GK921

SKU: orb1223452

Description

GK921 is a transglutaminase 2 (TGase 2) inhibitor. GK921 showed cytotoxicity to RCC (average GI50 in eight RCC cell lines: 0.905 μM). A single treatment with GK921 almost completely reduced tumor growth by stabilizing p53 in the ACHN and CAKI-1 preclinical xenograft tumor models. TGase 2 inhibitor GK921 abrogates RCC growth in xenograft tumor models, suggesting the possibility of a new therapeutic approach to RCC.

Key Properties

• CAS Number: 1025015-40-0
• MW: 344.42
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₀N₄O
• SMILES: C1CCN(C1)CCOc1c(nc2c(n1)cccn2)C#Cc1ccccc1
• Target: TGase
• Solubility: DMSO : ≥ 30 mg/mL 87.11 mM

Bioactivity

• 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.
• 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 9.05x10-7 M. GK921 rescues p53 levels and consequently induces apoptosis; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GK921 | GK-921 | GK 921

Quick Database Links

Gene Symbol

TGase