2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
CAS NO.：1025015-40-0 Product Name：1-(2-{3-(2-phenylethynyl)pyrido2,3-bpyrazin-2-yloxy}ethyl)pyrrolidine Synonyms：GK921;GK-921;1-(2-{3-(2-phenylethynyl)pyrido2,3-bpyrazin-2-yloxy}ethyl)pyrrolidine EINEC: Molecular Formula：C21H20N4O Molecular Weight：344.41
Target:
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].
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].
Kinase Assay
Cell Assay
Animal Administration
References
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