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dBET1是一种 PROTAC,由 BRD4 配体 JQ-1 和 cereblon E3 连接酶配体组成,靶向 BET 溴结构域 BRD4。
dBET6是一种高效、选择性和细胞可渗透的PROTAC,靶向Cereblon和BET,IC50为14 nM,表现出抗肿瘤活性。
dBET57是一种BRD4异双功能小分子配体(PROTAC),能显著且选择性降解BRD4 BD1(DC50/5小时=500 nM),但对BRD4 BD2无活性。
A1874是一种基于nutlin靶向 BRD4 的PROTAC,DC50 值为 32 nM,诱导细胞中的 BRD4 降解,抑制癌细胞的增殖。
ARV-771是一种高效、选择性、口服生物利用度良好的雄激素受体(AR)降解PROTAC。它通过与雄激素受体结合,促进其降解,抑制与AR相关的肿瘤生长。ARV-771在治疗包括转移性去势抵抗前列腺癌在内的多种前列腺癌中展示了显著的研究潜力。
SJ995973是一种有效的 BET 蛋白降解剂,利用 PROTAC 技术特异性靶向 BET 蛋白,在癌症和炎症性疾病的研究中显示出潜力。
PROTAC BET degrader-9 is PROTAC targeting on BET proteins, consist of a BET inhibitor HJB97 as the warhead ligand and Pomalidomide as CRBN ligand.
PROTAC BET Degrader 23 is a highly potent and efficacious PROTAC targeting on BET with DC50 value of 30pM for degradation of BRD4 in RS4;11 leukemia cell line.
PROTAC BRD9 Degrader-1 is a PROTAC targeting on BRD9, consist of a BRD9 bromodomain probe I-BRD9 as a warhead ligand and pomalidomide as the CRBN ligand.
BETd-246 is a second-generation BET bromodomain inhibitor. It causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation.
QCA570 is a potent PROTAC targeting on BET, consist of an optimized BET ligand QCA276 linked to a CRBN E3 ligand.
PROTAC BET degrader-25 is PROTAC targeting on BET proteins, consist of a BET inhibitor HJB97 as the warhead ligand and a Lenalidomide analogue as the CRBN ligand.
Tags: Bromodomain BET/PROTAC | PROTAC功能分子 | PROTAC Molecule | Bromodomain BET/PROTAC 相关产品
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