2. Signaling Pathways
  3. PROTAC
  4. PROTACs

PROTACs

PROTACs

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PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.

PROTACs Isoform Specific Products:

PROTACs Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-163705
    BR-cpd7 98.01%
    BR-cpd7 is a PROTAC degrader for fibroblast growth factor receptor FGFR1/2 with DC50 of 10 nM. BR-cpd7 arrests cell cycle, inhibits proliferations of FGFR1/2 aberrant activated tumor cells.
    BR-cpd7
  • HY-162749A
    G9D-4 TFA 99.44%
    G9D-4 TFA is a G9a PROTAC degrader. G9D-4 TFA induces G9a degradation, reduces H3K9me2 levels, and prevents GLP interference via the CRBN ternary complex, proteasome and ubiquitin-like modification-dependent pathways. G9D-4 TFA exerts antiproliferative activity and induces Apoptosis in pancreatic cancer cells. G9D-4 TFA can be used for research on pancreatic cancer.
    G9D-4 TFA
  • HY-168215
    YDR1 2951015-31-7 98.06%
    YDR1 is a potent PROTAC SMARCA2 degrader, with the DC50 of 7.7 nM. YDR1 plays an important role in SMARCA4 mutant cancers(Sturcture Note:(Blue: Cereblon ligand (HY-W087383), Black: linker；Pink: SMARCA2 ligand (HY-44012B)).
    YDR1
  • HY-161989
    DZ-837 3105664-95-4
    DZ-837 (compound 3d) is a PROTAC targeting BCL6 with a DC50 of approximately 600 nM. DZ-837 can induce cell cycle arrest and exert synergistic anticancer effects with Ibrutinib (HY-10997). DZ-837 is composed of PROTAC target protein ligand BCL6 ligand-2 (HY-161990) (red part), E3 ubiquitin ligase ligand Thalidomide-4-OH (HY-103596) (blue part), and PROTAC Linker (HY-W245803) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is 2-(2,6-Dioxopiperidin-3-yl)-4-((2-(2-hydroxyethoxy)ethyl)amino)isoindoline-1,3-dione (HY-W924949)[1].
    DZ-837
  • HY-148117
    MD13 2758431-97-7 99.96%
    MD13 is a macrophage migration inhibitory factor (MIF)-directed PROTAC with a Ki of 71 nM. MD13 can be used for cancer research.
    MD13
  • HY-146349
    PROTAC EGFR degrader 4 2882845-50-1 99.70%
    PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
    PROTAC EGFR degrader 4
  • HY-159579
    CW-3308 3055592-99-6 99.43%
    CW-3308 is an orally active BRD9 PROTAC degrader with an DC50 of 92 nM. CW-3308 forms a ternary complex with BRD9 and cereblon to mediate BRD9 degradation. CW-3308 inhibits the viability of synovial sarcoma and rhabdoid tumor cells. CW-3308 reduces BRD9 protein levels in xenograft tumor tissues and suppresses tumor growth in xenograft models. CW-3308 can be used for the research of synovial sarcoma and rhabdoid tumors.
    CW-3308
  • HY-139659
    ARD-61 2316837-08-6 99.57%
    ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice. ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    ARD-61
  • HY-175252
    PROTAC EGFR degrader 14 99.26%
    PROTAC EGFR degrader 14 is a potent and selective EGFR PROTACdegrader with a DC50 of about 2.9 nM and a Dmax of 93.1% for EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 selectively induces EGFRC797S degradation through a VHL and proteasome-dependent manner and downregulated EGFR-associated transcriptome and exhibits good selectivity over EGFRWT. PROTAC EGFR degrader 14 induces cell cycle arrest and apoptosis and significantly inhibits tumor growth. PROTAC EGFR degrader 14 can be used for the study of nonsmall cell lung cancer (NSCLC) (Pink: Target protein ligand: (HY-143337); Blue: E3 ligand (HY-125845); Black: Linker (HY-W004688)).
    PROTAC EGFR degrader 14
  • HY-161633
    PROTAC EGFR degrader 11 3034244-71-5 99.20%
    PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
    PROTAC EGFR degrader 11
  • HY-173679
    RBN012811 2569517-30-0 98.79%
    RBN012811 is a highly selective PROTAC-based PARP14 degrader. RBN012811 forms a ternary complex with cereblon by binding to the NAD+ site of PARP14, and mediates the specific degradation of PARP14 via the ubiquitin-proteasome pathway (IC50=10 nM). RBN012811 effectively depletes endogenous PARP14 in various cell lines and primary human macrophages, thereby downregulating IL-10 production and IFN-β mRNA levels, increasing phosphorylated STAT1 levels to enhance inflammatory signaling, and inhibiting interferon-induced ADPr condensate formation. RBN012811 also modulates viral replication, exhibiting increased HSV1 replication while reducing VSV replication. RBN012811 has important application value in research related to cancer and viral infections.
    RBN012811
  • HY-161101
    MG degrader 1 99.30%
    MG degrader 1 (Compd E14) is a PROTAC degrader of IKZF3, GSPT1, and GSPT2 with an EC50 value of 1.385 nM in MM.1S cells.
    MG degrader 1
  • HY-115568
    BETd-246 2140289-17-2 98.34%
    BETd-246 is a second-generation and PROTAC-based BET bromodomain (BRD) inhibitor connected by ligands for Cereblon and BET, exhibiting superior selectivity, potency and antitumor activity.
    BETd-246
  • HY-130256
    β-NF-JQ1 2380000-55-3 98.05%
    β-NF-JQ1 is a PROTAC that recruits Aryl Hydrocarbon Receptor E3 ligase to target proteins. β-NF-JQ1 is directed against bromodomain-containing (BRD) proteins using β-NF as an AhR ligand, induces the interaction of AhR and BRD proteins, and displays effective anticancer activity that correlated with protein knockdown activity.
    β-NF-JQ1
  • HY-145403
    PROTAC BRD9 Degrader-4 2633632-34-3 99.06%
    PROTAC BRD9 Degrader-4 is a BRD9 bifunctional PROTAC degrader for researching cancer.
    PROTAC BRD9 Degrader-4
  • HY-111875
    SNIPER(BRD)-1 2095244-54-3 99.68%
    SNIPER(BRD)-1 is a SNIPER degrader of BRD4, cIAP1 and XIAP. SNIPER(BRD)-1 has IC50 values of 6.8 nM, 17 nM and 49 nM for cIAP1, cIAP2 and XIAP, respectively. SNIPER(BRD)-1 can be used for cancer research.
    SNIPER(BRD)-1
  • HY-153220A
    (R)-Zelebrudomide 3024312-52-2 98.93%
    (R)-Zelebrudomide ((R)-NX-2127) ((R)-Compound 28) is an isomer of the BTK PROTAC degrader Zelebrudomide (HY-153220). (Pink: BTK ligand 10 (HY-168302); Black: (S)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168303); Blue: Thalidomide 5-fluoride (HY-W087383).
    (R)-Zelebrudomide
  • HY-128360
    dMCL1-2 2351218-88-5 99.29%
    dMCL1-2 is a potent, selective MCL1 PROTAC degrader based on a Cereblon ligand, with a KD value of 30 nM for binding to MCL1. dMCL1-2 induces ubiquitination and degradation of MCL1. dMCL1-2 degrades MCL1, cleaves Caspase-3, and induces Apoptosis. dMCL1-2 can be used in research related to multiple myeloma.
    dMCL1-2
  • HY-135382A
    PROTAC IRAK4 degrader-3 2374122-43-5 98.24%
    PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau.
    PROTAC IRAK4 degrader-3
  • HY-135309
    PROTAC ER Degrader-4 2361114-15-8 98.78%
    PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM.
    PROTAC ER Degrader-4
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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