Ligands for Target Protein for PROTAC

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.

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

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

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.

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.

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.

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).

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.

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].

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.

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.

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.

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].

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.

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.

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.

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

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

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.

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

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

SMARCA2 4-IN-3 serves as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) and is applicable in synthesis.

Hydroxyl-ML-210 serves as a ligand for target proteins in PROTAC applications (Ligands for Target Protein for PROTACs). It is utilized in synthesis processes.

Smurf1 ligand 1 serves as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) and is utilized in synthesis.

IBT6A-CO-ethyne is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). It is utilized in synthesis processes.

HPK1-IN-51, serving as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is utilized in synthesis processes.

MJBIA9836 is a ligand for PROTAC target proteins, utilized in the synthesis of PROTAC molecules such as MS41.

PIN1 inhibitor3 (Compound A0) is a PIN1 inhibitor with a dissociation constant (KD) of 25 nM and a half-maximal inhibitory concentration (IC50) of 150 nM. It serves as a target protein ligand for PROTAC synthesis and is applicable in cancer research.

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].

Naphthyridin-Me-dimethoxybenzene-COOH serves as a ligand for target proteins in PROTAC applications (Ligands for Target Protein for PROTACs). This compound is also utilized in synthetic processes.

CEP-1347-acid serves as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) and is utilized in synthesis.

HSD17B13 degrader 2, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is designed for synthesis applications.

Demethyl-NSC682769 is a ligand for target protein for PROTACs (Ligands for Target Protein for PROTACs). It can be utilized in synthesis processes.

BCL6ligand-2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). It can be utilized in synthesis.

SMARCA2 4-IN-2, serving as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is utilized in synthesis.

DCAF1 Ligand 1 (compound I-653) serves as the target protein ligand for PROTA CBRD4-DCAF1 degrader-1, exhibiting a DC50 value of 10~100 nM.

PD-L1 ligand 1 is classified as a PROTAC-targeted protein ligand, primarily utilized as a degradation agent for PD-L1.

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.

PROTAC BRD4 Ligand-3 serves as a ligand for target proteins in PROTACs (Ligands for Target Protein for PROTACs). It is utilized in the synthesis process.

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].

HPK1 ligand 1 is a ligand for the target protein of PROTACs (Ligands for Target Protein for PROTACs). It can be used for synthesis.

EP300 CBP ligand 1, classified as a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), serves a primary role in synthesis applications.

Napabucasin analogue, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is utilized in synthesis. This compound serves as an essential component in the targeted degradation of proteins through the PROTAC technology.

SMARCA2 4-ligand-3, a PROTAC target protein ligand (Ligands for Target Protein for PROTACs), is utilized in synthesis.