1. Signaling Pathways
  2. PROTAC
  3. Ligands for Target Protein for PROTAC

Ligands for Target Protein for PROTAC

Target Protein-binding Moiety

The PROTAC molecule consists of a target protein ligand and an E3 ubiquitin ligase ligand, with a linker binds them together. The ligand for target protein will lead to attachment of a PROTAC to the proteins of interest for ubiquitin and subsequent degradation.

Target proteins are usually proteins whose overexpression or accumulation may play important roles in the progress of diseases. Numbers of PROTACs have been developed to degrade kinases (such as MEK, KRAS, CDK and Bcr/Abl), transcription factors (such as p53, STAT, RAR, ER and AR), epigenetic tools (such as HDAC and BET bromodomain) and E3 ligase themselves (such as MDM2).

Ligands for Target Protein for PROTAC Related Products (293):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-130813
    BET-IN-6 2570470-39-0
    BET-IN-6 is a potent and high affnity BRD2/BRD4 inhibitor. BET-IN-6 is the ligand for target protein BRD2/4, and is used for the systhesis of PROTAC BRD2/BRD4 degrader-1 (HY-130612).
    BET-IN-6
  • HY-125908
    A-1210477-piperazinyl 2351218-72-7
    A-1210477-piperazinyl is a compound binds to protein myeloid cell leukemia 1 (MCL1) used for PROTAC technology.
    A-1210477-piperazinyl
  • HY-130988A
    Ipatasertib-NH2 dihydrochloride 1001264-73-8
    Ipatasertib-NH2 dihydrochloride is a ligand for target protein AKT for PROTAC (INY-03-041). INY-03-041 is composed of Ipatasertib-NH2, a ten-hydrocarbon linker, and a CRBN ligand Lenalidomide for E3 ubiquitin ligase.
    Ipatasertib-NH2 dihydrochloride
  • HY-13001S
    Quizartinib-d8 1300734-19-3
    Quizartinib-d8 (AC220-d8) is deuterium labeled Quizartinib. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis.
    Quizartinib-d<sub>8</sub>
  • HY-134592
    Piperidine-GNE-049-N-Boc 1936431-36-5 98.82%
    Piperidine-GNE-049-N-Boc is a ligand for target protein for PROTAC of dCBP-1 (HY-134582). dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
    Piperidine-GNE-049-N-Boc
  • HY-130981
    FN-1501-propionic acid 2408642-48-6
    FN-1501-propionic acid is a CDK2/9 ligand for PROTAC. FN-1501-propionic acid and a CRBN ligand have been used to design PROTAC CDK2/9 degrader (HY-130709).
    FN-1501-propionic acid
  • HY-107447S
    N-Deshydroxyethyl Dasatinib-d8 1189998-96-6
    N-Deshydroxyethyl Dasatinib-d8 is the deuterium labeled N-Deshydroxyethyl Dasatinib. N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825), the Dasatinib-based moiety, binds to IAP ligand via a linker to form SNIPER to degrade ABL[1].
    N-Deshydroxyethyl Dasatinib-d<sub>8</sub>
  • HY-169280
    PXR Ligand 2 3059971-00-2
    PXR Ligand 2 (Compound 55) is the target protein ligand for PROTAC SMARCA2/4-degrader-34 (HY-169279).
    PXR Ligand 2
  • HY-168230
    SMARCA2 ligand-9 1997320-33-8
    SMARCA2 ligand-9 is the ligand of SMARCA2. SMARCA2 ligand-9 can be used to synthesize PROTAC SMARCA2 degrader-27 (HY-168229).
    SMARCA2 ligand-9
  • HY-168676
    STING ligand-2 1307526-16-4
    STING ligand-2 is the ligand for STING, that can be used as target protein ligand in synthesis of PROTAC degrader STING-IN-10 (HY-168554).
    STING ligand-2
  • HY-138679
    Aberrant tau ligand 2 2417159-58-9
    Aberrant tau ligand 2 (Compound 4-12) is the ligand for tau protein and can be used as target protein ligand for synthesis of PROTAC degrader C004019 (HY-138669).
    Aberrant tau ligand 2
  • HY-170856
    RET ligand-4
    RET ligand-4 is the target protein ligand of YW-N-7 (TFA) (HY-170855A). YW-N-7 (TFA) is a PROTAC targeting RET kinase, which can be used for research in the field of cancer.
    RET ligand-4
  • HY-176044
    PCSK9 ligand 2 3039841-82-9
    PCSK9 ligand 2 is a target protein ligand for PROTAC PCSK9 autophagic degrader 2 (HY-176043), which can be used in antiatherosclerosis research.
    PCSK9 ligand 2
  • HY-135832
    Demethyl-RSL3 2375354-13-3
    Demethyl-RSL3 is a ligand for target protein for pROTAC.
    Demethyl-RSL3
  • HY-162841
    HPK1 ligand 1
    HPK1 ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). HPK1 ligand 1 can be used for synthesis PROTAC PD-L1 degrader-2 (HY-162816).
    HPK1 ligand 1
  • HY-151479
    GID4 Ligand 3 340007-39-8
    GID4 Ligand 3 (compound 16) is a binder of GID4 with an Kd value of 110 μM in vitro and an IC50 value of 148.5 μM. GID4 Ligand 3 can be used for the research related to cereblon and Von Hippel-Lindau.
    GID4 Ligand 3
  • HY-176124
    CDK2 ligand-2 3030281-30-9
    CDK2 ligand-2 is a PROTAC target protein ligand (Ligands for Target Protein for PROTAC). CDK2 ligand-2 combined with E3 Ligase Ligand-linker Conjugate 184 (HY-176125) can be used to synthesize PROTAC degrader (CDK2 degrader 2 (HY-163815)).
    CDK2 ligand-2
  • HY-168195
    DYR530 2410298-39-2
    DYR530 is a ligand for target protein (protein kinases DYRK1A) for PROTAC (HY-168194).
    DYR530
  • HY-169439
    Temozolomide-amino hydrochloride 449187-98-8
    Temozolomide-amino hydrochloride (compound 8) is an activity control for the target protein ligand of Naph-Se-TMZ (HY-169433).
    Temozolomide-amino hydrochloride
  • HY-172360
    HDAC6 ligand-3
    HDAC6 ligand-3 is a ligand for HDAC6 that can be used as target protein ligand for synthesis of PROTAC HDAC6 degrader 4 (HY-172359).
    HDAC6 ligand-3