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.

PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.

CPI-0610 carboxylic acid is an effective and selective small molecule inhibitor of bromine domain and outer end (BET) protein as a ligand of PROTAC target protein. CPI-0610 carboxylic acid may have anticancer and anticancer activities.

TMX-4153 is a bivalent degrader that selectively targets and rapidly degrades endogenous PIP4K2C through recruitment of the von Hippel-Lindau (VHL) E3 ligase complex, demonstrating a K D of 42 nM. It is applicable in the synthesis of PROTAC [1].

AZD9496 deacrylic acid phenol (AZD9496) represents a portion of the ligand that targets the protein for PROTAC ER Degrader-4 [1].

TSPO ligand-1 has affinity for peripheral and central benzodiazepine receptors.TSPO ligand-1 is an AUTAC4-binding protein in the transmembrane domain of the outer mitochondrial membrane, which induces mitochondrial autophagy and promotes intracellular mitochondrial regeneration.TSPO ligand-1 is involved in intracellular cholesterol transport, and can be used as a biomarker for brain injury and neurodegeneration. TSPO ligand-1 is involved in intracellular cholesterol transport and can be used as a biomarker for brain damage and neurodegeneration.

CFT1946 is a Bifunctional Degradation Activating Compound (BiDAC) degrader that contains a ligand targeting the BRAF kinase domain linked to a cereblon ligand. CFT1946 is able to degrade BRAF V600E (class I), G469A (class II), G466V (class III) mutations and p61-BRAFV600E splice variants while maintaining excellent selectivity for the proteome including WT BRAF and CRAF.

PROTAC PTK6 ligand-1 serves as an intermediate in the synthesis of BTK kinase inhibitors [1] and is utilized in the preparation of ARD-61 [2].

Tazemetostat de(methyl morpholine)-COOH (compound 7), a PROTAC ligand for EZH2, enables the synthesis of PROTACs targeting this enzyme and exhibits potent inhibition of cell viability in diffuse large B-cell lymphoma (DLBCL) and other lymphoma subtypes [1].

SMD-3040 TFA is a selective SMARCA2 degrader, consisting of SMARCA2 4 ligands, a linker, and VHL ligands, used in PROTAC drug synthesis. It effectively inhibits tumor growth in xenograft models [1].

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].

PROTAC BRD4 Ligand-2 Hydrochloride serves as a ligand targeting the BRD4 protein, specifically designed for use with PROTAC CFT-2718.

SLF-amido-C2-COOH (ZZY01-083) is an FKBP ligand with potential antimicrobial activity for the synthesis of PROTAC.

TMX-2039 is a pan-CDK inhibitor that targets cell cycle CDKs (CDK1, CDK2, CDK4, CDK5, and CDK6) and transcription CDKs (CDK7 and CDK9), with IC50 values of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5, and 25 nM, respectively. It serves as a ligand for the target protein in PROTAC applications.

SMARCA2 4-ligand-4 is a target protein ligand for PROTACs (Ligands for Target Protein for PROTACs). It is utilized in the synthesis of PROTAC SMARCA2 4 degrader-36.

PTPN2 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC) utilized in the synthesis of PVD-06.

IRAK4 ligand-12 is a target protein ligand for PROTAC (Ligand for Target Protein for PROTAC) and is utilized in the synthesis of KTX-951.

ER ligand-4 (compound 45a) is a PROTAC target protein ligand.

POI ligand 1 serves as a template for the non-selective HDAC inhibitor Vorinostat. It functions as a target protein ligand (PROTAC target protein ligand) in the creation of PROTAC HDAC degraders with anti-tumor properties. Additionally, POI ligand 1 is utilized in the synthesis of FF2049.

RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.

ER ligand-8 is a ligand of the estrogen receptor (Estrogen Receptor ERR) and can be used for the synthesis of the PROTAC molecule ERD-1233.

CypA ligand-2 serves as the target protein ligand for PROTAC RJS308. RJS308 is a PROTAC specifically designed to target CypA, demonstrating antiviral properties.

Aberrant tau degrader 2 (Compound 4-12) acts as a degrader of tau protein and serves as a target protein ligand for the synthesis of PROTAC degrader C004019.