Tetrahydrouridine (THU) (Synonyms: NSC 112907, THU) |
Catalog No.GC34089 |
A cytidine deaminase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 18771-50-1
Sample solution is provided at 25 µL, 10mM.
Tetrahydrouridine is a competitive, reversible inhibitor of cytidine deaminase (Ki values = 54 and 240 nM for human and E. coli enzymes, respectively).[1],[2] Its use, alone or in combination with the DNA methyltransferase inhibitor 5-fluoro-2’-deoxycytidine, is being evaluated in animal models and clinical trials for diseases, including cancer and mitochondrial DNA depletion syndrome.[3],[4],[5]
Reference:
[1]. Chabner, B.A., Johns, D.G., Coleman, C.N., et al. Purification and properties of cytidine deaminase from normal and leukemic granulocytes. J.Clin.Invest. 53(3), 922-931 (1974).
[2]. Cohen, R.M., and Woldender, R. Cytidine deaminase from Escherichia coli. Purification, properties and inhibition by the potential transition state analog 3,4,5,6-tetrahydrouridine. J.Biol.Chem. 246(24), 7561-7656 (1971).
[3]. Cámara, Y., González-Vioque, E., Scarpelli, M., et al. Administration of deoxyribonucleosides or inhibition of their catabolism as a pharmacological approach for mitochondrial DNA depletion syndrome. Hum.Mol.Genet. 23(9), 2459-2467 (2014).
[4]. Newman, E.M., Morgan, R.J., Kummar, S., et al. A phase I, pharmacokinetic, and pharmacodynamic evaluation of the DNA methyltransferase inhibitor 5-fluoro-2'-deoxycytidine, administered with tetrahydrouridine. Cancer Chemother. Pharmacol. 75(3), 537-546 (2015).
[5]. Yang, X., Lay, F., Han, H., et al. Targeting DNA methylation for epigenetic therapy. Trends in Pharamacological Sciences 31(11), 536-546 (2010).
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