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-181143
    PROTAC Tubulin degrader-2
    PROTAC Tubulin degrader-2 is a cereblon (CRBN)-dependent α/β-tubulin PROTAC degrader with DC50 values of 1.73 μM and 1.38 μM. PROTAC Tubulin degrader-2 can inhibit cancer cells proliferation and migration. PROTAC Tubulin degrader-2 can induce G2/M arrest, apoptosis, ROS accumulation. PROTAC Tubulin degrader-2 can be used for the research of cancer, such as non-small-cell lung cancer.
    PROTAC Tubulin degrader-2
  • HY-148521
    PROTAC FLT3/CDK9 degrader-1 3033084-05-5
    PROTAC FLT3/CDK9 degrader-1 is a potent FLT3 and CDK9 dual PROTAC degrader. PROTAC FLT3/CDK9 degrader-1 induces apoptosis and effective degradation of target proteins FLT3 and CDK9. PROTAC FLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML.
    PROTAC FLT3/CDK9 degrader-1
  • HY-181300
    PROTAC EZH2 Degrader-17 3093642-23-7
    PROTAC EZH2 Degrader-17 (compound 52) is a PROTAC protein degrader targeting EZH2 with an antiproliferative IC50 of 18.32 μM in lymphoma cells. PROTAC EZH2 Degrader-17 exhibits antiproliferative activity against lymphoma cells. PROTAC EZH2 Degrader-17 can be used for the research of lymphoma.
    PROTAC EZH2 Degrader-17
  • HY-168910
    PROTAC c-Met degrader-3
    PROTAC c-Met degrader-3 (Compound 22b) is a c-Met PROTAC degrader. PROTAC c-Met degrader-3 promotes ubiquitination and degradation of c-Met (DC50 of 0.59 nM in EBC-1 cells). PROTAC c-Met degrader-3 can be used for the research of lung cancer (Pink: c-Met ligand (HY-14721); Blue: E3 ligase CRBN ligand (HY-W249500); linker + E3 ligase ligand (HY-168911)).
    PROTAC c-Met degrader-3
  • HY-163851
    PROTAC Vif degrader-1
    PROTAC Vif degrader-1 (Compound L15) is a Vif PROTAC degrader. PROTAC Vif degrader-1 has antiviral activity against HIV-1 (EC50: 33.35 μM against HIV-1IIIB). Blue: CRBN ligand (HY-10984); Black: linker; Pink: HIV-1 inhibitor(HY-163852).
    PROTAC Vif degrader-1
  • HY-181534
    PROTAC TEAD1/IAP degrader-1
    PROTAC TEAD1/IAP degrader-1 (Compound A232) is a selective TEAD1 and cIAP1 PROTAC degrader, with DC50 values of 14 nM and 270 nM, respectively. PROTAC TEAD1/IAP degrader-1 promotes the ubiquitination and degradation of TEAD1 and cIAP1. PROTAC TEAD1/IAP degrader-1 downregulates the expression of the TEAD-dependent gene CTGF. PROTAC TEAD1/IAP degrader-1 exhibits anticancer activity against mesothelioma.
    PROTAC TEAD1/IAP degrader-1
  • HY-163870
    PROTAC SMARCA2/4-degrader-17 2568276-88-8
    PROTAC SMARCA2/4-degrader-17 (Compound I-345) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-17 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM. (Pink: Ligand for Target Protein (HY-159545); Black: Linker (HY-W053507); Blue: Ligand for E3 Ligase (HY-125845))
    PROTAC SMARCA2/4-degrader-17
  • HY-162813
    PROTAC SMARCA2/4-degrader-25
    PROTAC SMARCA2/4-degrader-25 (compound 7d) is a PROTAC targeting SMARCA2/4. PROTAC SMARCA2/4-degrader-25 is composed of E3 ligase (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC Linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and target protein ligand SMARCA2/4-ligand-3 (HY-162814) (red part). The conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845)[1].
    PROTAC SMARCA2/4-degrader-25
  • HY-175975
    PROTAC Akt3 Degrader-1 3048204-93-6
    PROTAC Akt3 Degrader-1 is a highly efficient and selective PROTAC degrader targeting Akt3. PROTAC Akt3 Degrader-1 shows weak antiproliferative activity in 36 cell lines. PROTAC Akt3 Degrader-1 can be used for the study of Triple-negative breast cancer and melanoma.
    PROTAC Akt3 Degrader-1
  • HY-178225
    PROTAC SMARCA2/4 degrader-39 3099581-74-2
    PROTAC SMARCA2/4 degrader-39 (Compound 7) is a selective degrader of SMARCA2 (BRM) and SMARCA4 (BRG1) PROTAC. PROTAC SMARCA2/4 degrader-39 is promising for research of oncology, such as non-small cell lung cancer and colorectal cancer. (Pink: BRM/BRG1 ligand 5 (HY-178886); Black: Linker Piperazine (HY-B0912); Blue: (S)-Deoxy-thalidomide (HY-168055))
    PROTAC SMARCA2/4 degrader-39
  • HY-181153
    PROTAC FGFR3 Degrader-1
    PROTAC FGFR3 Degrader-1 is a fibroblast growth factor receptor 3 (FGFR3) PROTAC degrader, promotes FGFR3 degradation via the ubiquitin-proteasome pathway, and inhibits the downstream FGFR3/PI3K/AKT signaling pathway. PROTAC FGFR3 Degrader-1 can be used for the research of hepatocellular carcinoma.
    PROTAC FGFR3 Degrader-1
  • HY-168634
    SJ46421
    SJ46421 is a (+)-JQ-1 (HY-13030) based KLHDC2-BRD3 PROTAC protein degrader. SJ46421 induces cooperative ternary complexes with KLHDC2 and BRD3BD2, with an IC50 of 7.8 nM. SJ46421 selectively inhibits KLHDC2 substrate ubiquitylation. SJ46421 promotes polyubiquitylation of the BD2 domain from BRD2, BRD3, or BRD4. SJ46421 possesses poor cell permeability. (Pink: ligand for target protein (HY-13030); Black: linker (HY-20797); Blue: E3 ligase ligand (HY-168536)).
    SJ46421
  • HY-180965
    Pro-PEG3-BA 3057939-64-4
    Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research.
    Pro-PEG3-BA
  • HY-170598
    HP211206 3119106-17-8
    HP211206 is a SARS-CoV-2 main protease (Mpro) PROTAC degrader. HP211206 effectively degrades SARS-CoV-2 Mpro and its drug-resistant mutants. HP211206 has an IC50 of 181.9 nM and a DC50 of 621 nM for Mpro. HP211206 has antiviral activity. (Pink: H117 (HY-170599); Black: linker (HY-B0236); Blue: E3 ligase ligand (HY-41547)).
    HP211206
  • HY-180985
    Azo-PROTAC-4C-cis
    Azo-PROTAC-4C-cis is a BCR-ABL PROTAC degrader, and its degradation efficiency of BCR-ABL is much lower than that of its trans isomer Azo-PROTAC-4C-trans (HY-180983). Azo-PROTAC-4C-cis is the product of the conformational transformation of Azo-PROTAC-4C-trans under ultraviolet (UV) light irradiation. Azo-PROTAC-4C-cis can be converted into highly active Azo-PROTAC-4C-trans under visible light, thereby initiating protein degradation. Azo-PROTAC-4C-cis can be used for the study of myeloid leukemia.
    Azo-PROTAC-4C-cis
  • HY-137344
    dAURK-4 2705844-81-9
    dAURK-4, an Alisertib (HY-10971) derivative, is a potent and selective AURKA (Aurora A) degrader. dAURK-4 has anticancer effects.
    dAURK-4
  • HY-180972
    PROTAC EML4-ALK Degrader-2 2417174-28-6
    PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research.
    PROTAC EML4-ALK Degrader-2
  • HY-176261
    DDD2
    DDD2 is a selective and potent VHL-mediated PROTAC NUDT5 degrader. DDD2 induces robust NUDT5 degradation. DDD2 can be used in cancer research, such as lymphocytic leukemia and osteosarcoma. (Structure Note: Pink: NUDT5 inhibitor (HY-176262); Blue: E3 (HY-125845); Black: linker (HY-W001958))
    DDD2
  • HY-178925
    PROTAC GPX4 degrader-5 3119292-91-7
    PROTAC GPX4 degrader-5 (compound N15) is an efficient and highly selective PROTAC GPX4 degrader (DC50 = 28 nM). PROTAC GPX4 degrader-5 can induce ferroptosis and has low toxicity to normal cells. PROTAC GPX4 degrader-5 can significantly increase ROS. PROTAC GPX4 degrader-5 exerts anti proliferative effects on various tumor cells. PROTAC GPX4 degrader-5 is commonly used in cancer research.
    PROTAC GPX4 degrader-5
  • HY-181261
    PROTAC CBP/P300 Degrader-2 3102127-45-4
    PROTAC CBP/P300 Degrader-2 (compound 2) is a PROTAC-based CBP/P300 degrader that can be used in the research of cancer, autoimmune, inflammatory, and neurodegenerative diseases.
    PROTAC CBP/P300 Degrader-2
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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