Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GK921 is a transglutaminase 2 (TGase) inhibitor.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 84.00 | |
5 mg | In stock | $ 126.00 | |
10 mg | In stock | $ 207.00 | |
25 mg | In stock | $ 331.00 | |
50 mg | In stock | $ 531.00 | |
100 mg | In stock | $ 725.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 137.00 |
Description | GK921 is a transglutaminase 2 (TGase) inhibitor. |
Targets&IC50 | TGase 2:8.93 μM |
In vitro | GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from GI50 of 10-10 to 10-4 M. The average GI50 is 9.05×10-7 M. GK921 rescues p53 levels and consequently induces apoptosis. The cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels increase in a concentration-dependent manner[1]. |
In vivo | A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models which suggests the possibility of a 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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55 mg/mL (159.69 mM)
You can also refer to dose conversion for different animals. More
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GK921 1025015-40-0 Proteases/Proteasome Glutaminase GK 921 GK-921 inhibit Inhibitor inhibitor