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GK921

Name: GK921
Brand: TargetMol
SKU: T3968
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3968Cas No. 1025015-40-0

GK921 is an inhibitor of transglutaminase 2 (TGase).

GK921

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Purity: 99.92%

Catalog No. T3968Cas No. 1025015-40-0

GK921 is an inhibitor of transglutaminase 2 (TGase).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
2 mg	$48	In Stock	In Stock
5 mg	$77	In Stock	In Stock
10 mg	$127	In Stock	In Stock
25 mg	$255	In Stock	In Stock
50 mg	$397	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$84	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.92%

Appearance:Solid

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	GK921 is an inhibitor of transglutaminase 2 (TGase).
Targets&IC50	TGase 2:8.93 μM
In vitro	GK921 inhibits TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from a GI50 of 10^-10 to 10^-4 M with an average GI50 of 9.05×10^-7 M. GK921 rescues p53 levels and consequently induces apoptosis, increasing c-PARP and p53 levels in a concentration-dependent manner[1].'
In vivo	A single treatment with GK921 significantly stabilizes p53 and nearly completely reduces tumor growth in the ACHN and CAKI-1 preclinical xenograft tumor models, suggesting a potential new therapeutic approach to RCC[1].
Kinase Assay	TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2
Cell Research	Cells are transfected with a BAX promoter luciferase reporter construct. After exposure to GK921 (0, 0.5, 1, 2.5, 5 μM), firefly and Renilla luciferase activities are measured using a dual luciferase assay kit and pRL-CMV as an internal control[1].

Chemical Properties

Molecular Weight	344.41
Formula	C₂₁H₂₀N₄O
Cas No.	1025015-40-0
Smiles	C(CN1CCCC1)Oc1nc2cccnc2nc1C#Cc1ccccc1
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 55 mg/mL (159.69 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.81 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9035 mL	14.5176 mL	29.0352 mL	145.1758 mL
5 mM	0.5807 mL	2.9035 mL	5.8070 mL	29.0352 mL
10 mM	0.2904 mL	1.4518 mL	2.9035 mL	14.5176 mL
20 mM	0.1452 mL	0.7259 mL	1.4518 mL	7.2588 mL
50 mM	0.0581 mL	0.2904 mL	0.5807 mL	2.9035 mL
100 mM	0.0290 mL	0.1452 mL	0.2904 mL	1.4518 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc