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GK921

Catalog No. T3968   CAS 1025015-40-0

GK921 is a transglutaminase 2 (TGase) inhibitor.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
GK921 Chemical Structure
GK921, CAS 1025015-40-0
Pack Size Availability Price/USD Quantity
2 mg In stock $ 84.00
5 mg In stock $ 126.00
10 mg In stock $ 207.00
25 mg In stock $ 331.00
50 mg In stock $ 531.00
100 mg In stock $ 725.00
1 mL * 10 mM (in DMSO) In stock $ 137.00
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Purity: 97.44%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GK921 is a transglutaminase 2 (TGase) inhibitor.
Targets&IC50 TGase 2:8.93 μM
In vitro GK921 inhibits the TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from GI50 of 10-10 to 10-4 M. The average GI50 is 9.05×10-7 M. GK921 rescues p53 levels and consequently induces apoptosis. The cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels increase in a concentration-dependent manner[1].
In vivo A single treatment with GK921 almost completely reduces tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models which suggests the possibility of a new therapeutic approach to RCC[1].
Kinase Assay TGase 2 from guinea pig liver is preincubated for 10 min with various concentrations of GK13 or GK921 in 0.1 mL of reaction buffer, with or without 10 mM CaCl2, followed by the addition of 0.4 mL of substrate solution containing 2
Cell Research Cells are transfected with a BAX promoter luciferase reporter construct. After exposure to GK921 (0, 0.5, 1, 2.5, 5 μM), firefly and Renilla luciferase activities are measured using a dual luciferase assay kit and pRL-CMV as an internal control[1].
Molecular Weight 344.41
Formula C21H20N4O
CAS No. 1025015-40-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (159.69 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Glutamine Metabolism Compound Library Anti-Cancer Metabolism Compound Library Anti-COVID-19 Compound Library Bioactive Compound Library Protease Inhibitor Library Bioactive Compounds Library Max Covalent Inhibitor Library NO PAINS Compound Library Inhibitor Library

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Keywords

GK921 1025015-40-0 Proteases/Proteasome Glutaminase GK 921 GK-921 inhibit Inhibitor inhibitor

 

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