ligands for target protein for protac

(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

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].

BI-4464, a highly selective ATP-competitive inhibitor of PTK2 FAK, exhibits an IC50 of 17 nM and serves as a PTK2 ligand for PROTAC (Proteolysis Targeting Chimera).

DUPA (N,N''-Carbonylbis[L-glutamic acid]) is used as the targeting moiety to actively deliver DTX for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.

m-PEG-azide (MW 2000) is a PEG-based linker used in PROTACs to join two essential ligands, facilitating the selective degradation of target proteins through the ubiquitin-proteasome system within cells.

Phthalimide-PEG3-C2-OTs (Compound 5) is a PROTAC linker composed of PEGs, utilized in the synthesis of various PROTACs that connect two distinct ligands through a linker. One ligand targets an E3 ubiquitin ligase, while the other targets the specific protein of interest, enabling selective protein degradation through the ubiquitin-proteasome system [1].

Thalidomide-5-NH-PEG1-NH2 hydrochloride is a Thalidomide-based cereblon ligand designed for CRBN protein recruitment. It facilitates the formation of PROTAC molecules by linking to target protein ligands, such as THAL-SNS-032, via a connector.

Pomalidomide 4'-PEG5-amine, a cereblon ligand designed for PROTAC research and development, features an integrated E3 ligase ligand and a PEG5 linker ending in an amine for easy conjugation to target protein ligands. It is among a series of functionalized tool molecules specifically crafted for PROTAC R&D.

VH 101, acid, a functionalized von-Hippel-Lindau (VHL) protein ligand, facilitates PROTAC research and development. It comprises an E3 ligase ligand and an alkyl linker featuring a terminal amine for easy conjugation to target protein ligands [1].

Diethylene Glycol Monobenzyl Ether is a PEG-based linker for PROTAC synthesis[1], facilitating the connection of target protein ligands and E3 ligase ligands to enable targeted protein degradation.

Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor.

7-Octynoic acid (compound 42) serves as a PROTAC linker for synthesizing various PROTACs, composed of two distinct ligands joined by this linker, where one ligand interacts with an E3 ubiquitin ligase and the other binds to the target protein, leveraging the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

VH 032 amide-alkylC7-acid is a specialized compound designed for PROTAC research and development, serving as a functionalized von-Hippel-Lindau (VHL) protein ligand. It combines an E3 ligase ligand with an alkylC7 linker, ending in a terminal carboxylic acid for efficient conjugation to target protein ligands. This compound is among a series of functionalized tool molecules aimed at facilitating PROTAC R&D efforts.