NC9 – Transglutaminase 2 Inhibitor small molecule (tool compound)

In cellular tests, NC9 has been shown to be selective for TG2 over other transglutaminases.

Contributors

Inventor Institute
Jeffrey Keillor University of Ottawa
Cat. #: 159669
Tool sub type: Inhibitor
Research Fields: Cancer;Cell signaling and signal transduction
Application: Has been shown to block TG2 transamidation activity inside cancer stem cells (SCC13 cells) resulting in abolished transamidase activity. Inhibitor blocks EMT and kills cancer stem cells. In mesothiolioma cancer stem cells, inhibition of TG2 reduces migration (invasion), and appears to increase markers of apoptosis.
Purpose: Inhibitor
Alternate name: NC9
Product description: Transglutaminases are a family of enzymes that are responsible for mediating the formation of protein crosslinks of several diverse structural proteins (including fibronectin and collagen) through a transamidation reaction between peptide Gln and Lys residues. Tissue transglutaminase (TG2) is a member of this protein family, and is ubiquitously expressed in tissues, primarily found in the cytosol, but is also expressed in the nucleus, membranes, cell surface and extracellularly. TG2 is also…
Additional notes: NC9 also inhibits FXIIIa. Patent: US20190389814, PCT/IB2017/052162
Molecular weight: 697.84
Selectivity: TG2
CAS number: 1352090-52-8
Primary target: Tissue transglutaminase (TG2)
Storage conditions: Dry, dark and at 0 – 4° C for short term (days to weeks) or -20° C for long term (months to years). Aliquot to avoid freeze-thaw cycles. Lasts up to 2 years with proper storage
Shipping conditions: Dry Ice
Solubility: Soluble in 100 ?M in 5% (v/v) DMSO / aqueous buffers
References:

Akbar et al. 2017. J Med Chem. 60(18):7910-7927. PMID: 28858494.

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