ZED-1227

Research use only, not for human use.

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.

ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor,with an IC50 of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 can be used for the research of celiac disease (CeD).

ZED-1227 (0.1 μΜ-1 μΜ; 24 hours) has no effect on metabolic activity and proliferation in Huh7 cells and CaCo2 cells,that suggests ZED-1227 has no cytotoxic activity.?ZED-1227 (0.002-0.2 mg/mL; 30 minutes) inhibits TG2 in the small intestinal mucosa in vitro.

ZED-1227 reduces the activity of intestinal TG2 induced by Polyinosinic:Polycytidylic acid (40 mg/kg) to normal control levels and subdues intestinal inflammation in mice.?ZED-1227 (5 mg/kg; i.g.) is able to inhibit TG2 in the small intestinal mucosa.Animal Model:BALB/c miceDosage:5 mg/kg Administration:Oral gavage Result:Inhibited TG2 in vivo in the small intestinal mucosa.

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Others

Other Targets

Glutaminase

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1542132-88-6

528.6

C26H36N6O6

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (236.47 mM; Ultrasonic )

CCC(CC)CNC(=O)Cn1cccc(NC(=O)[C@H](CC\C=C\C(=O)OC)NC(=O)c2cncn2C)c1=O

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(-20℃)

With Ice Pack

≥ 2 years