Name | ZED-1227 |
Description | ZED-1227 (TAK-227) is an orally active, selective and potent transglutaminase 2 (TG2) inhibitor with anticancer activity that blocks inflammation-induced TG2 expression and activation for the treatment of Celiac Disease. |
In vitro | ZED-1227, at concentrations ranging from 0.1 μM to 1 μM for 24 hours, does not impact metabolic activity and proliferation in Huh7 cells and CaCo2 cells. This lack of effect suggests that ZED-1227 does not exhibit cytotoxic activity[1].
In an in vitro setting, ZED-1227, when applied at concentrations between 0.002 and 0.2 mg/mL for 30 minutes, inhibits transglutaminase 2 (TG2) in the small intestinal mucosa[1]. |
In vivo | In mice, ZED-1227 reduces the activity of intestinal TG2 induced by Polyinosinic:Polycytidylic acid (40 mg/kg) to levels comparable to normal control levels. Additionally, ZED-1227 administration subdues intestinal inflammation in these mice[1].Furthermore, when administered orally (5 mg/kg; i.g.), ZED-1227 is effective in inhibiting TG2 in the small intestinal mucosa[1]. |
Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 100 mg/mL (189.18 mM), Sonication is recommended.
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Keywords | ZED-1227 | ZED1227 | ZED 1227 |
Inhibitors Related | Glutaminase C-IN-2 | Glutaminase C-IN-1 | BJJF078 | L-Albizziin | GK921 | Sirpiglenastat | GLS1 Inhibitor-7 | Glutaminase-IN-3 | 6-Diazo-5-oxo-L-nor-Leucine | Telaglenastat | UPGL00004 | BPTES |
Related Compound Libraries | Bioactive Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max |