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.

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.

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.

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.

BRD9 ligand-7 acts as the target protein ligand for PROTAC (Ligand for Target Protein for PROTAC) and is utilized in the synthesis of BRD9 Degrader-1.

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].

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.

AR ligand-29 serves as the target protein ligand for PROTACVinclozolinM2-2204, utilized in cancer research.

CSI118 TFA (Compound 1) serves as a ligand for the target protein in PROTAC applications. It is utilized in the synthesis of CSI86.

CCW16-C9-BocNH is an essential key component in the synthesis of targeted protein degraders and PROTACs.

'PAG 4'-piperazine-4-methylpiperidine is a specialized cereblon ligand employed in PROTAC research and development. It includes an E3 ligase ligand and a terminal piperidine, allowing for further chemical modifications to produce Protein Degraders with rigid linkers. This compound is part of a suite of functionalized tool molecules used in PROTAC R&D.

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

Pan-KRAS Ligand 1 serves as a ligand for the target protein of PROTAC (Ligand for Target Protein for PROTAC). This compound facilitates the synthesis of PROTAC Pan-KRAS Degrader 4.

BRM BRG1 ligand 2 serves as a target protein ligand for the synthesis of PROTAC BRM BRG1 degrader-2.

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.

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.

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

AK-068 is a STAT6 ligand with a Ki value of 6 nM, exhibiting at least 85-fold higher selectivity in binding to STAT6 over STAT5.

ER ligand-3, serving as the ligand for the target protein in PROTAC (Ligand for Target Protein for PROTAC), is utilized for the synthesis of PROTACER Degrader-12.

PROTAC IRAK4 ligand-5, a ligand for the target protein of PROTAC, is instrumental in the synthesis of KT-413.

PI3Kγ ligand 1 serves as a PROTAC target protein ligand (Ligand for Target Protein for PROTAC).

STING ligand-2 serves as a ligand for STING and can be utilized as the target protein ligand in the synthesis of the PROTAC degrader STING-IN-10.

HSP90-IN-35 is an inhibitor targeting Hsp90, exhibiting anticancer activity. It demonstrates an IC50 ranging from 0.05 to 0.5 μM against Her2. Additionally, HSP90-IN-35 can be utilized in the synthesis of PROTAC.

HDAC3 8 ligand-1 (compound 40) serves as a ligand for the target protein of PROTAC, utilized in the synthesis of YX968.