2. PROTAC
  3. Ligands for Target Protein for PROTAC

Ligands for Target Protein for PROTAC

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 (281):

Cat. No. Product Name Effect Purity
  • HY-13030
    (+)-JQ-1 99.90%
    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))[1]. (+)-JQ-1 also activates autophagy[2].
  • HY-114872
    SLF 99.91%
    SLF is a synthetic ligand for FK506-binding protein (FKBP) with an affinity of 3.1 μM for FKBP51 and an IC50 of 2.6 μM for FKBP12. SLF can be used in the synthesis of PROTAC[1][2][3].
  • HY-13001
    Quizartinib 99.08%
    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[1].
  • HY-129603
    SI-109 99.91%
    SI-109 is a potent STAT3 SH2 domain inhibitor (Ki=9 nM) with antitumor activity. SI-109 effectively inhibits the transcriptional activity of STAT3 (IC50=3 μM). SI-109 and an analog of CRBN ligand lenalidomide have been used to design PROTAC STAT3 degrader SD-36[1].
  • HY-10997
    Ibrutinib
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM[1].
  • HY-173136
    KDM4 ligand-1
    KDM4 ligand-1 is a ligand for target protein (histone lysine demethylase KDM4) for PROTACs. KDM4 ligand-1 can be used in the synthesis of PROTACs (HY-173135)[1].
  • HY-172740
    BCL6 ligand-3
    BCL6 ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). BCL6 ligand-3 can serve as an active control for the target protein ligand of BMS-986458 (HY-172736)[1].
  • HY-13001S
    Quizartinib-d8
    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[1].
  • HY-115729
    PROTAC CDK9 ligand-1 Chemical 99.75%
    PROTAC CDK9 ligand-1 is a CDK9 ligand that can be used in the synthesis of PROTACs.
  • HY-169280
    PXR Ligand 2
    PXR Ligand 2 (Compound 55) is the target protein ligand for PROTAC SMARCA2/4-degrader-34 (HY-169279)[1].
  • HY-130296
    Palbociclib-propargyl
    Palbociclib-propargyl is a ligand for target protein CDK6 for PROTAC, and binds to CRBN ligand via a PEG linker to make a PROTAC CP-10. CP-10 shows a DC50 of 2.1 nM for CDK6[1]. Palbociclib-propargyl is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-168230
    SMARCA2 ligand-9
    SMARCA2 ligand-9 is the ligand of SMARCA2. SMARCA2 ligand-9 can be used to synthesize PROTAC SMARCA2 degrader-27 (HY-168229)[1].
  • HY-134592
    Piperidine-GNE-049-N-Boc 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[1].
  • HY-168676
    STING ligand-2
    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)[1].
  • HY-168191
    TBL1X ligand 1
    TBL1X ligand 1 is a PROTAC target protein ligand and is used to synthesize PROTAC TBL1X degrader-1 (HY-168190)[1].
  • HY-138679
    Aberrant tau ligand 2
    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)[1].
  • HY-168683
    CDK8 ligand 1
    CDK8 ligand 1 is the ligand of CDK8. CDK8 ligand 1 can be used to synthesize LL-K8-22 (HY-149209)[1].
  • 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[1].
  • HY-159164
    PROTAC CRBN ligand-3
    PROTAC CRBN ligand-3 is a target protein ligand of RGB110 (HY-159087).
  • HY-158400
    TEAD ligand 1
    TEAD ligand 1 is the ligand for target protein TEAD. TEAD ligand 1 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342)[1].