| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 100 mg/mL (189.18 mM), Sonication is recommended.
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| Keywords | ZED-1227 | ZED1227 | ZED 1227 | TG2 | Glutaminase |
| Inhibitors Related | N-Phenylacrylamide | L-Methionine-DL-sulfoximine | JHU-083 | Decanoic Acid | BJJF078 | Cystamine | GK921 | Cystamine dihydrochloride | Telaglenastat | TG2-IN-3h | 6-Diazo-5-oxo-L-nor-Leucine | BPTES |
| Related Compound Libraries | Bioactive Compound Library | Glutamine Metabolism Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
