1. PROTAC
  2. PROTAC

PROTAC

The PROTAC molecule itself contains three distinct portions: a ligand for binding to the target protein, a ligand for binding to an E3 ligase, and a linker joining these two ligands.

PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. Effective redirection of ligase poly-ubiquitination activity toward a new substrate protein requires formation of a ligase:PROTAC:target ternary complex, an intermediate species that is crucial to the cellular activity of degrader molecules. A characteristic feature of PROTACs mode of action is their sub-stoichiometric catalytic activity that alleviates the requirement for target engagement and occupancy of traditional inhibitors. New PROTAC molecules designed guided by the crystal structure show exquisite selectivity for inducing cellular depletion of Brd4 over its BET family members Brd2 and Brd3.

PROTAC 相关产品 (7):

Cat. No. Product Name Effect Purity
  • HY-16954
    ARV-825 99.35%
    ARV-825 是一种 PROTAC 类的 BRD4 抑制剂。ARV-825 对 BRD4 的 BD1 和 BD2 结构域具有高亲和力,Kd 值分别为 90 和 28 nM。
  • HY-100972
    ARV-771 99.44%
    ARV-771 是 PROTAC 类的有效 BET 降解剂。对 BRD2, BRD3 和 BRD4 的 Kd 值分别为 4.7, 7.6 和 7.6 nM。
  • HY-101838
    dBET1 99.24%
    dBET1 是基于 PROTAC 技术的有效的 BRD4 蛋白质降解物,其 EC50 值为 430 nM。
  • HY-101763A
    Protein degrader 1 hydrochloride 98.63%
    Protein degrader 1 hydrochloride可用于HaloPROTACs的合成。
  • HY-107425
    MZ 1 >98.0%
    MZ 1 是基于 PROTAC 技术的 BRD4 蛋白质降解剂。
  • HY-103628
    PROTAC 6
    PROTAC 6 是一种有选择性的 CDK9 降解剂。
  • HY-112098
    PROTAC 15
    PROTAC 15 包含泛素 E3 连接酶结合基团,linker 和靶蛋白结合基团。PROTAC 15 的详细信息请参考专利文献 WO2017201449A1 中的化合物 P1。PROTAC 15 降低雌激素受体-α (ERα) 水平。
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