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-114407
    TD-428 2334525-50-5 98.81%
    TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
    TD-428
  • HY-148274
    KTX-582 2573298-13-0 98.65%
    KTX-582 is a potent IRAK4 degrader with DC50 values of 4 nM and 5 nM for IRAK4 and Ikaros, respectively. KTX-582 can induce apoptosis in MYD88MT DLBCL, and is efficient to induce in vivo tumor regressions in lymphoma model.
    KTX-582
  • HY-115728
    PROTAC CDK9 degrader-4 2411021-01-5 99.65%
    PROTAC CDK9 degrader-4 is a highly potent and efficacious CDK9 degrader for targeting transcription regulation.
    PROTAC CDK9 degrader-4
  • HY-149878
    BD-9136 3037514-38-5 98.81%
    BD-9136 is a potent and highly selective BRD4 PROTAC depressant. BD-9136 has low-nanomolar degradation potencies against BRD4 , and its degradation selectivity for BRD4 is 1000 times that of BRD2 and BRD3 proteins. BD-9136 has antitumor activity.(Pink: Desmethyl-QCA276 (HY-44103); Black: 3-(2-(4-Methylpiperazin-1-yl)ethyl)azetidin-3-ol; Blue: Thalidomide-4-OH (HY-103596))
    BD-9136
  • 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-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-138635
    PROTAC BRD4 Degrader-12 2417370-90-0 98.54%
    PROTAC BRD4 Degrader-12 (compound 9c) is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. PROTAC BRD4 Degrader-12 can be conjugated with STEAP1 and CLL1 antibodies to degrade the BRD4 protein in PC3 prostate cancer cells, with a DC50 of 0.39 nM and 0.24 nM, respectively.
    PROTAC BRD4 Degrader-12
  • HY-159607
    PRT3789 2755761-78-3
    PRT3789 is a SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 shows synergistic anti-proliferation effects with Adagrasib (HY-130149) in cancer cells. PRT3789 inhibits SMARCA4-mutated lung cancer proliferation. PRT3789 inhibits tumor growth in SMARCA4-deleted NSCLC models. Pink: SMARCA4 ligand (HY-44824) ; Blue: VHL ligand (HY-159465) ; Black: linker; VHL ligand+linker (HY-172738).
    PRT3789
  • 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. (Blue: LCL161 (HY-15518); Black: linker (HY-W008005); Pink: (+)-JQ-1 (HY-13030))
    SNIPER(BRD)-1
  • HY-153220A
    (R)-NX-2127 3024312-52-2 98.93%
    (R)-NX-2127 ((R)-Compound 28) is an isomer of the BTK PROTAC degrader NX-2127 (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)-NX-2127
  • HY-114228
    PROTAC BET degrader-2 2093388-33-9 98.21%
    PROTAC BET degrader-2 is a PROTAC connected by ligands for Cereblon and BET 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-152147
    SZUH280 2770263-77-7 99.38%
    SZUH280 is a potent and selective PROTAC HDAC8 degrader with a DC50 of 0.58 μM in A549 cells. SZUH280 induces cancer cell apoptosis. SZUH280 hampers DNA damage repair in cancer cells, promoting cellular radiosensitization.
    SZUH280
  • HY-128838
    PROTAC ERRα Degrader-1 2306388-84-9 98.22%
    PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.
    PROTAC ERRα Degrader-1
  • HY-159579
    CW-3308 3055592-99-6
    CW-3308 is an orally effective PROTAC that selectively targets BRD9 and is expected to be used to inhibit synovial sarcoma, rhabdomyoma, and other BRD9-dependent human diseases. CW-3308 is composed of PROTAC target protein ligand Naphthyridin-Me-dimethoxybenzene-COOH (HY-159596) (red part), Linker 3-Azaspiro[5.5]undecane-9-methanol (HY-159598) (black part), E3 ubiquitin ligase ligand Thalidomide-methylpyrrolidine (HY-159597) (blue part), where the conjugate of E3 ubiquitin ligase ligand + linker is Thalidomide-pyrrolidine-C-azaspiro (HY-159599)[1].
    CW-3308
  • HY-158684
    YX-02-030 3049076-98-1 99.86%
    YX-02-030M is a PROTAC MDM2 degrader. YX-02-030M inhibits MDM2-p53 binding and VHL-HIF1α binding with IC50s of 63 nM and 1.35 μM respectively. YX-02-030M binds MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, and effectively kills p53 mutant or deleted Triple-negative breast cancers (TNBC) cells. (Blue: VHL ligand; Black: linker; Pink: MDM2 inhibitor).
    YX-02-030
  • HY-158345
    PROTAC VHL-type degrader-1 2821804-13-9 98.01%
    PROTAC VHL-type degrader-1 (compound 9b) is a VHL-type PROTAC degrader. PROTAC VHL-type degrader-1 induces ATM degradation synergistically enhancing the efficacy of ATR inhibitor AZD6738.
    PROTAC VHL-type degrader-1
  • HY-163807
    22-SLF
    22-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM. 22-SLF interacts with C227 and C228 in FBXO22 to induce a ternary complex between FKBP12 and FBXO22, and degrades FKBP12 in a FBXO22-dependent manner. 22-SLF can be used for fundamental cancer research as a probe to study the FBXO22 degradation pathway. (Pink: FKBP12 ligand (HY-114872); Black: Linker (HY-163821); Blue: FBXO22 ligand (HY-163826)).
    22-SLF
  • HY-163502
    PROTAC STAT3 degrader-3 99.39%
    PROTAC STAT3 degrader-3 (S3D1) is a STAT3 PROTAC degrader with anticancer activity (Structural notes: (Blue: Cereblon ligand (HY-10984), Black: linker; Pink: Pentafluorobenzenesulfonamide(Me)-CH2-CONH-benzamide (HY-163526)).
    PROTAC STAT3 degrader-3
  • HY-161177
    PROTAC KRAS G12D degrader 2
    PROTAC KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPro). Protac KRAS G12D degrades SARS-CoV-2, 3-curd trypsin-like protease (3CLPRO). The PROTAC molecule is designed by partially coupling a GC-376-based dipeptidyl 3CLPro ligand with pomadomide via a piperazine-piperidine linker.
    PROTAC KRAS G12D degrader 2
  • HY-W998345
    SMART1 99.87%
    SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .
    SMART1
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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