protac crbn ligand-2

PROTACCRBN ligand-2 (12) is a derivative of Biguanide-PROTAC, demonstrating an EC50 of 0.15 mM in KP4 cells. It exhibits the ability to alter mitochondrial protein levels, specifically affecting complexes I and IV.

Thalidomide-4-OH (E3 ligase Ligand 2) (Cereblon ligand 2) is the Thalidomide-based Cereblon ligand used to recruit of CRBN protein. Thalidomide-4-OH (Cereblon ligand 2) is a linker to form PROTACs

Thalidomide-5-OH (2-(2,6-dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione) is the Thalidomide-based cereblon ligand that used in the recruitment of CRBN protein. It can be connected to the ligand for protein by a linker to form PROTAC.

Desmorpholinyl Navitoclax-NH-Me (Desmorpholinyl ABT-263-NH-Me) is a Bcl-xL inhibitor, which can be employed alongside a CRBN ligand to synthesize XZ739, a PROTAC BCL-XL degrader [1] [2].

K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in synthesizing PROTAC K-Ras Degrader-1, a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione is a CRBN-type E3 ubiquitin ligase ligand, which can be used in the preparation of PROTACs.

3-(4-Bromo-2-chlorophenyl)piperidine-2,6-dione acts as a ligand for CRBN type E3 ubiquitin ligase and is useful in the synthesis of PROTAC.

3-(5-Bromo-2-chlorophenyl)piperidine-2,6-dione is a ligand for CRBN-type E3 ubiquitin ligases and can be used in the synthesis of PROTACs (proteolysis-targeting chimeras).

TYK2ligand 2 is the TYK2 ligand of PROTACTYD-68. TYD-68 is a highly potent and selective CRBN-recruiting TYK2 PROTAC degrader with a DC50 value of 0.42 nM.

PDE4ligand 2 is a CRBN E3 ligase ligand. It is utilized in the synthesis of PROTACs, such as [PDE4degrader-1]. Additionally, PDE4ligand 2 is applicable in the study of autoimmune and anti-inflammatory diseases.

Thalidomide-OCH2-amide-PEG2-C2-Boc is an E3 ligase ligand-linker conjugate (E3 ligase Ligand-linker conjugate) composed of a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. It is used in the synthesis of PROTAC SARS-CoV-2 Degrader-1.

N-Descyclopropanecarbaldehyde Olaparib, an Olaparib analogue, incorporates a DOTA moiety. It acts as a CRBN-based ligand for the formation of novel dual EGFR and PARP PROTAC, DP-C-4[1]. N-Descyclopropanecarbaldehyde Olaparib is suitable for radiolabeling with F-18 or a fluorophore to visualize tumors using positron emission tomography (PET) or optical imaging[2].

LSN3106729 hydrochloride, the metabolite of Abemaciclib , is a CDK inhibitor with antitumor activity. LSN3106729 hydrochloride and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1]. [1]. Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non-Small Cell Lung Cancer: A Phase Ib Study. [2]. Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.

Thalidomide-NH-CH2-COOH ((2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)glycine) is a synthesized E3 ligase ligand-linker conjugate containing a Thalidomide-based cereblon ligand and a linker.

Abemaciclib metabolite M18 (LSN3106729) is a potent cyclin-dependent kinase (CDK) inhibitor with antitumor properties. It has been incorporated alongside a cereblon (CRBN) ligand to develop a proteolysis-targeting chimera (PROTAC) that selectively degrades CDK4/6 [1] [2].

Thalidomide-NH-(CH2)2-NH2 TFA, an alkyl-modified derivative of Thalidomide, functions as a Cereblon ligand to recruit CRBN proteins and serves as a crucial intermediate in the synthesis of CRBN-based PROTAC molecules targeting the SHP2 protein.