E3 Ligase Ligand
Proteolysis targeting chimeras (PROTACs) are bivalent ligands in which a compound that binds to the protein target of interest is connected to a second molecule that binds an E3 ligase via a linker. Potentially, a mode of action whereby a target protein is degraded has several advantages over a more traditional therapeutic approach based on inhibition. First, a PROTAC compound only needs to bring the E3 protein close to the target of interest. The PROTAC ligand acts like a catalyst, and even sub-stoichiometric amounts of a PROTAC therapeutic can be expected to achieve (near) complete protein degradation. In the absence of small-molecule E3 binders, other peptidic PROTACs were developed that were sufficiently small to be cell permeable. E3 ligase ligands used for PROTACs including: thalidomide derivatives targeting Cereblon. Bestatin and compound 7 are ligands of cIAP, nutlin is a ligand of MDM2.
References
1.Scheepstra M,et al. Comput Struct Biotechnol J. 2019;17:160–176.
References
1.Scheepstra M,et al. Comput Struct Biotechnol J. 2019;17:160–176.
PROTACs
E3 Ligase Ligand
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Golcadomide
产品货号 : M35741
cas no: 2379572-34-4
Golcadomide (CC-99282) 是一种有效的且具有口服活性的 CRBN E3 连接酶调节剂 (CELMoD)。Golcadomide 与 CRBN 共同诱导 Ikaros 和 Aiolos 的有效和靶向降解。Golcadomide 可用于非霍奇金淋巴瘤的研究。 -
Pomalidomide-amino-PEG3-NH2 hydrochloride
产品货号 : M35170
cas no: 2380273-75-4
Pomalidomide-amino-PEG3-NH2 hydrochloride 是一种合成的 E3 连接酶配体-linker 偶联物,包含基于 Pomalidomide 的 cereblon 配体和 1 个 linker,可用于合成 PROTAC。 -
HaloPROTAC3
产品货号 : M34617
cas no: 1799506-07-2
VH285-PEG5-C6-Cl (HaloPROTAC 3) 由 E3 配体与 16 个原子相连的复合分子,连接子的接头为 Halogen 基团。VH285-PEG5-C6-Cl 包含基于 VH285 的 VHL 配体和基于 alkyl/ether linker。VH285-PEG4-C4-Cl 是一种高效的 GFP-HaloTag7 降解剂,DC50 为 19 nM。VH285-PEG4-C4-Cl 在浓度为 625 nM 时诱导 90% GFP-Halotag 降解。VH285-PEG4-C4-Cl 与 VHL 结合,IC50 为 0.54 μM。 -
Pomalidomide-C2-NH2 hydrochloride
产品货号 : M24047
cas no: 2305369-00-8
Pomalidomide-C2-NH2 盐酸盐是一种合成的 E3 连接酶配体-接头缀合物,其中结合了基于 Pomalidomide 的 cereblon 配体和 PROTAC 技术中使用的接头。 -
Homo-PROTAC pVHL30 degrader 1
产品货号 : M24022
cas no: 2244684-49-7
Homo-PROTAC pVHL30 degrader 1 是一种基于 PROTAC 的有效 pVHL30 降解剂。