An irreversible inhibitor of TG2
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TG2-IN-1 (chloride)

Item No. 42340

Technical Information
Formal Name
1,3-dimethyl-2-[(2-oxopropyl)thio]-1H-imidazolium, monochloride
CAS Number
135273-74-4
Synonyms
  • D003
  • NTU283
  • R283
  • TG2 Inhibitor 1
  • Transglutaminase 2-IN-21
  • Transglutaminase 2 Inhibitor 1
Molecular Formula
C8H13N2OS • Cl
Formula Weight
Purity
≥98%
A solid
PBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
O=C(CSC1=[N+](C)C=CN1C)C.[Cl-]
InChi Code
InChI=1S/C8H13N2OS.ClH/c1-7(11)6-12-8-9(2)4-5-10(8)3;/h4-5H,6H2,1-3H3;1H/q+1;/p-1
InChi Key
NFZZAUJDSJWLTQ-UHFFFAOYSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TG2-IN-1 is an irreversible inhibitor of transglutaminase 2 (TG2).1 It inhibits guinea pig liver TG2 (IC50 = 4 µM) and inhibits recombinant human Factor XIIIa in a concentration-dependent manner.1,2 TG2-IN-1 (20-500 µM) reduces γ-glutamyl-ε-lysine isopeptide levels, a marker of TG2 activity, in SH-SY5Y cells but, paradoxically, potentiates amyloid-β-induced increases in γ-glutamyl-ε-lysine isopeptide levels in the same cells. It also promotes amyloid-β-induced apoptosis in SH-SY5Y cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Griffin, M., Mongeot, A., Collighan, R., et alSynthesis of potent water-soluble tissue transglutaminase inhibitors. Bioorg. Med. Chem. Lett. 18(20), 5559-5562 (2008).

    2. Heil, A., Weber, J., Büchold, C., et alDifferences in the inhibition of coagulation factor XIII-A from animal species revealed by Michael Acceptor- and thioimidazol based blockers. Thromb. Res. 131(5), e214-e222 (2013).

    3. Zhang, J., Ding, Y.-R., and Wang, R. Inhibition of tissue transglutaminase promotes Aβ-induced apoptosis in SH-SY5Y cells. Acta Pharmacol. Sin. 37(12), 1534-1542 (2016).