"Keillor TG2 Inhibitors" (acrylamide compounds)

Art. No.

Z017

Synonym

Keillor inhibitor VA4

Molecular Formula

C33H41N5O6S

Molecular Weight

635.77

Purity by HPLC

>95 % (214 nm)

Appearance

Yellow, fluorescent solid

Solubility

100 µM in 20% (v/v) DMSO / aqueous buffers. DMSO stock solutions can be stored at -20°C for at least 6 months. To avoid too many freeze-thaw cycles, we strongly recommend storage of aliquots.

Application

Irreversible transglutaminase inhibitor that shows good selectivity for tissue transglutaminase. KI = 13 µM; kinact/KI = 0.11 µM-1min-1 [1] Shown to lock tissue transglutaminase in an open conformation in living cells [2], and to abolish GTP binding[1]. Halts the proliferation and invasion of cancer stem cells with EC50 = 3.9 µM[1].

Storage

Store at -20°C, desiccate, keep away from light

Reference(s)

[1] A. Akbar et al. J. Med. Chem. 2017, 60, 7910-7927. [2] Kerr, C. et al. Oncogene 2017, 36, 2981-2990.

Note

INTENDED FOR RESEARCH USE ONLY, NOT FOR USE IN HUMAN, THERAPEUTIC OR DIAGNOSTIC APPLICATIONS.

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