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-178452
    PROTAC CDK4/6/9 degrader 1 3064994-97-1
    PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand (HY-168440), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-178512), E3 ligase ligand-linker conjugate (HY-178515)).
    PROTAC CDK4/6/9 degrader 1
  • HY-174443
    PROTAC sEH degrader-2
    PROTAC sEH degrader-2 is a PROTAC targeting degradation agent for soluble epoxide hydrolase (sEH) with pIC50 values of the catalytic domain of 8.37 (human sEH-H) and 7.12 (mouce sEH-H). PROTAC sEH degrader-2 can be used for the research related to inflammation and neuroinflammation, such as Alzheimer's disease. (Structure Note: Pink: sEH-H ligand (HY-174225); Blue: CRBN Ligand (HY-103597); Black: linker; E3 + linker (HY-141011))
    PROTAC sEH degrader-2
  • HY-179077
    PROTAC BTK/IKZF1/3 Degrader-1 2416130-49-7
    PROTAC BTK/IKZF1/3 Degrader-1 is a selective and orally active BCL6 and IKZF1/3 PROTAC degrader. PROTAC BTK/IKZF1/3 Degrader-1 exhibits antitumor activity. PROTAC BTK/IKZF1/3 Degrader-1 can be used for the research of cancer, such as lymphoma. (Structure Note: Pink: BCL6/IKZF1/3 ligand (HY-179076); Blue: CRBN ligand (HY-41547))
    PROTAC BTK/IKZF1/3 Degrader-1
  • HY-157561
    K2-B4-3e
    K2-B4-3e is a potent BRD4 PROTAC. K2-B4-3e induces BRD4 degradation with a DC50 value of 66 nM.
    K2-B4-3e
  • HY-149962
    PROTAC CDK9 degrader-5 2935587-89-4
    PROTAC CDK9 degrader-5 is a PROTAC targeting to CDK9 sepcifically. PROTAC CDK9 degrader-5 mediates CDK9 degradation via the proteasome. PROTAC CDK9 degrader-5 degrades CDK9 with DC50s of 0.10 μM and 0.14 μM for the CDK942 and CDK955 isoforms, respectively.
    PROTAC CDK9 degrader-5
  • HY-158331
    Gal-ARV-771
    Gal-ARV-771, PROTAC prodrug, is a gal modified ARV-771 (HY-100972). Gal-ARV-771 can be activated in SA-β-Gal-expressed cancer senescent cells to release ARV-771. Gal-ARV-771 induces selective degradation of BRD4 protein by the ubiquitin-proteasome pathway in senescent cells. Gal-ARV-771 promotes apoptosis of senescent cancer cells.
    Gal-ARV-771
  • HY-168251
    PROTAC BRM/BRG1 degrader-3 2933125-05-2
    PROTAC BRM/BRG1 degrader-3 (compound 304) is a PROTACs-based BRM/BRG1 degrader with a DC50 of less than 1 nM for BRM degradation in SW1573 cells and a DC50 of greater than 1 nM for BRG1 degradation in SW1573 cells. PROTAC BRM/BRG1 degrader-3 has anti-tumor activity and anti-proliferative activity against A549 cells (IC50=0.6 nM). (Structure Note: PINK, Target protein ligand (HY-168252); Blue, E3 (HY-168253); Black, linker (HY-69260)).
    PROTAC BRM/BRG1 degrader-3
  • HY-152145
    PROTAC SOS1 degrader-3 3029320-99-5
    PROTAC SOS1 degrader-3 is a potent PROTAC SOS1 degrader. PROTAC SOS1 degrader-3 effectively targeted SOS1 for degradation through the ubiquitin-proteasome system.
    PROTAC SOS1 degrader-3
  • HY-168247
    PROTAC BRM/BRG1 degrader-2 2933124-32-2
    PROTAC BRM/BRG1 degrader-2 (Example.004) is a PROTAC BRM/BRG1 degrader (DC50: < 10 nM in A549 cell; IC50: 15 nM for A549). Blue: E3 ligase ligand (HY-112078), Black: linker (HY-168249), Pink: BRM/BRG1 inhibitor (HY-168248).
    PROTAC BRM/BRG1 degrader-2
  • HY-156244
    PROTAC GDI2 Degrader-1
    PROTAC GDI2 Degrader-1 (compound 21) is a potent PROTAC GDI2 degrader. PROTAC GDI2 Degrader-1 exhibits excellent in vivo antitumor activity in the GDI2-overexpressing pancreatic xenograft models.
    PROTAC GDI2 Degrader-1
  • HY-161634
    PROTAC SOS1 degrader-8 3036155-11-7
    PROTAC SOS1 degrader-8 (Compd 1) is a PROTAC-based SOS1 degrader (Red: SOS1 Ligand (HY-161635), Black: linker (HY-W056267), Blue: E3 ligase ligand (HY-161637)).
    PROTAC SOS1 degrader-8
  • HY-137488
    PROTAC BRAF-V600E degrader-2 2417296-82-1
    PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth.
    PROTAC BRAF-V600E degrader-2
  • HY-132862
    ZXH-4-137 2711006-74-3
    ZXH-4-137 is a potent and selective CRBN degrader (PROTAC).
    ZXH-4-137
  • HY-178964
    PROTAC RET Degrader 1 2760847-82-1
    PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker).
    PROTAC RET Degrader 1
  • HY-143882
    MS5033 2376137-29-8
    MS5033 is a potent PROTAC-based AKT (protein kinase B) degrader, with a DC50 of 430 nM in PC3 cells.
    MS5033
  • HY-114322A
    cis-VZ185 2306193-98-4
    cis-VZ185 is a VHL-based PROTACs degrader with the activity of degrading BRD9 and BRD7. cis-VZ185 can be optimized from suboptimal compounds by optimizing the connection mode and linker, and has efficient, rapid and selective degradation of BRD9 and its homologous protein BRD7.
    cis-VZ185
  • HY-162464
    MPD2
    MPD2 is a Cereblon-binding ligand-based PROTAC that degrades MPro, the main protease of SARS-CoV-2. MPD2 effectively reduced MPro protein levels in 293T cells in a time-dependent manner (DC50=296 nM). MPD2 exhibited potent antiviral activity against multiple SARS-CoV-2 strains and had enhanced potency against Nirmatrelvir (HY-138687) resistant strains. MPD2 provides a new direction for antiviral drug development against SARS-CoV-2 and other emerging coronavirus pathogens (Sturcture Note:(Blue: Cereblon ligand (HY-14658), Black: linker (HY-W275882)；Red: SARS-CoV-2 MPro Inhibitor MP18 (HY-158763)).
    MPD2
  • HY-150400A
    XF056-132 2694057-55-9
    XF056-132 is the salt form of trifluoroacetic acid (TFA, HY-21182).
    XF056-132
  • HY-146368
    PROTAC VEGFR-2 degrader-1 2601594-19-6
    PROTAC VEGFR-2 degrader-1（PROTAC-1）, a PROTAC VEGFR-2 degrader, exhibits little VEGFR-2 inhibition (IC50> 1 μM) and anti-proliferative activity against EA.hy926 cells (IC50> 100 μM).
    PROTAC VEGFR-2 degrader-1
  • HY-159460
    PROTAC SMARCA2/4-degrader-8 2568507-14-0
    PROTAC SMARCA2/4-degrader-8 (Compound I-502) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2/4-degrader-8 degrades SMARCA2 with DC50 <100 nM in A549 and in MV411, degrades SMARCA4 with DC50<100 nM in MV411(Pink: Ligand for target protein (HY-159545); Black: Linker (HY-W063924); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
    PROTAC SMARCA2/4-degrader-8
Cat. No. Product Name / Synonyms Application Reactivity
PROTACs Isoform Comparison

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