GK921
CAS No. : 1025015-40-0
| Size | Price | Stock |
|---|---|---|
| 5mg | $95 | In-stock |
| 10mg | $155 | In-stock |
| 25mg | $310 | In-stock |
| 50mg | $496 | In-stock |
| 100mg | $700 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-12337 |
| M.Wt: | 344.41 |
| Formula: | C21H20N4O |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 30 mg/mL |
GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2. IC50 & Target: IC50: 7.71 μM (TGase)[1] 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; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed[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[1].
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