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GK921 showed cytotoxicity to RCC (average GI50 in eight RCC cell lines: 0.905 μM). A single treatment with GK921 almost completely reduced tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models. GK921 rescues p53 levels and consequently induces apoptosis; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed.
| Molecular Weight | 344.41 |
| Formula | C21H20N4O |
| CAS Number | 1025015-40-0 |
| Form | Solid |
| Solubility (25°C) | DMSO: ≥ 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Glutaminase Products |
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| Glutaminase C-IN-1
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| 6-Diazo-5-oxo-L-norleucine
6-Diazo-5-oxo-L-norleucine (Diazooxonorleucine, L-6-Diazo-5-oxonorleucine, DON) is an antibiotic isolated from Streptomyces, an antagonist of glutaminase with an IC50 value of about 1 mM for cKGA (renal glutamine). 6-Diazo-5-oxo-L-norleucine has analgesic, antibacterial, antiviral and anti-cancer properties. |
| L-Albizziin
L-albizziin (L-alpha-amino-beta-ureidopropionic acid) is a potent inhibitor of glutamase. L-albizziin interferes with the utilisation of L-glutamine by the Debaryomyces spp. enzyme probably in a competitive and reversible manner since L-albizziin is also a substrate of the enzyme. |
| Cystamine
Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. |
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