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-170869
    PROTAC FGFR1 degrader-1
    PROTAC FGFR1 degrader-1 (compound S2H) is a PROTAC degrader targeting FGFR1, with IC50=26.81 nM and DC50=39.78 nM in KG1a cells. PROTAC FGFR1 degrader-1 is composed of CRBN-type E3 ligase ligand (blue part) Pomalidomide (HY-10984), target protein ligand (red part) FGFR1 ligand-1 (HY-170871), and PROTAC linker (black part) 9-Bromononanoic acid (HY-W007587), in which the E3 ligase ligand and linker form a conjugate E3 Ligase Ligand-linker Conjugate 164 (HY-170870).
    PROTAC FGFR1 degrader-1
  • HY-123971
    HDAC6 degrader-4 2235382-05-3
    HDAC6 degrader-4 is a PROTAC and a selective HDAC6 degrader consists of a non-selective HDAC inhibitor and thalidomide-type E3 ligase ligand. HDAC6 degrader-4 can be used for cancer research.
    HDAC6 degrader-4
  • HY-174086
    PROTAC GPX4 degrader-4 3071165-43-7
    PROTAC GPX4 degrader-4 is a GPX4 PROTAC degrader (DC50: 5.32 nM). PROTAC GPX4 degrader-4 inhibits the activity of RT4, T24, and J82 cancer cells (IC50 values are 0.09, 2.97, and 7.58 μM, respectively). PROTAC GPX4 degrader-4 increases lipid ROS levels and induces ferroptosis in T24 and RT4 cells. PROTAC GPX4 degrader-4 has antitumor activity in T24 tumor-bearing BALB/c nude mouse model. PROTAC GPX4 degrader-4 can be used for bladder cancer research. (Pink: target protein ligand (HY-N0193); blue: E3 ligase ligand (HY-1035960); black: linker (HY-W013907); E3 ligase ligand + linker (HY-174087)).
    PROTAC GPX4 degrader-4
  • HY-169270
    PROTAC SMARCA2 degrader-19 2567913-00-0
    PROTAC SMARCA2 degrader-19 (Compound 46) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 in cell A549 and MV411 with a DC50 < 100 nM. PROTAC SMARCA2 degrader-19 degrades SMARCA4 in cell MV411 with a DC50 > 1000 nM.
    PROTAC SMARCA2 degrader-19
  • HY-176904
    JPS004 2559747-12-3
    JPS004 is a HDAC1-3 PROTAC degrader. JPS004 can induce degradation of HDAC1-3 and induce histone acetylation. JPS004 can induce cancer cells apoptosis. JPS004 can be used for the research of cancer. (Structure Note: Pink: HDAC1-3 ligand (HY-50934); Blue: VHL ligand (HY-125845);; HDAC1-3 ligand-Linker: (HY-176905))
    JPS004
  • HY-169271
    PROTAC SMARCA2 degrader-20 2660324-41-2
    PROTAC SMARCA2 degrader-20 (Compound I-40) is a PROTAC SMARCA2 degrader. PROTAC SMARCA2 degrader-20 has the potential for the research of cancer.
    PROTAC SMARCA2 degrader-20
  • HY-175527
    ALK degrader 2
    ALK degrader 2 is an orally active ALK degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM)-ALK protein levels (DC50 = 102 nM). ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528)).
    ALK degrader 2
  • HY-178873
    PROTAC K-Ras Degrader-7
    PROTAC K-Ras Degrader-7 is a potent PROTAC K-Ras degrader. PROTAC K-Ras Degrader-7 degrades K-Ras through recruiting the Keap1 E3 ubiquitin ligase. PROTAC K-Ras Degrader-7 can be used for research in pancreatic and colorectal cancers. (Pink: Nrf2 ligand: Nrf2 activator-22 (HY-178875); Blue: E3 ligand (HY-178874); target protein ligand +linker (HY-178888).
    PROTAC K-Ras Degrader-7
  • HY-143327
    PROTAC BRD4 Degrader-16 2585561-36-8
    PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC50 values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells.
    PROTAC BRD4 Degrader-16
  • HY-160264
    PROTAC ER Degrader-12
    PROTAC ER Degrader-12 (Compound 70) is an estrogen receptor PROTAC degrader (DC50: <10 nM), and inhibits MCF-7 proliferation (DC50: <10 nM). PROTAC ER Degrader-12 has anticancer effect. Pink: ER ligand (HY-169978); Blue: E3 ligase ligand (HY-138793); Black: linker (HY-30756).
    PROTAC ER Degrader-12
  • HY-161789
    PROTAC SARS-CoV-2 Mpro degrader-3
    PROTAC SARS-CoV-2 Mpro degrader-3 (Compound P2) exhibits antiviral activity through the degradation of the main protease (Mpro) of human coronaviruses (HCoVs) (DC50=27 μM). PROTAC SARS-CoV-2 Mpro degrader-3 inhibits the viral replication, with EC50 of 4.6 μM, 4.6 μM, and 0.71 μM, for human coronaviruses HCoV-229E, HCoV-OC43 and SARS-CoV-2, respectively. (Pink: ligand for target protein Mpro ligand 2 (HY-161791); Black: linker (HY-161792); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)) .
    PROTAC SARS-CoV-2 Mpro degrader-3
  • HY-178796
    PROTAC LRRK2 Degrader-4 2839664-99-0
    PROTAC LRRK2 Degrader-4 is a PROTAC LRRK2 degrader with a DC50 of 0.79 nM. PROTAC LRRK2 Degrader-4 can be used for research in Parkinson’s disease and inflammation. (Pink: LRRK2 ligand: LRRK2-IN-19 (HY-177016); Black: Linker (HY-178831); Blue: E3 ligand (HY-179222); E3+Linker (HY-178832).
    PROTAC LRRK2 Degrader-4
  • HY-168175
    PROTAC HDAC8 Degrader-2
    PROTAC HDAC8 Degrader-2 (compound 32a) is a degrader of HDAC8 with a DC50 of 8.9 nM and HDAC6 with a DC50 of 14.3 nM. PROTAC HDAC8 Degrader-2 is composed of PROTAC target protein ligand HDAC8 ligand 1 (HY-168176) (red part), E3 ligase ligand Thalidomide-4-OH (HY-103596) (blue part) and PROTAC Linker 1,5-Diaminopentane (HY-W540541) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is Thalidomide-NH-C5-NH2 (HY-134986).
    PROTAC HDAC8 Degrader-2
  • HY-168057
    PROTAC CDK2 Degrader-1 3024971-78-3
    PROTAC CDK2 Degrader-1 (Compound 41) is a PROTAC degrader for cyclin-dependent kinase 2 (CDK2). PROTAC CDK2 Degrader-1 inhibits the phosphorylation of RB protein in CDK2 dependent cell line OVCAR3 with an IC50 of 100-500 nM.
    PROTAC CDK2 Degrader-1
  • HY-160221
    PROTAC AR Degrader-7 2505495-83-8
    PROTAC AR Degrader-7 (compound 99) is a PROTAC targeting androgen receptor with an IC50 value of 3 nM. PROTAC AR Degrader-7 is composed of PROTAC target protein ligand AR ligand-32 (HY-170303) (red part), E3 ligase ligand E3 ligase Ligand 44 (HY-170304) (blue part) and PROTAC Linker N-Boc-piperazine (HY-30105) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 145 (HY-170305).
    PROTAC AR Degrader-7
  • HY-173631
    (S)-dHTC1 3081383-46-9
    (S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC50 value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC50 value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study.
    (S)-dHTC1
  • HY-161093
    PROTAC BRD4 Degrader-23
    PROTAC BRD4 Degrader-23 (compound 17) is an effective visible-light-controlled degrader. PROTAC BRD4 Degrader-23 can inhibit tumor cell proliferation under 405 nm light irradiation.
    PROTAC BRD4 Degrader-23
  • HY-177030
    RNase L ligand 3 3036649-51-8
    RNase L ligand 3 is a RNase L ligand. RNase L ligand 3 can be used for synthesis of F3-PEG8-RiboTAC (HY-176259).
    RNase L ligand 3
  • HY-161632
    PROTAC EGFR degrader 10 3034244-56-6
    PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM.
    PROTAC EGFR degrader 10
  • HY-142621
    BCPyr 2669844-82-8
    BCPyr is a PROTAC-class BTK degrader (DC50 = 800 nM). BCPyr consists of a PROTAC target protein ligand (red part) BTK ligand 11 (HY-168314), an E3 ubiquitin ligase ligand (blue part) E3 ligase Ligand 20 (HY-135997), and a PROTAC linker (black part) (5-(Bromomethyl)pyrazin-2-yl)methanol (HY-168315). E3 ubiquitin ligase+linker can form E3 Ligase Ligand-linker Conjugate 146 (HY-168316).
    BCPyr
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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