常用名:TD-165
产品描述:
TD-165, a PROTAC-based cereblon (CRBN) degrader, consists of a cereblon (CRBN) ligand-binding group, a linker, and a von Hippel-Landau (VHL) binding group[1].
靶点活性 Cereblon:20.4 nM (DC50)
体外活性 Administration of 0.1-10?μM TD-165 for 24 hours resulted in a concentration-dependent decrease in CRBN protein levels in HEK293T cells[1]. Administration of 0-100 nM TD-165 for 24 hours showed a 50% degradation concentration (DC50) of 20.4?nM and a maximum degradation (Dmax) value of 99.6%[1].
分子量 870.07
分子式 C46H59N7O8S
CAS No. 2305936-56-3
存储
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度
DMSO: 40 mg/mL (110.38 mM)
PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来,从而“劫持”细胞的泛素-蛋白酶体系统(UPS)来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标(而不是抑制靶蛋白的酶活性),目前有许多努力将先前无效的抑制剂分子改造为 PROTACs,用作下一代药物。
产地:西安
用途:科研!
厂家:西安齐岳生物科技有限公司
温馨提示:仅用于科研,不能用于人体实验!
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