM	0.1264 mL	0.6320 mL	1.2640 mL	3.1599 mL
	20 mM	0.0948 mL	0.4740 mL	0.9480 mL	2.3699 mL
	25 mM	0.0758 mL	0.3792 mL	0.7584 mL	1.8960 mL
	30 mM	0.0632 mL	0.3160 mL	0.6320 mL	1.5800 mL
	40 mM	0.0474 mL	0.2370 mL	0.4740 mL	1.1850 mL
	50 mM	0.0379 mL	0.1896 mL	0.3792 mL	0.9480 mL
	60 mM	0.0316 mL	0.1580 mL	0.3160 mL	0.7900 mL
	80 mM	0.0237 mL	0.1185 mL	0.2370 mL	0.5925 mL

GCN2-IN-7 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:

GCN2-IN-72396465-33-9Othersoral activityselectivityanti-tumor activityCD8⁺ T cellsInhibitorinhibitorinhibit

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GCN2-IN-7

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GCN2-IN-7 Related Antibodies

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GCN2-IN-7 Related Antibodies

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Complete Stock Solution Preparation Table

GCN2-IN-7 Related Classifications

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