| Bioactivity | DB008 is potent and selective PARP16 inhibitor with an IC50 value of 0.27 μM, containing an acrylamide electrophilic reagent. DB008 is membrane-permeable and marks PARP16 selectively[1]. |
| Invitro | DB008 (0-1 μM; 0-120 分钟; HEK 293T 细胞) 共价修饰 PARP16 的 Cys169，并在不可逆结合模式下表现出出色的全蛋白质组选择性[1]。DB008 (100 nM; 16小时; HAP1 WT 和 HAP1 PARP16 KO 细胞) 挽救营养饥饿诱导的可溶性 PARP16 损失[1]。 |
| Name | DB008 |
| Formula | C25H21FN4O3 |
| Molar Mass | 444.46 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| Reference | [1]. Bejan DS, et, al. Structure-guided design and characterization of a clickable, covalent PARP16 inhibitor. Chem Sci. 2022 Nov 16;13(46):13898-13906. |