Coumarin-SAHA 是一种荧光探针，用于确定 HDAC8 抑制剂复合物的结合亲和力 (kd) 和解离解离率 (koff)。
| Cas No. | 1260635-77-5 |
| 别名 | coumarin-Suberoylanilide Hydroxamic Acid |
| 化学名 | N1-hydroxy-N8-(4-methyl-2-oxo-2H-chromen-7-yl)-octanediamide |
| Canonical SMILES | O=C(CCCCCCC(NO)=O)NC1=CC2=C(C(C)=CC(O2)=O)C=C1 |
| 分子式 | C18H22N2O5 |
| 分子量 | 346.4 |
| 溶解度 | 5mg/mL in DMSO, 5mg/mL in DMF |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. [1] coumarin-Suberoylanilide hydroxamic acid (c-SAHA) is a SAHA derivative where the anilino "cap" group is replaced by 7-amino-4-methylcoumarin to produce a fluorescent probe that competitively binds HDAC. [2] The fluorescence excitation and emission maxima of free c-SAHA is 325 and 400 nm, respectively and is quenched by 50% when bound to HDAC8. [2] This probe can be used to determine binding affinities and dissociation off-rates of HDAC enzyme-inhibitor complexes and is well-suited for high-throughput screening. Reference:
[1]. Marks, P.A., and Breslow, R. Dimethyl sulfoxide to vorinostat: Development of this histone deacetylase inhibitor as an anticancer drug. Nat. Biotechnol. 25(1), 84-90 (2007).
[2]. Singh, R.K., Mandal, T., Balasubramanian, N., et al. Coumarin-suberoylanilide hydroxamic acid as a fluorescent probe for determining binding affinities and off-rates of histone deacetylase inhibitors. Anal. Biochem. 408(2), 309-315 (2011). |
