CAS No. : 1025015-40-0

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000163
Molecular Formula:C21H20N4O
Molecular Weight:344.41
Target:TGase 2 inhibitor
IC50:0.9 uM (GI50) [1]
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Appearance:Solid powder
Purity: > 98%
Cat No:I000163
Cas No:1025015-40-0

GK921 is a transglutaminase 2 (TGase 2) inhibitor with average GI50 of 0.9 uM in cancer cell lines.
IC50 value: 0.9 uM (GI50) [1]
Target: TGase 2 inhibitor
GK921 inhibited the tgase 2-induced polymerization of I-κBα and p53 in vitro in a dose-dependent manner. Oral administration of GK921 (8 mg/kg) began when tumors reached a volume of 100 mm3 and proceeded for 5 days/week. after 64 days of treatment, tumor volumes were significantly different in GK921-treated mice and vehicle-treated controls.

[1]. Ku BM, et al. Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models. J Cancer Res Clin Oncol. 2014 May;140(5):757-67.

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