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.

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.

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

Androgen receptor antagonist 1 is an orally available full antagonist of the androgen receptor (AR), with an IC50 value of 59 nM, demonstrating high potency against AR signaling. Androgen receptor antagonist 1 can further be employed in the synthesis of PROTAC AR degraders, which induce targeted protein degradation, achieving 24% and 47% AR protein reduction in LNCaP cells at concentrations of 1 μM and 10 μM, respectively, thereby offering significant utility in prostate cancer research.

CDK9-IN-10 is a potent inhibitor of CDK9 and serves as the ligand for the PROTAC CDK9 degrader-2.

AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.

SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.

(+)-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.

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.

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

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).

N-piperidine Ibrutinib is a potent BTK inhibitor with IC50s of 51.0 for WT BTK and 30.7 nM for C481S BTK respectively. N-piperidine Ibrutinib can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620. SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM.

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.

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.

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].

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.

BTK ligand 12 is a PROTAC target protein ligand serving as an active control for NRX-0492 (a BTK degradator).

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

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.

BCL6ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). It serves as an active control for the target protein ligand BMS-986458.