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

Ligands for Target Protein for PROTAC

Target Protein-binding Moiety

Ligands for Target Protein for PROTAC

Related Products

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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 (503):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-10181
    Dasatinib 302962-49-8 99.85%
    Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy, and can cross the blood-brain barrier.
    Dasatinib
  • HY-13030
    (+)-JQ-1 1268524-70-4 99.91%
    (+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
    (+)-JQ-1
  • HY-10997
    Ibrutinib 936563-96-1 99.97%
    Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
    Ibrutinib
  • HY-50878
    Crizotinib 877399-52-5 99.97%
    Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
    Crizotinib
  • HY-136057
    iFSP1 150651-39-1 99.96%
    iFSP1 is a potent, selective and glutathione-independent inhibitor of ferroptosis suppressor protein 1 (FSP1) (AIFM2) with an EC50 of 103 nM. iFSP1 selectively induces ferroptosis in GPX4-knockout cells which overexpressed FSP1. iFSP1 is able to sensitize a variety of human cancer cell lines to the ferroptosis inducer, such as (1S,3R)-RSL3 (HY-100218A).
    iFSP1
  • HY-179718
    TT-012-Br
    TT-012-Br (Compound 4) is a ligand for MITF and can be used for the synthesis of PROTACs, such as WZS0347 (HY-179717).
    TT-012-Br
  • HY-179716
    JAK1/2 ligand 1 1026028-96-5 99.91%
    JAK1/2 ligand 1 is the ligand of JAK1/2 and can be used for the synthesis of PROTACs, such as JAK1/2 Ligand-Linker Conjugates 1 (HY-179716).
    JAK1/2 ligand 1
  • HY-170602
    JNK1 ligand-1-NH-Ph-COOH 3047792-63-9 98.08%
    JNK1 ligand-1 (Compound P1) is a selective JNK1 inhibitor. JNK1 ligand-1 can be used as a JNK1 ligand to synthesize a series of PROTAC molecules, such as PROTAC JNK1-targeted-1 (HY-170601). PROTAC JNK1-targeted-1 can be used for the research of pulmonary fibrosis.
    JNK1 ligand-1-NH-Ph-COOH
  • HY-17447A
    Tranylcypromine hydrochloride 1986-47-6 99.91%
    Tranylcypromine hydrochloride (SKF 385 hydrochloride) is an irreversible inhibitor of lysine-specific demethylase 1 (LSD1/BHC110) and monoamine oxidase (MAO). Tranylcypromine hydrochloride inhibits LSD1, MAO A and MAO B with IC50s of 20.7, 2.3 and 0.95 μM, respectively. Tranylcypromine hydrochloride can be used for the research of depression.
    Tranylcypromine hydrochloride
  • HY-78695
    JQ-1 carboxylic acid 202592-23-2 99.69%
    JQ-1 carboxylic acid, a (+)-JQ-1 (HY-13030) derivative, is a potent BET bromodomain inhibitor. JQ-1 carboxylic acid can be used to synthesize PROTAC, which can target the degradation of BRD4.
    JQ-1 carboxylic acid
  • HY-129603
    SI-109 2429877-30-3 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.
    SI-109
  • HY-114872
    SLF 195513-96-3 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.
    SLF
  • HY-138539
    CBP/p300 ligand 2 2484741-78-6 99.39%
    CBP/p300 ligand 2 is a ligand for target protein for PROTAC of dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
    CBP/p300 ligand 2
  • HY-133073
    CCR7 Ligand 1 681514-83-0 99.19%
    CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.
    CCR7 Ligand 1
  • HY-19204
    Zinc phthalocyanine 14320-04-8 98.0%
    Zinc phthalocyanine (ZnPc) is commonly applied in industry (catalysts, photoconductors) and biomedical (photodynamic therapy, PDT). Zinc phthalocyanine can be used to photooxidise cyclohexane and is promising for research of solar-cell applications.
    Zinc phthalocyanine
  • HY-169182
    AK-068 2982851-09-0 99.57%
    AK-068 is a high-affinity and selective STAT6 ligand, with a Ki of 6 nM. AK-068 demonstrates at least >150- and >85-fold binding selectivity over STAT5A (Ki >1 μM) and STAT5B (Ki >500 μM) proteins, respectively. AK-068 is a ligand for target protein for PROTAC, can be used for synthesis of PROTACs.
    AK-068
  • HY-15724
    Vercirnon 698394-73-9 98.01%
    Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 μM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
    Vercirnon
  • HY-107443
    I-BET762 carboxylic acid 1300019-38-8 99.55%
    I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.
    I-BET762 carboxylic acid
  • HY-114420
    AP1867-2-(carboxymethoxy) 2230613-03-1 99.88%
    AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.
    AP1867-2-(carboxymethoxy)
  • HY-75578
    dTAG Targeting Ligand 1 755039-56-6 98.21%
    dTAG Targeting Ligand 1 (SUBSTITUTE SHEET 245) is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). dTAG Targeting Ligand 1 can be used for synthesis PROTACs.
    dTAG Targeting Ligand 1