GK921


CAS No. : 1025015-40-0

GK921,1025015-40-0
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
Product-Name:GK921
InChI:InChI=1S/C21H20N4O/c1-2-7-17(8-3-1)10-11-19-21(26-16-15-25-13-4-5-14-25)24-18-9-6-12-22-20(18)23-19/h1-3,6-9,12H,4-5,13-16H2
InChIKey:MNYJJHBAEYKXEG-UHFFFAOYSA-N
SMILES:C12=NC=CC=C1N=C(OCCN3CCCC3)C(C#CC4=CC=CC=C4)=N2

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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