1. Signaling Pathways
  2. PROTAC
  3. 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 (50):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-100972
    ARV-771 1949837-12-0 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.
    ARV-771
  • HY-16954
    ARV-825 1818885-28-7 99.37%
    ARV-825 is a BRD4 degrader based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.
    ARV-825
  • HY-101838
    dBET1 1799711-21-9 99.24%
    dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
    dBET1
  • HY-112588
    dBET6 1950634-92-0 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.
    dBET6
  • HY-107425
    MZ 1 1797406-69-9 98.51%
    MZ 1 is a BRD4 protein degrader based on PROTAC technology.
    MZ 1
  • HY-114305
    A1874 2064292-12-0 98.38%
    A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
    A1874
  • HY-111594
    Homo-PROTAC cereblon degrader 1 2244520-98-5 99.00%
    Homo-PROTAC cereblon degrader 1 (compound 15a) is a highly potent and efficient cereblon (CRBN) degrader with only minimal effects on IKZF1 and IKZF3.
    Homo-PROTAC cereblon degrader 1
  • HY-123937
    THAL-SNS-032 2139287-33-3
    THAL-SNS-032 is a selective CDK9 degrader PROTAC consisting of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).
    THAL-SNS-032
  • HY-101519
    BETd-260 2093388-62-4 99.35%
    BETd-260 is a potent BET degrader based on PROTAC technology, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.
    BETd-260
  • HY-112495
    HaloPROTAC 2 1799506-06-1 98.10%
    HaloPROTAC 2, a chloroalkane-containing PROTAC, induces degradation of HaloTag fusion proteins.
    HaloPROTAC 2
  • HY-103628
    PROTAC CDK9 Degrader-1 2118356-96-8 99.04%
    PROTAC CDK9 Degrader-1 is a selective CDK9 degrader.
    PROTAC CDK9 Degrader-1
  • HY-111433
    BRD4 degrader AT1 2098836-45-2 98.76%
    BRD4 degrader AT1 is a highly selective Brd4 degrader based on PROTAC technology, with a Kd of 44 nM for Brd4BD2 in cells.
    BRD4 degrader AT1
  • HY-114228
    PROTAC BET degrader-2 2093388-33-9 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.
    PROTAC BET degrader-2
  • HY-111519
    dTRIM24 2170695-14-2 98.20%
    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
    dTRIM24
  • HY-114229
    PROTAC BET degrader-3 98.64%
    PROTAC BET Degrader-3 is a potent BET degrader based on PROTAC.
    PROTAC BET degrader-3
  • HY-103633
    PROTAC BET Degrader-1 2093386-22-0 98.84%
    PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
    PROTAC BET Degrader-1
  • HY-111846
    PROTAC ERα Degrader-2 1351169-29-3
    PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
    PROTAC ERα Degrader-2
  • HY-111844
    PROTAC RAR Degrader-1 1351169-27-1
    PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
    PROTAC RAR Degrader-1
  • 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.
    PROTAC ERα Degrader-1
  • HY-112376
    MZP-54 2010159-47-2 98.05%
    MZP-54 is a selective degrader of BRD3/4 based on PROTAC technology, with a Kd of 4 nM for Brd4BD2.
    MZP-54
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