GCN2-IN-1

Name: GCN2-IN-1
Brand: MedChemExpress
SKU: HY-100877
Rating: 5.0 (25 reviews)

Cat. No.: HY-100877 Purity: 99.46%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC₅₀ of <0.3 μM in the enzyme assay and an IC₅₀ of 0.3-3 μM in the cell assay.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 1448693-69-3

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
500 mg	해외재고보유	Estimated Time of Arrival: December 31
1 g	해외재고보유	Estimated Time of Arrival: December 31
5 g	견적 받기
10 g	견적 받기

or 대량구매 문의

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 25 publication(s) in Google Scholar

25 Publications Citing Use of MCE GCN2-IN-1

Cell Imaging/Staining

: GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2025 Nov;27(11):1889-1901. [Abstract]; Ubiquitylation of whole-cell proteins and OMM proteins of cells cultured in medium supplemented with 0 mM or 1 mM Leu and/or 0 µM or 10 µM GCN2-IN-1 for 3 h. For each sample, 10 µg proteins were loaded. Ubiquitylation levels were normalized to the total OMM protein amount.

: GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2024 May 22;52(9):5356-5375. [Abstract]; U2OS cells were treated with a PERK inhibitor (GSK II, 40 μM), or with GCN2-IN-1 (4 μM), for 3 h prior to transfection. mRNA (1 μg) encoding GFP (green) was transfected, and cells were fixed 1.5 h post-transfection. Cells were stained using anti-G3BP1 (magenta).

: GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Oct 25;14(1):6777. [Abstract]; MDA-MB 231 cells were cultured for 72 hours in complete medium (CM) and medium containing 25% amino acids (low amino acid). Then, they were treated with (+) or (-) 1 μM GCN2-IN-1 for 72 hours, respectively, and Western blot analysis was performed to detect the expression of the proteins shown.

: GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Sep 8;14(1):5535. [Abstract]; After treating HeLa cells with the GCN2 inhibitor GCN2-IN-1 (A92) at progressively increasing concentrations for 5 hours, the specified proteins in the lysate were analyzed by immunoblotting.

: GCN2-IN-1 purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jul;30(7):1666-1678. [Abstract]; Immunoblotting of phosphorylated eIF2a (ser51) following treatment of A549 with CuET (2 h) +/–PERK inhibitor combined with siRNA against HRI or GCN2-IN-1 (10 μM; 30 min). Numbers below the blot indicate the signal ratio p-eIF2a/β-actin.

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Biological Activity
순도&문서
References
고객리뷰

제품 설명

GCN2-IN-1 is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC₅₀ of <0.3 μM in the enzyme assay and an IC₅₀ of 0.3-3 μM in the cell assay^[1].

IC₅₀ & Target

eIF2

In Vitro

GCN2-IN-1 (Compound A-92) is a GCN2 inhibitor, which may be useful as a chemotherapeutic drug for the treatment of cancer^[1].

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

분자량

402.41

화학식

C₁₉H₁₈N₁₀O

CAS No.

1448693-69-3

Appearance

Solid

Color

Light yellow to yellow

SMILES

C1(NC2=CN(C3CCOCC3)N=C2)=NC=C(N=NN4C5=CC6=C(C=C5)C=NN6)C4=N1

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

In Vitro:

DMSO : 50 mg/mL (124.25 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	2.4850 mL	12.4251 mL	24.8503 mL
5 mM	0.4970 mL	2.4850 mL	4.9701 mL
10 mM	0.2485 mL	1.2425 mL	2.4850 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기
농도 희석 계산기

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: ≥ 2.5 mg/mL (6.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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.

순도&문서

Purity: 99.46%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (250 KB) HNMR (282 KB) RP-HPLC (254 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Dieter Dorsch, et al. Triazolo[4,5-d]pyrimidine derivatives. WO2013110309A1.

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4850 mL	12.4251 mL	24.8503 mL	62.1257 mL
	5 mM	0.4970 mL	2.4850 mL	4.9701 mL	12.4251 mL
	10 mM	0.2485 mL	1.2425 mL	2.4850 mL	6.2126 mL
	15 mM	0.1657 mL	0.8283 mL	1.6567 mL	4.1417 mL
	20 mM	0.1243 mL	0.6213 mL	1.2425 mL	3.1063 mL
	25 mM	0.0994 mL	0.4970 mL	0.9940 mL	2.4850 mL
	30 mM	0.0828 mL	0.4142 mL	0.8283 mL	2.0709 mL
	40 mM	0.0621 mL	0.3106 mL	0.6213 mL	1.5531 mL
	50 mM	0.0497 mL	0.2485 mL	0.4970 mL	1.2425 mL
	60 mM	0.0414 mL	0.2071 mL	0.4142 mL	1.0354 mL
	80 mM	0.0311 mL	0.1553 mL	0.3106 mL	0.7766 mL
	100 mM	0.0249 mL	0.1243 mL	0.2485 mL	0.6213 mL

GCN2-IN-1 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-11448693-69-3Eukaryotic Initiation Factor (eIF)Inhibitorinhibitorinhibit

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GCN2-IN-1

고객리뷰

GCN2-IN-1 Related Antibodies

25 Publications Citing Use of MCE GCN2-IN-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

순도&문서

References

고객리뷰

GCN2-IN-1 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

GCN2-IN-1 Related Classifications

Keywords:

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고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report