| Name | GK921 |
| Description | GK921 is an inhibitor of transglutaminase 2 (TGase). |
| 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]. |
| 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 |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.81 mM), Sonication is recommended.
DMSO : 55 mg/mL (159.69 mM), Sonication is recommended.
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| Keywords | TGase | Inhibitor | inhibit | Glutaminase | GK-921 | GK921 | GK 921 |
| Inhibitors Related | N-Phenylacrylamide | L-Methionine-DL-sulfoximine | JHU-083 | Decanoic Acid | BJJF078 | IPN60090 | Cystamine | Cystamine dihydrochloride | Telaglenastat | TG2-IN-3h | 6-Diazo-5-oxo-L-nor-Leucine | BPTES |
| Related Compound Libraries | Bioactive Compound Library | Anti-Cancer Metabolism Compound Library | Glutamine Metabolism Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-COVID-19 Compound Library |
United States
