Boc-Lys(Tfa)-AMC is the conjugated fluorophore acetylated lysine substrate for assaying histone deacetylase (HDAC) isoform activities [1]. After being hydrolyzed, Boc-Lys(Tfa)-AMC will release the fluorogenic 4-methylcoumarin-7-amide (AMC), and the amount of the generated AMC can be measured at the excitation wavelength of 355nm and the emission wavelength of 460nm[2]. Boc-Lys(Tfa)-AMC is widely used as a model substrate to characterize the enzymatic activity of class IIa HDAC and to screen for HDAC5 inhibitors[3].
References:
[1] Luckhurst C A, Breccia P, Stott A J, et al. Potent, selective, and CNS-penetrant tetrasubstituted cyclopropane class IIa histone deacetylase (HDAC) inhibitors[J]. ACS Medicinal Chemistry Letters, 2016, 7(1): 34-39.
[2] Zaidi S A H, Thakore N, Singh S, et al. Histone deacetylases regulation by δ-opioids in human optic nerve head astrocytes[J]. Investigative ophthalmology & visual science, 2020, 61(11): 17-17.
[3] Mammen C, Hornung F M, Anzenhofer C, et al. In vitro characterization of the catalytic domain of human histone deacetylase 5[J]. Scientific Reports, 2026.
Boc-Lys(Tfa)-AMC是一种偶联了荧光基团的乙酰化赖氨酸底物，用于测定组蛋白去乙酰化酶(HDAC)亚型的活性[1]。水解后，Boc-Lys(Tfa)-AMC会释放出荧光团4-methylcoumarin-7-amide (AMC)，生成的AMC量可在激发波长355nm和发射波长460nm处进行测量[2]。Boc-Lys(Tfa)-AMC被广泛用作模型底物，以表征IIa类HDAC的酶活性并筛选HDAC5抑制剂[3]。