1. Signaling Pathways
  2. PROTAC
  3. PROTACs

PROTACs

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.

Cat. No. Product Name CAS No. Purity Chemical Structure
  • 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 3055593-64-8
    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-128408
    PROTAC BTK Degrader-4 2893795-12-3
    PROTAC BTK Degrader-4 (compound 15) is a potent PROTAC Bruton's tyrosine kinases (BTK) degrader (DC50 < 100 nM) with little immunomodulatory imide drug (IMiD) activity (DC50 = 0.345 μM, Dmax = 27.4%). PROTAC BTK Degrader-4 can be used for cancers, autoimmune diseases, and inflammatory diseases that are mediated by BTK.
    PROTAC BTK Degrader-4
  • 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).
    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-181732
    PROTAC TG2 Degrader-3 3054388-18-7
    PROTAC TG2 Degrader-3 is a TG2 (TGM2) PROTAC degrader. PROTAC TG2 Degrader-3 inhibits the adhesion and migration of ovarian cancer cells. PROTAC TG2 Degrader-3 can be used for the research of ovarian cancer.
    PROTAC TG2 Degrader-3
  • HY-180555
    SN38-(PEG)2-Pom-α
    SN38-(PEG)2-Pom-α is a selective PROTAC RPL15 degrader. SN38-(PEG)2-Pom-α induces ubiquitin-mediated degradation of RPL15 without affecting TOP1. SN38-(PEG)2-Pom-α induces damage-associated molecular pattern (DAMP) secretion from cancer cells, which activated cGAS-STING signaling in dendritic cells. SN38-(PEG)2-Pom-α enhances anti-PD-1 immunotherapy in a murine melanoma tumor model expressing human CRBN. SN38-(PEG)2-Pom-α can be used for melanoma research.
    SN38-(PEG)2-Pom-α
  • HY-179582
    PROTAC DNPH1 Degrader 1
    PROTAC DNPH1 Degrader 1 is a potent PROTAC DNPH1 degrader with a DC50 of 28 nM. PROTAC DNPH1 Degrader 1 mediates proteasome- and VHL-dependent DNPH1 knockdown, drives DNPH1 ubiquitination and proteasomal degradation. PROTAC DNPH1 Degrader 1 can be used for the research of brca1 mutant cancer.
    PROTAC DNPH1 Degrader 1
  • 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-181320
    PROTAC EZH2 Degrader-19 2653338-65-7
    PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of cancer.
    PROTAC EZH2 Degrader-19
  • 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.
    MPD2
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