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GK921 

Cat. No.: HY-12337 Purity: 98.81%
Data Sheet SDS Handling Instructions

GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.

For research use only. We do not sell to patients.
GK921 Chemical Structure

GK921 Chemical Structure

CAS No. : 1025015-40-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO $385 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.

IC50 & Target

IC50: 7.71 μM (TGase)[1]

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; a concentration-dependent increase in cleaved poly(ADP-ribose) polymerase (c-PARP) and p53 levels is observed[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[1].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.9035 mL 14.5176 mL 29.0352 mL
5 mM 0.5807 mL 2.9035 mL 5.8070 mL
10 mM 0.2904 mL 1.4518 mL 2.9035 mL
Kinase Assay
[1]

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 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mouse: GK921 is dissolved in DMSO. Vehicle alone and GK921 (8 mg/kg) are administered orally once per day, 5 days/week, for 64 days. The size of the primary tumors is measured every 2-3 days using calipers. Tumor volume is calculated[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

344.41

Formula

C₂₁H₂₀N₄O

CAS No.

1025015-40-0

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
GK921
Cat. No.:
HY-12337
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