| Identification | Back Directory | [Name]
2-Propenoic acid, 2-cyano-3-[4-(diphenylamino)phenyl]- | [CAS]
30388-31-9 | [Synonyms]
2-Propenoic acid, 2-cyano-3-[4-(diphenylamino)phenyl]- | [Molecular Formula]
C22H16N2O2 | [MOL File]
30388-31-9.mol | [Molecular Weight]
340.37 |
| Hazard Information | Back Directory | [Description]
DN-F01 is a potent cardiac sarcomere inhibitor, DNF01 targeting the cardiac muscle thin filament protein troponin complex. Functional studies show that DN-F01 has a strong inhibitory calcium-dependent effect on cardiac myofibrillar ATPase activity with an IC50 value of 11 ± 4 nmol/L. DN-F01 is shown to bind to a cardiac troponin C?troponin I chimera (cChimera) with a KD of ～50 nM using fluorescence spectroscopy, indicating that troponin is the likely target for DN-F01. NMR titrations of DNF01 to C35S and A-Cys cChimera show covalent and noncovalent binding of DN-F01 bound to the calcium-saturated cChimera. | [Uses]
DN-F01 has a strong inhibitory calcium-dependent effect on cardiac myofibrillar ATPase activity with an IC50 value of 11 ± 4 nmol/L. | [References]
[1] Cai F, et al. A Potent Fluorescent Reversible-Covalent Inhibitor of Cardiac Muscle Contraction. ACS Med Chem Lett. 2021 Aug 23;12(9):1503-1507. DOI:10.1021/acsmedchemlett.1c00366 |
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