Ligands for Target Protein for PROTAC

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.

(+)-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.

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.

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.

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

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.

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

The main body of PD0325901-O-C2-dioxolane is PD0325901, which is a typical non-ATP-competitive MEK1 2 (mitogen-activated protein kinase) inhibitor occupying a variant-binding pocket near the ATP-binding site, with anticancer effects of decreasing ERK phosphorylation and inhibiting cell proliferation.

UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.

SLF is a synthetic ligand for FKBP12, which increases Ca2+ efflux and protein synthesis to improve skeletal muscle function, and is used in the study of central nervous system diseases and cancer.

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).

Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) is based on Dasatinib which is an ABL inhibitor, binds to the IAP ligand via a linker, and forms SNIPER [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.

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.

Defactinib analogue-1 (Compound 7) serves as a ligand for the target protein FAK, and is utilized in the synthesis of PROTAC FAK degrader 1.

CCW16-C9-BocNH is composed of an RING finger protein 4 (RNF4)-recruiting ligand, includes a linker with both hydrophobic and hydrophilic elements, and features a pendant amine that reacts with a carboxylic acid on the target ligand. It is crucial for synthesizing protein degraders used in targeted protein degradation and PROTAC research.

PIN1ligand-1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). It can be utilized in synthesis processes.

TC13172-NH-COOH, a PROTAC target protein ligand, is utilized in the synthesis of MLKLPROTAC. This compound is also employed in the investigation of necroptotic-associated diseases.

NSC682769, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), serves as a precursor in synthesis.

Cbl-b-IN-21, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), serves as a key component in the synthesis process.

EP300 CBP ligand 2 (compound S19) serves as a specific ligand for the bromodomain of CREB binding protein (CBP) and E1A-associated protein (EP300). It plays a critical role in PROTAC technology by acting as a target protein ligand. By linking to an E3 ubiquitin ligase ligand via the PROTAC Linker, it facilitates the synthesis of PROTAC molecules capable of targeted protein degradation. For instance, when EP300 CBP ligand 2 is connected to the conjugate (E3 ubiquitin enzyme ligand + Linker) Thalidomide-NH-C10-Boc, it results in the formation of the PROTAC molecule dCE-2.

5-Br-4-Cl-Pyrrolo-pyroxypyridine serves as a ligand for target proteins in PROTACs (Ligands for Target Protein for PROTACs). This compound is utilized in the synthesis process.

MTH1 ligand 1 functions as a target protein ligand for MTH1, and is utilized in the synthesis of PROTACaTAG 2139.