1. PROTAC
  2. PROTAC

PROTAC

The PROTAC molecule itself contains three distinct portions: a ligand for binding to the target protein, a ligand for binding to an E3 ligase, and a linker joining these two ligands.

PROTACs (proteolysis-targeting chimaeras) are bifunctional molecules that bring a target protein into spatial proximity with an E3 ubiquitin ligase to trigger target ubiquitination and subsequent proteasomal degradation. Effective redirection of ligase poly-ubiquitination activity toward a new substrate protein requires formation of a ligase:PROTAC:target ternary complex, an intermediate species that is crucial to the cellular activity of degrader molecules. A characteristic feature of PROTACs mode of action is their sub-stoichiometric catalytic activity that alleviates the requirement for target engagement and occupancy of traditional inhibitors. New PROTAC molecules designed guided by the crystal structure show exquisite selectivity for inducing cellular depletion of Brd4 over its BET family members Brd2 and Brd3.

PROTAC Related Products (33):

Cat. No. Product Name Effect Purity
  • HY-16954
    ARV-825 99.37%
    ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
  • HY-100972
    ARV-771 99.44%
    ARV-771 is a potent bromodomain and extra-terminal (BET) proteins degrader based on PROTAC technology with Kd values of 4.7, 7.6, 7.6 nM against BRD2, BRD3 and BRD4, respectively.
  • HY-101838
    dBET1 99.24%
    dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
  • HY-112588
    dBET6 Inhibitor 99.40%
    dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.
  • HY-101763A
    Protein degrader 1 hydrochloride 98.63%
    Protein degrader 1 hydrochloride is used in the synthesis of HaloPROTACs.
  • HY-114228
    PROTAC BET degrader-2 98.21%
    PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression.
  • HY-114229
    PROTAC BET degrader-3 98.64%
    PROTAC BET Degrader-3 is a potent BET degrader based on PROTAC.
  • HY-112609
    QCA570
    QCA570 is a potent BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein.
  • HY-107425
    MZ 1 98.51%
    MZ 1 is a BRD4 protein degrader based on PROTAC technology.
  • HY-101519
    BETd-260 99.35%
    BETd-260 is a potent BET degrader based on PROTAC technology, with an IC50 of 30 pM against BRD4 protein in RS4;11 leukemia cell line.
  • HY-112495
    HaloPROTAC 2 98.10%
    HaloPROTAC 2, a chloroalkane-containing PROTAC, induces degradation of HaloTag fusion proteins.
  • HY-103628
    PROTAC CDK9 Degrader-1 99.04%
    PROTAC CDK9 Degrader-1 is a selective CDK9 degrader.
  • HY-107443
    Target Protein-binding moiety 4
    Target Protein-binding moiety 4 is a BRD4(1) inhibitor with an IC50 of 7.9 μM.
  • HY-111519
    dTRIM24 98.20%
    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
  • HY-111433
    BRD4 degrader AT1
    BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
  • HY-107445
    Target Protein-binding moiety 6
    Target Protein-binding moiety 6 is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
  • HY-103633
    PROTAC BET Degrader-1 98.30%
    PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
  • HY-112098
    PROTAC ERα Degrader-1
    PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
  • HY-112376
    MZP-54 98.05%
    MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.
  • HY-114402
    ARD-69
    ARD-69 is a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR).
Isoform Specific Products

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