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hTG2 inhibitor VA4

Names

[ CAS No. ]:
2088001-23-2

[ Name ]:
hTG2 inhibitor VA4

Biological Activity

[Description]:

hTG2 inhibitor VA4(VA4) is a novel potent, irreversible inhibitor of human tissue transglutaminase (hTG2) with Ki of 12.9 uM, allosterically abolishs its GTP binding ability with a high degree of selectivity and efficiency; inhibits both the transamidation and GTP binding activity of hTG2 in a cellular context, inhibits epidermal cancer stem cell invasion with EC50 of 3.9 uM.

[References]

References 1. Akbar A, et al. J Med Chem. 2017 Sep 28;60(18):7910-7927. 2. Feola J, et al. Brain Res. 2017 Aug 1;1668:1-11. View Related Products by Target Other Targets

Chemical & Physical Properties

[ Molecular Formula ]:
C33H41N5O6S

[ Molecular Weight ]:
635.78


Related Compounds