GK921

SKU: orb1303498

Description

GK921 is a potent and selective small molecule inhibitor of transglutaminase 2 (TGase 2). It is a valuable research tool for investigating TGase 2's role in fibrotic diseases, cancer, and celiac disease pathogenesis in both cellular and animal models.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 1025015-40-0
• MW: 344.41
• Purity: 99.92% (May vary between batches)
• Formula: C₂₁H₂₀N₄O
• SMILES: C(CN1CCCC1)Oc1nc2cccnc2nc1C#Cc1ccccc1
• Target: Glutaminase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.81 mM);DMSO:55 mg/mL (159.69 mM)

Bioactivity

• Target IC50:
  TGase 2:8.93 μM
• In Vivo:
  A single treatment with GK921 significantly stabilizes p53 and nearly completely reduces tumor growth in the ACHN and CAKI-1 preclinical xenograft tumor models, suggesting a potential new therapeutic approach to RCC.
• In Vitro:
  GK921 inhibits TGase 2-induced polymerization of I-κBα and p53 in a dose-dependent manner. The cytotoxicity of GK921 ranged from a GI50 of 10^-10 to 10^-4 M with an average GI50 of 9.05×10^-7 M. GK921 rescues p53 levels and consequently induces apoptosis, increasing c-PARP and p53 levels in a concentration-dependent manner.'
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TGase, inhibit, Glutaminase, GK921, GK-921, GK 921, Inhibitor

Compound Identifiers

PubChem CID

56682080