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GK921 CAS: 1025015-40-0

Category: Inhibitors
Product Name: GK921
Cat No: I000163
CAS No: 1025015-40-0
Molecular Formula: C21H20N4O
Molecular Weight: 344.41
SMILES: C12=NC=CC=C1N=C(OCCN3CCCC3)C(C#CC4=CC=CC=C4)=N2
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
Solubility: DMSO: ≥ 37 mg/mL
Target: TGase 2 inhibitor
IC50: 0.9 uM (GI50) [1]
CAS 1025015-40-0,GK921
  • Description

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.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References


[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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