| Bioactivity | AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020)[1]. | ||||||||||||
| Invitro | AR antagonist 1 (compound 29) hydrochloride 是 ARD-266 靶连接酶的配体。 ARD-266 是一种高效的基于 VHL E3 连接酶的雄激素受体 (AR) PROTAC 降解剂[1]。AR antagonist 1 与其 E3 连接酶复合物具有微摩尔结合亲和力，可成功用于设计高效的 PROTAC 降解剂[1]。PROTAC 包含两个不同的配体，通过一个接头连接； 一种是E3泛素连接酶的配体，另一种是靶蛋白的配体。PROTACs 利用细胞内泛素-蛋白酶体系统选择性降解靶蛋白[1]。 | ||||||||||||
| Name | AR antagonist 1 hydrochloride | ||||||||||||
| CAS | 1818885-55-0 | ||||||||||||
| Formula | C15H20Cl2N2O | ||||||||||||
| Molar Mass | 315.24 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Han X, et al. Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem. 2019 Dec 26;62(24):11218-11231. |
AR antagonist 1 hydrochloride
CAS: 1818885-55-0 F: C15H20Cl2N2O W: 315.24
AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands
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