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GK921
🥰Excellent
Catalog No. T3968Cas No. 1025015-40-0
GK921 is an inhibitor of transglutaminase 2 (TGase).
GK921
🥰Excellent
Purity: 99.49%
Catalog No. T3968Cas No. 1025015-40-0
GK921 is an inhibitor of transglutaminase 2 (TGase).
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $84 | In Stock | |
| 5 mg | $126 | In Stock | |
| 10 mg | $207 | In Stock | |
| 25 mg | $331 | In Stock | |
| 50 mg | $531 | In Stock | |
| 100 mg | $725 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $137 | In Stock |
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Purity:99.49%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| 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 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (159.69 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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