protac parp1 degrader

PROTAC PARP1 degrader is a degrader of PARP1 based on the PROTAC technology. PROTAC PARP1 degrader at 10 μM at 24 h inhibits MDA-MB-231 cell line (IC50 of 6.12 μM).

PROTAC PARP1 degrader-3 (Compound C6) 是一种针对PARP1的PROTAC降解剂，其DC50为58.14 nM。在癌细胞系SW-620和LOVO中，该化合物展现出细胞毒性，IC50分别为1.63 μM和2.84 μM。在BRCA突变的结肠癌细胞中，PROTAC PARP1 degrader-3 与SN-38共同使用表现出协同作用，组合指数 (CI) 为0.487。

PROTAC PARP1 degrader-2 (Compound 72) 作为一种PARP的PROTAC降解剂,在MDA-MB-231细胞中表现出极低的DC50值(<10 nM).此外,该化合物在抑制MDA-MB-436细胞活性方面同样表现出色,其IC50值亦<100 nM。

PROTAC PARP1 degrader-4 (Compound 180055) 是一种在 T47D 和 MDA-MB-231 细胞系中具有选择性降解活性的PARP1 PROTAC降解剂，DC50分别为180 nM和240 nM。它能够促进PARP1的泛素化和降解，并抑制PARP1酶活性，同时不引起明显的DNA诱捕效应。此化合物可有效抑制携带BRCA基因突变的肿瘤生长，对正常细胞则影响较小。

NH2-PEG7 is a para-aminomethylbenzyloxycarbonyl (PROTAC) linker compound consisting of a polyethylene glycol (PEG) chain. It finds application in the synthesis of the PROTAC PARP1 degrader called iRucaparib-AP6[1].

iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1. iRucaparib-AP6 is a highly efficient and specific PARP1 degrader based on Rucaparib by using the PROTAC approach.

Thalidomide-piperidine-C-Pip-C2-Pip-C2-OH (Compound C6) 是一种连接子与 E3 连接酶配体的偶联物，可用于合成 PROTAC PARP1 degrader-30。

Thalidomide-NH-PEG7 is a synthesized conjugate of an E3 ligase ligand and linker designed for use in antibody-drug conjugates (ADCs). This compound can be coupled to a protein ligand via a linker to create PROTAC iRucaparib-AP6, an extremely selective degrader of PARP1[1].

Pomalidomide 4'-PEG3-azide 是一个包含 Pomalidomide 的 cereblon 配体和 1 个 linker 的 E3 连接酶配体-linker 偶联物，可用于 iRucaparib-TP3 的合成。

(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthesized E3 ligase ligand-linker conjugate combining the (S,R,S)-AHPC-based VHL ligand with a 4-unit polyethylene glycol (PEG) linker, employed in PROteolysis TAgeting Chimera (PROTAC) technology. This compound facilitates the creation of vRucaparib-TP4, a potent PARP1 degrader demonstrating a half-maximal degrading concentration (DC50) of 82 nM[1].

Pomalidomide 5-piperidylamine 作为连接子与E3连接酶配体的复合物,可应用于合成 PROTAC PARP1 degrader-2.