GK921 Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
DMSO:31.5(Max Conc. mg/mL);91.46(Max Conc. mM)
Ethanol:30.0(Max Conc. mg/mL);87.1(Max Conc. mM)
Ethanol:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.41(Max Conc. mM)

form 

A solid

color 

Off-white to brown

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

SMILES

N4(CCCC4)CCOc1nc2c(nc1C#Cc3ccccc3)nccc2

Safety Information

WGK Germany 

WGK 3

Storage Class

11 - Combustible Solids

GK921 Usage And Synthesis

Uses

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

Biological Activity

GK921 is an orally active transglutaminase 2 (TG2, TGase 2) inhibitor (IC50 = 7.71 μM) th at effectively inhibits TG2-mediated I-KBα and p53 polymerization. GK921 induces growth arrest/cell death in renal cell carcinoma (RCC) cultures (ave GI50 = 9.05 μM) and abrogates RCC with increase in p53 level in mice in vivo (8 mg/kg 5x per wk; ACHN or CAKI-1 cells).

in vivo

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. DOI:10.1007/s00432-014-1623-5