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Ligands for Target Protein for PROTAC

Ligands for Target Protein for PROTAC connect to the E3 ligase ligand via a linker, forming heterodimeric PROTAC molecules. Ligands for Target Protein for PROTAC recognize and bind to the target protein with high affinity and selectivity, determining the specificity and efficiency of degradation at the target site. Small molecules, peptides, and antibody fragments can all serve as Ligands for Target Protein for PROTAC.

Ibrutinib
PCI-32765
T1835936563-96-1
Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
  • $34
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PROTAC BRD4 ligand-1
T125512313230-51-0In house
PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.
  • $125
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(+)-JQ-1
JQ1
T21101268524-70-4
(+)-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.
  • $30
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CPI-0610 carboxylic acid
T108791380089-81-5In house
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.
  • $316
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Quizartinib
AC220
T2066950769-58-1
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.
  • $53
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Navitoclax-piperazine
ABT-263-piperazine
T121862143096-93-7
Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor.
  • $67
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SLF-amido-C2-COOH
PROTAC FKBP12-binding moiety 1
T139141092369-24-8
SLF-amido-C2-COOH (ZZY01-083) is an FKBP ligand with potential antimicrobial activity for the synthesis of PROTAC.
  • $48
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SMARCA-BD ligand 1 for Protac
T138481997319-92-2In house
SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.
  • $61
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TFC-007
TFC007
T24870927878-49-7
TFC-007 is a selective and efficient hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, suppressing inflammatory factors. It can be used to synthesize H-PGDS degrader PROTAC (H-PGDS)-1 and study cedar pollen-induced guinea pig allergic rhinitis.
  • $64
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DUPA
N,N''-Carbonylbis[L-glutamic acid], (2S,2'S)-2,2'-Carbonylbis(Azanediyl)Dipentanedioic Acid
T19301302941-52-2
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.
  • $35
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CDK9-IN-10
T107423542-63-0In house
CDK9-IN-10 is a potent inhibitor of CDK9 and serves as the ligand for the PROTAC CDK9 degrader-2.
  • $30
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Apcin A HCL
T643391683535-53-6
Apcin A HCL is an anaphase-promoting complex (APC) inhibitor. Apcin-A HCL interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A HCL can be used to synthesize the PROTAC CP5V.
  • $89
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PD0325901-O-C2-dioxolane
T402172581116-22-3
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.
  • $99
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UNC6852
T139542688842-08-0
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.
  • $135
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Dasatinib carbaldehyde
PROTAC ABL binding moiety 4, BMS-354825 carbaldehyde
T185952112837-79-1
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].
  • $30
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SLF
T13888195513-96-3
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.
  • $99
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SMARCA-BD ligand 1 for PROTAC dihydrochloride
T138902369053-68-7
SMARCA-BD ligand 1 for PROTAC dihydrochloride binds to the BAF ATPase subunit SMARCA2 and is used for degrading SMARCA2 based on PROTAC.
  • $37
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BI-4464
T54801227948-02-8
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).
  • $31
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TSPO ligand-1
T735994560-08-1
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.
  • $30
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N-piperidine Ibrutinib hydrochloride
T121522231747-18-3
N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor, a BTK ligand, inhibits WT BTK and C481S BTK, which can be used to synthesize a range of PROTAC molecules.N-piperidine Ibrutinib hydrochloride has potential anticancer N-piperidine Ibrutinib hydrochloride has potential anticancer activity, inhibiting the growth and proliferation of cancer cells.
  • $48
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Androgen receptor antagonist 1
T103201338812-36-4In house
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.
  • $148
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N-piperidine Ibrutinib
T9408330785-90-5
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.
  • $62
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Desmorpholinyl Navitoclax-NH-Me
Desmorpholinyl Navitoclax-NH-Me, Desmorpholinyl ABT-263-NH-Me
T399102365172-82-1
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].
  • $46
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AR antagonist 1
T103591818885-54-9
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.
  • $30
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