EHNA HCl
PDE2 inhibitor / EHNA inhibits phosphodiesterase 2 (PDE2) (IC50 = 0.8 – 5.5 µM in a variety of tissues and species) over PDE1, PDE3, or PDE4 (IC50 values > 100 µM).1,2 It also inhibits adenosine deaminase (ADA), IC50 = 1.2 and 1.5 µM in human RBCs and astrocytoma cells, respectively3, which may be responsible for its ability to induce apoptosis in malignant pleural mesothelioma cell lines4. Because it blocks breakdown of adenosine to inosine and hypoxanthine, EHNA prevents formation of free radical substrates, protecting against cardiac reperfusion-mediated injury.5 It inhibits differentiation and maintains expression of pluripotency markers in hESCs, but not through inhibition of PDEs or ADA.6
Biochemicals & reagents
51350-19-7
NSC 263164
1) Podzuweit et al. (1995), Isoenzyme selective inhibition of cGMP-stimulated cyclic nucleotide phosphodiesterases by erythron-9-(2-hydroxy-3-nonyl) adenine; Cell Signal., 7 733 2) Méry et al. (1995), Erythro-9-(2-hydroxy-3-nonyl)adenine inhibits cyclic GMP-stimulated phosphodiesterase in isolated cardiac myocytes; Mol. Pharmacol., 48 121 3) Barankiewicz et al. (1997), Regulation of adenosine concentration and cytoprotective effects of novel reversible adenosine deaminase inhibitors; J. Pharmacol. Exp. Ther., 283 1230 4) Nakajima et al. (2015), Adenosine deaminase inhibitor EHNA exhibits a potent anticancer effect against malignant pleural mesothelioma; Cell Physiol. Biochem., 35 51 5) Abd-Elfattah and Wechsler (1994), Separation between ischemic and reperfusion injury by site specific entrapment of endogenous adenosine and inosine using NBMPR and EHNA; J. Card. Surg., 9 387 6) Burton et al. (2010), Erythro-9-(2-hydroxy-3-nonyl)adenine(EHNA) blocks differentiation and maintains the expression of pluripotency markers in human embryonic stem cells; Biochem. J., 432 575
RT
TARGET: PDE (Phosphodiesterase); DNA; RNA -- PATHWAY: Redox; DNA synthesis; cAMP / cGMP signaling -- RESEARCH AREA: Stem cells; Cell death; Oxidative stress -- DISEASE AREA: Cancer; IschemiaInfectious disease