| Bioactivity | EWP 815 is a disulfiram analogue, is a potent inhibitor of Ins(1,4)P2 phosphatase and Ins(1,4,5)P3 5-phosphatase. EWP 815 also inhibits enzyme dopamine β-hydroxylase activity[1][2]. |
| Target | Ins(1,4)P2 phosphatase; Ins(1,4,5)P3 5-phosphatase; dopamine β-hydroxylase |
| Invitro | EWP 815 inhibits thyrotropin-releasing hormone (TRH; 0.03 mM)-stimulated inositol phospholipid breakdown without affecting basal breakdown rates in prelabelled GH3 cells with IC50s of 83 mM (soluble enzymes) and 71 mM (particulate enzymes), respectively[1].EWP 815 (30 μM; 1 h) exerts higher inhibition on Ins(1,4)P2 phosphatase rather than Ins(1,4,5)P3 5-phosphatase with the mean [3H]Ins(1,4)P2/mean [3H]InsP recovery ratio of 2.6[1]. EWP 815 (6, 8 μM; 10 min) inhibits dephosphorylation of [3H]Ins(1,4,5)P3 5-phosphatase in particulate and soluble fractions with IC50s of 6 μM and 8 μM, respectively[1].EWP 815 (3-300 μM; 30 min) suppresses thyrotropin-releasing hormone (TRH)-stimulated (100 nM) inositol phospholipid production by 30% (100 μM) and 1.8% (300 μM), respectively, without affecting Ins(1,4,5)P3 binding[1]. |
| In Vivo | EWP 815 (50 mg/kg; i.p.; 30 min before killed) inhibits the enzyme dopamine β-hydroxylase activity in mice[2]. Animal Model: |
| Name | EWP 815 |
| CAS | 20231-01-0 |
| Formula | C12H22N4S4 |
| Molar Mass | 350.59 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [1]. Fowler CJ, et al. Inhibition of inositol 1,4,5-trisphosphate 5-phosphatase by micromolar concentrations of disulfiram and its analogues. Biochem J. 1993 Feb 1;289 ( Pt 3)(Pt 3):853-9. [2]. Carlsson A, et al. On the beta-hydroxylation of (+-)-alpha-methyldopamine in vivo. Eur J Pharmacol. 1968 Dec;5(1):85-92. |