1. Signaling Pathways
  2. PROTAC
  3. PROTAC

PROTAC

PROTACs (Proteolysis Targeting Chimeric Molecules) are heterobifunctional nanomolecules that structurally comprised of two functional motifs linked by a linker. One motif is a small molecule ligand for the target protein of interest, while the other recognizes a specific E3 ligase. By recruiting an E3 ligase to a target protein and formation of a ligase:PROTAC:target ternary complex, A PROTAC leads to polyubiquitylation and subsequent degradation of target through ubiquitin-proteasome system (UPS). PROTACs have desirable features such as the ability to target the “undruggable” proteome and overcome the accumulation of the drug targets and will be promising targeted therapeutics for cancers.

Among the hundreds of E3 ligases, VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and cIAP (cellular inhibitor of apoptosis 1) are reported to target kinases (such as MEK, KRAS, CDK and Bcr/Abl), transcription factors (such as p53, STAT, RAR, ER and AR), and epigenetic readers (BET bromodomain such as BRD family) and are most widely used in the development of PROTACs. There are also some specific types of PROTACs, such as homo-PROTACs and general PROTACs for tagged fusion proteins. Homo-PROTACs intend to dimerize an E3 ligase and then induce its self-degradation, while general PROTACs for tagged fusion proteins can bind to general tags(such as HaloTag and FKBP12) and then induce the degradation of fusion proteins.

PROTAC Isoform Specific Products:

  • von Hippel-Lindau (VHL)

  • Cereblon

  • MDM2

  • cIAP1

PROTAC Related Products (113):

Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-100972
    ARV-771 1949837-12-0 99.82%
    ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), 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-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-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 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to Thalidomide (HY-14658) with a linker.
    dBET1
  • HY-107425
    MZ 1 1797406-69-9 98.87%
    MZ 1 is a PROTAC BRD4 degrader. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. Kds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.
    MZ 1
  • HY-130604
    DT2216 2365172-42-3
    DT2216 is a potent and selective BCL-XL degrader based on PROTAC technology. SIAIS178 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
    DT2216
  • HY-130708
    UNC6852
    UNC6852 is a selective rolycomb repressive complex 2 (PRC2) degrader based on PROTAC and contains an EED (embryonic ectoderm development) ligand and a VHL ligand, with an IC50 of 247 nM for EED.
    UNC6852
  • HY-135345
    PROTAC FKBP Degrader-3 2079056-43-0
    PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader.
    PROTAC FKBP Degrader-3
  • HY-101519
    BETd-260 2093388-62-4 99.35%
    BETd-260 (ZBC 260) is a potent PROTAC BET degrader, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line.
    BETd-260
  • HY-112495
    VH032-PEG5-C6-Cl 1799506-06-1 98.10%
    VH032-PEG5-C6-Cl (HaloPROTAC 2) is a small molecule HaloPROTAC that incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
    VH032-PEG5-C6-Cl
  • 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-111556
    BSJ-03-123 2361493-16-3 99.45%
    BSJ-03-123 is a potent and novel CDK6-selective small-molecule degrader (PROTAC).
    BSJ-03-123
  • 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-123937
    THAL-SNS-032 2139287-33-3 99.16%
    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-129523
    PROTAC K-Ras Degrader-1 2378258-52-5 98.05%
    PROTAC K-Ras Degrader-1 (Compound 518) is potent K-Ras degrader based PROTAC, exhibits ≥70% degradation efficacy in SW1573 cells.
    PROTAC K-Ras Degrader-1
  • 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-123921
    Gefitinib-based PROTAC 3 2230821-27-7 99.98%
    Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.
    Gefitinib-based PROTAC 3
  • HY-114312
    MD-224 2136247-12-4 99.74%
    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
    MD-224
  • HY-122826
    ZXH-3-26 2243076-67-5 98.39%
    ZXH-3-26 is a selective PROTAC BRD4 degrader with a DC50/5h (DC50/5h referring to half-maximal degradation after 5 hours of treatment) of ~ 5 nM.
    ZXH-3-26
  • HY-111519
    dTRIM24 2170695-14-2 98.20%
    dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC.
    dTRIM24
Isoform Specific Products

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