2123480-72-6
中文名称
UbcH5c-IN-6d
英文名称
UbcH5c-IN-6d
CAS
2123480-72-6
分子式
C22H21BrO3
分子量
413.3
MOL 文件
2123480-72-6.mol

基本信息
中文别名
化合物 T13242 英文别名
UbcH5c-IN-1UbcH5c-IN-6d
UbcH5c IN 1,UbcH5cIN1,UbcH-5c-IN-1
Naphtho[1,2-b]furan-2(3H)-one, 8-[(2-bromophenyl)methoxy]-3a,4,5,9b-tetrahydro-6,9-dimethyl-3-methylene-, (3aS,9bR)-
物理化学性质
沸点559.8±50.0 °C(Predicted)
密度1.41±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
形态Solid
颜色White to off-white
常见问题列表
生物活性
UbcH5c-IN-1 (compound 6d) 是一种有效的、选择性的小分子泛素结合酶 UbcH5c 抑制剂,其与 E2 UbcH5c-IN-1 活性位点Cys85共价结合的 Kd 值为 283 nM,是开发新型类风湿性关节炎药物的先导化合物。靶点
Kd: 283 nM (E2 UbcH5c).
体内研究
UbcH5c-IN-1 (compound 6d) (5 and 20 mg/kg, p.o., daily, 10-20 days) treatment in Freund’s adjuvant (CFA)-induced adjuvant arthritis (AA) rat model results in appreciable decreases in the arthritis index score and hind paw swelling rate compared with those of the vehicle-treated AA model control group.
Animal Model: | Freund’s adjuvant (CFA)-induced adjuvant arthritis (AA) rat model. |
Dosage: | 5 and 20 mg/kg |
Administration: | Oral administration daily between day 10-20 postimmunization. |
Result: | Resulted in appreciable decreases in the arthritis index score and hind paw swelling rate compared with those of the vehicle-treated AA model control group. |