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GK921

  Cat. No.:  DC9855   Featured
Chemical Structure
1025015-40-0
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More than 5000 active chemicals with high quality for research!
Field of application
GK921 is a transglutaminase 2 (TGase 2) inhibitor with average GI50 of 0.9 uM in cancer cell lines.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1025015-40-0
Chemical 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
SMILES: C12=NC=CC=C1N=C(OCCN3CCCC3)C(C#CC4=CC=CC=C4)=N2
Formula: C21H20N4O
M.Wt: 344.41
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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